PMID-sentid	Pub_year	Sent_text	comp_official_name	comp_offset	protein_name	organism	prot_offset
27707886-3	2017	Here, the hypothesis was tested that the transcription factor drivers of castration-resistant prostate cancer (CRPC) clinical progression, including the androgen receptor (AR), are critically dependent on BRD4 and thus represent a sensitive solid tumor indication for the BET inhibitor ABBV-075.	mivebresib	286-294	bromodomain containing 4	Homo sapiens	205-209
27707886-5	2017	Furthermore, ABBV-075 disrupted DHT-stimulated recruitment of BET family member BRD4 to gene-regulatory regions cooccupied by AR, including the well-established PSA and TMPRSS2 enhancers.	mivebresib	13-21	bromodomain containing 4	Homo sapiens	80-84
28024472-0	2016	[Effect of BRD4 Inhibitor GSK525762A on Proliferation and Apoptosis of SUP-B15 Cells In Vitro and Its Possible Mechanism].	molibresib	26-36	bromodomain containing 4	Homo sapiens	11-15
28978850-11	2017	Several proteins, such as BRD4 and BCR-ABL, have been successfully degraded by CRL4CRBN using these technologies.	crl4crbn	79-87	bromodomain containing 4	Homo sapiens	26-30
28024472-1	2016	OBJECTIVE: To investigate the effect of BRD4 inhibitor GSK525762A on the proliferation and apoptosis of Philadelphia chromosome-positive acute lymphoblastic leukemia SUP-B15 cells and its mechanism.	molibresib	55-65	bromodomain containing 4	Homo sapiens	40-44
27764789-7	2016	Our study identified and validated Brd4, a key transcription factor, as a novel proline hydroxylation substrate.	Proline	80-87	bromodomain containing 4	Homo sapiens	35-39
27764789-8	2016	Functional analysis showed that the inhibition of proline hydroxylation pathway significantly reduced the proline hydroxylation abundance on Brd4 and affected Brd4-mediated transcriptional activity as well as cell proliferation in AML leukemia cells.	Proline	50-57	bromodomain containing 4	Homo sapiens	141-145
27764789-8	2016	Functional analysis showed that the inhibition of proline hydroxylation pathway significantly reduced the proline hydroxylation abundance on Brd4 and affected Brd4-mediated transcriptional activity as well as cell proliferation in AML leukemia cells.	Proline	50-57	bromodomain containing 4	Homo sapiens	159-163
27764789-8	2016	Functional analysis showed that the inhibition of proline hydroxylation pathway significantly reduced the proline hydroxylation abundance on Brd4 and affected Brd4-mediated transcriptional activity as well as cell proliferation in AML leukemia cells.	Proline	106-113	bromodomain containing 4	Homo sapiens	141-145
28881723-0	2017	Association of high microvessel alphavbeta3 and low PTEN with poor outcome in stage 3 neuroblastoma: rationale for using first in class dual PI3K/BRD4 inhibitor, SF1126.	SF 1126	162-168	bromodomain containing 4	Homo sapiens	146-150
28881723-8	2017	SF1126 inhibits BRD4 bromodomain binding to acetylated lysine residues with histone H3 as well as PI3K activity in the MYCN amplified neuroblastoma cell line IMR-32.	SF 1126	0-6	bromodomain containing 4	Homo sapiens	16-20
28881723-8	2017	SF1126 inhibits BRD4 bromodomain binding to acetylated lysine residues with histone H3 as well as PI3K activity in the MYCN amplified neuroblastoma cell line IMR-32.	Lysine	55-61	bromodomain containing 4	Homo sapiens	16-20
27573426-3	2016	Herein, we report AZD5153, a potent, selective, and orally available BET/BRD4 bromodomain inhibitor possessing a bivalent binding mode.	AZD5153	18-25	bromodomain containing 4	Homo sapiens	73-77
27650498-2	2016	BRD4, a BET family member protein, has been implicated in a number of types of cancer, and BET protein inhibitors (BETi) are efficacious in many preclinical cancer models.	beti	115-119	bromodomain containing 4	Homo sapiens	0-4
27496136-0	2016	Single Agent and Synergistic Activity of the "First-in-Class" Dual PI3K/BRD4 Inhibitor SF1126 with Sorafenib in Hepatocellular Carcinoma.	SF 1126	87-93	bromodomain containing 4	Homo sapiens	72-76
27496136-0	2016	Single Agent and Synergistic Activity of the "First-in-Class" Dual PI3K/BRD4 Inhibitor SF1126 with Sorafenib in Hepatocellular Carcinoma.	Sorafenib	99-108	bromodomain containing 4	Homo sapiens	72-76
27496136-3	2016	Hence, there is an unmet medical need to identify potent PI3K/BRD4 inhibitors, which can be used either alone or in combination with sorafenib to treat patients with advanced HCC.	Sorafenib	133-142	bromodomain containing 4	Homo sapiens	62-66
27573426-4	2016	Unlike previously described monovalent inhibitors, AZD5153 ligates two bromodomains in BRD4 simultaneously.	AZD5153	51-58	bromodomain containing 4	Homo sapiens	87-91
27496136-5	2016	We demonstrate that the active moiety of the SF1126 prodrug LY294002 binds to and blocks BRD4 interaction with the acetylated histone-H4 chromatin mark protein and displaced BRD4 coactivator protein from the transcriptional start site of MYC in Huh7 and SK-Hep1 HCC cell lines.	2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one	60-68	bromodomain containing 4	Homo sapiens	89-93
27496136-5	2016	We demonstrate that the active moiety of the SF1126 prodrug LY294002 binds to and blocks BRD4 interaction with the acetylated histone-H4 chromatin mark protein and displaced BRD4 coactivator protein from the transcriptional start site of MYC in Huh7 and SK-Hep1 HCC cell lines.	2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one	60-68	bromodomain containing 4	Homo sapiens	174-178
27573426-7	2016	The relationship between AZD5153 exposure and efficacy suggests that prolonged BRD4 target coverage is a primary efficacy driver.	AZD5153	25-32	bromodomain containing 4	Homo sapiens	79-83
27496136-7	2016	Treatment of SF1126 either alone or in combination with sorafenib showed significant antitumor activity in vivo Our results establish that SF1126 is a dual PI3K/BRD4 inhibitor.	SF 1126	13-19	bromodomain containing 4	Homo sapiens	161-165
27496136-7	2016	Treatment of SF1126 either alone or in combination with sorafenib showed significant antitumor activity in vivo Our results establish that SF1126 is a dual PI3K/BRD4 inhibitor.	Sorafenib	56-65	bromodomain containing 4	Homo sapiens	161-165
27573426-11	2016	This study establishes AZD5153 as a highly potent, orally available BET/BRD4 inhibitor and provides a rationale for clinical development in hematologic malignancies.	AZD5153	23-30	bromodomain containing 4	Homo sapiens	72-76
27496136-7	2016	Treatment of SF1126 either alone or in combination with sorafenib showed significant antitumor activity in vivo Our results establish that SF1126 is a dual PI3K/BRD4 inhibitor.	SF 1126	139-145	bromodomain containing 4	Homo sapiens	161-165
27266999-0	2016	Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors.	4,5-dihydro-benzodiazepinone	15-43	bromodomain containing 4	Homo sapiens	84-88
27496136-9	2016	Our data support the potential future consideration of a phase II clinical trial of SF1126, a clinically relevant dual "first-in-class" PI3K/BRD4 inhibitor in advanced HCC, and a potential combination with sorafenib.	SF 1126	84-90	bromodomain containing 4	Homo sapiens	141-145
27266999-3	2016	In this study, we made structural modifications of previously reported BRD4 inhibitors, to develop new chemical scaffold 3,4-dihydroquinoxalin-2(1H)-one.	3,4-Dihydro-1H-quinoxalin-2-one	121-152	bromodomain containing 4	Homo sapiens	71-75
27520485-11	2016	Chromatin immunoprecipitation assays showed that TPA elevated H3K27Ac enrichment in the COX2 promoter region, which is mediated by p300, and Brd4.	Tetradecanoylphorbol Acetate	49-52	bromodomain containing 4	Homo sapiens	141-145
27007123-1	2016	Brd4 is an epigenetic reader protein and a member of the BET (bromodomain and extra terminal domain) family of proteins with two bromodomains that recognize acetylated lysine residues.	Lysine	168-174	bromodomain containing 4	Homo sapiens	0-4
27580186-0	2016	Design, synthesis and biological evaluation of dihydroquinoxalinone derivatives as BRD4 inhibitors.	dihydroquinoxalinone	47-67	bromodomain containing 4	Homo sapiens	83-87
27580186-3	2016	In this study, we synthesized a series of dihydroquinoxalinone derivatives and evaluated their BRD4 inhibitory activities, obtaining compound 5i with IC50 value of 73nM of binding activity in BRD4(1) and 258nM of cellular activity in MV-4-11 cancer cell lines.	dihydroquinoxalinone	42-62	bromodomain containing 4	Homo sapiens	95-99
27580186-3	2016	In this study, we synthesized a series of dihydroquinoxalinone derivatives and evaluated their BRD4 inhibitory activities, obtaining compound 5i with IC50 value of 73nM of binding activity in BRD4(1) and 258nM of cellular activity in MV-4-11 cancer cell lines.	dihydroquinoxalinone	42-62	bromodomain containing 4	Homo sapiens	192-196
27707886-5	2017	Furthermore, ABBV-075 disrupted DHT-stimulated recruitment of BET family member BRD4 to gene-regulatory regions cooccupied by AR, including the well-established PSA and TMPRSS2 enhancers.	Dihydrotestosterone	32-35	bromodomain containing 4	Homo sapiens	80-84
27264992-1	2016	A range of isoxazole-containing amino acids was synthesized that displaced acetyl-lysine-containing peptides from the BAZ2A, BRD4(1), and BRD9 bromodomains.	Isoxazoles	11-20	bromodomain containing 4	Homo sapiens	125-129
27425608-5	2016	A miR-9 mimic represses stimulus-dependent targeting of BRD4 to SEs and blunts Pol II phosphorylation at proximal transcription start sites, without affecting BRD4 binding to SEs that control constitutively expressed cardiac genes.	ses	64-67	bromodomain containing 4	Homo sapiens	56-60
27264992-1	2016	A range of isoxazole-containing amino acids was synthesized that displaced acetyl-lysine-containing peptides from the BAZ2A, BRD4(1), and BRD9 bromodomains.	N(alpha)-acetyllysine	75-88	bromodomain containing 4	Homo sapiens	125-129
27264992-1	2016	A range of isoxazole-containing amino acids was synthesized that displaced acetyl-lysine-containing peptides from the BAZ2A, BRD4(1), and BRD9 bromodomains.	Peptides	100-108	bromodomain containing 4	Homo sapiens	125-129
27264992-5	2016	Selective monoalkylation of a histone H4-mimicking peptide, containing a lysine to cysteine residue substitution (K12C), resulted in acetyl-lysine mimic incorporation, with high affinity for the BRD4 bromodomain.	Peptides	51-58	bromodomain containing 4	Homo sapiens	195-199
27264992-5	2016	Selective monoalkylation of a histone H4-mimicking peptide, containing a lysine to cysteine residue substitution (K12C), resulted in acetyl-lysine mimic incorporation, with high affinity for the BRD4 bromodomain.	Lysine	73-79	bromodomain containing 4	Homo sapiens	195-199
27264992-5	2016	Selective monoalkylation of a histone H4-mimicking peptide, containing a lysine to cysteine residue substitution (K12C), resulted in acetyl-lysine mimic incorporation, with high affinity for the BRD4 bromodomain.	Cysteine	83-91	bromodomain containing 4	Homo sapiens	195-199
27264992-5	2016	Selective monoalkylation of a histone H4-mimicking peptide, containing a lysine to cysteine residue substitution (K12C), resulted in acetyl-lysine mimic incorporation, with high affinity for the BRD4 bromodomain.	k12c	114-118	bromodomain containing 4	Homo sapiens	195-199
27264992-5	2016	Selective monoalkylation of a histone H4-mimicking peptide, containing a lysine to cysteine residue substitution (K12C), resulted in acetyl-lysine mimic incorporation, with high affinity for the BRD4 bromodomain.	N(alpha)-acetyllysine	133-146	bromodomain containing 4	Homo sapiens	195-199
27238211-9	2016	Analysis of the binding interactions revealed that compounds 1 and 2 shared a common quinazolin core structure and bound to BRD4(I) in a non-acetylated lysine mimetic mode.	Lysine	152-158	bromodomain containing 4	Homo sapiens	124-131
27238211-11	2016	Four potential hit-to-lead optimization candidates have been found, two of them bound to BRD4(I) in a non-acetylated lysine mimetic mode, being selective BRD4(I) inhibitors.	Lysine	117-123	bromodomain containing 4	Homo sapiens	89-96
27238211-11	2016	Four potential hit-to-lead optimization candidates have been found, two of them bound to BRD4(I) in a non-acetylated lysine mimetic mode, being selective BRD4(I) inhibitors.	Lysine	117-123	bromodomain containing 4	Homo sapiens	154-161
27142751-0	2016	Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors.	dimethylisoxazoles	94-112	bromodomain containing 4	Homo sapiens	128-132
27219867-0	2016	Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains.	Water	16-21	bromodomain containing 4	Homo sapiens	59-63
26983878-8	2016	BETi preferentially target super-enhancer-regulated genes, and a super-enhancer in c-MYC was recently identified in HCT116 cells to which BRD4 and effector transcription factors of the WNT/beta-catenin/TCF and MEK/ERK pathways are recruited.	beti	0-4	bromodomain containing 4	Homo sapiens	138-142
26536665-10	2016	Finally, we also observe robust antitumor effects of MLN0128 when administered as a dual therapy with JQ1, a bromodomain protein BRD4 inhibitor.	INK128	53-60	bromodomain containing 4	Homo sapiens	129-133
26119939-12	2016	Lenalidomide displayed synergistic cytotoxicity with several structurally distinct BRD4 inhibitors (JQ-1, IBET151 and PFI-1).	Lenalidomide	0-12	bromodomain containing 4	Homo sapiens	83-87
25946208-2	2016	By taking advantage of the specific binding of BRD4 to acetylated lysine residues, we developed a FRET-based probe for visualizing histone H3 acetylation in living cells.	Lysine	66-72	bromodomain containing 4	Homo sapiens	47-51
26878240-6	2016	In turn, 7SK occupancy at enhancers coincides with that of Brd4 and is exquisitely sensitive to the bromodomain inhibitor JQ1.	(2s)-Tert-Butoxy[3-(3,4-Dihydro-2h-1-Benzopyran-6-Yl)-1-Methyl-1h-Indol-2-Yl]acetic Acid	9-12	bromodomain containing 4	Homo sapiens	59-63
26456956-0	2016	Downregulation of miR-329 promotes cell invasion by regulating BRD4 and predicts poor prognosis in hepatocellular carcinoma.	mir-329	18-25	bromodomain containing 4	Homo sapiens	63-67
26456956-11	2016	miR-329 could control cell invasion via regulating BRD4 expression and may be a prognostic marker in HCC.	mir-329	0-7	bromodomain containing 4	Homo sapiens	51-55
26731611-0	2016	4-Acyl Pyrrole Derivatives Yield Novel Vectors for Designing Inhibitors of the Acetyl-Lysine Recognition Site of BRD4(1).	4-acyl pyrrole	0-14	bromodomain containing 4	Homo sapiens	113-117
26731611-0	2016	4-Acyl Pyrrole Derivatives Yield Novel Vectors for Designing Inhibitors of the Acetyl-Lysine Recognition Site of BRD4(1).	N(alpha)-acetyllysine	79-92	bromodomain containing 4	Homo sapiens	113-117
26731611-7	2016	In the study presented here, we designed analogues of 1 to study the potential of substitutions on the 4-acyl pyrrole backbone to occupy additional sites within the substrate recognition site of BRD4(1).	4-acyl pyrrole	103-117	bromodomain containing 4	Homo sapiens	195-199
26735842-1	2016	A midthroughput screening follow-up program targeting the first bromodomain of the human BRD4 protein, BRD4(BD1), identified an acetylated-mimic xanthine derivative inhibitor.	Xanthine	145-153	bromodomain containing 4	Homo sapiens	89-93
26735842-1	2016	A midthroughput screening follow-up program targeting the first bromodomain of the human BRD4 protein, BRD4(BD1), identified an acetylated-mimic xanthine derivative inhibitor.	Xanthine	145-153	bromodomain containing 4	Homo sapiens	103-107
26976114-0	2016	Clinical Response of Carcinomas Harboring the BRD4-NUT Oncoprotein to the Targeted Bromodomain Inhibitor OTX015/MK-8628.	OTX015	112-119	bromodomain containing 4	Homo sapiens	46-50
27063978-1	2016	BACKGROUND: The first-in-class small molecule inhibitor OTX015 (MK-8628) specifically binds to bromodomain motifs BRD2, BRD3, and BRD4 of bromodomain and extraterminal (BET) proteins, inhibiting them from binding to acetylated histones, which occurs preferentially at super-enhancer regions that control oncogene expression.	OTX015	64-71	bromodomain containing 4	Homo sapiens	130-134
26707881-0	2016	Inhibition of BRD4 suppresses tumor growth and enhances iodine uptake in thyroid cancer.	Iodine	56-62	bromodomain containing 4	Homo sapiens	14-18
26707881-6	2016	Inhibition of BRD4 in thyroid cancer cells by JQ1 resulted in cell cycle arrest at G0/G1 phase and enhanced (131)I uptake in vitro and suppressed tumor growth in vivo.	Iodine-131	108-114	bromodomain containing 4	Homo sapiens	14-18
26158404-0	2015	Dual Screening of BPTF and Brd4 Using Protein-Observed Fluorine NMR Uncovers New Bromodomain Probe Molecules.	Fluorine	55-63	bromodomain containing 4	Homo sapiens	27-31
27581642-0	2016	Structure-Activity Relationship Study of N(6)-Benzoyladenine-Type BRD4 Inhibitors and Their Effects on Cell Differentiation and TNF-alpha Production.	N6-benzoyladenine	41-60	bromodomain containing 4	Homo sapiens	66-70
27581642-4	2016	We have reported potent N(6)-benzoyladenine-based inhibitors of BRD4, a BET family member that serves as a key mediator of transcriptional elongation.	N6-benzoyladenine	24-43	bromodomain containing 4	Homo sapiens	64-68
26504077-2	2016	A competition assay, based on a validated chemical kinetic model of steroid hormone action, is now used to identify two new factors (BRD4 and negative elongation factor (NELF)-E) and to define their sites and mechanisms of action.	Steroids	68-83	bromodomain containing 4	Homo sapiens	133-137
26504077-4	2016	Consistent with its complicated biochemistry, BRD4 is shown to alter both the maximal activity (Amax) and the steroid concentration required for half-maximal induction (EC50) of GR-mediated gene expression by acting at a minimum of three different kinetically defined steps.	Steroids	110-117	bromodomain containing 4	Homo sapiens	46-50
27290915-1	2016	BRD4, an epigenetic regulator that recognizes and binds the acetylated lysine residues in histone, has been reported as a potential therapeutic target for cancers.	Lysine	71-77	bromodomain containing 4	Homo sapiens	0-4
27290915-3	2016	In this review, we have systematically summarized a series of BRD4 binding compounds, which are divided into five categories based on the similarity of their chemical structures and respectively referred as JQ1 derivatives, tetrahydroquinoline derivatives, 3,5- dimethylisoxazole derivatives, 2-thiazolidinone derivatives and others.	1,2,3,4-tetrahydroquinoline	224-243	bromodomain containing 4	Homo sapiens	62-66
27290915-3	2016	In this review, we have systematically summarized a series of BRD4 binding compounds, which are divided into five categories based on the similarity of their chemical structures and respectively referred as JQ1 derivatives, tetrahydroquinoline derivatives, 3,5- dimethylisoxazole derivatives, 2-thiazolidinone derivatives and others.	3,5- dimethylisoxazole	257-279	bromodomain containing 4	Homo sapiens	62-66
27290915-3	2016	In this review, we have systematically summarized a series of BRD4 binding compounds, which are divided into five categories based on the similarity of their chemical structures and respectively referred as JQ1 derivatives, tetrahydroquinoline derivatives, 3,5- dimethylisoxazole derivatives, 2-thiazolidinone derivatives and others.	Thiazolidin-2-one	293-309	bromodomain containing 4	Homo sapiens	62-66
26546038-4	2015	Previously, SEs have been defined as having the highest density of Med1, Brd4 or H3K27ac by ChIP-seq.	ses	12-15	bromodomain containing 4	Homo sapiens	73-77
26985285-0	2016	Dihydropteridinone Inhibitors of BRD4.	2-Pteridinol, 3,4-dihydro- (7CI,8CI)	0-18	bromodomain containing 4	Homo sapiens	33-37
26416749-7	2015	The BRD4 inhibitor I-BET151 downregulated these SE-associated genes, yet also has anti-leukaemic activity.	GSK1210151A	19-27	bromodomain containing 4	Homo sapiens	4-8
27148573-7	2015	H3K27ac super-enhancer landscapes near MYC showed a pattern previously reported in acute myeloid leukemia (AML) that is sensitive to BRD4 inhibitors, and in line with this ETP-ALL blasts downregulated MYC in response to the BRD4 inhibitor JQ1.	Ethionamide	172-175	bromodomain containing 4	Homo sapiens	133-137
27148573-7	2015	H3K27ac super-enhancer landscapes near MYC showed a pattern previously reported in acute myeloid leukemia (AML) that is sensitive to BRD4 inhibitors, and in line with this ETP-ALL blasts downregulated MYC in response to the BRD4 inhibitor JQ1.	Ethionamide	172-175	bromodomain containing 4	Homo sapiens	224-228
25537515-6	2015	Furthermore, ChIP assays demonstrate that MYC upregulation in the everolimus resistant lines is mediated by increased association of the BRD4 transcription factor with the MYC gene.	Everolimus	66-76	bromodomain containing 4	Homo sapiens	137-141
26224795-7	2015	METHODS AND RESULTS: BRD4 is upregulated in lungs, distal PAs, and PASMCs of patients with PAH compared with controls.	Protactinium	58-61	bromodomain containing 4	Homo sapiens	21-25
26224795-7	2015	METHODS AND RESULTS: BRD4 is upregulated in lungs, distal PAs, and PASMCs of patients with PAH compared with controls.	pasmcs	67-73	bromodomain containing 4	Homo sapiens	21-25
26224795-9	2015	We further studied the molecular downstream targets of BRD4 by inhibiting its activity in PAH-PASMCs using a clinically available inhibitor JQ1.	pah-pasmcs	90-100	bromodomain containing 4	Homo sapiens	55-59
26083714-5	2015	Essential for this increase, the bromodomain protein BRD4 captures P-TEFb from 7SK snRNP to deliver to target genes and also enhances CDK9"s activity and resistance to inhibition.	(2s)-Tert-Butoxy[3-(3,4-Dihydro-2h-1-Benzopyran-6-Yl)-1-Methyl-1h-Indol-2-Yl]acetic Acid	79-82	bromodomain containing 4	Homo sapiens	53-57
26191363-2	2015	Particularly, replacement of the cyclopentyl group with a 3-bromobenzyl moiety afforded the most potent BRD4 inhibitor of the series (39j) with a K i = 8.7 nM, which was equipotent against PLK1.	3-bromobenzyl	58-71	bromodomain containing 4	Homo sapiens	104-108
26191363-4	2015	Meanwhile, substitution of the pyrimidine NH with an oxygen atom reversed the PLK1/BRD4 selectivity to convert BI-2536 into a BRD4-selective inhibitor, likely owing to the loss of a critical hydrogen bond in PLK1.	pyrimidine	31-41	bromodomain containing 4	Homo sapiens	83-87
26191363-4	2015	Meanwhile, substitution of the pyrimidine NH with an oxygen atom reversed the PLK1/BRD4 selectivity to convert BI-2536 into a BRD4-selective inhibitor, likely owing to the loss of a critical hydrogen bond in PLK1.	pyrimidine	31-41	bromodomain containing 4	Homo sapiens	126-130
26191363-4	2015	Meanwhile, substitution of the pyrimidine NH with an oxygen atom reversed the PLK1/BRD4 selectivity to convert BI-2536 into a BRD4-selective inhibitor, likely owing to the loss of a critical hydrogen bond in PLK1.	Oxygen	53-59	bromodomain containing 4	Homo sapiens	83-87
26191363-4	2015	Meanwhile, substitution of the pyrimidine NH with an oxygen atom reversed the PLK1/BRD4 selectivity to convert BI-2536 into a BRD4-selective inhibitor, likely owing to the loss of a critical hydrogen bond in PLK1.	Oxygen	53-59	bromodomain containing 4	Homo sapiens	126-130
26191363-4	2015	Meanwhile, substitution of the pyrimidine NH with an oxygen atom reversed the PLK1/BRD4 selectivity to convert BI-2536 into a BRD4-selective inhibitor, likely owing to the loss of a critical hydrogen bond in PLK1.	BI 2536	111-118	bromodomain containing 4	Homo sapiens	83-87
26191363-4	2015	Meanwhile, substitution of the pyrimidine NH with an oxygen atom reversed the PLK1/BRD4 selectivity to convert BI-2536 into a BRD4-selective inhibitor, likely owing to the loss of a critical hydrogen bond in PLK1.	BI 2536	111-118	bromodomain containing 4	Homo sapiens	126-130
26191363-4	2015	Meanwhile, substitution of the pyrimidine NH with an oxygen atom reversed the PLK1/BRD4 selectivity to convert BI-2536 into a BRD4-selective inhibitor, likely owing to the loss of a critical hydrogen bond in PLK1.	Hydrogen	191-199	bromodomain containing 4	Homo sapiens	83-87
25647019-0	2015	BRD4 promotes pancreatic ductal adenocarcinoma cell proliferation and enhances gemcitabine resistance.	gemcitabine	79-90	bromodomain containing 4	Homo sapiens	0-4
25647019-6	2015	An in vitro assay showed that the suppression of BRD4 impaired PDAC cell viability and proliferation.	pdac	63-67	bromodomain containing 4	Homo sapiens	49-53
25647019-8	2015	Furthermore, we showed that the expression of BRD4 was increased after treatment with gemcitabine (GEM).	gemcitabine	86-97	bromodomain containing 4	Homo sapiens	46-50
25647019-8	2015	Furthermore, we showed that the expression of BRD4 was increased after treatment with gemcitabine (GEM).	gemcitabine	99-102	bromodomain containing 4	Homo sapiens	46-50
25678016-0	2015	Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors.	N6-benzoyladenine	57-74	bromodomain containing 4	Homo sapiens	96-100
25678016-3	2015	As a part of our continuing structural development studies of thalidomide to obtain a broad spectrum of biological modifiers based on the "multi-template" approach, in this work we focused on BRD4-inhibitory activity, and discovered that N6-benzoyladenine derivatives exhibit this activity.	N6-benzoyladenine	238-255	bromodomain containing 4	Homo sapiens	192-196
25678016-4	2015	Structure-activity relationship studies led to N6-(2,4,5-trimethoxybenzoyl)adenine (29), which exhibits potent BRD4 bromodomain1 inhibitory activity with an IC50 value of 0.427muM.	n6-(2,4,5-trimethoxybenzoyl)adenine	47-82	bromodomain containing 4	Homo sapiens	111-115
25678016-5	2015	N6-Benzoyladenine appears to be a new chemical scaffold for development of BRD4 inhibitors.	N6-benzoyladenine	0-17	bromodomain containing 4	Homo sapiens	75-79
25559428-0	2015	Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2.	2-thiazolidinones	33-50	bromodomain containing 4	Homo sapiens	54-58
25559428-4	2015	Hereby, we report our efforts on discovery and optimization of a new series of 2-thiazolidinones as BRD4 inhibitors along our previous study.	2-thiazolidinones	79-96	bromodomain containing 4	Homo sapiens	100-104
26045013-1	2015	Phthalimide conjugates induce destabilization of target proteins such as BRD4 in vitro and in vivo.	phthalimide	0-11	bromodomain containing 4	Homo sapiens	73-77
26304078-0	2015	[In vitro study of BRD4 inhibitor GSK525762A against primary adult common B-cell acute lymphoblastic leukemia cells in vitro].	molibresib	34-44	bromodomain containing 4	Homo sapiens	19-23
26304078-1	2015	OBJECTIVE: To investigate the effects of bromodomain-containing protein 4 (BRD4) inhibitor GSK525762A on the proliferation and apoptosis of primary common B-cell acute lymphoblastic leukemia (common B-ALL) cells from adult patients, then to further explore the possible mechanisms.	molibresib	91-101	bromodomain containing 4	Homo sapiens	41-73
26304078-1	2015	OBJECTIVE: To investigate the effects of bromodomain-containing protein 4 (BRD4) inhibitor GSK525762A on the proliferation and apoptosis of primary common B-cell acute lymphoblastic leukemia (common B-ALL) cells from adult patients, then to further explore the possible mechanisms.	molibresib	91-101	bromodomain containing 4	Homo sapiens	75-79
26191363-0	2015	BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536.	BI 2536	85-92	bromodomain containing 4	Homo sapiens	0-4
26191363-0	2015	BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536.	BI 2536	85-92	bromodomain containing 4	Homo sapiens	58-62
26191363-1	2015	A focused library of analogues of the dual PLK1 kinase/BRD4 bromodomain inhibitor BI-2536 was prepared and then analyzed for BRD4 and PLK1 inhibitory activities.	BI 2536	82-89	bromodomain containing 4	Homo sapiens	55-59
25944566-2	2015	Here we demonstrate that bromodomain inhibitors (BETi), JQ1, I-BET151, I-BET762, exert potent anti-tumour activity against primary and established OS cell lines, mediated by inhibition of BRD4.	beti	49-53	bromodomain containing 4	Homo sapiens	188-192
25788266-4	2015	Here, we investigated the association between genome-wide occupancy of histone H4 acetylation at lysine 12 (H4K12ac) and BRD4 in the context of estrogen-induced transcription.	Lysine	97-103	bromodomain containing 4	Homo sapiens	121-125
25703523-1	2015	The 2-amine-9H-purine scaffold was identified as a weak bromodomain template and was developed via iterative structure based design into a potent nanomolar ligand for the bromodomain of human BRD9 with small residual micromolar affinity toward the bromodomain of BRD4.	2-amine-9h-purine	4-21	bromodomain containing 4	Homo sapiens	263-267
25603177-1	2015	Post-translational modifications have been identified to be of great importance in cancers and lysine acetylation, which can attract the multifunctional transcription factor BRD4, has been identified as a potential therapeutic target.	Lysine	95-101	bromodomain containing 4	Homo sapiens	174-178
24435446-1	2014	The bromodomain and extra-terminal (BET) protein family members, including BRD4, bind to acetylated lysines on histones and regulate the expression of important oncogenes, for example, c-MYC and BCL2.	Lysine	100-107	bromodomain containing 4	Homo sapiens	75-79
25340539-0	2014	Phosphorylation of HPV-16 E2 at serine 243 enables binding to Brd4 and mitotic chromosomes.	Serine	32-38	bromodomain containing 4	Homo sapiens	62-66
25340539-6	2014	However, substitution by the polar uncharged residues asparagine or glutamine abrogated Brd4 and mitotic chromosome binding.	Asparagine	54-64	bromodomain containing 4	Homo sapiens	88-92
25340539-6	2014	However, substitution by the polar uncharged residues asparagine or glutamine abrogated Brd4 and mitotic chromosome binding.	Glutamine	68-77	bromodomain containing 4	Homo sapiens	88-92
25340539-9	2014	Thus, phosphorylation of serine 243 in the hinge region of HPV-16 E2 is essential for interaction with Brd4 and required for host chromosome binding.	Serine	25-31	bromodomain containing 4	Homo sapiens	103-107
24976024-8	2014	Results reveal that the compounds ZINC01411240, ZINC19632618 and ZINC04818522 could be potential drug candidates for targeting BRD4.	zinc01411240	34-46	bromodomain containing 4	Homo sapiens	127-131
24976024-8	2014	Results reveal that the compounds ZINC01411240, ZINC19632618 and ZINC04818522 could be potential drug candidates for targeting BRD4.	serum sodium transport inhibitor	48-60	bromodomain containing 4	Homo sapiens	127-131
24976024-8	2014	Results reveal that the compounds ZINC01411240, ZINC19632618 and ZINC04818522 could be potential drug candidates for targeting BRD4.	zinc04818522	65-77	bromodomain containing 4	Homo sapiens	127-131
25097667-6	2014	RESULTS: Mutation of a conserved asparagine crucial for binding to acetylated lysines in the bromodomains of BRD3, BRD4 and TRIM24 all resulted in reduction of FRAP recovery times, indicating loss of or significantly reduced binding to acetylated chromatin, as did the addition of known inhibitors.	Asparagine	33-43	bromodomain containing 4	Homo sapiens	115-119
25097667-6	2014	RESULTS: Mutation of a conserved asparagine crucial for binding to acetylated lysines in the bromodomains of BRD3, BRD4 and TRIM24 all resulted in reduction of FRAP recovery times, indicating loss of or significantly reduced binding to acetylated chromatin, as did the addition of known inhibitors.	Lysine	78-85	bromodomain containing 4	Homo sapiens	115-119
24860166-6	2014	Brd4 PID shows a surprising sequence motif similarity to the trans-activating Tat protein from HIV-1, which includes a core RxL motif, a polybasic cluster known as arginine-rich motif, and a C-terminal leucine motif.	Arginine	164-172	bromodomain containing 4	Homo sapiens	0-4
24860166-6	2014	Brd4 PID shows a surprising sequence motif similarity to the trans-activating Tat protein from HIV-1, which includes a core RxL motif, a polybasic cluster known as arginine-rich motif, and a C-terminal leucine motif.	Leucine	202-209	bromodomain containing 4	Homo sapiens	0-4
24860166-7	2014	Mutation of these motifs to alanine significantly diminished the stimulatory effect of Brd4 and fully abrogated its activation potential in presence of Hexim1.	Alanine	28-35	bromodomain containing 4	Homo sapiens	87-91
24985178-0	2014	[Effect of bromdomain protein 4 inhibitor GSK525762A on the proliferation and apoptosis of B-cell acute lymphoblastic leukemia cells and its mechanism].	molibresib	42-52	bromodomain containing 4	Homo sapiens	11-31
24985178-1	2014	OBJECTIVE: To investigate the effect of bromdomain protein 4 (BRD4) inhibitor GSK525762A on the proliferation, apoptosis of B-cell acute lymphoblastic leukemia cell line RS4;11 cells, and to further explore the mechanism.	molibresib	78-88	bromodomain containing 4	Homo sapiens	40-60
24985178-1	2014	OBJECTIVE: To investigate the effect of bromdomain protein 4 (BRD4) inhibitor GSK525762A on the proliferation, apoptosis of B-cell acute lymphoblastic leukemia cell line RS4;11 cells, and to further explore the mechanism.	molibresib	78-88	bromodomain containing 4	Homo sapiens	62-66
24985178-2	2014	METHODS: Compared with Jurkat leukemia cells, the activity of BRD4 on RS4; 11 cells were inhibited by the inhibitor GSK525762A.	molibresib	116-126	bromodomain containing 4	Homo sapiens	62-66
24568369-0	2014	Acetyl-lysine binding site of bromodomain-containing protein 4 (BRD4) interacts with diverse kinase inhibitors.	N(alpha)-acetyllysine	0-13	bromodomain containing 4	Homo sapiens	30-62
24568369-0	2014	Acetyl-lysine binding site of bromodomain-containing protein 4 (BRD4) interacts with diverse kinase inhibitors.	N(alpha)-acetyllysine	0-13	bromodomain containing 4	Homo sapiens	64-68
24568369-3	2014	Among these, the PLK1 inhibitor BI2536 and the JAK2 inhibitor TG101209 displayed strongest inhibitory potential against BRD4 (IC50=25 nM and 130 nM, respectively) and high selectivity for BET bromodomains.	BI 2536	32-38	bromodomain containing 4	Homo sapiens	120-124
24568369-3	2014	Among these, the PLK1 inhibitor BI2536 and the JAK2 inhibitor TG101209 displayed strongest inhibitory potential against BRD4 (IC50=25 nM and 130 nM, respectively) and high selectivity for BET bromodomains.	TG101209	62-70	bromodomain containing 4	Homo sapiens	120-124
25941994-2	2015	Bromodomain protein 4 (BRD4) regulates gene transcription by binding to acetylated histone H3 lysine 27 (H3K27Ac) on the chromatin.	Lysine	94-100	bromodomain containing 4	Homo sapiens	0-21
25941994-2	2015	Bromodomain protein 4 (BRD4) regulates gene transcription by binding to acetylated histone H3 lysine 27 (H3K27Ac) on the chromatin.	Lysine	94-100	bromodomain containing 4	Homo sapiens	23-27
25290579-2	2014	We test the sensitivity, accuracy, and speed of this method with small molecule ligands (+)-JQ1, BI2536, Dinaciclib, TG101348, and acetaminophen using three bromodomains Brd4, BrdT, and BPTF.	Fedratinib	117-125	bromodomain containing 4	Homo sapiens	170-174
25290579-2	2014	We test the sensitivity, accuracy, and speed of this method with small molecule ligands (+)-JQ1, BI2536, Dinaciclib, TG101348, and acetaminophen using three bromodomains Brd4, BrdT, and BPTF.	Acetaminophen	131-144	bromodomain containing 4	Homo sapiens	170-174
25290579-4	2014	Fluorine labeling only modestly affected the Brd4 structure and function assessed by isothermal titration calorimetry, circular dichroism, and X-ray crystallography.	Fluorine	0-8	bromodomain containing 4	Homo sapiens	45-49
25338565-0	2014	[Effect of BRD4 inhibitor GSK525762A on proliferation and apoptosis of KU812 leukemic cells and its mechanism].	molibresib	26-36	bromodomain containing 4	Homo sapiens	11-15
25338565-1	2014	This study was purposed to investigate the effect of bromodomain-containing protein 4 (BRD4) inhibitor GSK525762A on the proliferation and apoptosis of chronic myeloid leukemia blast crisis KU812 cells and its mechanism.	molibresib	103-113	bromodomain containing 4	Homo sapiens	53-85
25338565-1	2014	This study was purposed to investigate the effect of bromodomain-containing protein 4 (BRD4) inhibitor GSK525762A on the proliferation and apoptosis of chronic myeloid leukemia blast crisis KU812 cells and its mechanism.	molibresib	103-113	bromodomain containing 4	Homo sapiens	87-91
24939842-5	2014	Here, we report a novel role of phosphorylated Ser(10) of histone H3 (H3S10ph) in governing the functional transition of BRD4.	Serine	47-50	bromodomain containing 4	Homo sapiens	121-125
24939842-5	2014	Here, we report a novel role of phosphorylated Ser(10) of histone H3 (H3S10ph) in governing the functional transition of BRD4.	histone h3	58-68	bromodomain containing 4	Homo sapiens	121-125
24939842-5	2014	Here, we report a novel role of phosphorylated Ser(10) of histone H3 (H3S10ph) in governing the functional transition of BRD4.	h3s10ph	70-77	bromodomain containing 4	Homo sapiens	121-125
24939842-6	2014	We identified that the acetylated lysines 5 and 8 of nucleosomal histone H4 (H4K5ac/K8ac) is the BRD4 binding site, and the protein phosphatase PP1alpha and class I histone deacetylase (HDAC1/2/3) signaling pathways are essential for the stress-induced BRD4 release from chromatin.	Lysine	34-41	bromodomain containing 4	Homo sapiens	97-101
24939842-6	2014	We identified that the acetylated lysines 5 and 8 of nucleosomal histone H4 (H4K5ac/K8ac) is the BRD4 binding site, and the protein phosphatase PP1alpha and class I histone deacetylase (HDAC1/2/3) signaling pathways are essential for the stress-induced BRD4 release from chromatin.	Lysine	34-41	bromodomain containing 4	Homo sapiens	253-257
24939842-7	2014	In the unstressed state, phosphorylated H3S10 prevents the deacetylation of nucleosomal H4K5ac/K8ac by HDAC1/2/3, thereby locking up the majority of BRD4 onto chromatin.	h3s10	40-45	bromodomain containing 4	Homo sapiens	149-153
24939842-8	2014	Upon stress, PP1alpha-mediated dephosphorylation of H3S10ph allows the deacetylation of nucleosomal H4K5ac/K8ac by HDAC1/2/3, thereby leading to the release of chromatin-bound BRD4 for subsequent recruitment of P-TEFb to enhance the expression of inducible genes.	h3s10ph	52-59	bromodomain containing 4	Homo sapiens	176-180
24939842-9	2014	Therefore, our study revealed a novel mechanism that the histone cross-talk between H3S10ph and H4K5ac/K8ac connects PP1alpha and HDACs to govern the functional transition of BRD4.	h3s10ph	84-91	bromodomain containing 4	Homo sapiens	175-179
24972113-8	2014	We have shown chemical probes (e.g., BD-2) made from such linkers could be used for simultaneous in situ imaging and covalent labeling of endogenous BRD-4 (an important epigenetic protein) via a rapid, copper-free, tetrazine-cyclopropene ligation reaction (k2 > 5 M(-1) s(-1)).	Copper	202-208	bromodomain containing 4	Homo sapiens	149-154
24972113-8	2014	We have shown chemical probes (e.g., BD-2) made from such linkers could be used for simultaneous in situ imaging and covalent labeling of endogenous BRD-4 (an important epigenetic protein) via a rapid, copper-free, tetrazine-cyclopropene ligation reaction (k2 > 5 M(-1) s(-1)).	1,2,3,4-tetrazine	215-224	bromodomain containing 4	Homo sapiens	149-154
24972113-8	2014	We have shown chemical probes (e.g., BD-2) made from such linkers could be used for simultaneous in situ imaging and covalent labeling of endogenous BRD-4 (an important epigenetic protein) via a rapid, copper-free, tetrazine-cyclopropene ligation reaction (k2 > 5 M(-1) s(-1)).	cyclopropene	225-237	bromodomain containing 4	Homo sapiens	149-154
24972113-9	2014	The key features of our cyclopropenes, with their unique C-1 linkage to BRD-4-targeting moiety, are their tunable reactivity and solubility, relative stability, and synthetic accessibility.	cyclopropene	24-37	bromodomain containing 4	Homo sapiens	72-77
25120803-5	2014	Moreover immunohistochemistry (ICH) was used to detect the expression of BRD4 in UCBs.	ucbs	81-85	bromodomain containing 4	Homo sapiens	73-77
24767840-3	2014	Using a fragment-based in silico screening approach, we identified two small molecules that bind to the first bromodomain of BRD4 with low-micromolar affinity and favorable ligand efficiency (0.37 kcal/mol per non-hydrogen atom), selectively over other families of bromodomains.	Hydrogen	214-222	bromodomain containing 4	Homo sapiens	125-129
24733848-3	2014	The bromodomain and extraterminal (BET) proteins, Brd2, Brd3, Brd4, and BrdT, bind to acetylated lysine residues on histone or nonhistone proteins recruiting transcriptional regulators and thus activating or repressing gene transcription.	Lysine	97-103	bromodomain containing 4	Homo sapiens	62-66
24763052-4	2014	Knock down of BRD4 or treatment with the BRD4 inhibitor JQ1 resulted in decreased reactive oxygen species (ROS) production and increased cell viability under H2O2 exposure.	Reactive Oxygen Species	82-105	bromodomain containing 4	Homo sapiens	14-18
24763052-4	2014	Knock down of BRD4 or treatment with the BRD4 inhibitor JQ1 resulted in decreased reactive oxygen species (ROS) production and increased cell viability under H2O2 exposure.	Reactive Oxygen Species	82-105	bromodomain containing 4	Homo sapiens	41-45
24763052-4	2014	Knock down of BRD4 or treatment with the BRD4 inhibitor JQ1 resulted in decreased reactive oxygen species (ROS) production and increased cell viability under H2O2 exposure.	Reactive Oxygen Species	107-110	bromodomain containing 4	Homo sapiens	14-18
24763052-4	2014	Knock down of BRD4 or treatment with the BRD4 inhibitor JQ1 resulted in decreased reactive oxygen species (ROS) production and increased cell viability under H2O2 exposure.	Reactive Oxygen Species	107-110	bromodomain containing 4	Homo sapiens	41-45
24533473-2	2014	Quantitative chemoproteomic profiling shows that LY294002 and LY303511, a close analogue devoid of PI3K activity, inhibit the BET bromodomain proteins BRD2, BRD3, and BRD4 that comprise a family of targets structurally unrelated to PI3K.	2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one	49-57	bromodomain containing 4	Homo sapiens	167-171
24763052-4	2014	Knock down of BRD4 or treatment with the BRD4 inhibitor JQ1 resulted in decreased reactive oxygen species (ROS) production and increased cell viability under H2O2 exposure.	Hydrogen Peroxide	158-162	bromodomain containing 4	Homo sapiens	14-18
24763052-4	2014	Knock down of BRD4 or treatment with the BRD4 inhibitor JQ1 resulted in decreased reactive oxygen species (ROS) production and increased cell viability under H2O2 exposure.	Hydrogen Peroxide	158-162	bromodomain containing 4	Homo sapiens	41-45
24584072-8	2014	The BRD4 inhibitor JQ1 downregulates expression of these targets and induces growth arrest and apoptosis in persister cells, at doses well tolerated by GSI-sensitive cells.	2-(5-Chlorothiophen-2-Yl)-N-[(3s)-1-(4-{2-[(Dimethylamino)methyl]-1h-Imidazol-1-Yl}-2-Fluorophenyl)-2-Oxopyrrolidin-3-Yl]ethanesulfonamide	152-155	bromodomain containing 4	Homo sapiens	4-8
24584101-5	2014	Nanomolar activity on BRD4 by BI-2536 and TG-101348, which are clinical PLK1 and JAK2-FLT3 kinase inhibitors, respectively, is particularly noteworthy as these combinations of activities on independent oncogenic pathways exemplify a new strategy for rational single-agent polypharmacological targeting.	Bismuth	30-32	bromodomain containing 4	Homo sapiens	22-26
24584101-5	2014	Nanomolar activity on BRD4 by BI-2536 and TG-101348, which are clinical PLK1 and JAK2-FLT3 kinase inhibitors, respectively, is particularly noteworthy as these combinations of activities on independent oncogenic pathways exemplify a new strategy for rational single-agent polypharmacological targeting.	Thioguanine	42-44	bromodomain containing 4	Homo sapiens	22-26
24576043-6	2014	For example, drugs such as triptolide that targets the general transcription factors TFIIH and JQ1 to inhibit BRD4 are administered to target the high proliferative rate of cancer cells.	triptolide	27-37	bromodomain containing 4	Homo sapiens	110-114
24533473-2	2014	Quantitative chemoproteomic profiling shows that LY294002 and LY303511, a close analogue devoid of PI3K activity, inhibit the BET bromodomain proteins BRD2, BRD3, and BRD4 that comprise a family of targets structurally unrelated to PI3K.	LY 303511	62-70	bromodomain containing 4	Homo sapiens	167-171
24313754-2	2014	Commercially sourced and de novo synthesized substituted [1,2,4]triazolo[4,3-a]phthalazines are potent inhibitors of both the BET bromodomains such as BRD4 as well as bromodomains outside the BET family such as BRD9, CECR2, and CREBBP.	[1,2,4]triazolo[4,3-a]phthalazines	57-91	bromodomain containing 4	Homo sapiens	151-155
23752175-10	2013	Western blotting and reverse transcription-PCR confirm that c-MYC, CDC25A and BRD4 are all downregulated after treatment with KPT-276.	KPT-276	126-133	bromodomain containing 4	Homo sapiens	78-82
24360279-4	2013	Brd4-dependent JMJD6 recruitment on A-PEs mediates erasure of H4R3me(2(s)), which is directly read by 7SK snRNA, and decapping/demethylation of 7SK snRNA, ensuring the dismissal of the 7SK snRNA/HEXIM inhibitory complex.	(2s)-Tert-Butoxy[3-(3,4-Dihydro-2h-1-Benzopyran-6-Yl)-1-Methyl-1h-Indol-2-Yl]acetic Acid	102-105	bromodomain containing 4	Homo sapiens	0-4
24360279-4	2013	Brd4-dependent JMJD6 recruitment on A-PEs mediates erasure of H4R3me(2(s)), which is directly read by 7SK snRNA, and decapping/demethylation of 7SK snRNA, ensuring the dismissal of the 7SK snRNA/HEXIM inhibitory complex.	(2s)-Tert-Butoxy[3-(3,4-Dihydro-2h-1-Benzopyran-6-Yl)-1-Methyl-1h-Indol-2-Yl]acetic Acid	144-147	bromodomain containing 4	Homo sapiens	0-4
24360279-4	2013	Brd4-dependent JMJD6 recruitment on A-PEs mediates erasure of H4R3me(2(s)), which is directly read by 7SK snRNA, and decapping/demethylation of 7SK snRNA, ensuring the dismissal of the 7SK snRNA/HEXIM inhibitory complex.	(2s)-Tert-Butoxy[3-(3,4-Dihydro-2h-1-Benzopyran-6-Yl)-1-Methyl-1h-Indol-2-Yl]acetic Acid	144-147	bromodomain containing 4	Homo sapiens	0-4
24360279-4	2013	Brd4-dependent JMJD6 recruitment on A-PEs mediates erasure of H4R3me(2(s)), which is directly read by 7SK snRNA, and decapping/demethylation of 7SK snRNA, ensuring the dismissal of the 7SK snRNA/HEXIM inhibitory complex.	hexim	195-200	bromodomain containing 4	Homo sapiens	0-4
23086925-0	2012	Bromodomain-containing protein 4 (BRD4) regulates RNA polymerase II serine 2 phosphorylation in human CD4+ T cells.	Serine	68-74	bromodomain containing 4	Homo sapiens	0-32
23576556-5	2013	Cocrystal structures showed that PFI-1 acts as an acetyl-lysine (Kac) mimetic inhibitor efficiently occupying the Kac binding site in BRD4 and BRD2.	N(alpha)-acetyllysine	50-63	bromodomain containing 4	Homo sapiens	134-138
23576556-5	2013	Cocrystal structures showed that PFI-1 acts as an acetyl-lysine (Kac) mimetic inhibitor efficiently occupying the Kac binding site in BRD4 and BRD2.	4-Quinolinecarbamic acid, 2-butoxy-, 2-(diethylamino)ethyl ester	65-68	bromodomain containing 4	Homo sapiens	134-138
23530754-0	2013	Fragment-based drug discovery of 2-thiazolidinones as inhibitors of the histone reader BRD4 bromodomain.	2-thiazolidinones	33-50	bromodomain containing 4	Homo sapiens	87-91
24015967-2	2013	This paper describes the discovery and structure-activity relationships (SAR) of potent benzodiazepine inhibitors that disrupt the function of the BET family of bromodomains (BRD2, BRD3, and BRD4).	Benzodiazepines	88-102	bromodomain containing 4	Homo sapiens	191-195
24100334-5	2013	It is also advised to avoid DMSO when searching for low-affinity fragments that interact with bromodomains since DMSO binds in the acetylated lysine-recognition pocket of BRD4.	Dimethyl Sulfoxide	113-117	bromodomain containing 4	Homo sapiens	171-175
24100334-5	2013	It is also advised to avoid DMSO when searching for low-affinity fragments that interact with bromodomains since DMSO binds in the acetylated lysine-recognition pocket of BRD4.	Lysine	142-148	bromodomain containing 4	Homo sapiens	171-175
23762261-8	2013	Clusters of retinoid-regulated genes were selectively dependent on BRD4 and/or AF9 expression, which correlated with RAR association to transcribed regions.	Retinoids	12-20	bromodomain containing 4	Homo sapiens	67-71
23517011-4	2013	Cellular studies demonstrate that the phenol and acetate derivatives of the lead compounds showed strong antiproliferative effects on MV4;11 acute myeloid leukemia cells, as shown for other BET bromodomain inhibitors and genetic BRD4 knockdown, whereas the reported compounds showed no general cytotoxicity in other cancer cell lines tested.	Phenol	38-44	bromodomain containing 4	Homo sapiens	229-233
23517011-4	2013	Cellular studies demonstrate that the phenol and acetate derivatives of the lead compounds showed strong antiproliferative effects on MV4;11 acute myeloid leukemia cells, as shown for other BET bromodomain inhibitors and genetic BRD4 knockdown, whereas the reported compounds showed no general cytotoxicity in other cancer cell lines tested.	Acetates	49-56	bromodomain containing 4	Homo sapiens	229-233
23086925-0	2012	Bromodomain-containing protein 4 (BRD4) regulates RNA polymerase II serine 2 phosphorylation in human CD4+ T cells.	Serine	68-74	bromodomain containing 4	Homo sapiens	34-38
23086925-2	2012	We used genome-wide chromatin immunoprecipitation sequencing in primary human CD4+ T cells to reveal that BRD4 co-localizes with Ser-2-phosphorylated Pol II (Pol II Ser-2) at both enhancers and promoters of active genes.	Serine	129-132	bromodomain containing 4	Homo sapiens	106-110
23086925-2	2012	We used genome-wide chromatin immunoprecipitation sequencing in primary human CD4+ T cells to reveal that BRD4 co-localizes with Ser-2-phosphorylated Pol II (Pol II Ser-2) at both enhancers and promoters of active genes.	Serine	165-168	bromodomain containing 4	Homo sapiens	106-110
23086925-4	2012	A large number of JQ1-disrupted BRD4 binding regions exhibited diacetylated H4 (lysine 5 and -8) and H3K27 acetylation (H3K27ac), which correlated with the presence of histone acetyltransferases and deacetylases.	Lysine	80-86	bromodomain containing 4	Homo sapiens	32-36
23086925-7	2012	Our findings suggest that BRD4-driven Pol II phosphorylation at serine 2 plays an important role in regulating lineage-specific gene transcription in human CD4+ T cells.	Serine	64-70	bromodomain containing 4	Homo sapiens	26-30
23027873-5	2012	BRD4 phosphorylates PTEFb/CDK9 at either Thr-29 or Thr-186, depending on its relative abundance, which represses or activates CDK9 CTD kinase activity, respectively.	Threonine	41-44	bromodomain containing 4	Homo sapiens	0-4
23154982-3	2012	The expression of p15(INK4b), a cyclin-dependent kinase inhibitor (CDKI) gene, in PGCs is selectively activated by P-TEFb and its recruiting molecule, Brd4, when the amount of active P-TEFb is increased due to reduction of the 7SK snRNP, and PGCs consequently undergo growth arrest.	(2s)-Tert-Butoxy[3-(3,4-Dihydro-2h-1-Benzopyran-6-Yl)-1-Methyl-1h-Indol-2-Yl]acetic Acid	227-230	bromodomain containing 4	Homo sapiens	151-155
23027873-5	2012	BRD4 phosphorylates PTEFb/CDK9 at either Thr-29 or Thr-186, depending on its relative abundance, which represses or activates CDK9 CTD kinase activity, respectively.	Threonine	51-54	bromodomain containing 4	Homo sapiens	0-4
22952229-8	2012	Indeed, JQ1 transiently increased levels of free P-TEFb and BRD4 P-TEFb and SEC P-TEFb complexes in cells.	sec p-tefb	76-86	bromodomain containing 4	Homo sapiens	60-64
22645123-4	2012	We showed that our BET (Bromodomain and Extra-Terminal domain)-specific bromodomain inhibitor MS417, designed to block BRD4 binding to the acetylated NF-kappaB, effectively attenuates NF-kappaB transcriptional activation of proinflammatory genes in kidney cells treated with TNFalpha or infected by HIV.	MS417	94-99	bromodomain containing 4	Homo sapiens	119-123
22649058-2	2012	IKKalpha can also be recruited directly to the promoter of NF-kappaB-dependent genes by NF-kappaB where it phosphorylates histone H3 at serine 10, triggering recruitment of the bromodomain-containing protein 4 and the positive transcription elongation factor b. Herein, we report that IKKalpha travels with the elongating form of ribonucleic acid polymerase II together with heterochromatin protein 1 gamma (HP1gamma) at NF-kappaB-dependent genes in activated macrophages.	Serine	136-142	bromodomain containing 4	Homo sapiens	177-209
22544982-1	2012	A novel MCAP-cycloaddition sequence has been applied to the facile synthesis of beta-carboline intermediates to gain rapid access to novel derivatives of yohimbine-like and corynanthe-like compounds that may be easily diversified by cross-coupling reactions and N-derivatizations to generate small compound libraries.	norharman	80-94	bromodomain containing 4	Homo sapiens	8-12
22509028-4	2012	We report that BRD4 is an atypical kinase that binds to the carboxyl-terminal domain (CTD) of RNA polymerase II and directly phosphorylates its serine 2 (Ser2) sites both in vitro and in vivo under conditions where other CTD kinases are inactive.	serine 2	144-152	bromodomain containing 4	Homo sapiens	15-19
22544982-1	2012	A novel MCAP-cycloaddition sequence has been applied to the facile synthesis of beta-carboline intermediates to gain rapid access to novel derivatives of yohimbine-like and corynanthe-like compounds that may be easily diversified by cross-coupling reactions and N-derivatizations to generate small compound libraries.	Yohimbine	154-163	bromodomain containing 4	Homo sapiens	8-12
17942543-5	2008	In the presence of roscovitine, IE2, cyclin T1, Brd4, HDAC1, and HDAC2 accumulate at the transcriptosome.	Roscovitine	19-30	bromodomain containing 4	Homo sapiens	48-52
21890894-4	2011	Here, by analyzing the dynamics of Brd4 during ultraviolet or hexamethylene bisacetamide treatment, we show that the signal-induced release of chromatin-bound Brd4 is essential for its functional transition.	hexamethylene bisacetamide	62-88	bromodomain containing 4	Homo sapiens	35-39
21890894-4	2011	Here, by analyzing the dynamics of Brd4 during ultraviolet or hexamethylene bisacetamide treatment, we show that the signal-induced release of chromatin-bound Brd4 is essential for its functional transition.	hexamethylene bisacetamide	62-88	bromodomain containing 4	Homo sapiens	159-163
21890894-6	2011	Upon treatment, Brd4 is released from chromatin, mostly due to signal-triggered deacetylation of nucleosomal histone H4 at acetylated-lysine 5/8 (H4K5ac/K8ac).	acetylated-lysine	123-140	bromodomain containing 4	Homo sapiens	16-20
21983563-3	2011	RNA polymerase II large subunit (Pol II) and bromodomain protein 4 (BRD4) were recruited to the locus in a different sequential order on interphase initiation versus post-mitotic re-activation resulting from the recognition by BRD4 of increased levels of histone H4 Lys 5 acetylation (H4K5ac) on the previously activated locus.	Lysine	266-269	bromodomain containing 4	Homo sapiens	45-66
21983563-3	2011	RNA polymerase II large subunit (Pol II) and bromodomain protein 4 (BRD4) were recruited to the locus in a different sequential order on interphase initiation versus post-mitotic re-activation resulting from the recognition by BRD4 of increased levels of histone H4 Lys 5 acetylation (H4K5ac) on the previously activated locus.	Lysine	266-269	bromodomain containing 4	Homo sapiens	68-72
21983563-3	2011	RNA polymerase II large subunit (Pol II) and bromodomain protein 4 (BRD4) were recruited to the locus in a different sequential order on interphase initiation versus post-mitotic re-activation resulting from the recognition by BRD4 of increased levels of histone H4 Lys 5 acetylation (H4K5ac) on the previously activated locus.	Lysine	266-269	bromodomain containing 4	Homo sapiens	227-231
20715035-0	2010	Interaction of propionylated and butyrylated histone H3 lysine marks with Brd4 bromodomains.	Lysine	56-62	bromodomain containing 4	Homo sapiens	74-78
20808803-5	2010	Glycerol gradient sedimentation analysis was used to demonstrate that the same Brd4 protein transfected into HeLa cells caused the release of P-TEFb and HEXIM1 from the 7SK snRNP in vivo.	Glycerol	0-8	bromodomain containing 4	Homo sapiens	79-83
20201073-8	2010	Lastly, both the Brd4 and HEXIM1 proteins interact with P-TEFb at or very near speckle domains and treatment of cells with the Cdk9 inhibitor flavopiridol alters this distribution.	alvocidib	142-154	bromodomain containing 4	Homo sapiens	17-21
20495683-1	2009	Bromodomain-containing protein 4 (Brd4) contains two tandem bromodomains (BD1 and BD2) that bind preferentially to acetylated lysine residues found in histones and nonhistone proteins.	Lysine	126-132	bromodomain containing 4	Homo sapiens	0-32
20495683-1	2009	Bromodomain-containing protein 4 (Brd4) contains two tandem bromodomains (BD1 and BD2) that bind preferentially to acetylated lysine residues found in histones and nonhistone proteins.	Lysine	126-132	bromodomain containing 4	Homo sapiens	34-38
22084242-4	2012	Notably, P-TEFb complexes associated with short BRD4 contain HEXIM1 and 7SK snRNA, implicating the PID in the liberation of P-TEFb from the 7SK small nuclear ribonucleoprotein complex (7SK snPNP).	(2s)-Tert-Butoxy[3-(3,4-Dihydro-2h-1-Benzopyran-6-Yl)-1-Methyl-1h-Indol-2-Yl]acetic Acid	72-75	bromodomain containing 4	Homo sapiens	48-52
22084242-4	2012	Notably, P-TEFb complexes associated with short BRD4 contain HEXIM1 and 7SK snRNA, implicating the PID in the liberation of P-TEFb from the 7SK small nuclear ribonucleoprotein complex (7SK snPNP).	(2s)-Tert-Butoxy[3-(3,4-Dihydro-2h-1-Benzopyran-6-Yl)-1-Methyl-1h-Indol-2-Yl]acetic Acid	140-143	bromodomain containing 4	Homo sapiens	48-52
22046134-10	2011	The Brd4 inhibitor JQ1 and the pTEFb inhibitors DRB and Flavopiridol significantly reduce Cp, but not LMP1 transcript production indicating that Brd4 and pTEFb are required for Cp transcription.	alvocidib	56-68	bromodomain containing 4	Homo sapiens	145-149
20871596-5	2010	High potency and specificity towards a subset of human bromodomains is explained by co-crystal structures with bromodomain and extra-terminal (BET) family member BRD4, revealing excellent shape complementarity with the acetyl-lysine binding cavity.	N(alpha)-acetyllysine	219-232	bromodomain containing 4	Homo sapiens	162-166
19828451-4	2009	Complex formation of BD1 with a histone H3 tail polypeptide encompassing residues 12-19 showed binding of the Nzeta-acetylated lysine 14 to the conserved asparagine 140 of Brd4.	nzeta-acetylated lysine	110-133	bromodomain containing 4	Homo sapiens	172-176
19828451-4	2009	Complex formation of BD1 with a histone H3 tail polypeptide encompassing residues 12-19 showed binding of the Nzeta-acetylated lysine 14 to the conserved asparagine 140 of Brd4.	Asparagine	154-164	bromodomain containing 4	Homo sapiens	172-176
19103749-2	2009	In this study, we demonstrate that bromodomains of Brd4 bind to acetylated lysine-310.	Lysine	75-81	bromodomain containing 4	Homo sapiens	51-55
19103749-3	2009	Brd4 enhances transcriptional activation of NF-kappaB and the expression of a subset of NF-kappaB-responsive inflammatory genes in an acetylated lysine-310-dependent manner.	Lysine	145-151	bromodomain containing 4	Homo sapiens	0-4
19103749-4	2009	Bromodomains of Brd4 and acetylated lysine-310 of RelA are both required for the mutual interaction and coactivation function of Brd4.	Lysine	36-42	bromodomain containing 4	Homo sapiens	129-133
19103749-6	2009	Our results identify Brd4 as a novel coactivator of NF-kappaB through specifically binding to acetylated lysine-310 of RelA.	Lysine	105-111	bromodomain containing 4	Homo sapiens	21-25
17088358-6	2007	Site-directed mutagenesis of a serine residue at position 62 of McaP, predicted to be important for the lipolytic activity of the protein, resulted in loss of hydrolysis of p-nitrophenyl ester of caproate.	Serine	31-37	bromodomain containing 4	Homo sapiens	64-68
17088358-6	2007	Site-directed mutagenesis of a serine residue at position 62 of McaP, predicted to be important for the lipolytic activity of the protein, resulted in loss of hydrolysis of p-nitrophenyl ester of caproate.	p-nitrophenyl ester	173-192	bromodomain containing 4	Homo sapiens	64-68
17088358-6	2007	Site-directed mutagenesis of a serine residue at position 62 of McaP, predicted to be important for the lipolytic activity of the protein, resulted in loss of hydrolysis of p-nitrophenyl ester of caproate.	hexanoic acid	196-204	bromodomain containing 4	Homo sapiens	64-68
16611886-4	2006	By analyzing the binding of Brd4 to a series of alanine-scanning substitution mutants of the human papillomavirus type 16 E2 N-terminal transactivation domain, we found that amino acids required for Brd4 binding were also required for transcriptional activation but not for viral DNA replication.	Alanine	48-55	bromodomain containing 4	Homo sapiens	28-32
16542442-9	2006	CONCLUSION: Docetaxel may be considered for initial chemotherapy in young patients presenting with a midline carcinoma with bone marrow involvement and cytogenetic and molecular genetic finding of a t(15;19)/BRD4-NUT-rearrangement.	Docetaxel	12-21	bromodomain containing 4	Homo sapiens	208-212
12840145-9	2003	Providing biochemical support, salt solubility of Brd4 was markedly reduced upon increased histone acetylation.	Salts	31-35	bromodomain containing 4	Homo sapiens	50-54
16339075-4	2006	We found that Brd4 was rapidly released from chromosomes upon treatment with antimicrotubule drugs, including the reversible agent nocodazole.	Nocodazole	131-141	bromodomain containing 4	Homo sapiens	14-18
16339075-5	2006	Yet, when nocodazole was withdrawn, Brd4 was reloaded onto chromosomes, and cells proceeded to complete cell division.	Nocodazole	10-20	bromodomain containing 4	Homo sapiens	36-40
16339075-7	2006	Consequently, Brd4+/- cells were impaired in their ability to recover from nocodazole-induced mitotic arrest: a large fraction of +/- cells failed to reach anaphase after drug withdrawal, and those that entered anaphase showed an increased frequency of abnormal chromosomal segregation.	Nocodazole	75-85	bromodomain containing 4	Homo sapiens	14-18
16339075-8	2006	The reloading defect observed in Brd4+/- cells coincided with selective hypoacetylation of lysine residues on H3 and H4.	Lysine	91-97	bromodomain containing 4	Homo sapiens	33-37
16339075-9	2006	The histone deacetylase inhibitor trichostatin A increased global histone acetylation and perturbed nocodazole-induced Brd4 unloading.	trichostatin A	34-48	bromodomain containing 4	Homo sapiens	119-123
16339075-9	2006	The histone deacetylase inhibitor trichostatin A increased global histone acetylation and perturbed nocodazole-induced Brd4 unloading.	Nocodazole	100-110	bromodomain containing 4	Homo sapiens	119-123
16542442-0	2006	Midline carcinoma with t(15;19) and BRD4-NUT fusion oncogene in a 30-year-old female with response to docetaxel and radiotherapy.	Docetaxel	102-111	bromodomain containing 4	Homo sapiens	36-40
16109377-4	2005	In stress-induced cells, the 7SK/HEXIM1-bound P-TEFb is quantitatively converted into the Brd4-associated form.	(2s)-Tert-Butoxy[3-(3,4-Dihydro-2h-1-Benzopyran-6-Yl)-1-Methyl-1h-Indol-2-Yl]acetic Acid	29-32	bromodomain containing 4	Homo sapiens	90-94
9048422-4	1996	The McAP precursor contains an amino Cys(St-Bu) and an internal Lys(Ser).	amino cys	31-40	bromodomain containing 4	Homo sapiens	4-8
9048422-4	1996	The McAP precursor contains an amino Cys(St-Bu) and an internal Lys(Ser).	st-bu	41-46	bromodomain containing 4	Homo sapiens	4-8
9048422-4	1996	The McAP precursor contains an amino Cys(St-Bu) and an internal Lys(Ser).	Lysine	64-67	bromodomain containing 4	Homo sapiens	4-8
9048422-4	1996	The McAP precursor contains an amino Cys(St-Bu) and an internal Lys(Ser).	Serine	68-71	bromodomain containing 4	Homo sapiens	4-8
7549530-1	1995	Determination of chloramphenicol (CAP) residues in egg by gas chromatography/high-resolution mass spectrometry (GC/HRMS) with negative chemical ionization and gas chromatography with electron capture detection (GC-ECD) is described.	Chloramphenicol	17-32	bromodomain containing 4	Homo sapiens	34-37
7549530-2	1995	A cleanup based on acetonitrile extraction followed by solid-phase extraction with silica gel and gel filtration columns was developed for extraction of CAP residues from whole egg.	acetonitrile	19-31	bromodomain containing 4	Homo sapiens	153-156
33972798-0	2021	Cell-surface SLC nucleoside transporters and purine levels modulate BRD4-dependent chromatin states.	purine	45-51	bromodomain containing 4	Homo sapiens	68-72
33972798-6	2021	Intersection of the two orthogonal approaches reveal that loss of transporters involved with purine transport or inhibition of de novo purine synthesis lead to dysfunction of BRD4-dependent transcriptional regulation.	purine	93-99	bromodomain containing 4	Homo sapiens	175-179
33972798-6	2021	Intersection of the two orthogonal approaches reveal that loss of transporters involved with purine transport or inhibition of de novo purine synthesis lead to dysfunction of BRD4-dependent transcriptional regulation.	purine	135-141	bromodomain containing 4	Homo sapiens	175-179
33798846-0	2021	Design, synthesis, and biological activity evaluation of a series of novel sulfonamide derivatives as BRD4 inhibitors against acute myeloid leukemia.	Sulfonamides	75-86	bromodomain containing 4	Homo sapiens	102-106
33972798-7	2021	Through mechanistic characterization of the metabolic circuitry, we elucidate the convergence of SLC-mediated purine uptake and de novo purine synthesis on BRD4-chromatin occupancy.	purine	110-116	bromodomain containing 4	Homo sapiens	156-160
33972798-7	2021	Through mechanistic characterization of the metabolic circuitry, we elucidate the convergence of SLC-mediated purine uptake and de novo purine synthesis on BRD4-chromatin occupancy.	purine	136-142	bromodomain containing 4	Homo sapiens	156-160
33972798-8	2021	Moreover, adenine-related metabolite supplementation effectively restores BRD4 functionality on purine impairment.	Adenine	10-17	bromodomain containing 4	Homo sapiens	74-78
33798846-2	2021	In this study, we disclosed a series of phenylisoxazole sulfonamide derivatives as potent BRD4 inhibitors.	phenylisoxazole sulfonamide	40-67	bromodomain containing 4	Homo sapiens	90-94
33972798-8	2021	Moreover, adenine-related metabolite supplementation effectively restores BRD4 functionality on purine impairment.	purine	96-102	bromodomain containing 4	Homo sapiens	74-78
33972798-9	2021	Our study highlights the specific role of purine/adenine metabolism in modulating BRD4-dependent epigenetic states.	purine	42-48	bromodomain containing 4	Homo sapiens	82-86
33972798-9	2021	Our study highlights the specific role of purine/adenine metabolism in modulating BRD4-dependent epigenetic states.	Adenine	49-56	bromodomain containing 4	Homo sapiens	82-86
33799525-6	2021	In addition, we explore the role of BRD4"s acetyl-lysine binding bromodomains in mediating these interactions by using a highly selective competitive bromodomain inhibitor.	N(alpha)-acetyllysine	43-56	bromodomain containing 4	Homo sapiens	36-40
33802888-0	2021	Synthesis and Structure-Activity Relationships of Aristoyagonine Derivatives as Brd4 Bromodomain Inhibitors with X-ray Co-Crystal Research.	aristoyagonine	50-64	bromodomain containing 4	Homo sapiens	80-84
33802888-4	2021	Herein, we report the design, synthesis, and X-ray studies of novel aristoyagonine (benzo[6,7]oxepino[4,3,2-cd]isoindol-2(1H)-one) derivatives and investigate their inhibitory effect against Brd4 bromodomain.	aristoyagonine	68-82	bromodomain containing 4	Homo sapiens	191-195
33802888-4	2021	Herein, we report the design, synthesis, and X-ray studies of novel aristoyagonine (benzo[6,7]oxepino[4,3,2-cd]isoindol-2(1H)-one) derivatives and investigate their inhibitory effect against Brd4 bromodomain.	benzo[6,7]oxepino[4,3,2-cd]isoindol-2(1h)-one	84-129	bromodomain containing 4	Homo sapiens	191-195
33802888-6	2021	Co-crystal structures of these five inhibitors with human Brd4 bromodomain demonstrated that it has a key binding mode occupying the hydrophobic pocket, which is known to be the acetylated lysine binding site.	Lysine	189-195	bromodomain containing 4	Homo sapiens	58-62
33799525-11	2021	We conclude that BRD4 recruits multiple transcription factors during RSV infection in a manner dependent on acetyl-lysine binding domain interactions.	N(alpha)-acetyllysine	108-121	bromodomain containing 4	Homo sapiens	17-21
34523489-0	2022	Epigenetic regulator BRD4 is involved in cadmium-induced acute kidney injury via contributing to lysosomal dysfunction, autophagy blockade and oxidative stress.	Cadmium	41-48	bromodomain containing 4	Homo sapiens	21-25
34942306-5	2022	In preclinical models, this study demonstrated that activated MAPK/PI3K-AKT pathway and cell cycle-related proteins induced the resistance to palbociclib, which was overcome by the addition of the bromodomain protein 4 (BRD4) inhibitor AZD5153.	palbociclib	142-153	bromodomain containing 4	Homo sapiens	197-218
34942306-5	2022	In preclinical models, this study demonstrated that activated MAPK/PI3K-AKT pathway and cell cycle-related proteins induced the resistance to palbociclib, which was overcome by the addition of the bromodomain protein 4 (BRD4) inhibitor AZD5153.	palbociclib	142-153	bromodomain containing 4	Homo sapiens	220-224
34942306-5	2022	In preclinical models, this study demonstrated that activated MAPK/PI3K-AKT pathway and cell cycle-related proteins induced the resistance to palbociclib, which was overcome by the addition of the bromodomain protein 4 (BRD4) inhibitor AZD5153.	AZD5153	236-243	bromodomain containing 4	Homo sapiens	197-218
34942306-5	2022	In preclinical models, this study demonstrated that activated MAPK/PI3K-AKT pathway and cell cycle-related proteins induced the resistance to palbociclib, which was overcome by the addition of the bromodomain protein 4 (BRD4) inhibitor AZD5153.	AZD5153	236-243	bromodomain containing 4	Homo sapiens	220-224
34523489-6	2022	Resultantly, Cd promotes the recruitment of BRD4 to lysosomal gene promoter regions to make it as a transcriptional regulator.	Cadmium	13-15	bromodomain containing 4	Homo sapiens	44-48
34523489-7	2022	Pharmacological and genetic inhibition of BRD4 alleviates Cd-inhibited lysosomal gene transcript levels and lysosomal function, leading to the alleviation of Cd-induced autophagy inhibition.	Cadmium	58-60	bromodomain containing 4	Homo sapiens	42-46
34523489-7	2022	Pharmacological and genetic inhibition of BRD4 alleviates Cd-inhibited lysosomal gene transcript levels and lysosomal function, leading to the alleviation of Cd-induced autophagy inhibition.	Cadmium	158-160	bromodomain containing 4	Homo sapiens	42-46
34523489-8	2022	Moreover, inhibition of BRD4 relieves Cd-induced oxidative stress and concurrent cytotoxicity, which is counteracted by the inhibition of autophagy via Atg5 knockdown, indicating that alleviation of oxidative stress by BRD4 inhibition is ascribed to its restoration of autophagic flux.	Cadmium	38-40	bromodomain containing 4	Homo sapiens	24-28
34523489-8	2022	Moreover, inhibition of BRD4 relieves Cd-induced oxidative stress and concurrent cytotoxicity, which is counteracted by the inhibition of autophagy via Atg5 knockdown, indicating that alleviation of oxidative stress by BRD4 inhibition is ascribed to its restoration of autophagic flux.	Cadmium	38-40	bromodomain containing 4	Homo sapiens	219-223
34523489-9	2022	Collectively, these results demonstrate that BRD4 acts as a transcriptional repressor to mediate lysosomal dysfunction, autophagy blockade and oxidative stress during Cd exposure, which may be a potential therapeutic target for Cd-induced AKI.	Cadmium	167-169	bromodomain containing 4	Homo sapiens	45-49
34523489-9	2022	Collectively, these results demonstrate that BRD4 acts as a transcriptional repressor to mediate lysosomal dysfunction, autophagy blockade and oxidative stress during Cd exposure, which may be a potential therapeutic target for Cd-induced AKI.	Cadmium	228-230	bromodomain containing 4	Homo sapiens	45-49
34499862-4	2022	We demonstrate that electroporated recombinant von Hippel-Lindau (VHL) protein, covalently functionalized at its ligandable cysteine with JQ1 or dasatinib, induces degradation of BRD4 or tyrosine kinases, respectively.	Cysteine	124-132	bromodomain containing 4	Homo sapiens	179-183
34499862-4	2022	We demonstrate that electroporated recombinant von Hippel-Lindau (VHL) protein, covalently functionalized at its ligandable cysteine with JQ1 or dasatinib, induces degradation of BRD4 or tyrosine kinases, respectively.	Dasatinib	145-154	bromodomain containing 4	Homo sapiens	179-183
34954522-5	2022	These results suggest that overexpression of BRD4 protein, through suppression of BRD4 degradation, may contribute to BETi-resistance.	beti	118-122	bromodomain containing 4	Homo sapiens	45-49
34954522-5	2022	These results suggest that overexpression of BRD4 protein, through suppression of BRD4 degradation, may contribute to BETi-resistance.	beti	118-122	bromodomain containing 4	Homo sapiens	82-86
34954522-10	2022	These results indicate that the CDK4/6-UCHL5-BRD4 axis confers resistance to BETi by suppressing BRD4 degradation.	beti	77-81	bromodomain containing 4	Homo sapiens	45-49
34954522-10	2022	These results indicate that the CDK4/6-UCHL5-BRD4 axis confers resistance to BETi by suppressing BRD4 degradation.	beti	77-81	bromodomain containing 4	Homo sapiens	97-101
34727389-5	2022	CPI-203, a small-molecule bromodomain-containing protein 4 (BRD4) inhibitor, which can potently inhibit the PD-L1 expression in vitro and vivo, combined with PD-1 antibody improved the response to immunotherapy in a liver cancer model.	CPI203	0-7	bromodomain containing 4	Homo sapiens	26-58
34782346-4	2022	By preventing the recruitment of BRD4 to p65-bound cis-regulatory elements, BETi suppressed the induction of inflammatory gene expression, including the key NF-kappaB target genes BIRC2 (cIAP1) and BIRC3 (cIAP2).	beti	76-80	bromodomain containing 4	Homo sapiens	33-37
34700270-3	2022	In this study, we designed and synthesized a series of PROTACs based on our recently reported dual BET/PLK1 inhibitor WNY0824, which led to the discovery of an isoform-selective and potent BRD4-PROTAC 12a (WWL0245).	wny0824	118-125	bromodomain containing 4	Homo sapiens	189-193
34727389-5	2022	CPI-203, a small-molecule bromodomain-containing protein 4 (BRD4) inhibitor, which can potently inhibit the PD-L1 expression in vitro and vivo, combined with PD-1 antibody improved the response to immunotherapy in a liver cancer model.	CPI203	0-7	bromodomain containing 4	Homo sapiens	60-64
34956562-0	2021	Propofol Inhibits Thyroid Cancer Cell Proliferation, Migration, and Invasion by Suppressing SHH and PI3K/AKT Signaling Pathways via the miR-141-3p/BRD4 Axis.	Propofol	0-8	bromodomain containing 4	Homo sapiens	147-151
34913726-3	2022	Apabetalone (APA), a selective inhibitor of bromodomain (BRD) and extra-terminal (BET) proteins, prevents BRD4 interactions with chromatin thus modulating transcriptional programs in different organs.	apabetalone	0-11	bromodomain containing 4	Homo sapiens	106-110
34913726-3	2022	Apabetalone (APA), a selective inhibitor of bromodomain (BRD) and extra-terminal (BET) proteins, prevents BRD4 interactions with chromatin thus modulating transcriptional programs in different organs.	apabetalone	13-16	bromodomain containing 4	Homo sapiens	106-110
34956562-9	2021	Overexpression of BRD4 can partially reverse the restraining effect of miR-141-3p on the TPC-1 cell phenotype.	mir-141-3p	71-81	bromodomain containing 4	Homo sapiens	18-22
34956562-11	2021	Conclusion: Propofol can inhibit the activity of SHH and PI3K/AKT pathways by targeting downregulating BRD4 through miR-141-3p, thereby inhibiting the phenotype of TPC-1 cells.	Propofol	12-20	bromodomain containing 4	Homo sapiens	103-107
34956562-11	2021	Conclusion: Propofol can inhibit the activity of SHH and PI3K/AKT pathways by targeting downregulating BRD4 through miR-141-3p, thereby inhibiting the phenotype of TPC-1 cells.	mir-141-3p	116-126	bromodomain containing 4	Homo sapiens	103-107
34729902-5	2021	Utilizing integrative computer-assisted atomistic techniques, analyses revealed that the dual-inhibitory activity of WNY0824 against BRD4 and PLK1 proteins is mediated by conserved residues present in the binding cavities of both proteins which are shown to elicit various strong intermolecular interactions and thus favour binding affinity.	wny0824	117-124	bromodomain containing 4	Homo sapiens	133-137
34333666-6	2021	We investigated the effect of ZEN-3365, a novel BRD4 inhibitor, on AML cells in regard to the HH pathway.	zen-3365	30-38	bromodomain containing 4	Homo sapiens	48-52
34333666-8	2021	Our findings strongly support the evaluation of the BRD4 inhibitor ZEN-3365 as a new therapeutic option in AML.	zen-3365	67-75	bromodomain containing 4	Homo sapiens	52-56
34710811-2	2021	6-(2,4-difluorophenoxy)-5-((ethylmethyl)pyridine-3-yl)-8-methylpyrrolo(1,2-a) pyrazin-1(2H)-one (Cpd38) is an inhibitor possessing high inhibition rate and tailored specificity towards bromodomain-containing protein 4 (BRD4).	6-(2,4-difluorophenoxy)-5-((ethylmethyl)pyridine-3-yl)-8-methylpyrrolo(1,2-a) pyrazin-1(2h)-one	0-95	bromodomain containing 4	Homo sapiens	185-217
34710811-2	2021	6-(2,4-difluorophenoxy)-5-((ethylmethyl)pyridine-3-yl)-8-methylpyrrolo(1,2-a) pyrazin-1(2H)-one (Cpd38) is an inhibitor possessing high inhibition rate and tailored specificity towards bromodomain-containing protein 4 (BRD4).	6-(2,4-difluorophenoxy)-5-((ethylmethyl)pyridine-3-yl)-8-methylpyrrolo(1,2-a) pyrazin-1(2h)-one	0-95	bromodomain containing 4	Homo sapiens	219-223
34710811-8	2021	Furthermore, the hydrogen bond acceptor/donator ratio was approximately 4:1 in Cpd38-BRD4 system compared with 2:1 in Cpd38-EP300 system.	Hydrogen	17-25	bromodomain containing 4	Homo sapiens	85-89
34926269-0	2021	Preclinical Evaluation of a Novel Dual Targeting PI3Kdelta/BRD4 Inhibitor, SF2535, in B-Cell Acute Lymphoblastic Leukemia.	sf2535	75-81	bromodomain containing 4	Homo sapiens	59-63
34926269-6	2021	To study this, we utilized SF2535, a novel small molecule dual inhibitor which can specifically target the PI3Kdelta isoform and BRD4.	sf2535	27-33	bromodomain containing 4	Homo sapiens	129-133
34926269-8	2021	SF2535 significantly downregulates both c-Myc mRNA and protein expression through inhibition of BRD4 at the c-Myc promoter site and decreases p-AKT expression through inhibition of the PI3Kdelta/AKT pathway.	sf2535	0-6	bromodomain containing 4	Homo sapiens	96-100
34730838-10	2021	Circ_0000376 competitively bound to miR-488-3p to regulate the expression of BRD4.	mir-488-3p	36-46	bromodomain containing 4	Homo sapiens	77-81
34730838-11	2021	Rescue experiments showed that miR-488-3p deficiency reversed the effects of circ_0000376 downregulation, and miR-488-3p restoration-suppressed cell proliferation, migration and invasion were recovered by BRD4 overexpression.	mir-488-3p	31-41	bromodomain containing 4	Homo sapiens	205-209
34730838-11	2021	Rescue experiments showed that miR-488-3p deficiency reversed the effects of circ_0000376 downregulation, and miR-488-3p restoration-suppressed cell proliferation, migration and invasion were recovered by BRD4 overexpression.	mir-488-3p	110-120	bromodomain containing 4	Homo sapiens	205-209
33820450-1	2021	Bromodomain-containing protein 4 (BRD4) binds acetylated lysine residues on the N-terminal tails of histones through two bromodomains (BD1 and BD2) to regulate gene transcription.	Lysine	57-63	bromodomain containing 4	Homo sapiens	0-32
33820450-1	2021	Bromodomain-containing protein 4 (BRD4) binds acetylated lysine residues on the N-terminal tails of histones through two bromodomains (BD1 and BD2) to regulate gene transcription.	Lysine	57-63	bromodomain containing 4	Homo sapiens	34-38
33820450-3	2021	Here we report the characterisation of a natural product 3",4",7,8-tetrahydroxyflavone as a novel and potent selective BRD4 inhibitor.	3",4",7,8-tetrahydroxyflavone	57-86	bromodomain containing 4	Homo sapiens	119-123
33820450-5	2021	Co-crystal structures show 3",4",7,8-tetrahydroxyflavone binds to the acetylated lysine binding pocket of BRD4-BD1 or BRD4-BD2, but establishes more interactions with BRD4-BD2 than BRD4-BD1.	3",4",7,8-tetrahydroxyflavone	27-56	bromodomain containing 4	Homo sapiens	106-110
33820450-5	2021	Co-crystal structures show 3",4",7,8-tetrahydroxyflavone binds to the acetylated lysine binding pocket of BRD4-BD1 or BRD4-BD2, but establishes more interactions with BRD4-BD2 than BRD4-BD1.	3",4",7,8-tetrahydroxyflavone	27-56	bromodomain containing 4	Homo sapiens	118-122
33820450-5	2021	Co-crystal structures show 3",4",7,8-tetrahydroxyflavone binds to the acetylated lysine binding pocket of BRD4-BD1 or BRD4-BD2, but establishes more interactions with BRD4-BD2 than BRD4-BD1.	3",4",7,8-tetrahydroxyflavone	27-56	bromodomain containing 4	Homo sapiens	167-171
33820450-5	2021	Co-crystal structures show 3",4",7,8-tetrahydroxyflavone binds to the acetylated lysine binding pocket of BRD4-BD1 or BRD4-BD2, but establishes more interactions with BRD4-BD2 than BRD4-BD1.	3",4",7,8-tetrahydroxyflavone	27-56	bromodomain containing 4	Homo sapiens	181-185
33820450-5	2021	Co-crystal structures show 3",4",7,8-tetrahydroxyflavone binds to the acetylated lysine binding pocket of BRD4-BD1 or BRD4-BD2, but establishes more interactions with BRD4-BD2 than BRD4-BD1.	Lysine	81-87	bromodomain containing 4	Homo sapiens	106-110
33820450-5	2021	Co-crystal structures show 3",4",7,8-tetrahydroxyflavone binds to the acetylated lysine binding pocket of BRD4-BD1 or BRD4-BD2, but establishes more interactions with BRD4-BD2 than BRD4-BD1.	Lysine	81-87	bromodomain containing 4	Homo sapiens	118-122
33820450-6	2021	Our data suggest 3",4",7,8-tetrahydroxyflavone as a potent selective inhibitor of BRD4-BD2 with a novel chemical scaffold.	3",4",7,8-tetrahydroxyflavone	17-46	bromodomain containing 4	Homo sapiens	82-86
34813314-4	2021	Therefore, we designed, synthetized, and optimized a dual PARP/BRD4 inhibitor III-16, with a completely new structure and high selectivity against PARP1/2 and BRD4.	iii-16	78-84	bromodomain containing 4	Homo sapiens	63-67
34813314-4	2021	Therefore, we designed, synthetized, and optimized a dual PARP/BRD4 inhibitor III-16, with a completely new structure and high selectivity against PARP1/2 and BRD4.	iii-16	78-84	bromodomain containing 4	Homo sapiens	159-163
34813314-7	2021	The advantages of III-16 over Olaparib suggest that dual PARP/BRD4 inhibitors are novel and promising agents for the treatment of advanced pancreatic cancer.	iii-16	18-24	bromodomain containing 4	Homo sapiens	62-66
34813314-7	2021	The advantages of III-16 over Olaparib suggest that dual PARP/BRD4 inhibitors are novel and promising agents for the treatment of advanced pancreatic cancer.	olaparib	30-38	bromodomain containing 4	Homo sapiens	62-66
34829934-7	2021	BETi degraded NPM1c in the cytosol while BRD4 is degraded in the nucleus which suggests that restoration of the NPM1/BRD4 equilibrium in the nucleus of NPM1c cells is essential for the efficacy of BETi.	beti	197-201	bromodomain containing 4	Homo sapiens	41-45
34845959-6	2021	Instead of significant hydrogen bondings with amino acid residue Ans140 as reported in previous research, the molecular docking modelling suggested a novel docking pose that involves the amino acid residues (Trp81, Pro82, Val87, Leu92, Leu94, Cys136, Asp144, and Ile146) at the active site of BRD4.	Hydrogen	23-31	bromodomain containing 4	Homo sapiens	293-297
34845959-6	2021	Instead of significant hydrogen bondings with amino acid residue Ans140 as reported in previous research, the molecular docking modelling suggested a novel docking pose that involves the amino acid residues (Trp81, Pro82, Val87, Leu92, Leu94, Cys136, Asp144, and Ile146) at the active site of BRD4.	ans140	65-71	bromodomain containing 4	Homo sapiens	293-297
34829934-7	2021	BETi degraded NPM1c in the cytosol while BRD4 is degraded in the nucleus which suggests that restoration of the NPM1/BRD4 equilibrium in the nucleus of NPM1c cells is essential for the efficacy of BETi.	beti	197-201	bromodomain containing 4	Homo sapiens	117-121
34676032-0	2021	Substituted 2,3-Benzodiazepines Derivatives as Bromodomain BRD4 Inhibitors.	2,3-benzodiazepines	12-31	bromodomain containing 4	Homo sapiens	59-63
34519605-1	2021	BACKGROUND: Bromodomain-containing protein 4 (BRD4) binds acetylated lysine residues on histones to facilitate the epigenetic regulation of many genes, and it plays a key role in many cancer types.	Lysine	69-75	bromodomain containing 4	Homo sapiens	12-44
34519605-1	2021	BACKGROUND: Bromodomain-containing protein 4 (BRD4) binds acetylated lysine residues on histones to facilitate the epigenetic regulation of many genes, and it plays a key role in many cancer types.	Lysine	69-75	bromodomain containing 4	Homo sapiens	46-50
34765643-5	2021	Using a highly selective small-molecule BRD4 inhibitor (ZL0454) developed by us, we extend these findings to identify the gene regulatory network dependent on BRD4 bromodomain (BD) interactions.	CHEMBL4159382	56-62	bromodomain containing 4	Homo sapiens	40-44
34765643-5	2021	Using a highly selective small-molecule BRD4 inhibitor (ZL0454) developed by us, we extend these findings to identify the gene regulatory network dependent on BRD4 bromodomain (BD) interactions.	CHEMBL4159382	56-62	bromodomain containing 4	Homo sapiens	159-163
34733788-3	2021	ARV-825, consisting of a BRD4 inhibitor conjugated with a cereblon ligand using proteolysis-targeting chimera (PROTAC) technology, was proven to decrease the tumor growth effectively and continuously.	ARV-825	0-7	bromodomain containing 4	Homo sapiens	25-29
34733788-9	2021	ARV-825 induced degradation of BRD4, BRD2, BRD3, c-MYC, and polo-like kinase 1 (PLK1) proteins in four gastric cancer cell lines.	ARV-825	0-7	bromodomain containing 4	Homo sapiens	31-35
34733788-13	2021	ARV-825 treatment significantly reduced tumor growth without toxic side effects and downregulated the expression of BRD4 in vivo.	ARV-825	0-7	bromodomain containing 4	Homo sapiens	116-120
34733788-15	2021	ARV-825, a BRD4 inhibitor, could effectively suppress the growth and elevate the apoptosis of gastric cancer cells via transcription downregulation of c-MYC and PLK1.	ARV-825	0-7	bromodomain containing 4	Homo sapiens	11-15
34333275-9	2021	A hypothesized mechanism underlying responses to ICPI in the low TMB, PD-L1 negative index cases is the predicted high affinity of the BRD4-NUT fusion peptide to MHC complexes.	1,2,4,5-tetramethoxybenzene	65-68	bromodomain containing 4	Homo sapiens	135-139
34565342-12	2021	Mechanistically, the co-treatment of JQ1 or OTX-015 with temsirolimus significantly downregulated the expression levels of phosphorylated 4EBP1/p70-S6K/eIF4E (mTOR components) and BRD4 (BET protein)/MYCN proteins.	temsirolimus	57-69	bromodomain containing 4	Homo sapiens	180-184
34564701-6	2021	Further research found that HAT1 increased PVT1 expression to induce gemcitabine resistance, which enhanced the binding of bromodomain containing 4 (BRD4) to the PVT1 promoter, thereby promoting PVT1 transcription.	gemcitabine	69-80	bromodomain containing 4	Homo sapiens	123-147
34175826-9	2021	We found that PM2.5 DMSO extracts, which promoted the contraction and migration of hASMCs, was accompanied by an increase in the levels of BRD4, kallikrein 14 (KLK14), bradykinin 2 receptor (B2R), matrix metalloproteinases2(MMP-2), matrix metalloproteinases9(MMP-9), vimentin and bradykinin (BK) secretion, while ZL0420 and BRD4 gene silencing could reverse this response.	Dimethyl Sulfoxide	20-24	bromodomain containing 4	Homo sapiens	139-143
34175826-9	2021	We found that PM2.5 DMSO extracts, which promoted the contraction and migration of hASMCs, was accompanied by an increase in the levels of BRD4, kallikrein 14 (KLK14), bradykinin 2 receptor (B2R), matrix metalloproteinases2(MMP-2), matrix metalloproteinases9(MMP-9), vimentin and bradykinin (BK) secretion, while ZL0420 and BRD4 gene silencing could reverse this response.	Dimethyl Sulfoxide	20-24	bromodomain containing 4	Homo sapiens	324-328
34175826-11	2021	In addition, PM2.5 DMSO extracts can promote the contraction and migration of hASMCs by increasing BRD4 expression.	Dimethyl Sulfoxide	19-23	bromodomain containing 4	Homo sapiens	99-103
34520194-6	2021	MS83 effectively reduces protein levels of BRD4 and BRD3, but not BRD2, in cells in a concentration-, time-, KEAP1- and UPS-dependent manner.	ms83	0-4	bromodomain containing 4	Homo sapiens	43-47
34564701-6	2021	Further research found that HAT1 increased PVT1 expression to induce gemcitabine resistance, which enhanced the binding of bromodomain containing 4 (BRD4) to the PVT1 promoter, thereby promoting PVT1 transcription.	gemcitabine	69-80	bromodomain containing 4	Homo sapiens	149-153
34540687-1	2021	I-BET151 is an inhibitor of bromodomain and extra-terminal domain (BET) proteins that selectively inhibits BET family members (BRD2, BRD3, BRD4, and BRDT).	GSK1210151A	0-8	bromodomain containing 4	Homo sapiens	139-143
34526906-0	2021	Corrigendum: 7-Ethyl-10-Hydroxycamptothecin, A DNA Topoisomerase I Inhibitor, Performs BRD4 Inhibitory Activity and Inhibits Human Leukemic Cell Growth.	Irinotecan	13-43	bromodomain containing 4	Homo sapiens	87-91
34512660-5	2021	By upregulating Myc and GLUT1 expression, Brd4 facilitates glucose uptake and energy production in mitochondria, subsequently supporting naive CD8+ T-cell survival.	Glucose	59-66	bromodomain containing 4	Homo sapiens	42-46
34279939-5	2021	We demonstrate that BRD4BD1L94V can be combined with the dTAG approach to achieve simultaneous degrader-mediated depletion of their respective protein fusions.	tagatose	57-61	bromodomain containing 4	Homo sapiens	20-24
34160250-4	2021	Introduction of BRD4 inhibitor AZD5153 to senescent epithelial cells reversed this effect and reduced SASP related inflammatory molecule release in TMNK-1 or EAhy926 as representative human endothelial cell line, when exposed to cell culture medium (CM) derived from A549 cells expressing SARS-CoV-2 spike protein, also exhibited a senescence phenotype with enhanced p16, p21, SA-beta-galactosidase expression, and triggered SASP pathways.	AZD5153	31-38	bromodomain containing 4	Homo sapiens	16-20
35395439-0	2022	Adjusted degradation of BRD4 S and BRD4 L based on fine structural modifications of the pyrrolopyridone scaffold.	pyrrolopyridone	88-103	bromodomain containing 4	Homo sapiens	24-28
34290255-3	2021	Here, we show that cancer-associated fibroblast (CAF)-activated stromal signaling, interleukin-6/8-JAK2, induces BRD4 phosphorylation at tyrosine 97/98 in colorectal cancer, resulting in BRD4 stabilization due to interaction with the deubiquitinase UCHL3.	Tyrosine	137-145	bromodomain containing 4	Homo sapiens	113-117
34290255-3	2021	Here, we show that cancer-associated fibroblast (CAF)-activated stromal signaling, interleukin-6/8-JAK2, induces BRD4 phosphorylation at tyrosine 97/98 in colorectal cancer, resulting in BRD4 stabilization due to interaction with the deubiquitinase UCHL3.	Tyrosine	137-145	bromodomain containing 4	Homo sapiens	187-191
34290255-4	2021	BRD4 phosphorylation at tyrosine 97/98 also displays increased binding to chromatin but reduced binding to BET inhibitors, resulting in resistance to BET inhibitors.	Tyrosine	24-32	bromodomain containing 4	Homo sapiens	0-4
34350133-0	2021	CPI-637 as a Potential Bifunctional Latency-Reversing Agent That Targets Both the BRD4 and TIP60 Proteins.	CPI-637	0-7	bromodomain containing 4	Homo sapiens	82-86
34350133-5	2021	We demonstrate here for the first time that a dual-target inhibitor with a specific suppressive effect on both BRD4 and TIP60, CPI-637, could reactivate latent HIV-1 in vitro by permitting Tat to bind positive transcription elongation factor b (P-TEFb) and assembling Tat-super-elongation complex (SEC) formation.	CPI-637	127-134	bromodomain containing 4	Homo sapiens	111-115
34350133-6	2021	In addition, CPI-637-mediated TIP60 downregulation further stimulated BRD4 dissociation from the HIV-1 long terminal repeat (LTR) promoter, allowing Tat to more effectively bind P-TEFb compared to BRD4 inhibition alone.	CPI-637	13-20	bromodomain containing 4	Homo sapiens	70-74
34350133-6	2021	In addition, CPI-637-mediated TIP60 downregulation further stimulated BRD4 dissociation from the HIV-1 long terminal repeat (LTR) promoter, allowing Tat to more effectively bind P-TEFb compared to BRD4 inhibition alone.	CPI-637	13-20	bromodomain containing 4	Homo sapiens	197-201
34180651-10	2021	Thereon, a complex structure of sulfasalazine was obtained that involves two bromodomains and could be a potential starting point for the design of a bivalent BRD4 inhibitor.	Sulfasalazine	32-45	bromodomain containing 4	Homo sapiens	159-163
34336926-0	2021	Regulation of Carbohydrate-Responsive Metabolic Genes by Histone Acetylation and the Acetylated Histone Reader BRD4 in the Gene Body Region.	Carbohydrates	14-26	bromodomain containing 4	Homo sapiens	111-115
34336926-2	2021	Carbohydrate intake-mediated induction of metabolic gene expression is regulated by histone acetylation and the histone acetylation reader bromodomain-containing protein 4 (BRD4) on the gene body region, which corresponds to the transcribed region of the gene.	Carbohydrates	0-12	bromodomain containing 4	Homo sapiens	173-177
34336926-3	2021	In this review, we introduce carbohydrate-responsive metabolic gene regulation by (i) transcription factors and epigenetic memory in promoter/enhancer regions (promoter/enhancer-based epigenetics), and (ii) histone acetylation and BRD4 in the gene body region (gene body-based epigenetics).	Carbohydrates	29-41	bromodomain containing 4	Homo sapiens	231-235
34336926-8	2021	In conclusion, histone acetylation and BRD4 binding in the gene body region as well as transcription factor binding in promoter/enhancer regions regulate the expression of carbohydrate-responsive metabolic genes in many metabolic organs.	Carbohydrates	172-184	bromodomain containing 4	Homo sapiens	39-43
34336926-9	2021	Insulin resistant and diabetic conditions induce the development of metabolic diseases, including type 2 diabetes, by reducing the expression of BRD4-targeted carbohydrate-responsive metabolic genes in white adipose tissue and by inducing the expression of BRD4-targeted carbohydrate-responsive metabolic genes in the liver, small intestine, and innate leukocytes including monocytes/macrophages and neutrophils.	Carbohydrates	159-171	bromodomain containing 4	Homo sapiens	145-149
34336926-9	2021	Insulin resistant and diabetic conditions induce the development of metabolic diseases, including type 2 diabetes, by reducing the expression of BRD4-targeted carbohydrate-responsive metabolic genes in white adipose tissue and by inducing the expression of BRD4-targeted carbohydrate-responsive metabolic genes in the liver, small intestine, and innate leukocytes including monocytes/macrophages and neutrophils.	Carbohydrates	271-283	bromodomain containing 4	Homo sapiens	257-261
34336890-7	2021	BRD4 expression was positively correlated with the severity of liver fibrosis, and also correlated with the serum levels of aspartate aminotransferase and total bilirubin.	Bilirubin	161-170	bromodomain containing 4	Homo sapiens	0-4
34144267-9	2021	Intriguingly, these defects in DNA repair were reversed upon erlotinib treatment, which caused activation and nuclear import of p38 MAPK to promote DNA repair with increased protein levels of 53BP1 and BRD4 and foci formation of 53BP1.	Erlotinib Hydrochloride	61-70	bromodomain containing 4	Homo sapiens	202-206
34144267-10	2021	Remarkably, inhibition of p38 MAPK or BRD4 re-sensitized PIK3R2-depleted cells to erlotinib.	Erlotinib Hydrochloride	82-91	bromodomain containing 4	Homo sapiens	38-42
34105560-7	2021	A focused analysis on the highly conserved water network in the binding site of BRD4-BD1 is performed to identify the positions of these water molecules across the crystal structures.	Water	43-48	bromodomain containing 4	Homo sapiens	80-84
34105560-7	2021	A focused analysis on the highly conserved water network in the binding site of BRD4-BD1 is performed to identify the positions of these water molecules across the crystal structures.	Water	137-142	bromodomain containing 4	Homo sapiens	80-84
34160902-0	2021	Trichostatin A promotes esophageal squamous cell carcinoma cell migration and EMT through BRD4/ERK1/2-dependent pathway.	trichostatin A	0-14	bromodomain containing 4	Homo sapiens	90-94
34160902-14	2021	Interestingly, inhibition of BRD4 suppressed TSA-induced ESCC cell migration and attenuated TSA-induced ERK1/2 activation and upregulation of Slug and PAI-1 levels.	trichostatin A	45-48	bromodomain containing 4	Homo sapiens	29-33
34160902-16	2021	Both branches of TSA-induced ESCC cell migration appear to favor the EMT process, while BRD4 is responsible for two separable ERK1/2-dependent signaling pathways in TSA-mediated ESCC cell migration.	trichostatin A	17-20	bromodomain containing 4	Homo sapiens	88-92
34160902-16	2021	Both branches of TSA-induced ESCC cell migration appear to favor the EMT process, while BRD4 is responsible for two separable ERK1/2-dependent signaling pathways in TSA-mediated ESCC cell migration.	trichostatin A	165-168	bromodomain containing 4	Homo sapiens	88-92
34557659-0	2021	The BTK/PI3K/BRD4 axis inhibitor SRX3262 overcomes Ibrutinib resistance in mantle cell lymphoma.	srx3262	33-40	bromodomain containing 4	Homo sapiens	13-17
34557659-0	2021	The BTK/PI3K/BRD4 axis inhibitor SRX3262 overcomes Ibrutinib resistance in mantle cell lymphoma.	ibrutinib	51-60	bromodomain containing 4	Homo sapiens	13-17
34557659-2	2021	Here, we developed the first-in-class BTK/PI3K/BRD4 axis inhibitor SRX3262, which simultaneously blocks three interrelated MCL driver pathways - BTK, PI3K-AKT-mTOR and MYC.	srx3262	67-74	bromodomain containing 4	Homo sapiens	47-51
34557659-3	2021	SRX3262 concomitantly binds to BTK, PI3K, and BRD4, exhibits potent in vitro and in vivo activity against MCL, and overcomes the Ibrutinib resistance resulting from the BTK-C481S mutation.	srx3262	0-7	bromodomain containing 4	Homo sapiens	46-50
34557659-4	2021	Our results reveal that SRX3262 inhibits IgM-induced BTK and AKT phosphorylation and abrogates binding of BRD4 to MYC loci.	srx3262	24-31	bromodomain containing 4	Homo sapiens	106-110
34249442-4	2021	The insensitivity is driven by a unique non-genetic mechanism that involves clonal selection for a pre-existing cell subpopulation with ample acetylated histones and sufficient nuclear phase-separated BRD4 droplets to counteract BETi antagonism.	beti	229-233	bromodomain containing 4	Homo sapiens	201-205
34140798-11	2021	In addition, BRD4 was directly targeted by miR-331-3p, and BRD4 deficiency neutralized the effects of miR-331-3p repression on LPS-triggered injury in LPS-treated FHCs.	mir-331-3p	102-112	bromodomain containing 4	Homo sapiens	13-17
34258104-0	2021	Concurrent targeting of MAP3K3 and BRD4 by miR-3140-3p overcomes acquired resistance to BET inhibitors in neuroblastoma cells.	mir-3140-3p	43-54	bromodomain containing 4	Homo sapiens	35-39
34258104-5	2021	We previously identified miR-3140-3p as a potent candidate for nucleic acid therapeutics for cancer, which directly targets BRD4.	mir-3140-3p	25-36	bromodomain containing 4	Homo sapiens	124-128
34258104-6	2021	We demonstrated that miR-3140-3p suppresses tumor cell growth in MYCN-amplified NB by downregulating MYCN and MYC through BRD4 suppression.	mir-3140-3p	21-32	bromodomain containing 4	Homo sapiens	122-126
34094834-0	2021	The poly(ADP-ribosyl)ation of BRD4 mediated by PARP1 promoted pathological cardiac hypertrophy.	poly(adp-ribosyl)	4-21	bromodomain containing 4	Homo sapiens	30-34
34094834-4	2021	BRD4 silencing or BET inhibitors JQ1 and MS417 prevented cardiac hypertrophic responses induced by isoproterenol (ISO), whereas overexpression of BRD4 promoted cardiac hypertrophy, confirming the critical role of BRD4 in pathological cardiac hypertrophy.	Isoproterenol	99-112	bromodomain containing 4	Homo sapiens	0-4
34094834-4	2021	BRD4 silencing or BET inhibitors JQ1 and MS417 prevented cardiac hypertrophic responses induced by isoproterenol (ISO), whereas overexpression of BRD4 promoted cardiac hypertrophy, confirming the critical role of BRD4 in pathological cardiac hypertrophy.	Isoproterenol	99-112	bromodomain containing 4	Homo sapiens	213-217
34094834-4	2021	BRD4 silencing or BET inhibitors JQ1 and MS417 prevented cardiac hypertrophic responses induced by isoproterenol (ISO), whereas overexpression of BRD4 promoted cardiac hypertrophy, confirming the critical role of BRD4 in pathological cardiac hypertrophy.	Isoproterenol	114-117	bromodomain containing 4	Homo sapiens	0-4
34094834-9	2021	In response to hypertrophic stimuli like ISO, PARylation level of BRD4 was elevated, along with enhanced interactions between BRD4 and PARP1.	Isoproterenol	41-44	bromodomain containing 4	Homo sapiens	66-70
34094834-9	2021	In response to hypertrophic stimuli like ISO, PARylation level of BRD4 was elevated, along with enhanced interactions between BRD4 and PARP1.	Isoproterenol	41-44	bromodomain containing 4	Homo sapiens	126-130
35395439-0	2022	Adjusted degradation of BRD4 S and BRD4 L based on fine structural modifications of the pyrrolopyridone scaffold.	pyrrolopyridone	88-103	bromodomain containing 4	Homo sapiens	35-39
35395439-1	2022	Novel pyrrolopyridone BET degraders were designed and synthesized based on the binding mode between the pyrrolopyridone BET inhibitor with the BRD4 protein.	pyrrolopyridone	6-21	bromodomain containing 4	Homo sapiens	143-147
35395439-1	2022	Novel pyrrolopyridone BET degraders were designed and synthesized based on the binding mode between the pyrrolopyridone BET inhibitor with the BRD4 protein.	pyrrolopyridone	104-119	bromodomain containing 4	Homo sapiens	143-147
35395439-3	2022	Modification of warhead on pyrrolopyridone BET degraders significantly regulates BRD4 isoform (long and short) protein degradation, which induces differential cell cycle arrest and apoptosis on MV-4-11 cells.	warhead	16-23	bromodomain containing 4	Homo sapiens	81-85
35395439-3	2022	Modification of warhead on pyrrolopyridone BET degraders significantly regulates BRD4 isoform (long and short) protein degradation, which induces differential cell cycle arrest and apoptosis on MV-4-11 cells.	pyrrolopyridone	27-42	bromodomain containing 4	Homo sapiens	81-85
35633739-5	2022	We recently showed that SF2523, a dual activity small molecule that inhibits PI3K and BRD4, acts synergistically with the antiviral drugs remdesivir and MU-UNMC-2.	remdesivir	138-148	bromodomain containing 4	Homo sapiens	86-90
35633739-5	2022	We recently showed that SF2523, a dual activity small molecule that inhibits PI3K and BRD4, acts synergistically with the antiviral drugs remdesivir and MU-UNMC-2.	mu-unmc-2	153-162	bromodomain containing 4	Homo sapiens	86-90
35264812-0	2022	Design, synthesis and pharmacological characterization of N-(3-ethylbenzo(d)isoxazol-5-yl) sulfonamide derivatives as BRD4 inhibitors against acute myeloid leukemia.	n-(3-ethylbenzo(d)isoxazol-5-yl) sulfonamide	58-102	bromodomain containing 4	Homo sapiens	118-122
35461311-7	2022	Inhibition of Pin1 and BRD4 significantly suppressed high-glucose (HG)-induced GC cell proliferation and migration.	Glucose	58-65	bromodomain containing 4	Homo sapiens	23-27
35461311-7	2022	Inhibition of Pin1 and BRD4 significantly suppressed high-glucose (HG)-induced GC cell proliferation and migration.	Mercury	67-69	bromodomain containing 4	Homo sapiens	23-27
35480096-7	2022	Moreover, addition of the bromodomain-containing protein 4 inhibitor AZD5153 increased the anticancer effect of talazoparib via MUS81 inhibition in gastric cancer cells, and this combination effect was largely impaired when MUS81 was knocked down.	AZD5153	69-76	bromodomain containing 4	Homo sapiens	26-58
35480096-7	2022	Moreover, addition of the bromodomain-containing protein 4 inhibitor AZD5153 increased the anticancer effect of talazoparib via MUS81 inhibition in gastric cancer cells, and this combination effect was largely impaired when MUS81 was knocked down.	talazoparib	112-123	bromodomain containing 4	Homo sapiens	26-58
35403781-5	2022	Gene expression of HDAC1, HDAC2, SIRT1, MTA1, KAT2B, KAT6A, KAT6B, and BRD4 indicated the cisplatin activates the epigenetic machinery.	Cisplatin	90-99	bromodomain containing 4	Homo sapiens	71-75
35167374-0	2022	BRD4 promotes the migration and invasion of bladder cancer through the Sonic hedgehog signaling pathway and enhances cisplatin resistance.	Cisplatin	117-126	bromodomain containing 4	Homo sapiens	0-4
35167374-6	2022	We further found that cisplatin (DDP) suppressed the migration and invasion of BCa cells in vitro and inhibited tumor growth in vivo; however overexpression of BRD4 weakened the pharmacological effects of DDP.	Cisplatin	22-31	bromodomain containing 4	Homo sapiens	160-164
35167374-6	2022	We further found that cisplatin (DDP) suppressed the migration and invasion of BCa cells in vitro and inhibited tumor growth in vivo; however overexpression of BRD4 weakened the pharmacological effects of DDP.	ddp	33-36	bromodomain containing 4	Homo sapiens	160-164
34258104-9	2021	miR-3140-3p efficiently downregulated MYCN expression by directly targeting the MAP3K3-ERK1/2 pathway in addition to BRD4 suppression, inhibiting tumor cell growth in BETi-acquired resistant NB cells.	mir-3140-3p	0-11	bromodomain containing 4	Homo sapiens	117-121
35318165-0	2022	Development of BRD4 inhibitors as anti-inflammatory agents and antidotes for arsenicals.	Arsenicals	77-87	bromodomain containing 4	Homo sapiens	15-19
35318165-5	2022	In this context, the development of potent small molecule inhibitors of BRD4 could serve as potential antidotes for arsenicals.	Arsenicals	116-126	bromodomain containing 4	Homo sapiens	72-76
35349485-6	2022	The anti-fibrotic effect of BRD4 inhibition was at least in part mediated by downregulation of Ca2+/calmodulin-dependent protein kinase II alpha (CaMKII-alpha) and reduction of intracellular calcium concentrations.	Calcium	191-198	bromodomain containing 4	Homo sapiens	28-32
35399501-0	2022	AZD5153, a Bivalent BRD4 Inhibitor, Suppresses Hepatocarcinogenesis by Altering BRD4 Chromosomal Landscape and Modulating the Transcriptome of HCC Cells.	AZD5153	0-7	bromodomain containing 4	Homo sapiens	20-24
35399501-0	2022	AZD5153, a Bivalent BRD4 Inhibitor, Suppresses Hepatocarcinogenesis by Altering BRD4 Chromosomal Landscape and Modulating the Transcriptome of HCC Cells.	AZD5153	0-7	bromodomain containing 4	Homo sapiens	80-84
35399501-2	2022	Here, we determined the anti-HCC efficacy of AZD5153, a potent bivalent BRD4 inhibitor, and elucidated its underlying molecular mechanism of action.	AZD5153	45-52	bromodomain containing 4	Homo sapiens	72-76
35399501-10	2022	In conclusion, our results identified novel targets of BRD4 in the HCCLM3 cell genome and demonstrated anti-HCC efficacy of AZD5153, which was potentiated in combination with an NAMPT inhibitor.	AZD5153	124-131	bromodomain containing 4	Homo sapiens	55-59
35402244-6	2022	At present, the PTMs of BRD4 mainly include ubiquitination and phosphorylation; the former mainly regulates the stability of the BRD4 protein and mediates BETi resistance, while the latter is related to the biological functions of BRD4, such as transcriptional regulation, cofactor recruitment, chromatin binding and so on.	beti	155-159	bromodomain containing 4	Homo sapiens	24-28
35402244-6	2022	At present, the PTMs of BRD4 mainly include ubiquitination and phosphorylation; the former mainly regulates the stability of the BRD4 protein and mediates BETi resistance, while the latter is related to the biological functions of BRD4, such as transcriptional regulation, cofactor recruitment, chromatin binding and so on.	beti	155-159	bromodomain containing 4	Homo sapiens	231-235
35303940-0	2022	BRD4 inhibitor GNE987 exerts anti-cancer effects by targeting super-enhancers in neuroblastoma.	gne987	15-21	bromodomain containing 4	Homo sapiens	0-4
35303940-3	2022	This study aimed to characterize the activity of the SEs inhibitor GNE987, which targets BRD4, in NB.	gne987	67-73	bromodomain containing 4	Homo sapiens	89-93
35303940-4	2022	RESULTS: In this study, we found that nanomolar concentrations of GNE987 markedly diminished NB cell proliferation and survival via degrading BRD4.	gne987	66-72	bromodomain containing 4	Homo sapiens	142-146
35303940-6	2022	Consistent with in vitro results, GNE987 administration (0.25 mg/kg) markedly decreased the tumor size in the xenograft model, with less toxicity, and induced similar BRD4 protein degradation to that observed in vitro.	gne987	34-40	bromodomain containing 4	Homo sapiens	167-171
35303940-10	2022	CONCLUSION: GNE987 destroyed the abnormal transcriptional regulation of oncogenes in NB by downregulating BRD4, which could be a potential therapeutic candidate for NB.	gne987	12-18	bromodomain containing 4	Homo sapiens	106-110
35432890-5	2022	Further, small molecule (+)-JQ1- and rapamycin-derived iPr acyl silanes were shown to selectively label recombinant BRD4-BD1 and FKBP12, respectively, with minimal background.	Sirolimus	37-46	bromodomain containing 4	Homo sapiens	116-120
35308165-8	2022	Inhibition of autophagy by 3-methyladenine (3-MA) partially reversed the antisenescence and antiapoptotic effects of BRD4.	3-methyladenine	44-48	bromodomain containing 4	Homo sapiens	117-121
35264812-3	2022	Most compounds exhibited potent BRD4 binding activities with DeltaTm values exceeding 6  C. Two crystal structures of 11h and 11r in complex with BRD4(1) were obtained to characterize the binding patterns.	2,6-disulfonic acid anthraquinone	118-121	bromodomain containing 4	Homo sapiens	32-36
35264812-3	2022	Most compounds exhibited potent BRD4 binding activities with DeltaTm values exceeding 6  C. Two crystal structures of 11h and 11r in complex with BRD4(1) were obtained to characterize the binding patterns.	2,6-disulfonic acid anthraquinone	118-121	bromodomain containing 4	Homo sapiens	146-150
35264812-4	2022	Compounds 11h and 11r were effective for BRD4(1) binding and showed remarkable anti-proliferative activity against MV4-11 cells with IC50 values of 0.78 and 0.87 muM.	2,6-disulfonic acid anthraquinone	10-13	bromodomain containing 4	Homo sapiens	41-45
35264812-4	2022	Compounds 11h and 11r were effective for BRD4(1) binding and showed remarkable anti-proliferative activity against MV4-11 cells with IC50 values of 0.78 and 0.87 muM.	11R	18-21	bromodomain containing 4	Homo sapiens	41-45
35091172-6	2022	III-7 reversed Olaparib-induced adaptive resistance and induced cell cycle arrest and DNA damage by perturbing PARP1 and BRD4-involved signaling pathways.	olaparib	15-23	bromodomain containing 4	Homo sapiens	121-125
35123163-0	2022	Activatable fluorescence molecular imaging and anti-tumor effects investigation of GSH-sensitive BRD4 ligands.	Glutathione	83-86	bromodomain containing 4	Homo sapiens	97-101
35123163-2	2022	We herein present the design, chemical synthesis, cellular imaging and biological assessment of a novel tumor-sensitive BRD4 ligand (compound 4) by introducing anticancer BRD4 inhibitor into naphthalimide moiety (fluorescent reporter) via a sulfonamide unit as glutathione (GSH)-specific cleavable linker.	Naphthalimides	191-204	bromodomain containing 4	Homo sapiens	120-124
35123163-2	2022	We herein present the design, chemical synthesis, cellular imaging and biological assessment of a novel tumor-sensitive BRD4 ligand (compound 4) by introducing anticancer BRD4 inhibitor into naphthalimide moiety (fluorescent reporter) via a sulfonamide unit as glutathione (GSH)-specific cleavable linker.	Naphthalimides	191-204	bromodomain containing 4	Homo sapiens	171-175
35123163-2	2022	We herein present the design, chemical synthesis, cellular imaging and biological assessment of a novel tumor-sensitive BRD4 ligand (compound 4) by introducing anticancer BRD4 inhibitor into naphthalimide moiety (fluorescent reporter) via a sulfonamide unit as glutathione (GSH)-specific cleavable linker.	Sulfonamides	241-252	bromodomain containing 4	Homo sapiens	120-124
35123163-2	2022	We herein present the design, chemical synthesis, cellular imaging and biological assessment of a novel tumor-sensitive BRD4 ligand (compound 4) by introducing anticancer BRD4 inhibitor into naphthalimide moiety (fluorescent reporter) via a sulfonamide unit as glutathione (GSH)-specific cleavable linker.	Sulfonamides	241-252	bromodomain containing 4	Homo sapiens	171-175
35123163-2	2022	We herein present the design, chemical synthesis, cellular imaging and biological assessment of a novel tumor-sensitive BRD4 ligand (compound 4) by introducing anticancer BRD4 inhibitor into naphthalimide moiety (fluorescent reporter) via a sulfonamide unit as glutathione (GSH)-specific cleavable linker.	Glutathione	261-272	bromodomain containing 4	Homo sapiens	120-124
35123163-2	2022	We herein present the design, chemical synthesis, cellular imaging and biological assessment of a novel tumor-sensitive BRD4 ligand (compound 4) by introducing anticancer BRD4 inhibitor into naphthalimide moiety (fluorescent reporter) via a sulfonamide unit as glutathione (GSH)-specific cleavable linker.	Glutathione	261-272	bromodomain containing 4	Homo sapiens	171-175
35123163-2	2022	We herein present the design, chemical synthesis, cellular imaging and biological assessment of a novel tumor-sensitive BRD4 ligand (compound 4) by introducing anticancer BRD4 inhibitor into naphthalimide moiety (fluorescent reporter) via a sulfonamide unit as glutathione (GSH)-specific cleavable linker.	Glutathione	274-277	bromodomain containing 4	Homo sapiens	120-124
35123163-2	2022	We herein present the design, chemical synthesis, cellular imaging and biological assessment of a novel tumor-sensitive BRD4 ligand (compound 4) by introducing anticancer BRD4 inhibitor into naphthalimide moiety (fluorescent reporter) via a sulfonamide unit as glutathione (GSH)-specific cleavable linker.	Glutathione	274-277	bromodomain containing 4	Homo sapiens	171-175
35123163-3	2022	Upon reaction with abundant intramolecular GSH in cancer cells or free GSH in aqueous solution (pH = 7.4), sulfonamide cleavage of 4 occurs, leading to the release of BRD4 inhibitor and concomitant fluorescence-on.	Glutathione	43-46	bromodomain containing 4	Homo sapiens	167-171
35123163-3	2022	Upon reaction with abundant intramolecular GSH in cancer cells or free GSH in aqueous solution (pH = 7.4), sulfonamide cleavage of 4 occurs, leading to the release of BRD4 inhibitor and concomitant fluorescence-on.	Glutathione	71-74	bromodomain containing 4	Homo sapiens	167-171
35123163-3	2022	Upon reaction with abundant intramolecular GSH in cancer cells or free GSH in aqueous solution (pH = 7.4), sulfonamide cleavage of 4 occurs, leading to the release of BRD4 inhibitor and concomitant fluorescence-on.	Sulfonamides	107-118	bromodomain containing 4	Homo sapiens	167-171
35146591-0	2022	Susceptibility of Lung Carcinoma Cells to Nanostructured Lipid Carrier of ARV-825, a BRD4 Degrading Proteolysis Targeting Chimera.	omega-N-Allylarginine	74-77	bromodomain containing 4	Homo sapiens	85-89
34982556-4	2022	The X-ray crystal structural analysis of ZL0590 in complex with human BRD4 BD1 and the associated mutagenesis study illustrate a first-in-class nonacetylated lysine (KAc) binding site located at the helix alphaB and alphaC interface that contains important BRD4 residues (e.g., Glu151) not commonly shared among other family members and is spatially distinct from the classic KAc recognition pocket.	ZL0590	41-47	bromodomain containing 4	Homo sapiens	70-74
34982556-4	2022	The X-ray crystal structural analysis of ZL0590 in complex with human BRD4 BD1 and the associated mutagenesis study illustrate a first-in-class nonacetylated lysine (KAc) binding site located at the helix alphaB and alphaC interface that contains important BRD4 residues (e.g., Glu151) not commonly shared among other family members and is spatially distinct from the classic KAc recognition pocket.	ZL0590	41-47	bromodomain containing 4	Homo sapiens	257-261
34982556-4	2022	The X-ray crystal structural analysis of ZL0590 in complex with human BRD4 BD1 and the associated mutagenesis study illustrate a first-in-class nonacetylated lysine (KAc) binding site located at the helix alphaB and alphaC interface that contains important BRD4 residues (e.g., Glu151) not commonly shared among other family members and is spatially distinct from the classic KAc recognition pocket.	Lysine	158-164	bromodomain containing 4	Homo sapiens	70-74
34982556-4	2022	The X-ray crystal structural analysis of ZL0590 in complex with human BRD4 BD1 and the associated mutagenesis study illustrate a first-in-class nonacetylated lysine (KAc) binding site located at the helix alphaB and alphaC interface that contains important BRD4 residues (e.g., Glu151) not commonly shared among other family members and is spatially distinct from the classic KAc recognition pocket.	Lysine	158-164	bromodomain containing 4	Homo sapiens	257-261
34995979-0	2022	Design, synthesis, and evaluation of novel pyridone derivatives as potent BRD4 inhibitors for the potential treatment of prostate cancer.	Pyridones	43-51	bromodomain containing 4	Homo sapiens	74-78
35007061-4	2022	Here, we address this challenge via a structure-activity relationship study using 1,4,5-trisubstituted imidazoles against the BRD4 N-terminal bromodomain (D1).	1,4,5-trisubstituted imidazoles	82-113	bromodomain containing 4	Homo sapiens	126-130
34995979-2	2022	Herein, we designed and synthesized a series of 5-(1-benzyl-1H-indazol-6-yl)-4-ethoxy-1-methylpyridin-2(1H)-one derivatives as novel BRD4 inhibitors for prostate cancer.	5-(1-benzyl-1h-indazol-6-yl)-4-ethoxy-1-methylpyridin-2(1h)	48-107	bromodomain containing 4	Homo sapiens	133-137
34935961-2	2022	While inactive P-TEFbs are mainly sequestered in the 7SK snRNP complex in a chromatin-free state, most of its active forms are in complex with its recruitment factors, Brd4 and SEC, in a chromatin-associated state.	Phosphorus	15-16	bromodomain containing 4	Homo sapiens	168-172
35198433-8	2021	Combining YKL-5-124 with the BRD4 inhibitor JQ1 resulted in synergistic cytotoxicity.	YKL-5-124	10-19	bromodomain containing 4	Homo sapiens	29-33
35198433-11	2021	Conclusions: The combination of CDK7 and BRD4 inhibition provides a therapeutic option for neuroblastoma and suggests that the addition of YKL-5-124 could improve the therapeutic efficacy of JQ1 and delay resistance to BRD4 inhibition.	YKL-5-124	139-148	bromodomain containing 4	Homo sapiens	41-45
35198433-11	2021	Conclusions: The combination of CDK7 and BRD4 inhibition provides a therapeutic option for neuroblastoma and suggests that the addition of YKL-5-124 could improve the therapeutic efficacy of JQ1 and delay resistance to BRD4 inhibition.	YKL-5-124	139-148	bromodomain containing 4	Homo sapiens	219-223
34935961-2	2022	While inactive P-TEFbs are mainly sequestered in the 7SK snRNP complex in a chromatin-free state, most of its active forms are in complex with its recruitment factors, Brd4 and SEC, in a chromatin-associated state.	tefbs	17-22	bromodomain containing 4	Homo sapiens	168-172
34935961-3	2022	Thus, switching from inactive 7SK snRNP to active P-TEFb (Brd4/P-TEFb or SEC/P-TEFb) is essential for global gene expression.	Phosphorus	50-51	bromodomain containing 4	Homo sapiens	58-62
34935961-3	2022	Thus, switching from inactive 7SK snRNP to active P-TEFb (Brd4/P-TEFb or SEC/P-TEFb) is essential for global gene expression.	tefb	52-56	bromodomain containing 4	Homo sapiens	58-62
34994556-5	2022	We further establish that EN106 can be used as a covalent recruiter for FEM1B in TPD applications by demonstrating that a PROTAC linking EN106 to the BET bromodomain inhibitor JQ1 or the kinase inhibitor dasatinib leads to the degradation of BRD4 and BCR-ABL, respectively.	EN106	26-31	bromodomain containing 4	Homo sapiens	242-246
34994556-5	2022	We further establish that EN106 can be used as a covalent recruiter for FEM1B in TPD applications by demonstrating that a PROTAC linking EN106 to the BET bromodomain inhibitor JQ1 or the kinase inhibitor dasatinib leads to the degradation of BRD4 and BCR-ABL, respectively.	EN106	137-142	bromodomain containing 4	Homo sapiens	242-246
35046638-0	2022	Berbamine Suppresses the Growth of Gastric Cancer Cells by Inactivating the BRD4/c-MYC Signaling Pathway.	berbamine	0-9	bromodomain containing 4	Homo sapiens	76-80
34387610-0	2022	Circular RNA circ-CCT3 promotes bortezomib resistance in multiple myeloma via modulating miR-223-3p/BRD4 axis.	Bortezomib	32-42	bromodomain containing 4	Homo sapiens	100-104
34387610-12	2022	Moreover, miR-223-3p increased bortezomib sensitivity by inhibiting BRD4.	mir-223-3p	10-20	bromodomain containing 4	Homo sapiens	68-72
34387610-12	2022	Moreover, miR-223-3p increased bortezomib sensitivity by inhibiting BRD4.	Bortezomib	31-41	bromodomain containing 4	Homo sapiens	68-72
34387610-13	2022	Downregulation of circ-CCT3 attenuated bortezomib resistance of multiple myeloma via regulating miR-223-3p/BRD4 pathway, which provided a new potential target for multiple myeloma chemoresistance.	Bortezomib	39-49	bromodomain containing 4	Homo sapiens	107-111
35083874-7	2022	RESULTS: BRD4 inhibitors JQ1 and ARV-771 were identified as the most promising drugs both in the cisplatin and radiation screening projects in two NSCLC cell lines.	Cisplatin	97-106	bromodomain containing 4	Homo sapiens	9-13
33862375-3	2021	A series of compounds (14-23, 38-41, 43, 47-49) bearing triazolopyridazine motif exhibited remarkable BRD4 protein inhibitory activities.	tetraazaisoindole	56-74	bromodomain containing 4	Homo sapiens	102-106
35159127-0	2022	Discovery of a Novel Aminocyclopropenone Compound That Inhibits BRD4-Driven Nucleoporin NUP210 Expression and Attenuates Colorectal Cancer Growth.	aminocyclopropenone	21-40	bromodomain containing 4	Homo sapiens	64-68
35159127-10	2022	In conclusion, our findings highlighted an aminocyclopropenone compound as a novel therapeutic drug blocking BRD4 assembly, thereby preventing BRD4-driven oncogenic functions in cancer cells.	aminocyclopropenone	43-62	bromodomain containing 4	Homo sapiens	109-113
35159127-10	2022	In conclusion, our findings highlighted an aminocyclopropenone compound as a novel therapeutic drug blocking BRD4 assembly, thereby preventing BRD4-driven oncogenic functions in cancer cells.	aminocyclopropenone	43-62	bromodomain containing 4	Homo sapiens	143-147
33094643-5	2021	Our data revealed that BRD4 expression was elevated in trophoblast cells stimulated with hydrogen peroxide.	Hydrogen Peroxide	89-106	bromodomain containing 4	Homo sapiens	23-27
33907583-6	2021	The compounds with naphthalene-1,4-dione had cytotoxic effects against the Ty82 cell line, a NUT midline carcinoma cell line, whose proliferation is dependent on brd4 activity.	1,4-naphthoquinone	19-40	bromodomain containing 4	Homo sapiens	162-166
34045230-3	2021	Together, BRD4 and CDK9 phosphorylate serine 2 (pSer2) of heptad repeats in the C-terminal domain of RPB1, the large subunit of pol II, promoting transcriptional elongation.	Serine	38-44	bromodomain containing 4	Homo sapiens	10-14
34039605-3	2021	Here, we show that BRD4 is methylated on chromatin at lysine-99 by the protein lysine methyltransferase SETD6.	Lysine	54-60	bromodomain containing 4	Homo sapiens	19-23
34039605-3	2021	Here, we show that BRD4 is methylated on chromatin at lysine-99 by the protein lysine methyltransferase SETD6.	Lysine	79-85	bromodomain containing 4	Homo sapiens	19-23
33638254-2	2021	By taking BI-2536 (PLK1 and BRD4 inhibitor) as the lead compound, sixteen novel BRD4 inhibitors with the 4,4-difluoro-1-methyl-N,6-diphenyl-5,6-dihydro-4H-pyrimido[4,5-b] [1,2,4] triazolo[4,3-d] [1,4] diazepine-8-amine structure were designed and synthetized.	BI 2536	10-17	bromodomain containing 4	Homo sapiens	80-84
33638254-3	2021	Among the target compounds, compound 15h exhibited outstanding inhibition for BRD4-BD1 (IC50 value of 0.42 muM) in the BRD4-BD1 inhibitory activity assay.	(1s)-1-(1-{3-[4-(1,3-Benzothiazol-2-Ylamino)phenoxy]pyrazin-2-Yl}piperidin-4-Yl)ethanol	37-40	bromodomain containing 4	Homo sapiens	78-82
33638254-3	2021	Among the target compounds, compound 15h exhibited outstanding inhibition for BRD4-BD1 (IC50 value of 0.42 muM) in the BRD4-BD1 inhibitory activity assay.	(1s)-1-(1-{3-[4-(1,3-Benzothiazol-2-Ylamino)phenoxy]pyrazin-2-Yl}piperidin-4-Yl)ethanol	37-40	bromodomain containing 4	Homo sapiens	119-123
34031359-6	2021	We show that BRD4 inhibitors reduce the expression of SatIII, restoring etoposide sensitivity.	Etoposide	72-81	bromodomain containing 4	Homo sapiens	13-17
33094643-7	2021	Knockdown of BRD4, or treatment with a BRD4 inhibitor, markedly increased the levels of cell proliferation and invasion and decreased apoptosis and ROS production following the hydrogen peroxide challenge.	ros	148-151	bromodomain containing 4	Homo sapiens	13-17
33094643-7	2021	Knockdown of BRD4, or treatment with a BRD4 inhibitor, markedly increased the levels of cell proliferation and invasion and decreased apoptosis and ROS production following the hydrogen peroxide challenge.	ros	148-151	bromodomain containing 4	Homo sapiens	39-43
33094643-7	2021	Knockdown of BRD4, or treatment with a BRD4 inhibitor, markedly increased the levels of cell proliferation and invasion and decreased apoptosis and ROS production following the hydrogen peroxide challenge.	Hydrogen Peroxide	177-194	bromodomain containing 4	Homo sapiens	13-17
33094643-7	2021	Knockdown of BRD4, or treatment with a BRD4 inhibitor, markedly increased the levels of cell proliferation and invasion and decreased apoptosis and ROS production following the hydrogen peroxide challenge.	Hydrogen Peroxide	177-194	bromodomain containing 4	Homo sapiens	39-43
33094643-10	2021	Overall, these results demonstrated that BRD4 inhibition attenuated hydrogen peroxide-induced oxidative stress injury in trophoblast cells by enhancing Nrf2 activation via the downregulation of Keap1.	Hydrogen Peroxide	68-85	bromodomain containing 4	Homo sapiens	41-45
33480647-9	2021	These results suggest that dual PI3K/BRD4 inhibitor, SF1126, has antitumor activity in ES models.	SF 1126	53-59	bromodomain containing 4	Homo sapiens	37-41
33995089-0	2021	Case Report: 7-Ethyl-10-Hydroxycamptothecin, a DNA Topoisomerase I Inhibitor, Performs BRD4 Inhibitory Activity and Inhibits Human Leukemic Cell Growth.	Irinotecan	13-43	bromodomain containing 4	Homo sapiens	87-91
33995089-2	2021	In our study, SN-38 was characterized as a potent and reversible BRD4 inhibitor [IC50 = 660.2 nM against BRD4 (BD1) and IC50 = 547.7 nM against BRD4 (BD2)] in biochemical assay using drug repurposing strategy.	Irinotecan	14-19	bromodomain containing 4	Homo sapiens	65-69
33995089-2	2021	In our study, SN-38 was characterized as a potent and reversible BRD4 inhibitor [IC50 = 660.2 nM against BRD4 (BD1) and IC50 = 547.7 nM against BRD4 (BD2)] in biochemical assay using drug repurposing strategy.	Irinotecan	14-19	bromodomain containing 4	Homo sapiens	105-109
33995089-2	2021	In our study, SN-38 was characterized as a potent and reversible BRD4 inhibitor [IC50 = 660.2 nM against BRD4 (BD1) and IC50 = 547.7 nM against BRD4 (BD2)] in biochemical assay using drug repurposing strategy.	Irinotecan	14-19	bromodomain containing 4	Homo sapiens	105-109
33995089-3	2021	Additional cellular assay suggested that SN-38 can bind BRD4 in human leukemic cell K562 and inhibit cell growth with IC50 = 0.2798 muM in a BRD4 dependent manner partially.	Irinotecan	41-46	bromodomain containing 4	Homo sapiens	56-60
33995089-3	2021	Additional cellular assay suggested that SN-38 can bind BRD4 in human leukemic cell K562 and inhibit cell growth with IC50 = 0.2798 muM in a BRD4 dependent manner partially.	Irinotecan	41-46	bromodomain containing 4	Homo sapiens	141-145
33995089-4	2021	Additionally, mechanism study indicated that SN-38 can induce the accumulation of BRD4 substrate c-Myc and cleavage of caspase 3.	Irinotecan	45-50	bromodomain containing 4	Homo sapiens	82-86
33995089-5	2021	In sum, our findings identified BRD4 as a new target of SN-38 and reveals SN-38 as a modifier of histone acetylation reader for the first time, which may provide a new insight for further optimization of dual target inhibitor.	Irinotecan	56-61	bromodomain containing 4	Homo sapiens	32-36
33888130-0	2021	BRD4 PROTAC degrader ARV-825 inhibits T-cell acute lymphoblastic leukemia by targeting "Undruggable" Myc-pathway genes.	omega-N-Allylarginine	21-24	bromodomain containing 4	Homo sapiens	0-4
33888130-9	2021	BRD4, BRD3 and BRD2 proteins were detected by western blot in cells treated with ARV-825.	omega-N-Allylarginine	81-84	bromodomain containing 4	Homo sapiens	0-4
33833509-13	2021	Additionally, miR-145-5p mimics protected against CSE-induced cell injury through targeting BRD4.	mir-145-5p	14-24	bromodomain containing 4	Homo sapiens	92-96
33840312-6	2022	The MCAP Score was correlated with serum carotenoids and serum omega-3 fatty acids, and improvements in the score were associated with weight loss over six months of study.	Carotenoids	41-52	bromodomain containing 4	Homo sapiens	4-8
33840312-6	2022	The MCAP Score was correlated with serum carotenoids and serum omega-3 fatty acids, and improvements in the score were associated with weight loss over six months of study.	Fatty Acids, Omega-3	63-82	bromodomain containing 4	Homo sapiens	4-8
33796404-9	2021	Metabolic modulation with metformin modifies the acetylation pattern in the B7-H6 promoter, impairing BRD4 binding, thereby inhibiting B7-H6 expression.	Metformin	26-35	bromodomain containing 4	Homo sapiens	102-106
33838899-7	2021	Several genes were potential Bromodomain-containing protein 4 (Brd4) targets, making Brd4 inhibitors - JQ1, AZD5153 - and cyclin-dependent kinase (Brd4"s binding partner) inhibitors - dinaciclib - potential therapeutic agents.	AZD5153	108-115	bromodomain containing 4	Homo sapiens	29-61
33838899-7	2021	Several genes were potential Bromodomain-containing protein 4 (Brd4) targets, making Brd4 inhibitors - JQ1, AZD5153 - and cyclin-dependent kinase (Brd4"s binding partner) inhibitors - dinaciclib - potential therapeutic agents.	AZD5153	108-115	bromodomain containing 4	Homo sapiens	63-67
33838899-7	2021	Several genes were potential Bromodomain-containing protein 4 (Brd4) targets, making Brd4 inhibitors - JQ1, AZD5153 - and cyclin-dependent kinase (Brd4"s binding partner) inhibitors - dinaciclib - potential therapeutic agents.	AZD5153	108-115	bromodomain containing 4	Homo sapiens	85-89
33838899-7	2021	Several genes were potential Bromodomain-containing protein 4 (Brd4) targets, making Brd4 inhibitors - JQ1, AZD5153 - and cyclin-dependent kinase (Brd4"s binding partner) inhibitors - dinaciclib - potential therapeutic agents.	AZD5153	108-115	bromodomain containing 4	Homo sapiens	85-89
33838899-7	2021	Several genes were potential Bromodomain-containing protein 4 (Brd4) targets, making Brd4 inhibitors - JQ1, AZD5153 - and cyclin-dependent kinase (Brd4"s binding partner) inhibitors - dinaciclib - potential therapeutic agents.	dinaciclib	184-194	bromodomain containing 4	Homo sapiens	29-61
33838899-7	2021	Several genes were potential Bromodomain-containing protein 4 (Brd4) targets, making Brd4 inhibitors - JQ1, AZD5153 - and cyclin-dependent kinase (Brd4"s binding partner) inhibitors - dinaciclib - potential therapeutic agents.	dinaciclib	184-194	bromodomain containing 4	Homo sapiens	63-67
33838899-7	2021	Several genes were potential Bromodomain-containing protein 4 (Brd4) targets, making Brd4 inhibitors - JQ1, AZD5153 - and cyclin-dependent kinase (Brd4"s binding partner) inhibitors - dinaciclib - potential therapeutic agents.	dinaciclib	184-194	bromodomain containing 4	Homo sapiens	85-89
33838899-7	2021	Several genes were potential Bromodomain-containing protein 4 (Brd4) targets, making Brd4 inhibitors - JQ1, AZD5153 - and cyclin-dependent kinase (Brd4"s binding partner) inhibitors - dinaciclib - potential therapeutic agents.	dinaciclib	184-194	bromodomain containing 4	Homo sapiens	85-89
33749556-0	2022	Piecing the fragments together: Dynamical insights into the enhancement of BRD4-BD1 (BET protein) druggability in cancer chemotherapy using novel 8-methyl-pyrrolo[1,2-a]pyrazin-1(2H)-one derivatives.	8-methyl-pyrrolo[1,2-a]pyrazin-1(2h)-one	146-186	bromodomain containing 4	Homo sapiens	75-79
33736688-12	2021	In this line, reporter gene assays with combinatorial treatment of 3i-1000 and the BET bromodomain inhibitor (+)-JQ1 demonstrated the cooperative role of GATA4 and BRD4 in the modulation of chamber-specific cardiac gene expression.	GATA4-IN-3	67-74	bromodomain containing 4	Homo sapiens	164-168
33712563-8	2021	Importantly, siRNA knockdown demonstrated that JQ1 resistant cell lines are still dependent on BRD4 expression for survival and we found that phosphorylation of BRD4 is elevated in resistant LACs, identifying casein kinase 2 (CK2) as a candidate protein mediating this effect.	lacs	191-195	bromodomain containing 4	Homo sapiens	161-165
33712563-9	2021	Inhibition of CK2, as well as downstream transcriptional targets of phosphorylated BRD4-including AXL and activators of the PI3K pathway-synergize with JQ1 to inhibit BETi resistant LAC.	beti	167-171	bromodomain containing 4	Homo sapiens	83-87
33712563-10	2021	Overall, this demonstrates that the mechanism of resistance to BETi varies depending on cancer type, with LAC cells developing JQ1 resistance independent of MYC regulation, and identifying CK2 phosphorylation of BRD4 as a potential target to overcome resistance in this cancer.	beti	63-67	bromodomain containing 4	Homo sapiens	212-216
33611824-8	2021	In addition, apigenin inhibited proliferation, invasion, and EMT of Hela and CaSki cells by regulating miR-152-5p/BRD4 axis.	Apigenin	13-21	bromodomain containing 4	Homo sapiens	114-118
33688653-10	2021	One Sentence Summary: Evidence of in silico designed chemotype (SF2523) targeting PI3K-alpha/mTOR/BRD4 inhibits SARS-CoV-2 infection and is highly synergistic with remdesivir.	remdesivir	164-174	bromodomain containing 4	Homo sapiens	98-102
33654218-3	2021	One representative compound, 19 (Y06014), bound to BRD4(1) in the low micromolar range and demonstrated high selectivity for BRD4(1) over other non-BET bromodomain-containing proteins.	y06014	33-39	bromodomain containing 4	Homo sapiens	51-55
33654218-3	2021	One representative compound, 19 (Y06014), bound to BRD4(1) in the low micromolar range and demonstrated high selectivity for BRD4(1) over other non-BET bromodomain-containing proteins.	y06014	33-39	bromodomain containing 4	Homo sapiens	125-129
33611824-9	2021	Apigenin suppresses proliferation, invasion, and induced EMT of cervical carcinoma cells by regulation of miR-152-5p/BRD4 axis.	Apigenin	0-8	bromodomain containing 4	Homo sapiens	117-121
33290278-8	2020	In conclusion, BRD4 is a novel cofactor of FXR for maintaining BA homeostasis and hepatoprotection.	Bile Acids and Salts	63-65	bromodomain containing 4	Homo sapiens	15-19
33597515-3	2021	Here we show that cellular proteins, which form condensates at low salt concentrations, including FUS, TDP-43, Brd4, Sox2, and Annexin A11, can reenter a phase-separated regime at high salt concentrations.	Salts	185-189	bromodomain containing 4	Homo sapiens	111-115
33310044-0	2021	Co-delivery of EGFR and BRD4 siRNA by cell-penetrating peptides-modified redox-responsive complex in triple negative breast cancer cells.	Peptides	55-63	bromodomain containing 4	Homo sapiens	24-28
33310044-4	2021	MATERIALS AND METHODS: In the present study, we developed GALA- and CREKA-modified PEG-SS-PEI to deliver siRNAs targeting on EGFR and BRD4 for TNBC therapy.	peg-ss-pei	83-93	bromodomain containing 4	Homo sapiens	134-138
33718091-8	2021	Treatments with I-BET762, I-BET726, and CPI-203 could inhibit the proliferation, migration, and invasion of PCa cell lines including PC-3, LNCaP, and C42B, and could also regulate the histone crotonylation and androgen receptor signaling pathways via the regulation of BRD4 expression.	CPI203	40-47	bromodomain containing 4	Homo sapiens	269-273
32975004-0	2021	Selective N-terminal BRD4 bromodomain inhibitors by targeting non-conserved residues and structured water displacement.	Water	100-105	bromodomain containing 4	Homo sapiens	21-25
33392965-0	2021	Structural modification of 4, 5-dihydro-[1, 2, 4] triazolo [4, 3-f] pteridine derivatives as BRD4 inhibitors using 2D/3D-QSAR and molecular docking analysis.	4, 5-dihydro-[1, 2, 4] triazolo [4, 3-f] pteridine	27-77	bromodomain containing 4	Homo sapiens	93-97
33532187-0	2021	Design, synthesis, and biological evaluation of quinazolin-4(3H)-one derivatives co-targeting poly(ADP-ribose) polymerase-1 and bromodomain containing protein 4 for breast cancer therapy.	quinazolin-4(3h)	48-64	bromodomain containing 4	Homo sapiens	128-160
33520370-4	2021	We identified BRD4 inhibitors (BRD4i) as potent partners that, in combination with idelalisib, were capable of synergistically exerting anti-proliferative activity and inducing cell apoptosis in a panel of aggressive NHL cell lines through continuous suppression of PI3K pathways.	idelalisib	83-93	bromodomain containing 4	Homo sapiens	14-18
33191086-0	2021	Design, synthesis and biological evaluation of imidazolopyridone derivatives as novel BRD4 inhibitors.	imidazolopyridone	47-64	bromodomain containing 4	Homo sapiens	86-90
33191086-2	2021	In this study, using the BRD4 inhibitor Fragment 9 as a lead compound, a series of imidazolopyridone derivatives were designed and tested for their inhibitory activity against BRD4 protein in vitro.	imidazolopyridone	83-100	bromodomain containing 4	Homo sapiens	25-29
33191086-2	2021	In this study, using the BRD4 inhibitor Fragment 9 as a lead compound, a series of imidazolopyridone derivatives were designed and tested for their inhibitory activity against BRD4 protein in vitro.	imidazolopyridone	83-100	bromodomain containing 4	Homo sapiens	176-180
32647323-5	2021	Fedratinib exerts off-target inhibitory activity against bromodomain-containing protein 4 (BRD4); combination JAK/STAT and BRD4 inhibition was shown to synergistically block NF-kB hyperactivation and inflammatory cytokine production, attenuating disease burden and reversing bone marrow fibrosis in animal models of MPNs.	Fedratinib	0-10	bromodomain containing 4	Homo sapiens	57-89
32647323-5	2021	Fedratinib exerts off-target inhibitory activity against bromodomain-containing protein 4 (BRD4); combination JAK/STAT and BRD4 inhibition was shown to synergistically block NF-kB hyperactivation and inflammatory cytokine production, attenuating disease burden and reversing bone marrow fibrosis in animal models of MPNs.	Fedratinib	0-10	bromodomain containing 4	Homo sapiens	91-95
32897000-6	2020	Mechanistic studies revealed that DNP could downregulate the expression of COX-2 and PD-L1 in vitro and vivo , inhibit the secretion of prostaglandin, reduce the expression of BC-associated protein BRD4 and phosphorylation of extracellular signal-regulated kinases 1/2 (Erk1/2), and block the oncogene c-Myc in BC cells.	2,4-Dinitrophenol	34-37	bromodomain containing 4	Homo sapiens	198-202
33413475-3	2021	The Bromodomain (BD) and Extra-Terminal Domain (ET) protein, BRD4, is an important epigenetic reader that interacts with acetyl-histones and a variety of chromatin and transcriptional regulators to control gene expression, including HIV.	acetyl-histones	121-136	bromodomain containing 4	Homo sapiens	61-65
33077265-4	2021	This study provides support for selective HDAC/BRD4 dual inhibitors as epigenetic probes based on pyrrolopyridone core for the future biological evaluation in different cancer cell lines.	pyrrolopyridone	98-113	bromodomain containing 4	Homo sapiens	47-51
33408470-0	2020	MiR-218 Inhibits CSE-Induced Apoptosis and Inflammation in BEAS-2B by Targeting BRD4.	mir-218	0-7	bromodomain containing 4	Homo sapiens	80-84
33408470-12	2020	Conclusion: Overexpression of miR-218 inhibited CSE-induced apoptosis and inflammation in BEAS-2B cells by targeting BRD4 expression.	mir-218	30-37	bromodomain containing 4	Homo sapiens	117-121
32860796-0	2020	A 7-methoxybicoumarin derivative selectively inhibits BRD4 BD2 for anti-melanoma therapy.	7-methoxybicoumarin	2-21	bromodomain containing 4	Homo sapiens	54-58
32883643-0	2020	Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors.	indol-2-one	47-59	bromodomain containing 4	Homo sapiens	82-86
33138352-3	2020	To support the bromodomain inhibitor discovery process, here we report the first application of protein-observed fluorine (PrOF) NMR to the tandem bromodomains of BRD4 and BRDT to quantify the selectivity of their interactions with acetylated histones as well as small molecules.	Fluorine	113-121	bromodomain containing 4	Homo sapiens	163-167
33138352-3	2020	To support the bromodomain inhibitor discovery process, here we report the first application of protein-observed fluorine (PrOF) NMR to the tandem bromodomains of BRD4 and BRDT to quantify the selectivity of their interactions with acetylated histones as well as small molecules.	prof	123-127	bromodomain containing 4	Homo sapiens	163-167
33138352-3	2020	To support the bromodomain inhibitor discovery process, here we report the first application of protein-observed fluorine (PrOF) NMR to the tandem bromodomains of BRD4 and BRDT to quantify the selectivity of their interactions with acetylated histones as well as small molecules.	acetylated histones	232-251	bromodomain containing 4	Homo sapiens	163-167
33138352-4	2020	We further determine the selectivity profile of a new class of ligands, 1,4-acylthiazepanes, and find them to have >=3-10-fold selectivity for the C-terminal bromodomain of both BRD4 and BRDT.	1,4-acylthiazepanes	72-91	bromodomain containing 4	Homo sapiens	178-182
32868081-5	2020	Using the in vivo transfection of BRD4 siRNA, we found that BRD4 suppression markedly alleviated VCR-induced neuropathic pain.	Vincristine	97-100	bromodomain containing 4	Homo sapiens	34-38
32868081-5	2020	Using the in vivo transfection of BRD4 siRNA, we found that BRD4 suppression markedly alleviated VCR-induced neuropathic pain.	Vincristine	97-100	bromodomain containing 4	Homo sapiens	60-64
32861663-6	2020	Because DHA is the predominant component of fish oil, our data suggest that this nontoxic dietary supplement could be administered with BRD4 inhibitor during therapy for CRC, which lay an important foundation for the development of therapeutic regimens for CRC.	Docosahexaenoic Acids	8-11	bromodomain containing 4	Homo sapiens	136-140
32860796-5	2020	Using various biochemical assays, the 7-methoxycoumarin derivative N13 was identified as a potent inhibitor of BRD4 BD2.	herniarin	38-55	bromodomain containing 4	Homo sapiens	111-115
32860796-5	2020	Using various biochemical assays, the 7-methoxycoumarin derivative N13 was identified as a potent inhibitor of BRD4 BD2.	2-{3-[3-(1h-Benzimidazol-2-Yl)-1h-Indazol-6-Yl]-1h-Pyrazol-5-Yl}-N-(3-Fluorophenyl)acetamide	67-70	bromodomain containing 4	Homo sapiens	111-115
32860796-6	2020	Compared with the well-known BRD4 inhibitor JQ1, N13 exhibited higher potency against BRD4 BD2 and much higher specificity for BRD4 BD2 over BRD4 BD1.	2-{3-[3-(1h-Benzimidazol-2-Yl)-1h-Indazol-6-Yl]-1h-Pyrazol-5-Yl}-N-(3-Fluorophenyl)acetamide	49-52	bromodomain containing 4	Homo sapiens	29-33
32860796-6	2020	Compared with the well-known BRD4 inhibitor JQ1, N13 exhibited higher potency against BRD4 BD2 and much higher specificity for BRD4 BD2 over BRD4 BD1.	2-{3-[3-(1h-Benzimidazol-2-Yl)-1h-Indazol-6-Yl]-1h-Pyrazol-5-Yl}-N-(3-Fluorophenyl)acetamide	49-52	bromodomain containing 4	Homo sapiens	86-90
32860796-6	2020	Compared with the well-known BRD4 inhibitor JQ1, N13 exhibited higher potency against BRD4 BD2 and much higher specificity for BRD4 BD2 over BRD4 BD1.	2-{3-[3-(1h-Benzimidazol-2-Yl)-1h-Indazol-6-Yl]-1h-Pyrazol-5-Yl}-N-(3-Fluorophenyl)acetamide	49-52	bromodomain containing 4	Homo sapiens	86-90
32860796-6	2020	Compared with the well-known BRD4 inhibitor JQ1, N13 exhibited higher potency against BRD4 BD2 and much higher specificity for BRD4 BD2 over BRD4 BD1.	2-{3-[3-(1h-Benzimidazol-2-Yl)-1h-Indazol-6-Yl]-1h-Pyrazol-5-Yl}-N-(3-Fluorophenyl)acetamide	49-52	bromodomain containing 4	Homo sapiens	86-90
32860796-7	2020	Additionally, N13 inhibited the proliferation of two kinds of BRD4-overexpressing melanoma cell lines.	2-{3-[3-(1h-Benzimidazol-2-Yl)-1h-Indazol-6-Yl]-1h-Pyrazol-5-Yl}-N-(3-Fluorophenyl)acetamide	14-17	bromodomain containing 4	Homo sapiens	62-66
32860796-9	2020	To our knowledge, N13 is the first 7-methoxybicoumarin-based BRD4 BD2 inhibitor described to date and may function as a new scaffold for developing more specific and potent therapeutic agents against BRD4 BD2.	2-{3-[3-(1h-Benzimidazol-2-Yl)-1h-Indazol-6-Yl]-1h-Pyrazol-5-Yl}-N-(3-Fluorophenyl)acetamide	18-21	bromodomain containing 4	Homo sapiens	61-65
32860796-9	2020	To our knowledge, N13 is the first 7-methoxybicoumarin-based BRD4 BD2 inhibitor described to date and may function as a new scaffold for developing more specific and potent therapeutic agents against BRD4 BD2.	2-{3-[3-(1h-Benzimidazol-2-Yl)-1h-Indazol-6-Yl]-1h-Pyrazol-5-Yl}-N-(3-Fluorophenyl)acetamide	18-21	bromodomain containing 4	Homo sapiens	200-204
32860796-9	2020	To our knowledge, N13 is the first 7-methoxybicoumarin-based BRD4 BD2 inhibitor described to date and may function as a new scaffold for developing more specific and potent therapeutic agents against BRD4 BD2.	7-methoxybicoumarin	35-54	bromodomain containing 4	Homo sapiens	61-65
32860796-9	2020	To our knowledge, N13 is the first 7-methoxybicoumarin-based BRD4 BD2 inhibitor described to date and may function as a new scaffold for developing more specific and potent therapeutic agents against BRD4 BD2.	7-methoxybicoumarin	35-54	bromodomain containing 4	Homo sapiens	200-204
32898554-0	2020	Protein kinase C inhibitor anchored BRD4 PROTAC PEGylated nanoliposomes for the treatment of vemurafenib-resistant melanoma.	Vemurafenib	93-104	bromodomain containing 4	Homo sapiens	36-40
32333502-9	2020	Conversely, low FOXA1, BRD4 and H3K27ac levels were observed at regulatory sites that responded strongly to androgen stimulation, and AR interactions at these sites was blocked by darolutamide.	darolutamide	180-192	bromodomain containing 4	Homo sapiens	23-27
32961679-2	2020	Based on studies that HDAC6 and BRD4 are potential therapeutic targets of HNSCC, we hypothesized that the combination treatment of BET inhibitor JQ1 and HDAC6-selective inhibitor ACY-241 could exhibit synergistic anticancer effects in human papillomavirus (HPV)-positive and HPV-negative HNSCC cells.	Citarinostat	179-186	bromodomain containing 4	Homo sapiens	32-36
33162822-7	2020	In addition, the role of BRD4 on monosodium uric acid crystals (MSU)-induced pyroptosis was verified in BRD4 siRNA-transfected THP-1 cells.	monosodium uric acid crystals	33-62	bromodomain containing 4	Homo sapiens	25-29
33162822-7	2020	In addition, the role of BRD4 on monosodium uric acid crystals (MSU)-induced pyroptosis was verified in BRD4 siRNA-transfected THP-1 cells.	monosodium uric acid crystals	33-62	bromodomain containing 4	Homo sapiens	104-108
32978368-10	2020	BRD4 degradation and p53 protein elevation, as well as apoptosis induction and oxidative stress were detected in A1874-treated colon cancer tissues.	A1874	113-118	bromodomain containing 4	Homo sapiens	0-4
32978368-11	2020	Together, A1874 inhibits colon cancer cell growth through both BRD4-dependent and -independent mechanisms.	A1874	10-15	bromodomain containing 4	Homo sapiens	63-67
32968148-0	2020	Bardoxolone conjugation enables targeted protein degradation of BRD4.	2-cyano-3,12-dioxoolean-1,9-dien-28-oic acid	0-11	bromodomain containing 4	Homo sapiens	64-68
32968148-4	2020	Herein we demonstrate efficient proteasome-mediated degradation of BRD4 by a bifunctional small molecule linking the KEAP1-Nrf2 activator bardoxolone to a BRD4 inhibitor JQ1.	2-cyano-3,12-dioxoolean-1,9-dien-28-oic acid	138-149	bromodomain containing 4	Homo sapiens	67-71
32968148-4	2020	Herein we demonstrate efficient proteasome-mediated degradation of BRD4 by a bifunctional small molecule linking the KEAP1-Nrf2 activator bardoxolone to a BRD4 inhibitor JQ1.	2-cyano-3,12-dioxoolean-1,9-dien-28-oic acid	138-149	bromodomain containing 4	Homo sapiens	155-159
32859084-8	2020	While the potentiation of CHK1i-mediated effects by BETi was BET-BRD4-dependent, MYC expression was BET-BRD4-independent.	beti	52-56	bromodomain containing 4	Homo sapiens	65-69
32913560-7	2020	Importantly, IBET-151 abrogates the growth of vismodegib-resistant EAC cells and downregulates HH/GLI by reducing the occupancy of BRD4 at the GLI1 locus.	GSK1210151A	13-21	bromodomain containing 4	Homo sapiens	131-135
32782441-12	2020	BRD4 could directly bind to miR-338-3p in MM cells and miR-338-3p exerted an anti-tumor role through targeting BRD4.	mir-338-3p	28-38	bromodomain containing 4	Homo sapiens	0-4
32782441-12	2020	BRD4 could directly bind to miR-338-3p in MM cells and miR-338-3p exerted an anti-tumor role through targeting BRD4.	mir-338-3p	55-65	bromodomain containing 4	Homo sapiens	0-4
32782441-12	2020	BRD4 could directly bind to miR-338-3p in MM cells and miR-338-3p exerted an anti-tumor role through targeting BRD4.	mir-338-3p	55-65	bromodomain containing 4	Homo sapiens	111-115
32559581-7	2020	In summary, through a combination of computational and crystal-based structure optimization, DC-CPin711 showed potent in vitro inhibitory activities to CBP bromodomain with a decent selectivity towards BRD4 bromodomains and good cellular activity to leukemia cells, which could further be applied to related biological and translational studies as well as serve as a lead compound for future development of potent and selective CBP bromodomain inhibitors.	dc-cpin711	93-103	bromodomain containing 4	Homo sapiens	202-206
32631570-0	2020	Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors.	6-phenyl-1,3a,4,10b-tetrahydro-2h-benzo[c]thiazolo[4,5-e]azepin-2-one	53-122	bromodomain containing 4	Homo sapiens	148-152
32631570-2	2020	By replacing the methyltriazole ring of the BRD4 inhibitor I-BET-762 with an N-methylthiazolidone heterocyclic ring, fifteen novel BRD4 inhibitors were designed and synthesized.	4-methyl-1H-1,2,3-triazole	17-31	bromodomain containing 4	Homo sapiens	44-48
32631570-2	2020	By replacing the methyltriazole ring of the BRD4 inhibitor I-BET-762 with an N-methylthiazolidone heterocyclic ring, fifteen novel BRD4 inhibitors were designed and synthesized.	4-methyl-1H-1,2,3-triazole	17-31	bromodomain containing 4	Homo sapiens	131-135
32631570-2	2020	By replacing the methyltriazole ring of the BRD4 inhibitor I-BET-762 with an N-methylthiazolidone heterocyclic ring, fifteen novel BRD4 inhibitors were designed and synthesized.	molibresib	59-68	bromodomain containing 4	Homo sapiens	44-48
32631570-2	2020	By replacing the methyltriazole ring of the BRD4 inhibitor I-BET-762 with an N-methylthiazolidone heterocyclic ring, fifteen novel BRD4 inhibitors were designed and synthesized.	molibresib	59-68	bromodomain containing 4	Homo sapiens	131-135
32631570-2	2020	By replacing the methyltriazole ring of the BRD4 inhibitor I-BET-762 with an N-methylthiazolidone heterocyclic ring, fifteen novel BRD4 inhibitors were designed and synthesized.	n-methylthiazolidone	77-97	bromodomain containing 4	Homo sapiens	131-135
32631570-3	2020	Compound 13f had a hydrophobic acetylcyclopentanyl side chain, showing the most potent BRD4 inhibitory activity in the BRD4-BD1 inhibition assay (IC50 value of 110 nM), it also significantly suppressed the proliferation of MV-4-11 cells with high BRD4 level (IC50 value of 0.42 muM).	13F	9-12	bromodomain containing 4	Homo sapiens	87-91
32631570-3	2020	Compound 13f had a hydrophobic acetylcyclopentanyl side chain, showing the most potent BRD4 inhibitory activity in the BRD4-BD1 inhibition assay (IC50 value of 110 nM), it also significantly suppressed the proliferation of MV-4-11 cells with high BRD4 level (IC50 value of 0.42 muM).	13F	9-12	bromodomain containing 4	Homo sapiens	119-123
32631570-3	2020	Compound 13f had a hydrophobic acetylcyclopentanyl side chain, showing the most potent BRD4 inhibitory activity in the BRD4-BD1 inhibition assay (IC50 value of 110 nM), it also significantly suppressed the proliferation of MV-4-11 cells with high BRD4 level (IC50 value of 0.42 muM).	13F	9-12	bromodomain containing 4	Homo sapiens	119-123
32631570-5	2020	As the downstream-protein of BRD4, c-Myc was in significantly low expression by compound 13f treatment in a dose-dependent manner.	13F	89-92	bromodomain containing 4	Homo sapiens	29-33
32631570-6	2020	All the findings supported that this novel compound 13f provided a perspective for developing effective BRD4 inhibitors.	13F	52-55	bromodomain containing 4	Homo sapiens	104-108
32499570-2	2020	Bromodomain containing 4 (BRD4) is a chromatin protein that associates with acetylated histone lysines and facilitates transcription.	Lysine	95-102	bromodomain containing 4	Homo sapiens	0-24
32499570-2	2020	Bromodomain containing 4 (BRD4) is a chromatin protein that associates with acetylated histone lysines and facilitates transcription.	Lysine	95-102	bromodomain containing 4	Homo sapiens	26-30
32499570-8	2020	Our chromatin immunoprecipitation assay showed that JQ1 reduced the BRD4 binding to the histone H3 lysine 27 acetylation-enriched sites in the MMP2 locus.	Lysine	99-105	bromodomain containing 4	Homo sapiens	68-72
32522824-6	2020	Furthermore, the acetyltransferase p300 acetylated JMJD1A at lysine (K) 421, a modification that recruits the BET family member BRD4 to block JMJD1A degradation and promote JMJD1A recruitment to AR targets.	Lysine	61-67	bromodomain containing 4	Homo sapiens	128-132
32453591-3	2020	Novel pyrrolopyridone BETi leveraged novel interactions with L92/L94 confirmed by a cocrystal structure of 27 with BRD4.	pyrrolopyridone	6-21	bromodomain containing 4	Homo sapiens	115-119
32747750-10	2020	Our data indicate H3K27Ac/BRD4 epigenetics regulates the HGF/c-MET pathway in ATLs; targeting this pathway may improve treatment of aggressive non-PB-ATLs.	Lead	147-149	bromodomain containing 4	Homo sapiens	26-30
32793596-5	2020	Our screening analysis revealed that JQ1 and IBET-762, inhibitors of epigenetic reader BRD4, and LBH589, a pan inhibitor of histone deacetylases (HDACs), exhibited synergy with VS-6063 in mitigating tumor cell viability.	molibresib	45-53	bromodomain containing 4	Homo sapiens	87-91
32821285-7	2020	Mechanistically, apabetalone reduces the cytokine-driven increase in BRD4 BET occupancy at the CRP promoter, confirming that transcription of CRP is BET-dependent.	apabetalone	17-28	bromodomain containing 4	Homo sapiens	69-73
32453591-3	2020	Novel pyrrolopyridone BETi leveraged novel interactions with L92/L94 confirmed by a cocrystal structure of 27 with BRD4.	beti	22-26	bromodomain containing 4	Homo sapiens	115-119
32350070-8	2020	We conclude that association of E2 with the Brd4 CTM is necessary for viral genome replication and suggest that this interaction can be regulated by phosphorylation of E2 Y138.IMPORTANCE Papillomavirus (PV) is a double-stranded DNA tumor virus infecting the cutaneous and mucosal epithelium.	Estradiol	32-34	bromodomain containing 4	Homo sapiens	44-48
32478362-2	2020	A key dihydroquinoxalinone intermediate of a BRD4 inhibitor was synthesized using biomimetic asymmetric reduction.	dihydroquinoxalinone	6-26	bromodomain containing 4	Homo sapiens	45-49
32350070-11	2020	Employing a quasivirus infection model and selection for G418 resistant genomes, we demonstrated that Y138 is a critical residue for Brd4 association and that inability to complex with Brd4 does not support episomal replication.	y138	102-106	bromodomain containing 4	Homo sapiens	133-137
32371576-0	2020	Combined targeting of the BRD4-NUT-p300 axis in NUT midline carcinoma by dual selective bromodomain inhibitor, NEO2734.	HLA-B*27:34 antigen	111-118	bromodomain containing 4	Homo sapiens	26-30
32575711-3	2020	While blocking BRD4 interaction with acetylated histones using BET inhibitors (BETis) has been tested in clinical trials, many cancers have acquired BETi resistance.	beti	79-83	bromodomain containing 4	Homo sapiens	15-19
32657160-5	2020	Residue-based free energy decomposition method was wielded to unveil contributions of independent residues to inhibitor bindings and the data signify that hydrogen bonding interactions and hydrophobic interactions are decisive factors affecting bindings of inhibitors to BRD4(1).	Hydrogen	155-163	bromodomain containing 4	Homo sapiens	271-275
32575711-7	2020	Using CRISPR/Cas9 gene editing, we replaced endogenous BRD4 with a non-phosphorylatable mutant and demonstrated that CDK1-mediated BRD4 phosphorylation contributes to BETi resistance.	beti	167-171	bromodomain containing 4	Homo sapiens	55-59
32575711-7	2020	Using CRISPR/Cas9 gene editing, we replaced endogenous BRD4 with a non-phosphorylatable mutant and demonstrated that CDK1-mediated BRD4 phosphorylation contributes to BETi resistance.	beti	167-171	bromodomain containing 4	Homo sapiens	131-135
32575711-8	2020	CDK1 over-activation frequently observed in cancers has the potential to cause aberrant BRD4 hyperphosphorylation persisting outside of mitosis to strengthen its target gene binding and confer BETi resistance.	beti	193-197	bromodomain containing 4	Homo sapiens	88-92
32559187-6	2020	Combination treatment of MM cells with ARV 825 and AZD 4573 markedly reduced their protein expression of BRD 2, BRD 4, MYC and phosphorylated RNA pol II as compared to each single agent alone.	omega-N-Allylarginine	39-42	bromodomain containing 4	Homo sapiens	112-117
32575577-5	2020	BRD4 regulated epigenome related to fatty acid metabolism and the forkhead box P1 (Foxp1) pathway, which occupied the PPARgamma2 promoter to modulate glucocorticoid-induced adipocytic activity.	Fatty Acids	36-46	bromodomain containing 4	Homo sapiens	0-4
32575577-6	2020	In vivo, BRD4 inhibitor JQ-1 treatment mitigated methylprednisolone-induced suppression of bone mass, trabecular microstructure, mineral acquisition, and osteogenic differentiation.	Methylprednisolone	49-67	bromodomain containing 4	Homo sapiens	9-13
32575577-10	2020	Collective investigations convey a new epigenetic insight into acetyl histone reader BRD4 control of osteogenesis and adipogenesis in skeleton, and highlight the remedial effects of the BRD4 inhibitor on glucocorticoid-induced osteoporosis.	acetyl histone	63-77	bromodomain containing 4	Homo sapiens	85-89
32559187-6	2020	Combination treatment of MM cells with ARV 825 and AZD 4573 markedly reduced their protein expression of BRD 2, BRD 4, MYC and phosphorylated RNA pol II as compared to each single agent alone.	azd	51-54	bromodomain containing 4	Homo sapiens	112-117
32527308-9	2020	Mechanically, miR-101 targeted and negatively regulated BRD4 expression.	mir-101	14-21	bromodomain containing 4	Homo sapiens	56-60
32149490-0	2020	Covalent-Fragment Screening of BRD4 Identifies a Ligandable Site Orthogonal to the Acetyl-Lysine Binding Sites.	N(alpha)-acetyllysine	83-96	bromodomain containing 4	Homo sapiens	31-35
32527308-0	2020	MiR-101-containing extracellular vesicles bind to BRD4 and enhance proliferation and migration of trophoblasts in preeclampsia.	mir-101	0-7	bromodomain containing 4	Homo sapiens	50-54
32527308-12	2020	CONCLUSION: In summary, EV-encapsulated miR-101 promoted proliferation and migration of placental trophoblasts through the inhibition of BRD4 expression via NF-kappaB/CXCL11 inactivation.	mir-101	40-47	bromodomain containing 4	Homo sapiens	137-141
32371868-2	2020	I-BET726 is a novel BRD4 inhibitor.	4-(1-acetyl-4-((4-chlorophenyl)amino)-2-methyl-1,2,3,4-tetrahydroquinolin-6-yl)benzoic acid	0-8	bromodomain containing 4	Homo sapiens	20-24
32371868-7	2020	I-BET726 not only downregulated BRD4-regulated proteins (c-Myc, Bcl-2, and cyclin D1), but also inhibited sphingosine kinase 1 (SphK1) and Akt signalings in SCC cells.	4-(1-acetyl-4-((4-chlorophenyl)amino)-2-methyl-1,2,3,4-tetrahydroquinolin-6-yl)benzoic acid	0-8	bromodomain containing 4	Homo sapiens	32-36
32371868-10	2020	Downregulation of BRD4-regulated proteins and inhibition of the SphK1-Akt signaling were detected in I-BET726-treated A431 xenograft tumor tissues.	4-(1-acetyl-4-((4-chlorophenyl)amino)-2-methyl-1,2,3,4-tetrahydroquinolin-6-yl)benzoic acid	101-109	bromodomain containing 4	Homo sapiens	18-22
32324495-3	2020	The BETs (bromodomain and extraterminal-containing protein family), which includes BRD2, BRD3, and BRD4 and the testis-restricted BRDT, are epigenetic reader proteins that bind to specific acetylated lysine residues on histone tails where they facilitate the assembly of transcription complexes including transcription factors and transcriptional machinery like RNA Polymerase II.	Lysine	200-206	bromodomain containing 4	Homo sapiens	99-103
32694708-2	2020	Here, we developed a new generation of highly potent thienopyranone (TP)-based inhibitors for the BET bromodomains (BDs) of the transcriptional regulator BRD4 that have the ability to simultaneously bind to phosphatidylinositol-3 kinase (PI3K) and/or cyclin-dependent kinases 4/6 (CDK4/6).	thienopyranone	53-67	bromodomain containing 4	Homo sapiens	154-158
32694708-2	2020	Here, we developed a new generation of highly potent thienopyranone (TP)-based inhibitors for the BET bromodomains (BDs) of the transcriptional regulator BRD4 that have the ability to simultaneously bind to phosphatidylinositol-3 kinase (PI3K) and/or cyclin-dependent kinases 4/6 (CDK4/6).	tp	69-71	bromodomain containing 4	Homo sapiens	154-158
32694708-5	2020	We further demonstrate that concurrent disruption of the acetyllysine binding function of BRD4 and the kinase activities of PI3K and CDK4/6 by the TP inhibitor improves efficacy in several cancer models.	N-epsilon-Acetyl-L-lysine	57-69	bromodomain containing 4	Homo sapiens	90-94
32551032-0	2020	BRD4 inhibitor nitroxoline enhances the sensitivity of multiple myeloma cells to bortezomib in vitro and in vivo by promoting mitochondrial pathway-mediated cell apoptosis.	nitroxoline	15-26	bromodomain containing 4	Homo sapiens	0-4
32551032-0	2020	BRD4 inhibitor nitroxoline enhances the sensitivity of multiple myeloma cells to bortezomib in vitro and in vivo by promoting mitochondrial pathway-mediated cell apoptosis.	Bortezomib	81-91	bromodomain containing 4	Homo sapiens	0-4
32361153-0	2020	Development of small-molecule BRD4 degraders based on pyrrolopyridone derivative.	pyrrolopyridone	54-69	bromodomain containing 4	Homo sapiens	30-34
32361153-5	2020	Herein, we present the design, synthesis, and biological evaluation of pyrrolopyridone derivative-based BRD4 degraders.	pyrrolopyridone	71-86	bromodomain containing 4	Homo sapiens	104-108
32361153-7	2020	Anti-proliferative activity of 32a against BxPC3 cell line (IC50 = 0.165 muM) was improved by about 7-fold as compared to the BRD4 inhibitor ABBV-075.	mivebresib	141-149	bromodomain containing 4	Homo sapiens	126-130
32220972-4	2020	This study developed a dual BET and PLK1 inhibitor WNY0824 with nanomolar and equipotent inhibition of BRD4 and PLK1.	wny0824	51-58	bromodomain containing 4	Homo sapiens	103-107
32366905-6	2020	Mechanistically, A-485 inhibited p300-mediated histone acetylation, leading to disruption of BRD4-NUT binding to hyperacetylated megadomains.	A-485	17-22	bromodomain containing 4	Homo sapiens	93-97
32255647-0	2020	Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffolding Hopping, Optimization and Pharmacological Evaluation.	Chromones	33-41	bromodomain containing 4	Homo sapiens	78-82
32255647-2	2020	Herein, we report the design, synthesis, and pharmacological evaluation of novel chromone derivatives via scaffold hopping to discover a new class of orally bioavailable BRD4 selective inhibitors.	Chromones	81-89	bromodomain containing 4	Homo sapiens	170-174
32199616-2	2020	Bromodomain and extra terminal domain (BET) protein BRD4 binds to super-enhancers (SEs) that drive high expression of oncogenes in many cancers.	ses	83-86	bromodomain containing 4	Homo sapiens	52-56
32188727-0	2020	Epigenetic suppression of HIV in myeloid cells by the BRD4-selective small molecule modulator ZL0580.	ZL0580	94-100	bromodomain containing 4	Homo sapiens	54-58
32188727-4	2020	Our group has recently identified a BRD4-selective small molecule modulator (ZL0580) that induces epigenetic suppression of HIV.	ZL0580	77-83	bromodomain containing 4	Homo sapiens	36-40
32188727-14	2020	We here report that the BRD4-seletive small molecule modulator, ZL0580, induces potent and durable suppression of HIV in human microglial and monocytic cell lines.	ZL0580	64-70	bromodomain containing 4	Homo sapiens	24-28
32392533-7	2020	Inhibition of BRD4 by siBRD4 or inhibitors such as JQ-1 or I-BET762 prevented the aging of macrophages and lipid accumulation in the LPS-induced senescent macrophages by decreasing expression of SASP in autocrine and paracrine senescence.	molibresib	59-67	bromodomain containing 4	Homo sapiens	14-18
32149490-5	2020	Inspired by our computational prediction of hotspots adjacent to nonhomologous cysteine residues within the C-terminal BRD4 bromodomain (BRD4-BD2), we performed a midthroughput mass spectrometry screen to identify cysteine-reactive fragments that covalently and selectively modify BRD4.	Cysteine	79-87	bromodomain containing 4	Homo sapiens	119-123
32149490-5	2020	Inspired by our computational prediction of hotspots adjacent to nonhomologous cysteine residues within the C-terminal BRD4 bromodomain (BRD4-BD2), we performed a midthroughput mass spectrometry screen to identify cysteine-reactive fragments that covalently and selectively modify BRD4.	Cysteine	79-87	bromodomain containing 4	Homo sapiens	137-141
32149490-5	2020	Inspired by our computational prediction of hotspots adjacent to nonhomologous cysteine residues within the C-terminal BRD4 bromodomain (BRD4-BD2), we performed a midthroughput mass spectrometry screen to identify cysteine-reactive fragments that covalently and selectively modify BRD4.	Cysteine	79-87	bromodomain containing 4	Homo sapiens	137-141
32149490-5	2020	Inspired by our computational prediction of hotspots adjacent to nonhomologous cysteine residues within the C-terminal BRD4 bromodomain (BRD4-BD2), we performed a midthroughput mass spectrometry screen to identify cysteine-reactive fragments that covalently and selectively modify BRD4.	Cysteine	214-222	bromodomain containing 4	Homo sapiens	119-123
32149490-5	2020	Inspired by our computational prediction of hotspots adjacent to nonhomologous cysteine residues within the C-terminal BRD4 bromodomain (BRD4-BD2), we performed a midthroughput mass spectrometry screen to identify cysteine-reactive fragments that covalently and selectively modify BRD4.	Cysteine	214-222	bromodomain containing 4	Homo sapiens	137-141
32149490-5	2020	Inspired by our computational prediction of hotspots adjacent to nonhomologous cysteine residues within the C-terminal BRD4 bromodomain (BRD4-BD2), we performed a midthroughput mass spectrometry screen to identify cysteine-reactive fragments that covalently and selectively modify BRD4.	Cysteine	214-222	bromodomain containing 4	Homo sapiens	137-141
32149490-9	2020	Overall, we demonstrate the potential of targeting sites orthogonal to bromodomain acetyl-lysine binding sites to develop bivalent and covalent inhibitors that displace BRD4 from chromatin.	N(alpha)-acetyllysine	83-96	bromodomain containing 4	Homo sapiens	169-173
32100443-16	2020	Up-regulated BRD4 ultimately promoted cell proliferation and cell survival Down-regulated POU6F2-AS2 showed enhanced sensitivity of 5-FU.	Fluorouracil	132-136	bromodomain containing 4	Homo sapiens	13-17
32314893-0	2020	[Effect of miR-204-5p on the proliferation, migration, and invasion on tongue squamous cell carcinoma SCC25 cells by targeting bromodomain-containing protein 4].	mir-204-5p	11-21	bromodomain containing 4	Homo sapiens	127-159
32314893-3	2020	TargetScan and dual luciferase reporter assay were used to confirm the target relationship between miR-204-5p and BRD4.	mir-204-5p	99-109	bromodomain containing 4	Homo sapiens	114-118
32314893-5	2020	RT-qPCR and Western blot were used to detect the effects of miR-204-5p mimics and inhibitors on BRD4 expression.	mir-204-5p	60-70	bromodomain containing 4	Homo sapiens	96-100
32314893-6	2020	Transwell and CCK8 assays were used to detect the effects of miR-204-5p on proliferation, migration, and invasion through BRD4 regulation.	mir-204-5p	61-71	bromodomain containing 4	Homo sapiens	122-126
32314893-11	2020	When miR-204-5p and BRD4 were overexpressed in SCC25 cells, BRD4 can make up for the inhibitory effect of miR-204-5p on SCC25 cells.	mir-204-5p	5-15	bromodomain containing 4	Homo sapiens	60-64
32314893-11	2020	When miR-204-5p and BRD4 were overexpressed in SCC25 cells, BRD4 can make up for the inhibitory effect of miR-204-5p on SCC25 cells.	mir-204-5p	106-116	bromodomain containing 4	Homo sapiens	20-24
32314893-11	2020	When miR-204-5p and BRD4 were overexpressed in SCC25 cells, BRD4 can make up for the inhibitory effect of miR-204-5p on SCC25 cells.	mir-204-5p	106-116	bromodomain containing 4	Homo sapiens	60-64
32314893-12	2020	CONCLUSIONS: miR-204-5p could inhibit proliferation, migration and invasion in tongue squamous cell carcinoma SCC25 cells by targeting BRD4 gene.	mir-204-5p	13-23	bromodomain containing 4	Homo sapiens	135-139
31813613-4	2020	Herein, we present our design, synthesis and biological evaluation of a new class of PROTAC BRD4 degraders, which were based on a potent dihydroquinazolinone-based BRD4 inhibitor compound 6 and lenalidomide/pomalidomide as ligand for E3 ligase cereblon.	3,4-dihydroquinazolin-2(1H)-one	137-157	bromodomain containing 4	Homo sapiens	92-96
32163373-0	2020	ARV-825-induced BRD4 protein degradation as a therapy for thyroid carcinoma.	ARV-825	0-7	bromodomain containing 4	Homo sapiens	16-20
32163373-11	2020	Taken together, ARV-825 induces BRD4 protein degradation and inhibits thyroid carcinoma cell growth in vitro and in vivo.	ARV-825	16-23	bromodomain containing 4	Homo sapiens	32-36
32151278-10	2020	We found that RNAi depletion of the BET family members, bromodomain-containing protein 4 (BRD4) and bromodomain-containing protein 2 (BRD2) inhibited expression of two melanin synthesis enzymes, TYR and TYRP1.	Melanins	168-175	bromodomain containing 4	Homo sapiens	56-88
32151278-10	2020	We found that RNAi depletion of the BET family members, bromodomain-containing protein 4 (BRD4) and bromodomain-containing protein 2 (BRD2) inhibited expression of two melanin synthesis enzymes, TYR and TYRP1.	Melanins	168-175	bromodomain containing 4	Homo sapiens	90-94
32151278-10	2020	We found that RNAi depletion of the BET family members, bromodomain-containing protein 4 (BRD4) and bromodomain-containing protein 2 (BRD2) inhibited expression of two melanin synthesis enzymes, TYR and TYRP1.	Tyrosine	195-198	bromodomain containing 4	Homo sapiens	56-88
32151278-10	2020	We found that RNAi depletion of the BET family members, bromodomain-containing protein 4 (BRD4) and bromodomain-containing protein 2 (BRD2) inhibited expression of two melanin synthesis enzymes, TYR and TYRP1.	Tyrosine	195-198	bromodomain containing 4	Homo sapiens	90-94
32195191-7	2020	Pharmacologic inhibition of BRD4, and thereby c-MYC, partially abrogated resistance to AZD1775.	adavosertib	87-94	bromodomain containing 4	Homo sapiens	28-32
31724259-0	2020	BRD4 promotes glioma cell stemness via enhancing miR-142-5p-mediated activation of Wnt/beta-catenin signaling.	mir-142-5p	49-59	bromodomain containing 4	Homo sapiens	0-4
31724259-6	2020	Importantly, inhibition of miR-142-5p or reactivation of Wnt/beta-catenin signaling rescues the inhibition of BRD4 knockdown on glioma cell stemness.	mir-142-5p	27-37	bromodomain containing 4	Homo sapiens	110-114
31587361-0	2020	In silico design and molecular basis for the selectivity of Olinone toward the first over the second bromodomain of BRD4.	Olinone	60-67	bromodomain containing 4	Homo sapiens	116-120
32184777-0	2020	BRD4 Inhibition by AZD5153 Promotes Antitumor Immunity via Depolarizing M2 Macrophages.	AZD5153	19-26	bromodomain containing 4	Homo sapiens	0-4
32184777-5	2020	AZD5153 inhibiting BRD4, as a potential therapeutic strategy for HGSOC, was demonstrated to confer controversial plasticity on TAMs, which shows the need to uncover its impact on TAMs in HGSOC.	AZD5153	0-7	bromodomain containing 4	Homo sapiens	19-23
32184777-8	2020	This modification occurs on MAF transcripts in TAMs and modified by BRD4, which is the target of AZD5153.	AZD5153	97-104	bromodomain containing 4	Homo sapiens	68-72
32099528-5	2020	The effects of BRD4 on the cell proliferation were detected by colony formation assay and sulforhodamine B assay.	lissamine rhodamine B	90-106	bromodomain containing 4	Homo sapiens	15-19
31792058-7	2020	Remarkably, a chimeric BET protein comprising the N-terminal half of the structurally similar short BRD4 isoform (BRD4S) and the C-terminal half of BRD2 functioned similarly to intact BRD2.	Nitrogen	50-51	bromodomain containing 4	Homo sapiens	100-104
31707348-4	2020	In the study, our results showed that BRD4 expression was up-regulated in human and mouse hypertrophied hearts, and importantly these effects were modulated by reactive oxygen species (ROS) generation.	Oxygen	169-175	bromodomain containing 4	Homo sapiens	38-42
31813613-0	2020	Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide.	3,4-dihydroquinazolin-2(1H)-one	61-81	bromodomain containing 4	Homo sapiens	35-39
31813613-0	2020	Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide.	lenalidomide	97-109	bromodomain containing 4	Homo sapiens	35-39
31813613-0	2020	Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide.	pomalidomide	110-122	bromodomain containing 4	Homo sapiens	35-39
32080280-4	2020	We show here that cells coexpressing BRD4 and cereblon (CRBN) tagged with the Fluoppi system formed detectable foci in both live and fixed cells only when treated with BRD4-targeting degraders utilizing CRBN as an E3 ligase in dose- and time-dependent manners.	fluoppi	78-85	bromodomain containing 4	Homo sapiens	37-41
32080280-4	2020	We show here that cells coexpressing BRD4 and cereblon (CRBN) tagged with the Fluoppi system formed detectable foci in both live and fixed cells only when treated with BRD4-targeting degraders utilizing CRBN as an E3 ligase in dose- and time-dependent manners.	fluoppi	78-85	bromodomain containing 4	Homo sapiens	168-172
32110043-11	2020	BRD4 downregulation could repress DUB3-induced EZH2 production, and MG132 reversed DUB3 decreasing-mediated BRD4 downregulation.	benzyloxycarbonylleucyl-leucyl-leucine aldehyde	68-73	bromodomain containing 4	Homo sapiens	108-112
31908141-3	2020	Mechanistically, PCAF acetylation of ISX at lysine 69 promotes the interaction with acetylated bromodomain-containing protein 4 (BRD4) at lysine 332 in tumor cells, and the translocation of the resulting complex into the nucleus.	tyrosyl-lysine	44-50	bromodomain containing 4	Homo sapiens	95-127
31908141-3	2020	Mechanistically, PCAF acetylation of ISX at lysine 69 promotes the interaction with acetylated bromodomain-containing protein 4 (BRD4) at lysine 332 in tumor cells, and the translocation of the resulting complex into the nucleus.	tyrosyl-lysine	44-50	bromodomain containing 4	Homo sapiens	129-133
31908141-3	2020	Mechanistically, PCAF acetylation of ISX at lysine 69 promotes the interaction with acetylated bromodomain-containing protein 4 (BRD4) at lysine 332 in tumor cells, and the translocation of the resulting complex into the nucleus.	tyrosyl-lysine	138-144	bromodomain containing 4	Homo sapiens	95-127
31908141-3	2020	Mechanistically, PCAF acetylation of ISX at lysine 69 promotes the interaction with acetylated bromodomain-containing protein 4 (BRD4) at lysine 332 in tumor cells, and the translocation of the resulting complex into the nucleus.	tyrosyl-lysine	138-144	bromodomain containing 4	Homo sapiens	129-133
31957165-6	2020	Knockout of BRD4 in vitro suppressed KIT expression, which led to inactivation of the KIT/PI3K/AKT/mTOR pathway, impeded migration and cell growth and made the resistant GIST cells sensitive to imatinib.	imatinib	194-202	bromodomain containing 4	Homo sapiens	12-16
31957165-7	2020	The expression of KIT was repressed by a BRD4 inhibitor JQ1, which also induced myristoylated-AKT-suppressible caspases 3 and 9 activities, induced LC3-II, exhibited dose-dependent therapeutic synergy with imatinib and attenuated the activation of the PI3K/AKT/mTOR pathway.	imatinib	206-214	bromodomain containing 4	Homo sapiens	41-45
32002032-13	2020	A subsequent rescue experiment indicated that the upregulation of BRD4 may reverse the apoptosis-promoting effect induced by miRNA-608.	mirna-608	125-134	bromodomain containing 4	Homo sapiens	66-70
31708100-6	2020	In addition, the expression level of BRD4 was high in HCT116 cells exposed to 5-FU that showed lower apoptosis against the parental cells.	Fluorouracil	78-82	bromodomain containing 4	Homo sapiens	37-41
31708100-7	2020	Moreover, the 5-FU-resistance was reversed significantly by BRD4 knockdown or inhibition.	Fluorouracil	14-18	bromodomain containing 4	Homo sapiens	60-64
31813613-4	2020	Herein, we present our design, synthesis and biological evaluation of a new class of PROTAC BRD4 degraders, which were based on a potent dihydroquinazolinone-based BRD4 inhibitor compound 6 and lenalidomide/pomalidomide as ligand for E3 ligase cereblon.	3,4-dihydroquinazolin-2(1H)-one	137-157	bromodomain containing 4	Homo sapiens	164-168
31813613-4	2020	Herein, we present our design, synthesis and biological evaluation of a new class of PROTAC BRD4 degraders, which were based on a potent dihydroquinazolinone-based BRD4 inhibitor compound 6 and lenalidomide/pomalidomide as ligand for E3 ligase cereblon.	lenalidomide	194-206	bromodomain containing 4	Homo sapiens	92-96
31813613-4	2020	Herein, we present our design, synthesis and biological evaluation of a new class of PROTAC BRD4 degraders, which were based on a potent dihydroquinazolinone-based BRD4 inhibitor compound 6 and lenalidomide/pomalidomide as ligand for E3 ligase cereblon.	lenalidomide	194-206	bromodomain containing 4	Homo sapiens	164-168
31813613-4	2020	Herein, we present our design, synthesis and biological evaluation of a new class of PROTAC BRD4 degraders, which were based on a potent dihydroquinazolinone-based BRD4 inhibitor compound 6 and lenalidomide/pomalidomide as ligand for E3 ligase cereblon.	pomalidomide	207-219	bromodomain containing 4	Homo sapiens	92-96
31813613-4	2020	Herein, we present our design, synthesis and biological evaluation of a new class of PROTAC BRD4 degraders, which were based on a potent dihydroquinazolinone-based BRD4 inhibitor compound 6 and lenalidomide/pomalidomide as ligand for E3 ligase cereblon.	pomalidomide	207-219	bromodomain containing 4	Homo sapiens	164-168
31882553-3	2020	RESULTS: Treatment with BRD4 inhibitor I-BET151 exerted a dose-dependent inhibitory effect on cell proliferation in MCL cell lines.	GSK1210151A	39-47	bromodomain containing 4	Homo sapiens	24-28
31815566-1	2020	Introduction: The bromodomain-containing protein 4 (BRD4), a member of the bromodomain and extra-terminal (BET) family, functions as an "epigenetic reader" that binds to acetylated lysine (KAc) residues on histone tails sophisticatedly regulating chromatin structure and gene expression.	tyrosyl-lysine	181-187	bromodomain containing 4	Homo sapiens	18-50
31815566-1	2020	Introduction: The bromodomain-containing protein 4 (BRD4), a member of the bromodomain and extra-terminal (BET) family, functions as an "epigenetic reader" that binds to acetylated lysine (KAc) residues on histone tails sophisticatedly regulating chromatin structure and gene expression.	tyrosyl-lysine	181-187	bromodomain containing 4	Homo sapiens	52-56
31815566-1	2020	Introduction: The bromodomain-containing protein 4 (BRD4), a member of the bromodomain and extra-terminal (BET) family, functions as an "epigenetic reader" that binds to acetylated lysine (KAc) residues on histone tails sophisticatedly regulating chromatin structure and gene expression.	4-Quinolinecarbamic acid, 2-butoxy-, 2-(diethylamino)ethyl ester	189-192	bromodomain containing 4	Homo sapiens	18-50
31815566-1	2020	Introduction: The bromodomain-containing protein 4 (BRD4), a member of the bromodomain and extra-terminal (BET) family, functions as an "epigenetic reader" that binds to acetylated lysine (KAc) residues on histone tails sophisticatedly regulating chromatin structure and gene expression.	4-Quinolinecarbamic acid, 2-butoxy-, 2-(diethylamino)ethyl ester	189-192	bromodomain containing 4	Homo sapiens	52-56
31534014-3	2020	Here, we demonstrated that PARP inhibitor (olaparib)-resistant epithelial ovarian cancer (EOC) cells exhibited an elevated aldehyde dehydrogenase (ALDH) activity, mainly contributed by increased expression of ALDH1A1 due to olaparib-induced expression of BRD4, a member of bromodomain and extraterminal (BET) family protein.	olaparib	43-51	bromodomain containing 4	Homo sapiens	255-259
31701109-1	2019	As a member of the bromodomain and extra terminal domain (BET) protein family, bromodomain-containing protein 4 (BRD4) is an epigenetic reader and can recognize acetylated lysine residues in histones.	tyrosyl-lysine	172-178	bromodomain containing 4	Homo sapiens	79-111
31875566-7	2019	Here, we find that BRD4, an acetyl-histone-binding chromatin reader, inhibits the PCNA-unloading activity of ATAD5-RLC.	acetyl phosphate	28-34	bromodomain containing 4	Homo sapiens	19-23
31875566-9	2019	BRD4-ATAD5 binds to acetyl-histones in nascent chromatin.	acetyl phosphate	20-26	bromodomain containing 4	Homo sapiens	0-4
31875566-11	2019	Disruption of the interaction between BRD4 and acetyl-histones or between BRD4 and ATAD5 reduces the PCNA amount on chromatin.	acetyl phosphate	47-53	bromodomain containing 4	Homo sapiens	38-42
31875566-13	2019	Thus, acetyl-histone-bound BRD4 fine-tunes PCNA unloading from nascent DNA.	acetyl phosphate	6-12	bromodomain containing 4	Homo sapiens	27-31
31697807-0	2019	AMP-activated protein kinase links acetyl-CoA homeostasis to BRD4 recruitment in acute myeloid leukemia.	acetyl phosphate	35-41	bromodomain containing 4	Homo sapiens	61-65
31886177-2	2019	The aim of this study was to examine whether combining a novel BRD4 inhibitor, ITH-47, with the antimitotic estradiol analogue, ESE-15-ol, would have a synergistic effect on inhibiting the growth of two different breast cancer cell lines in vitro.	ith-47	79-85	bromodomain containing 4	Homo sapiens	63-67
31886177-3	2019	Our docking and molecular dynamics studies showed that compared to JQ1, ITH-47 showed a similar binding mode with hydrogen bonds forming between the ligand nitrogens of the pyrazole, ASN99, and water of the BRD4 protein.	Water	194-199	bromodomain containing 4	Homo sapiens	207-211
31701109-1	2019	As a member of the bromodomain and extra terminal domain (BET) protein family, bromodomain-containing protein 4 (BRD4) is an epigenetic reader and can recognize acetylated lysine residues in histones.	tyrosyl-lysine	172-178	bromodomain containing 4	Homo sapiens	113-117
31720974-2	2019	Here, we utilized an integrated footprinting strategy incorporating both hydrogen-deuterium exchange (HDX) and hydroxyl radical footprinting (i.e., fast photochemical oxidation of proteins (FPOP)) for molecular-level characterization of the interaction of human bromodomain-containing protein 4 (BRD4) with a hydrophobic benzodiazepine inhibitor.	Benzodiazepines	321-335	bromodomain containing 4	Homo sapiens	262-294
31753913-5	2019	We also discovered the bromo-and-extra-terminal (BET) BRD proteins, BRD2 and BRD4, as negative regulators of transcription-associated RNA-DNA hybrids (R-loops) as inhibition of BRD2 or BRD4 increased R-loop formation, which generated DSBs.	1,2-di-(4-sulfamidophenyl)-4-butylpyrazolidine-3,5-dione	234-238	bromodomain containing 4	Homo sapiens	77-81
31753913-5	2019	We also discovered the bromo-and-extra-terminal (BET) BRD proteins, BRD2 and BRD4, as negative regulators of transcription-associated RNA-DNA hybrids (R-loops) as inhibition of BRD2 or BRD4 increased R-loop formation, which generated DSBs.	1,2-di-(4-sulfamidophenyl)-4-butylpyrazolidine-3,5-dione	234-238	bromodomain containing 4	Homo sapiens	185-189
30879350-0	2019	Discovery of novel coumarin derivatives as potent and orally bioavailable BRD4 inhibitors based on scaffold hopping.	coumarin	19-27	bromodomain containing 4	Homo sapiens	74-78
31712669-7	2019	The novel combination of romidepsin and JQ1, a BRD4 inhibitor was investigated and showed synergy.	romidepsin	25-35	bromodomain containing 4	Homo sapiens	47-51
31814132-7	2019	This resulted in (1) a common substructure (ethyl-benzene) in 60% of selected BRD4-inhibitors, and (2) four compounds that increased ApoA-I: hesperetin, equilenin, 9(S)-HOTrE, and cymarin.	ethylbenzene	44-57	bromodomain containing 4	Homo sapiens	78-82
31814132-8	2019	Whether these increases are regulated via BRD4 inhibition and the ethyl-benzene structure inhibits BRD4 requires further study.	ethylbenzene	66-79	bromodomain containing 4	Homo sapiens	99-103
31527063-3	2019	Here we reported a novel benzoxazinone derivative YLT-LL-11 as potential BRD4 inhibitor and further investigated the biological activities against DLBCL.	Benzoxazines	25-38	bromodomain containing 4	Homo sapiens	73-77
31527063-3	2019	Here we reported a novel benzoxazinone derivative YLT-LL-11 as potential BRD4 inhibitor and further investigated the biological activities against DLBCL.	ylt-ll-11	50-59	bromodomain containing 4	Homo sapiens	73-77
31527063-7	2019	Taken together, these results revealed that BRD4 inhibitor YLT-LL-11 can down regulate growth-associated transcription factors MYC in DLBCL thus resulted in cell growth inhibition and apoptosis.	ylt-ll-11	59-68	bromodomain containing 4	Homo sapiens	44-48
31692901-7	2019	The epigenetic mark 8-oxoG is bound by a pleiotropic DNA repair enzyme, 8-oxoguanine DNA glycosylase (OGG1), which induces conformational changes in adjacent DNA to recruit the NFkappaB bromodomain-containing protein 4 (BRD4) complex.	5-hydroxy-8-oxo-7,8-dihydroguanosine	20-26	bromodomain containing 4	Homo sapiens	220-224
31857846-0	2019	Pharmacokinetics-Driven Optimization of 7-Methylimidazo[1,5-a]pyrazin-8(7H)-one as Novel BRD4 Inhibitors.	2-methyl-6-(4-methoxyphenyl)-3,7-dihydroimidazo(1,2-alpha)pyrazin-3-one	40-79	bromodomain containing 4	Homo sapiens	89-93
31857841-6	2019	We screened a 3D-enriched fragment library against BRD4(D1) via 1H CPMG NMR with a protein-observed 19F NMR secondary assay.	Hydrogen	64-71	bromodomain containing 4	Homo sapiens	51-55
31780938-2	2019	The bromodomain and extraterminal (BET) protein family (BRD2, BRD3, BRD4, and BRDT) are epigenetic readers that, via bromodomains, regulate gene transcription by binding to acetylated lysine residues on histones and master transcriptional factors.	tyrosyl-lysine	184-190	bromodomain containing 4	Homo sapiens	68-72
31832310-4	2019	Through binding to bromodomains and the phosphorylation-dependent interaction domain of bromodomain protein 4 (BRD4) via the C-terminus, GLTSCR1 blocks oncogenic transcriptional elongation.	Carbon	125-126	bromodomain containing 4	Homo sapiens	88-109
31832310-4	2019	Through binding to bromodomains and the phosphorylation-dependent interaction domain of bromodomain protein 4 (BRD4) via the C-terminus, GLTSCR1 blocks oncogenic transcriptional elongation.	Carbon	125-126	bromodomain containing 4	Homo sapiens	111-115
30879350-3	2019	Starting from scaffold hopping of the reported compound dihydroquinazolinone (PFI-1), a series of coumarin derivatives were designed and synthesised as a new chemotype of BRD4 inhibitors.	3,4-dihydroquinazolin-2(1H)-one	56-76	bromodomain containing 4	Homo sapiens	171-175
30879350-3	2019	Starting from scaffold hopping of the reported compound dihydroquinazolinone (PFI-1), a series of coumarin derivatives were designed and synthesised as a new chemotype of BRD4 inhibitors.	coumarin	98-106	bromodomain containing 4	Homo sapiens	171-175
31042405-2	2019	BRD4 (bromodomain-containing protein 4), a member of the BET (bromodomain and extra-terminal motif) family, has been identified as a critical epigenetic driver for cardiovascular diseases.Objectives: To explore the therapeutic potential in PAH of RVX208, a clinically available BET inhibitor.Methods: Microvascular endothelial cells, smooth muscle cells isolated from distal pulmonary arteries of patients with PAH, rats with Sugen5416 + hypoxia- or monocrotaline + shunt-induced PAH, and rats with RV pressure overload induced by pulmonary artery banding were treated with RVX208 in three independent laboratories.Measurements and Main Results: BRD4 is upregulated in the remodeled pulmonary vasculature of patients with PAH, where it regulates FoxM1 and PLK1, proteins implicated in the DNA damage response.	Monocrotaline	450-463	bromodomain containing 4	Homo sapiens	0-4
31042405-2	2019	BRD4 (bromodomain-containing protein 4), a member of the BET (bromodomain and extra-terminal motif) family, has been identified as a critical epigenetic driver for cardiovascular diseases.Objectives: To explore the therapeutic potential in PAH of RVX208, a clinically available BET inhibitor.Methods: Microvascular endothelial cells, smooth muscle cells isolated from distal pulmonary arteries of patients with PAH, rats with Sugen5416 + hypoxia- or monocrotaline + shunt-induced PAH, and rats with RV pressure overload induced by pulmonary artery banding were treated with RVX208 in three independent laboratories.Measurements and Main Results: BRD4 is upregulated in the remodeled pulmonary vasculature of patients with PAH, where it regulates FoxM1 and PLK1, proteins implicated in the DNA damage response.	Monocrotaline	450-463	bromodomain containing 4	Homo sapiens	6-38
31325480-0	2019	BRD4 contributes to high-glucose-induced podocyte injury by modulating Keap1/Nrf2/ARE signaling.	Glucose	25-32	bromodomain containing 4	Homo sapiens	0-4
31325480-6	2019	BRD4 inhibition by small interfering RNA or its chemical inhibitor (JQ1) markedly repressed HG-induced apoptosis and reactive oxygen species (ROS) production.	Reactive Oxygen Species	117-140	bromodomain containing 4	Homo sapiens	0-4
31325480-6	2019	BRD4 inhibition by small interfering RNA or its chemical inhibitor (JQ1) markedly repressed HG-induced apoptosis and reactive oxygen species (ROS) production.	Reactive Oxygen Species	142-145	bromodomain containing 4	Homo sapiens	0-4
31421967-0	2019	Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors.	3,5-Dimethylisoxazole	47-68	bromodomain containing 4	Homo sapiens	97-101
31421967-0	2019	Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors.	Pyridones	73-81	bromodomain containing 4	Homo sapiens	97-101
31421967-3	2019	Therein, pyridone derivatives were more effective against BRD4 protein and human leukemia cell lines MV4-11.	Pyridones	9-17	bromodomain containing 4	Homo sapiens	58-62
31421967-5	2019	Moreover, in western blot assay, compound 11e induced down-regulation of C-Myc, which is a significant downstream gene of BRD4.	N-[(2-Amino-1,3-Benzothiazol-6-Yl)carbonyl]glycine	42-45	bromodomain containing 4	Homo sapiens	122-126
31421967-7	2019	Taken together, our results suggested that compound 11e and its derivatives were a class of novel structural potential BRD4 inhibitors and could serve as lead compounds for further exploration.	N-[(2-Amino-1,3-Benzothiazol-6-Yl)carbonyl]glycine	52-55	bromodomain containing 4	Homo sapiens	119-123
31311807-6	2019	In an acetylation-dependent manner, BRD4 recognized acetylated lysine 146 (K146) and K187 on Snail to prevent Snail recognition by its E3 ubiquitin ligases FBXL14 and beta-Trcp1, thereby inhibiting Snail polyubiquitination and proteasomal degradation.	Lysine	63-69	bromodomain containing 4	Homo sapiens	36-40
31394259-0	2019	BRD4 PROTAC as a novel therapeutic approach for the treatment of vemurafenib resistant melanoma: Preformulation studies, formulation development and in vitro evaluation.	Vemurafenib	65-76	bromodomain containing 4	Homo sapiens	0-4
31406246-7	2019	We also showed that TAZ, YAP, and their partner TEAD are direct targets of BRD4 and that treatment with BETi downregulates their expression.	beti	104-108	bromodomain containing 4	Homo sapiens	75-79
31329163-8	2019	Mechanistically different from the BET/BRD4 pan-inhibitor JQ1, which nonselectively binds to BD1 and BD2 domains of all BET proteins, ZL0580 selectively bound to BD1 domain of BRD4.	ZL0580	134-140	bromodomain containing 4	Homo sapiens	176-180
31254363-4	2019	Mechanistically, ISO treatment decreases H3K27me2/3 modifications on the atrial natriuretic factor (ANF) promoter by suppressing NSD3 and inhibits the association between NSD3 and bromodomain-containing protein 4 (BRD4), thus suppressing the BRD4-mediated H3K27ac modifications, which ultimately promote ANF transcription and cardiomyocyte hypertrophy.	Isoproterenol	17-20	bromodomain containing 4	Homo sapiens	180-212
31254363-4	2019	Mechanistically, ISO treatment decreases H3K27me2/3 modifications on the atrial natriuretic factor (ANF) promoter by suppressing NSD3 and inhibits the association between NSD3 and bromodomain-containing protein 4 (BRD4), thus suppressing the BRD4-mediated H3K27ac modifications, which ultimately promote ANF transcription and cardiomyocyte hypertrophy.	Isoproterenol	17-20	bromodomain containing 4	Homo sapiens	214-218
31254363-4	2019	Mechanistically, ISO treatment decreases H3K27me2/3 modifications on the atrial natriuretic factor (ANF) promoter by suppressing NSD3 and inhibits the association between NSD3 and bromodomain-containing protein 4 (BRD4), thus suppressing the BRD4-mediated H3K27ac modifications, which ultimately promote ANF transcription and cardiomyocyte hypertrophy.	Isoproterenol	17-20	bromodomain containing 4	Homo sapiens	242-246
30720865-9	2019	In conclusion, targeting LOL using preclinical/clinical drugs, such as BRD4 inhibitors, may represent a promising approach to inhibit luminal breast cancer progression and tamoxifen resistance.	Tamoxifen	172-181	bromodomain containing 4	Homo sapiens	71-75
31142662-6	2019	Furthermore, Mus81 promoted migration of gastric cancer cells both in vitro and in vivo We conducted a drug screen using a collection of preclinical and FDA-approved drugs and found that the BRD4 inhibitor AZD5153 inhibited the expression of Mus81 and ZEB1 by regulating the epigenetic factor Sirt5.	AZD5153	206-213	bromodomain containing 4	Homo sapiens	191-195
31142662-8	2019	Importantly, we demonstrate that the BRD4 inhibitor AZD5153 can potentially be used as an effective antimetastasis drug because of its effect on Mus81.	AZD5153	52-59	bromodomain containing 4	Homo sapiens	37-41
31492561-8	2019	Notably, somatic mutation analysis indicated that CIMP-H patients presented with a higher mutation burden of BRD4, DDIAS and NOX1.	cimp-h	50-56	bromodomain containing 4	Homo sapiens	109-113
31239290-0	2019	Targeted and Interactome Proteomics Revealed the Role of PHD2 in Regulating BRD4 Proline Hydroxylation.	Proline	81-88	bromodomain containing 4	Homo sapiens	76-80
31239290-2	2019	Our previous study identified and validated Bromodomain-containing protein 4 (BRD4) as a proline hydroxylation substrate in cancer cells.	Proline	89-96	bromodomain containing 4	Homo sapiens	44-76
31239290-2	2019	Our previous study identified and validated Bromodomain-containing protein 4 (BRD4) as a proline hydroxylation substrate in cancer cells.	Proline	89-96	bromodomain containing 4	Homo sapiens	78-82
31239290-4	2019	In this study, we developed targeted quantification assays using parallel-reaction monitoring and biochemical analysis to identify the major regulatory enzyme of BRD4 proline hydroxylation.	Proline	167-174	bromodomain containing 4	Homo sapiens	162-166
31239290-6	2019	Our findings revealed that PHD2 is the key regulatory enzyme of BRD4 proline hydroxylation and the modification significantly affects BRD4 interactions with key transcription factors as well as BRD4-mediated transcriptional activation.	Proline	69-76	bromodomain containing 4	Homo sapiens	64-68
31239290-6	2019	Our findings revealed that PHD2 is the key regulatory enzyme of BRD4 proline hydroxylation and the modification significantly affects BRD4 interactions with key transcription factors as well as BRD4-mediated transcriptional activation.	Proline	69-76	bromodomain containing 4	Homo sapiens	134-138
31239290-6	2019	Our findings revealed that PHD2 is the key regulatory enzyme of BRD4 proline hydroxylation and the modification significantly affects BRD4 interactions with key transcription factors as well as BRD4-mediated transcriptional activation.	Proline	69-76	bromodomain containing 4	Homo sapiens	134-138
31239290-7	2019	Taken together, this study provided mechanistic insights into the oxygen-dependent modification of BRD4 and revealed new roles of the pathway in regulating BRD4-dependent gene expression.	Oxygen	66-72	bromodomain containing 4	Homo sapiens	99-103
31239290-7	2019	Taken together, this study provided mechanistic insights into the oxygen-dependent modification of BRD4 and revealed new roles of the pathway in regulating BRD4-dependent gene expression.	Oxygen	66-72	bromodomain containing 4	Homo sapiens	156-160
31257080-0	2019	Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208.	apabetalone	95-102	bromodomain containing 4	Homo sapiens	80-84
31257080-2	2019	In this study, we introduced the pharmacophore of fibrates to a BRD4 inhibitor, RVX-208, to design dual-active hypolipidemic compounds, and found that some of new analogues showed favorable hypolipidemic activities.	apabetalone	80-87	bromodomain containing 4	Homo sapiens	64-68
31523195-0	2019	BRD4 Inhibitor AZD5153 Suppresses the Proliferation of Colorectal Cancer Cells and Sensitizes the Anticancer Effect of PARP Inhibitor.	AZD5153	15-22	bromodomain containing 4	Homo sapiens	0-4
31531200-7	2019	A BRD4-D1 cocrystal structure indicates that the 1,2,3-triazole is acting as a N-epsilon-acetylated lysine mimic.	Triazoles	49-63	bromodomain containing 4	Homo sapiens	2-6
31531200-7	2019	A BRD4-D1 cocrystal structure indicates that the 1,2,3-triazole is acting as a N-epsilon-acetylated lysine mimic.	n-epsilon-acetylated lysine	79-106	bromodomain containing 4	Homo sapiens	2-6
31523195-2	2019	AZD5153, a novel specific BRD4 inhibitor, showed potent anticancer effects in several cancer types, but its therapeutic potential has not been fully evaluated in colorectal cancer cells.	AZD5153	0-7	bromodomain containing 4	Homo sapiens	26-30
31523195-3	2019	Objective: We sought to evaluate the therapeutic potential of BRD4 inhibition of by AZD5153 and its combined anticancer cancer effect with PARP inhibitor BMN673 in vitro and in vivo in colorectal cancer.	AZD5153	84-91	bromodomain containing 4	Homo sapiens	62-66
31523195-3	2019	Objective: We sought to evaluate the therapeutic potential of BRD4 inhibition of by AZD5153 and its combined anticancer cancer effect with PARP inhibitor BMN673 in vitro and in vivo in colorectal cancer.	talazoparib	154-160	bromodomain containing 4	Homo sapiens	62-66
31523195-11	2019	Western blotting showed that AZD5153 inhibited the expression of c-Myc and increased expression of the apoptosis markers, cleaved caspase-3 and poly(ADP-ribose) polymerase (PARP), besides, we found that BRD4 knockdown could also inhibited cell proliferation and induced cell apoptosis.	AZD5153	29-36	bromodomain containing 4	Homo sapiens	203-207
31300040-3	2019	In vitro studies have implicated the BET protein BRD4 as an epigenetic driver of inflammation and atherogenesis, suggesting that BETi may be clinically effective in combating VI.	beti	129-133	bromodomain containing 4	Homo sapiens	49-53
31300040-7	2019	BRD4 abundance on inflammatory and adhesion gene promoters and enhancers was reduced by apabetalone.	apabetalone	88-99	bromodomain containing 4	Homo sapiens	0-4
31288832-6	2019	Moreover, BETi suppressed MYC transcription and decreased BRD4 binding to MYC promoter in DHL cells.	beti	10-14	bromodomain containing 4	Homo sapiens	58-62
31079968-0	2019	Design, synthesis and biological evaluation of novel 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as potential BRD4 inhibitors.	4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine	53-96	bromodomain containing 4	Homo sapiens	122-126
31266503-2	2019	Bromodomain and extra-terminal (BET) proteins (BRD2, BRD3, BRD4 and BRDT) are chromatin readers essential for maintaining proper gene transcription by specifically binding acetylated lysine residues.	Lysine	183-189	bromodomain containing 4	Homo sapiens	59-63
31209349-3	2019	Here, we use a chemical proteomic strategy that leverages broadly reactive, cysteine-directed electrophilic fragments coupled to selective ligands for intracellular proteins (for example, SLF for FKBP12, JQ1 for BRD4) to screen for heterobifunctional degrader compounds (or proteolysis targeting chimeras, PROTACs) that operate by covalent adduction of E3 ligases.	Cysteine	76-84	bromodomain containing 4	Homo sapiens	212-216
31003769-0	2019	MicroRNA-146b-5p protects oligodendrocyte precursor cells from oxygen/glucose deprivation-induced injury through regulating Keap1/Nrf2 signaling via targeting bromodomain-containing protein 4.	Oxygen	63-69	bromodomain containing 4	Homo sapiens	159-191
30606790-4	2019	ARV 825 rapidly and efficiently degraded BRD 2 and BRD 4.	omega-N-Allylarginine	0-3	bromodomain containing 4	Homo sapiens	51-56
31059052-8	2019	Furthermore, the inhibited miR-125b contributed directly toward the upstream protein BRD4 3"-UTR of Jagged-1, ultimately activating the Notch signaling pathway with the upregulation of Jagged-1.	mir-125b	27-35	bromodomain containing 4	Homo sapiens	85-89
31133746-0	2019	MTHFD1 interaction with BRD4 links folate metabolism to transcriptional regulation.	Folic Acid	35-41	bromodomain containing 4	Homo sapiens	24-28
30690335-0	2019	3-Hydroxyisoindolin-1-one derivates: Synthesis by palladium-catalyzed CH activation as BRD4 inhibitors against human acute myeloid leukemia (AML) cells.	1H-Isoindol-1-one, 2,3-dihydro-3-hydroxy-	0-25	bromodomain containing 4	Homo sapiens	87-91
30690335-0	2019	3-Hydroxyisoindolin-1-one derivates: Synthesis by palladium-catalyzed CH activation as BRD4 inhibitors against human acute myeloid leukemia (AML) cells.	Palladium	50-59	bromodomain containing 4	Homo sapiens	87-91
30690335-3	2019	In this study, we made further structural modifications of our previously reported BRD4 inhibitors, to develop new chemical scaffold 3-Hydroxyisoindolin-1-One.	1H-Isoindol-1-one, 2,3-dihydro-3-hydroxy-	133-158	bromodomain containing 4	Homo sapiens	83-87
31059052-9	2019	In conclusion, the proliferation of HaCaT cells mediated by the Jagged-1/Notch signaling pathway was decreased with the miR-125b-mediated inhibition of BRD4 expression.	mir-125b	120-128	bromodomain containing 4	Homo sapiens	152-156
30421459-7	2019	The level of E6 directly correlated with the extent of cisplatin sensitivity and was shown to be increased in newly established drug-resistant cell line variants, while reducing E6 expression using Brd4-inhibitors enhanced chemoresponse when co-delivered with cisplatin.	Cisplatin	260-269	bromodomain containing 4	Homo sapiens	198-202
30421459-8	2019	Inhibition of Brd4 could represent a new therapeutic option by increasing treatment response in cervical cancer cells and might allow lower cisplatin dosages, thus reducing negative side effects.	Cisplatin	140-149	bromodomain containing 4	Homo sapiens	14-18
30842331-0	2019	Phosphorylation of a Conserved Tyrosine in the Papillomavirus E2 Protein Regulates Brd4 Binding and Viral Replication.	Tyrosine	31-39	bromodomain containing 4	Homo sapiens	83-87
30842331-13	2019	The current study demonstrates that FGFR3 phosphorylates E2 at tyrosine 138, which inhibits association with the C-terminal peptide of Brd4.	Tyrosine	63-71	bromodomain containing 4	Homo sapiens	135-139
30970245-2	2019	The acetyl-lysine binding protein BRD4 has been previously suggested to function as a transcriptional "bookmark" on mitotic chromatin.	N(alpha)-acetyllysine	4-17	bromodomain containing 4	Homo sapiens	34-38
31037138-4	2019	Methods: Expression of BRD4 mRNA and protein was determined by bioinformatics interrogation of publically available databases, primary HNSCC samples and 4NQO-induced HNSCC animal model.	4-Nitroquinoline-1-oxide	153-157	bromodomain containing 4	Homo sapiens	23-27
30565859-0	2019	Structural and thermodynamic characterization of the binding of isoliquiritigenin to the first bromodomain of BRD4.	isoliquiritigenin	64-81	bromodomain containing 4	Homo sapiens	110-114
30565859-1	2019	Bromodomain-containing protein 4 (BRD4) recognizes the acetylated lysine of histone H4 via its bromodomains, leading to the recruitment of positive transcription elongation factor b.	Lysine	66-72	bromodomain containing 4	Homo sapiens	0-32
30565859-1	2019	Bromodomain-containing protein 4 (BRD4) recognizes the acetylated lysine of histone H4 via its bromodomains, leading to the recruitment of positive transcription elongation factor b.	Lysine	66-72	bromodomain containing 4	Homo sapiens	34-38
30565859-3	2019	Using X-ray crystallographic screening, we identified the BRD4 inhibitory activity of isoliquiritigenin (ISL), a natural chalcone found in licorice.	isoliquiritigenin	86-103	bromodomain containing 4	Homo sapiens	58-62
30565859-3	2019	Using X-ray crystallographic screening, we identified the BRD4 inhibitory activity of isoliquiritigenin (ISL), a natural chalcone found in licorice.	isoliquiritigenin	105-108	bromodomain containing 4	Homo sapiens	58-62
30565859-3	2019	Using X-ray crystallographic screening, we identified the BRD4 inhibitory activity of isoliquiritigenin (ISL), a natural chalcone found in licorice.	Chalcone	121-129	bromodomain containing 4	Homo sapiens	58-62
30565859-4	2019	Structural analysis revealed that ISL bound to BRD4 with a novel binding mode and squeezed out one of the six conserved water molecules that form a strong hydrogen bond network.	Water	120-125	bromodomain containing 4	Homo sapiens	47-51
29931583-0	2019	Dual targeting of bromodomain-containing 4 by AZD5153 and BCL2 by AZD4320 against B-cell lymphomas concomitantly overexpressing c-MYC and BCL2.	AZD5153	46-53	bromodomain containing 4	Homo sapiens	18-42
29931583-0	2019	Dual targeting of bromodomain-containing 4 by AZD5153 and BCL2 by AZD4320 against B-cell lymphomas concomitantly overexpressing c-MYC and BCL2.	AZD4320	66-73	bromodomain containing 4	Homo sapiens	18-42
29931583-3	2019	We first used AZD5153, a novel bivalent inhibitor for bromodomain-containing 4 (BRD4), in DHL- and DEL-derived cell lines, because BRD4 regulates disease type-oriented key molecules for oncogenesis.	AZD5153	14-21	bromodomain containing 4	Homo sapiens	54-78
29931583-3	2019	We first used AZD5153, a novel bivalent inhibitor for bromodomain-containing 4 (BRD4), in DHL- and DEL-derived cell lines, because BRD4 regulates disease type-oriented key molecules for oncogenesis.	AZD5153	14-21	bromodomain containing 4	Homo sapiens	80-84
29931583-3	2019	We first used AZD5153, a novel bivalent inhibitor for bromodomain-containing 4 (BRD4), in DHL- and DEL-derived cell lines, because BRD4 regulates disease type-oriented key molecules for oncogenesis.	AZD5153	14-21	bromodomain containing 4	Homo sapiens	131-135
29931583-9	2019	These results provide a rationale for dual targeting of BRD4 and BCL2 using AZD5153 and AZD4320 as a therapeutic strategy against DHL and DEL.	Cysteamine	130-133	bromodomain containing 4	Homo sapiens	56-60
29931583-9	2019	These results provide a rationale for dual targeting of BRD4 and BCL2 using AZD5153 and AZD4320 as a therapeutic strategy against DHL and DEL.	del	138-141	bromodomain containing 4	Homo sapiens	56-60
30554080-0	2019	Design, synthesis and biological evaluation of novel indole derivatives as potential HDAC/BRD4 dual inhibitors and anti-leukemia agents.	indole	53-59	bromodomain containing 4	Homo sapiens	90-94
30554080-3	2019	In this work, a series of indole derivatives that combine the inhibitory activities of BRD4 and HDAC into one molecule were designed and synthesized through the structure-based design method.	indole	26-32	bromodomain containing 4	Homo sapiens	87-91
30369550-8	2019	SNIPER(BRD)-3 contained an N-methylated LCL-161 derivative as the IAP ligand, which prevented it from binding IAPs, and resulted in the abrogated degradation of cIAP1, XIAP, and BRD4.	Nitrogen	1-2	bromodomain containing 4	Homo sapiens	178-182
31059052-0	2019	miR-125b-mediated regulation of cell proliferation through the Jagged-1/Notch signaling pathway by inhibiting BRD4 expression in psoriasis.	mir-125b	0-8	bromodomain containing 4	Homo sapiens	110-114
31059052-2	2019	The aim of the present study was to investigate the mechanism by which microRNA-125b (miR-125b) inhibits the activation of the bromodomain-containing protein 4 (BRD4)/Notch signaling pathway in psoriasis.	mir-125b	86-94	bromodomain containing 4	Homo sapiens	127-159
31059052-2	2019	The aim of the present study was to investigate the mechanism by which microRNA-125b (miR-125b) inhibits the activation of the bromodomain-containing protein 4 (BRD4)/Notch signaling pathway in psoriasis.	mir-125b	86-94	bromodomain containing 4	Homo sapiens	161-165
30652495-12	2019	The antioxidant N-acetylcysteine prevents CSE-induced miR-29b downregulation and BRD4 and IL-8 upregulation.	Acetylcysteine	16-32	bromodomain containing 4	Homo sapiens	81-85
30539410-11	2019	We also found that, by displacing BRD4 from chromatin using the BET inhibitor iBET762, MEC cells lose their colony forming capacities and undergo G1 cell cycle arrest and senescence.	molibresib	78-85	bromodomain containing 4	Homo sapiens	34-38
30321559-13	2019	A novel small-molecule BRD4 inhibitor (ZL0454) disrupts BRD4 binding to the NF-kappaB-RNA polymerase II complex and inhibits its histone acetyltransferase activity.	CHEMBL4159382	39-45	bromodomain containing 4	Homo sapiens	23-27
30321559-13	2019	A novel small-molecule BRD4 inhibitor (ZL0454) disrupts BRD4 binding to the NF-kappaB-RNA polymerase II complex and inhibits its histone acetyltransferase activity.	CHEMBL4159382	39-45	bromodomain containing 4	Homo sapiens	56-60
30611741-5	2019	We here assessed the therapeutic efficacy of the orally bioavailable BRD4 inhibitor, MK-8628, in preclinical models of medulloblastoma.	OTX015	85-92	bromodomain containing 4	Homo sapiens	69-73
31037138-6	2019	Therapeutic efficiency of BRD4 targeting by JQ1 was assessed in three preclinical models including xenograft model, 4NQO-induced model and patients-derived xenograft model.	4-Nitroquinoline-1-oxide	116-120	bromodomain containing 4	Homo sapiens	26-30
31037138-8	2019	Results: Significant upregulation of BRD4 was found in primary HNSCC samples and 4NQO-induced HNSCC model.	4-Nitroquinoline-1-oxide	81-85	bromodomain containing 4	Homo sapiens	37-41
30829648-1	2019	Anti-leukemic effect of BET/BRD4 (BETP) protein inhibition has been largely attributed to transcriptional downregulation of cellular anabolic/anti-apoptotic processes but its effect on bone marrow microenvironment, a sanctuary favoring persistence of leukemia stem/progenitor cells, is unexplored.	4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine	34-38	bromodomain containing 4	Homo sapiens	28-32
30606676-3	2019	The optimized dimethylisoxazole aryl-benzimidazole inhibitor exhibited high potency towards BRD4 and related BET proteins in biochemical and cell-based assays and inhibited tumor growth in two proof-of-concept preclinical animal models.	dimethylisoxazole aryl-benzimidazole	14-50	bromodomain containing 4	Homo sapiens	92-96
30529546-0	2019	Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.	5-((1h-imidazol-1-yl)methyl)quinolin-8-ol	19-60	bromodomain containing 4	Homo sapiens	82-114
30529546-1	2019	Bromodomain-containing protein 4 (BRD4), an epigenetic reader of acetyl lysine, has emerged as a promising therapeutic target for many diseases including cancer, inflammation and heart failure.	acetyl lysine	65-78	bromodomain containing 4	Homo sapiens	0-32
30529546-1	2019	Bromodomain-containing protein 4 (BRD4), an epigenetic reader of acetyl lysine, has emerged as a promising therapeutic target for many diseases including cancer, inflammation and heart failure.	acetyl lysine	65-78	bromodomain containing 4	Homo sapiens	34-38
30529546-2	2019	Our previous study reported that nitroxoline, an FDA approved antibiotic, showed potential BRD4 inhibitory activity and antiproliferation activity against leukemia cell lines.	nitroxoline	33-44	bromodomain containing 4	Homo sapiens	91-95
30761268-0	2019	BRD4 Inhibition Enhances Azacitidine Efficacy in Acute Myeloid Leukemia and Myelodysplastic Syndromes.	Azacitidine	25-36	bromodomain containing 4	Homo sapiens	0-4
30761268-6	2019	Furthermore, the inhibition of BRD4 in vitro with JQ1 or shRNA induced leukemia cell apoptosis, especially when combined to azacitidine, and triggered the activation of the DNA damage response pathway.	Azacitidine	124-135	bromodomain containing 4	Homo sapiens	31-35
30761268-8	2019	Our results indicate that the BRD4-dependent transcriptional program is a defective pathway in MDS and AML pathogenesis and its inhibition induces apoptosis of leukemia cells, which is enhanced in combination with HMA or an ATR inhibitor.	5-(N,N-hexamethylene)amiloride	214-217	bromodomain containing 4	Homo sapiens	30-34
30153047-4	2019	We therefore tested two novel highly selective BRD4 inhibitors, ZL0420 and ZL0454, for their effects on chronic airway remodeling produced by repetitive TLR3 agonist challenges, and compared their efficacy with that of two nonselective bromodomain and extraterminal (BET) protein inhibitors, JQ1 and RVX208.	ZL0420	64-70	bromodomain containing 4	Homo sapiens	47-51
30647404-1	2019	First-generation bromodomain extra-terminal protein (BETP) inhibitors (BETi) (e.g., OTX015) that disrupt binding of BETP BRD4 to chromatin transcriptionally attenuate AML-relevant progrowth and prosurvival oncoproteins.	4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine	53-57	bromodomain containing 4	Homo sapiens	121-125
30153047-4	2019	We therefore tested two novel highly selective BRD4 inhibitors, ZL0420 and ZL0454, for their effects on chronic airway remodeling produced by repetitive TLR3 agonist challenges, and compared their efficacy with that of two nonselective bromodomain and extraterminal (BET) protein inhibitors, JQ1 and RVX208.	CHEMBL4159382	75-81	bromodomain containing 4	Homo sapiens	47-51
30272279-3	2018	Bromodomain-containing protein 4 (BRD4) is an epigenetic reader protein that binds to acetylated lysine on histones and has been reported to serve critical roles in numerous types of cancers.	Lysine	97-103	bromodomain containing 4	Homo sapiens	0-32
30476723-9	2019	Apabetalone reduced the size of BRD4-rich enhancers, consistent with disrupting BRD4 association with chromatin.	apabetalone	0-11	bromodomain containing 4	Homo sapiens	32-36
30476723-9	2019	Apabetalone reduced the size of BRD4-rich enhancers, consistent with disrupting BRD4 association with chromatin.	apabetalone	0-11	bromodomain containing 4	Homo sapiens	80-84
30476723-11	2019	Apabetalone reduced levels of BRD4 on many of these enhancers, which correlated with decreased expression of the associated gene.	apabetalone	0-11	bromodomain containing 4	Homo sapiens	30-34
30260047-0	2019	Computational study on the selective inhibition mechanism of MS402 to the first and second bromodomains of BRD4.	MS402	61-66	bromodomain containing 4	Homo sapiens	107-111
30260047-3	2019	MS402 is a domain-selective inhibitor of BRD4-BD1 over BRD4-BD2 reported recently.	MS402	0-5	bromodomain containing 4	Homo sapiens	41-45
30260047-3	2019	MS402 is a domain-selective inhibitor of BRD4-BD1 over BRD4-BD2 reported recently.	MS402	0-5	bromodomain containing 4	Homo sapiens	55-59
30260047-6	2019	Results demonstrate BRD4-BD1 binds to MS402 with lower binding free energy than BRD4-BD2.	MS402	38-43	bromodomain containing 4	Homo sapiens	20-24
30260047-7	2019	Residues Gln85, Pro86, Asn140, and Ile146 are crucial for MS402"s selectively binding to BRD4-BD1.	MS402	58-63	bromodomain containing 4	Homo sapiens	89-93
30272279-3	2018	Bromodomain-containing protein 4 (BRD4) is an epigenetic reader protein that binds to acetylated lysine on histones and has been reported to serve critical roles in numerous types of cancers.	Lysine	97-103	bromodomain containing 4	Homo sapiens	34-38
30242092-9	2018	Combined, our study demonstrates that BRD4-HOXB13-HOTBIN10 regulatory circuit maintains the malignant state of CRPCs and identifies a core proproliferative network driving ADT resistance that is targetable with potent dual-activity bromodomain-kinase inhibitors.	adt	172-175	bromodomain containing 4	Homo sapiens	38-42
30411639-3	2018	In the current study, we performed an in silico screening of a small-molecule chemical library against the acetyl-lysine binding site of the first bromodomain (BD1) in BRD4 protein.	N(alpha)-acetyllysine	107-120	bromodomain containing 4	Homo sapiens	168-172
30411639-6	2018	Molecular dynamics simulation studies show that in free-form BRD4 the reported conserved water molecules are not retained at their specific positoins due to flexibiliy in the ZA-loop.	Water	89-94	bromodomain containing 4	Homo sapiens	61-65
30411639-7	2018	In BRD4-ligand complexes the number and positions of conserved water molecules depends on the bound ligand.	Water	63-68	bromodomain containing 4	Homo sapiens	3-7
30411639-8	2018	Identified potential inhibitors bind stably at the acetyl-lysine binding pocket of BRD4 and form direct and water-mediated hydrogen bonds with higher occupancy which may contribute to ligand specificity towards BRD4-BD1.	N(alpha)-acetyllysine	51-64	bromodomain containing 4	Homo sapiens	83-87
30411639-8	2018	Identified potential inhibitors bind stably at the acetyl-lysine binding pocket of BRD4 and form direct and water-mediated hydrogen bonds with higher occupancy which may contribute to ligand specificity towards BRD4-BD1.	N(alpha)-acetyllysine	51-64	bromodomain containing 4	Homo sapiens	211-215
30411639-8	2018	Identified potential inhibitors bind stably at the acetyl-lysine binding pocket of BRD4 and form direct and water-mediated hydrogen bonds with higher occupancy which may contribute to ligand specificity towards BRD4-BD1.	Water	108-113	bromodomain containing 4	Homo sapiens	83-87
30411639-8	2018	Identified potential inhibitors bind stably at the acetyl-lysine binding pocket of BRD4 and form direct and water-mediated hydrogen bonds with higher occupancy which may contribute to ligand specificity towards BRD4-BD1.	Water	108-113	bromodomain containing 4	Homo sapiens	211-215
30411639-8	2018	Identified potential inhibitors bind stably at the acetyl-lysine binding pocket of BRD4 and form direct and water-mediated hydrogen bonds with higher occupancy which may contribute to ligand specificity towards BRD4-BD1.	Hydrogen	123-131	bromodomain containing 4	Homo sapiens	83-87
30411639-8	2018	Identified potential inhibitors bind stably at the acetyl-lysine binding pocket of BRD4 and form direct and water-mediated hydrogen bonds with higher occupancy which may contribute to ligand specificity towards BRD4-BD1.	Hydrogen	123-131	bromodomain containing 4	Homo sapiens	211-215
30466442-2	2018	Inhibition of BRD4 shortcuts the communication between SEs and target promoters with a subsequent cell-specific repression of oncogenes to which cancer cells are addicted and cell death.	ses	55-58	bromodomain containing 4	Homo sapiens	14-18
30466442-3	2018	To date, this is the most credited mechanism of action of BET inhibitors, a class of small molecules targeting BET proteins which are currently in clinical trials in several cancer settings.However, recent evidence indicates that BRD4 relevance in cancer goes beyond its role in transcription regulation and identifies this protein as a keeper of genome stability.Indeed, a non-transcriptional role of BRD4 in controlling DNA damage checkpoint activation and repair as well as telomere maintenance has been proposed, throwing new lights into the multiple functions of this protein and opening new perspectives on the use of BETi in cancer.	beti	624-628	bromodomain containing 4	Homo sapiens	230-234
30466442-6	2018	Furthermore, in light of the transversal function of BRD4, we provide new interpretation for the cytotoxic activity of BETi and we discuss new possibilities for a wide and focused employment of these drugs in clinical settings.	beti	119-123	bromodomain containing 4	Homo sapiens	53-57
30385738-6	2018	Among them, compound BDF-1253 showed an approximately four-fold improvement in BRD4 inhibition compared with the prototype Nitroxoline and had good selectivity for BET proteins against other bromodomain proteins or epi-enzymes in biochemical assays.	bdf-1253	21-29	bromodomain containing 4	Homo sapiens	79-83
30268702-0	2018	Discovery and lead identification of quinazoline-based BRD4 inhibitors.	Quinazolines	37-48	bromodomain containing 4	Homo sapiens	55-59
30268702-1	2018	A new series of quinazoline-based analogs as potent bromodomain-containing protein 4 (BRD4) inhibitors is described.	Quinazolines	16-27	bromodomain containing 4	Homo sapiens	52-84
30268702-1	2018	A new series of quinazoline-based analogs as potent bromodomain-containing protein 4 (BRD4) inhibitors is described.	Quinazolines	16-27	bromodomain containing 4	Homo sapiens	86-90
30037819-6	2018	Moreover, inhibition of c-myc by BRD4 antagonists sensitizes for imipridone-induced apoptosis in stem-like GBM cells in vitro and in vivo Imipridones affect energy metabolism by suppressing both glycolysis and oxidative phosphorylation, which is accompanied by a compensatory activation of the serine-one carbon-glycine (SOG) pathway, involving the transcription factor ATF4.	imipridone	65-75	bromodomain containing 4	Homo sapiens	33-37
30037819-6	2018	Moreover, inhibition of c-myc by BRD4 antagonists sensitizes for imipridone-induced apoptosis in stem-like GBM cells in vitro and in vivo Imipridones affect energy metabolism by suppressing both glycolysis and oxidative phosphorylation, which is accompanied by a compensatory activation of the serine-one carbon-glycine (SOG) pathway, involving the transcription factor ATF4.	imipridones	138-149	bromodomain containing 4	Homo sapiens	33-37
30037819-6	2018	Moreover, inhibition of c-myc by BRD4 antagonists sensitizes for imipridone-induced apoptosis in stem-like GBM cells in vitro and in vivo Imipridones affect energy metabolism by suppressing both glycolysis and oxidative phosphorylation, which is accompanied by a compensatory activation of the serine-one carbon-glycine (SOG) pathway, involving the transcription factor ATF4.	Serine	294-300	bromodomain containing 4	Homo sapiens	33-37
30037819-6	2018	Moreover, inhibition of c-myc by BRD4 antagonists sensitizes for imipridone-induced apoptosis in stem-like GBM cells in vitro and in vivo Imipridones affect energy metabolism by suppressing both glycolysis and oxidative phosphorylation, which is accompanied by a compensatory activation of the serine-one carbon-glycine (SOG) pathway, involving the transcription factor ATF4.	carbon-glycine	305-319	bromodomain containing 4	Homo sapiens	33-37
30037819-6	2018	Moreover, inhibition of c-myc by BRD4 antagonists sensitizes for imipridone-induced apoptosis in stem-like GBM cells in vitro and in vivo Imipridones affect energy metabolism by suppressing both glycolysis and oxidative phosphorylation, which is accompanied by a compensatory activation of the serine-one carbon-glycine (SOG) pathway, involving the transcription factor ATF4.	Sudan Orange G	321-324	bromodomain containing 4	Homo sapiens	33-37
30300821-0	2018	NF-kappaB signaling activation via increases in BRD2 and BRD4 confers resistance to the bromodomain inhibitor I-BET151 in U937 cells.	GSK1210151A	110-118	bromodomain containing 4	Homo sapiens	57-61
30153557-4	2018	We report our studies on the concomitant use of the BRD4 inhibitor I-BET151 and AURKA inhibitor alisertib.	GSK1210151A	67-75	bromodomain containing 4	Homo sapiens	52-56
30253095-5	2018	Selectivity for the BRD4 N-terminal bromodomain (BRD4(1)) over its second bromodomain (BRD4(2)) arises from the displacement of ordered waters and the conformational flexibility of lysine-141 in BRD4(1).	Lysine	181-187	bromodomain containing 4	Homo sapiens	20-24
30253095-5	2018	Selectivity for the BRD4 N-terminal bromodomain (BRD4(1)) over its second bromodomain (BRD4(2)) arises from the displacement of ordered waters and the conformational flexibility of lysine-141 in BRD4(1).	Lysine	181-187	bromodomain containing 4	Homo sapiens	49-53
30253095-5	2018	Selectivity for the BRD4 N-terminal bromodomain (BRD4(1)) over its second bromodomain (BRD4(2)) arises from the displacement of ordered waters and the conformational flexibility of lysine-141 in BRD4(1).	Lysine	181-187	bromodomain containing 4	Homo sapiens	49-53
30253095-5	2018	Selectivity for the BRD4 N-terminal bromodomain (BRD4(1)) over its second bromodomain (BRD4(2)) arises from the displacement of ordered waters and the conformational flexibility of lysine-141 in BRD4(1).	Lysine	181-187	bromodomain containing 4	Homo sapiens	49-53
30304769-8	2018	Marked cytotoxicity was found following bromodomain-containing protein 4 (BRD4) inhibition with AZD5153, suggesting a strict dependency of this particular subtype of T-ALL on the activity of super-enhancers.	AZD5153	96-103	bromodomain containing 4	Homo sapiens	40-72
30304769-8	2018	Marked cytotoxicity was found following bromodomain-containing protein 4 (BRD4) inhibition with AZD5153, suggesting a strict dependency of this particular subtype of T-ALL on the activity of super-enhancers.	AZD5153	96-103	bromodomain containing 4	Homo sapiens	74-78
30165024-4	2018	Here we describe the design of covalent inhibitors of BRD4(BD1) that target a methionine in the binding pocket by attaching an epoxide warhead to a suitably oriented noncovalent inhibitor.	Methionine	78-88	bromodomain containing 4	Homo sapiens	54-58
30102854-5	2018	Here, we report that benzo[e]pyrimido-[5,4- b]diazepine-6(11H)-ones, versatile ATP-site directed kinase pharmacophores utilized in the development of inhibitors of multiple kinases, including several previously reported kinase chemical probes, are also capable of exhibiting potent BRD4-dependent pharmacology.	benzo(e)pyrimido-(5,4-b)diazepine-6(11H)-one	21-67	bromodomain containing 4	Homo sapiens	282-286
30102854-5	2018	Here, we report that benzo[e]pyrimido-[5,4- b]diazepine-6(11H)-ones, versatile ATP-site directed kinase pharmacophores utilized in the development of inhibitors of multiple kinases, including several previously reported kinase chemical probes, are also capable of exhibiting potent BRD4-dependent pharmacology.	Adenosine Triphosphate	79-82	bromodomain containing 4	Homo sapiens	282-286
30102854-8	2018	Co-crystallography of seven representative inhibitors with the first bromodomain of BRD4 demonstrate that distinct atropisomeric conformers recognize the kinase ATP-site and the BRD4 acetyl lysine binding site, conformational preferences supported by rigid docking studies.	Adenosine Triphosphate	161-164	bromodomain containing 4	Homo sapiens	84-88
30102854-8	2018	Co-crystallography of seven representative inhibitors with the first bromodomain of BRD4 demonstrate that distinct atropisomeric conformers recognize the kinase ATP-site and the BRD4 acetyl lysine binding site, conformational preferences supported by rigid docking studies.	acetyl lysine	183-196	bromodomain containing 4	Homo sapiens	84-88
30102854-8	2018	Co-crystallography of seven representative inhibitors with the first bromodomain of BRD4 demonstrate that distinct atropisomeric conformers recognize the kinase ATP-site and the BRD4 acetyl lysine binding site, conformational preferences supported by rigid docking studies.	acetyl lysine	183-196	bromodomain containing 4	Homo sapiens	178-182
30165024-4	2018	Here we describe the design of covalent inhibitors of BRD4(BD1) that target a methionine in the binding pocket by attaching an epoxide warhead to a suitably oriented noncovalent inhibitor.	Epoxy Compounds	127-134	bromodomain containing 4	Homo sapiens	54-58
30135075-0	2018	Genetic modifiers of the BRD4-NUT dependency of NUT midline carcinoma uncovers a synergism between BETis and CDK4/6is.	betis	99-104	bromodomain containing 4	Homo sapiens	25-29
29930091-2	2018	Here we demonstrate that the SE-enriched transcriptional coactivators BRD4 and MED1 form nuclear puncta at SEs that exhibit properties of liquid-like condensates and are disrupted by chemicals that perturb condensates.	Selenium	29-31	bromodomain containing 4	Homo sapiens	70-74
29930091-2	2018	Here we demonstrate that the SE-enriched transcriptional coactivators BRD4 and MED1 form nuclear puncta at SEs that exhibit properties of liquid-like condensates and are disrupted by chemicals that perturb condensates.	ses	107-110	bromodomain containing 4	Homo sapiens	70-74
30041464-0	2018	Flavonoids as Putative Epi-Modulators: Insight into Their Binding Mode with BRD4 Bromodomains Using Molecular Docking and Dynamics.	Flavonoids	0-10	bromodomain containing 4	Homo sapiens	76-80
30012592-1	2018	The importance of BET protein BRD4 in gene transcription is well recognized through the study of chemical modulation of its characteristic tandem bromodomain (BrD) binding to lysine-acetylated histones and transcription factors.	Lysine	175-181	bromodomain containing 4	Homo sapiens	30-34
30012592-3	2018	Here, we report a thienodiazepine-based bivalent BrD inhibitor, MS645, that affords spatially constrained tandem BrD inhibition and consequently sustained repression of BRD4 transcriptional activity in blocking proliferation of solid-tumor cells including a panel of triple-negative breast cancer (TNBC) cells.	thienodiazepine	18-33	bromodomain containing 4	Homo sapiens	169-173
30012592-3	2018	Here, we report a thienodiazepine-based bivalent BrD inhibitor, MS645, that affords spatially constrained tandem BrD inhibition and consequently sustained repression of BRD4 transcriptional activity in blocking proliferation of solid-tumor cells including a panel of triple-negative breast cancer (TNBC) cells.	N,N'-(decane-1,10-diyl)bis{2-[(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetamide}	64-69	bromodomain containing 4	Homo sapiens	169-173
30041464-11	2018	Based on these results, amentoflavone was experimentally tested for BRD4 inhibition, showing activity in the micromolar range.	amentoflavone	24-37	bromodomain containing 4	Homo sapiens	68-72
29996811-2	2018	A new small molecular inhibitor, JQ1, targeting BRD4, which recognizes the acetylated lysine residues, has been shown to induce cell cycle arrest in different cancers by inhibiting MYC oncogene.	Lysine	86-92	bromodomain containing 4	Homo sapiens	48-52
30036377-6	2018	Furthermore, we demonstrate that a novel BET inhibitor, AZD5153, is highly active in BRD4-amplified patient derived xenografts and uncover Neuregulin-1 as a novel BRD4 effector.	AZD5153	56-63	bromodomain containing 4	Homo sapiens	85-89
30036377-6	2018	Furthermore, we demonstrate that a novel BET inhibitor, AZD5153, is highly active in BRD4-amplified patient derived xenografts and uncover Neuregulin-1 as a novel BRD4 effector.	AZD5153	56-63	bromodomain containing 4	Homo sapiens	163-167
29776834-2	2018	Here we report that our previously developed 3,5-dimethylisoxazole-based BET bromodomain ligand (OXFBD02) inhibits interactions of BRD4(1) with the RelA subunit of NF-kappaB, in addition to histone H4.	3,5-Dimethylisoxazole	45-66	bromodomain containing 4	Homo sapiens	131-135
29776834-5	2018	Molecular dynamics simulations assisted our understanding of the role played by an internal hydrogen bond in altering the affinity of this series of molecules for BRD4(1).	Hydrogen	92-100	bromodomain containing 4	Homo sapiens	163-167
29776834-6	2018	OXFBD04 shows improved BRD4(1) affinity (IC50 = 166 nM), optimised physicochemical properties (LE = 0.43; LLE = 5.74; SFI = 5.96), and greater metabolic stability (t1/2 = 388 min).	OXFBD04	0-7	bromodomain containing 4	Homo sapiens	23-27
29808961-0	2018	Design, Synthesis, and in vitro Biological Evaluation of 3,5-Dimethylisoxazole Derivatives as BRD4 Inhibitors.	3,5-Dimethylisoxazole	57-78	bromodomain containing 4	Homo sapiens	94-98
29808961-2	2018	In this study, 3,5-dimethylisoxazole derivatives were designed and synthesized with excellent stability in liver microsomes as potent BRD4 inhibitors, and were evaluated for their BRD4 inhibitory activities in vitro.	3,5-Dimethylisoxazole	15-36	bromodomain containing 4	Homo sapiens	134-138
29808961-2	2018	In this study, 3,5-dimethylisoxazole derivatives were designed and synthesized with excellent stability in liver microsomes as potent BRD4 inhibitors, and were evaluated for their BRD4 inhibitory activities in vitro.	3,5-Dimethylisoxazole	15-36	bromodomain containing 4	Homo sapiens	180-184
29717765-0	2018	Bromodomain-containing protein 4 is critical for the antiproliferative and pro-apoptotic effects of gambogic acid in anaplastic thyroid cancer.	gambogic acid	100-113	bromodomain containing 4	Homo sapiens	0-32
29717765-5	2018	Next, it was demonstrated that GA decreased the expression of bromodomain-containing protein 4 (BRD4), which has been reported to function as an oncogene in various types of cancer.	gambogic acid	31-33	bromodomain containing 4	Homo sapiens	62-94
29717765-5	2018	Next, it was demonstrated that GA decreased the expression of bromodomain-containing protein 4 (BRD4), which has been reported to function as an oncogene in various types of cancer.	gambogic acid	31-33	bromodomain containing 4	Homo sapiens	96-100
29717765-8	2018	Notably, ectopic BRD4 expression significantly weakened the biological effects of GA on ATC cells in vitro and in vivo, which suggested that GA served its anticancer functions partially via downregulating BRD4.	gambogic acid	82-84	bromodomain containing 4	Homo sapiens	17-21
29636547-4	2018	Inhibition of BRD4 by JQ1 or AZD5153 resulted in a rapid, time-dependent reduction in CHK1 phosphorylation and aberrant DNA replication re-initiation.	AZD5153	29-36	bromodomain containing 4	Homo sapiens	14-18
29636547-5	2018	Furthermore, BRD4 inhibition sensitized cancer cells to various replication stress-inducing agents, and synergized with ATR inhibitor AZD6738 to induce cell killing across a number of cancer cell lines.	ceralasertib	134-141	bromodomain containing 4	Homo sapiens	13-17
29743242-3	2018	Phosphorylation of a second highly conserved T-loop site, Ser-175, alters the competitive binding of Tat and the host recruitment factor bromodomain containing 4 (BRD4) to P-TEFb.	Serine	58-61	bromodomain containing 4	Homo sapiens	137-161
29743242-3	2018	Phosphorylation of a second highly conserved T-loop site, Ser-175, alters the competitive binding of Tat and the host recruitment factor bromodomain containing 4 (BRD4) to P-TEFb.	Serine	58-61	bromodomain containing 4	Homo sapiens	163-167
29941841-8	2018	We believe that predicted models will help us to understand the structural requirements of BRD4 protein inhibitors that belong to quinolinone and quinazolinone classes for the designing of better active compounds.	Quinolones	130-141	bromodomain containing 4	Homo sapiens	91-95
29941841-8	2018	We believe that predicted models will help us to understand the structural requirements of BRD4 protein inhibitors that belong to quinolinone and quinazolinone classes for the designing of better active compounds.	Quinazolinones	146-159	bromodomain containing 4	Homo sapiens	91-95
29730189-0	2018	Design, synthesis and biological evaluation of benzo[cd]indol-2(1H)-ones derivatives as BRD4 inhibitors.	benzo[cd]indol-2(1h)-ones	47-72	bromodomain containing 4	Homo sapiens	88-92
29567272-7	2018	RESULTS: In cultured cells, inhibition of BRD4 by siRNA or INCB054329 reduced expression and function of BRCA1 and RAD51, reduced HR reporter activity, and sensitized the cells to olaparib-induced growth inhibition, DNA damage induction and apoptosis.	olaparib	180-188	bromodomain containing 4	Homo sapiens	42-46
29684085-2	2018	Brd4 is recruited to the HIV LTR by interactions with acetyl-histones3 (AcH3) and AcH4.	acetyl-histones3	54-70	bromodomain containing 4	Homo sapiens	0-4
29596834-0	2018	AZD5153, a novel BRD4 inhibitor, suppresses human thyroid carcinoma cell growth in vitro and in vivo.	AZD5153	0-7	bromodomain containing 4	Homo sapiens	17-21
29596834-2	2018	AZD5153 is a novel and specific Bromodomain-containing protein 4 (BRD4) inhibitor.	AZD5153	0-7	bromodomain containing 4	Homo sapiens	32-64
29596834-2	2018	AZD5153 is a novel and specific Bromodomain-containing protein 4 (BRD4) inhibitor.	AZD5153	0-7	bromodomain containing 4	Homo sapiens	66-70
29622725-3	2018	We found that BRD4 acts as general coactivator of RNA polymerase II-dependent transcription, which is broadly repressed upon high-dose BETi treatment.	beti	135-139	bromodomain containing 4	Homo sapiens	14-18
29596834-8	2018	BRD4-regulated proteins, including c-Myc, Bcl-2 and cyclin D1, were significantly downregulated following AZD5153 treatment in TPC-1 and primary cancer cells.	AZD5153	106-113	bromodomain containing 4	Homo sapiens	0-4
29596834-10	2018	BRD4-dependent proteins, Myc, Bcl-2 and cyclin D1, were also downregulated in AZD5153-treated tumor tissues.	AZD5153	78-85	bromodomain containing 4	Homo sapiens	0-4
29596834-11	2018	Collectively, the results suggest that targeting BRD4 by AZD5153 inhibits human thyroid carcinoma cell growth in vitro and in vivo.	AZD5153	57-64	bromodomain containing 4	Homo sapiens	49-53
29649741-2	2018	Compounds ZL0420 (28) and ZL0454 (35) were identified as potent and selective BRD4 inhibitors with nanomolar binding affinities to bromodomains (BDs) of BRD4.	ZL0420	10-16	bromodomain containing 4	Homo sapiens	78-82
29649741-2	2018	Compounds ZL0420 (28) and ZL0454 (35) were identified as potent and selective BRD4 inhibitors with nanomolar binding affinities to bromodomains (BDs) of BRD4.	ZL0420	10-16	bromodomain containing 4	Homo sapiens	153-157
29649741-2	2018	Compounds ZL0420 (28) and ZL0454 (35) were identified as potent and selective BRD4 inhibitors with nanomolar binding affinities to bromodomains (BDs) of BRD4.	CHEMBL4159382	26-32	bromodomain containing 4	Homo sapiens	78-82
29649741-2	2018	Compounds ZL0420 (28) and ZL0454 (35) were identified as potent and selective BRD4 inhibitors with nanomolar binding affinities to bromodomains (BDs) of BRD4.	CHEMBL4159382	26-32	bromodomain containing 4	Homo sapiens	153-157
29649741-3	2018	Both of them can be well docked into the acetyl-lysine (KAc) binding pocket of BRD4, forming key interactions including the critical hydrogen bonds with Asn140 directly and Tyr97 indirectly via a H2O molecule.	N(alpha)-acetyllysine	41-54	bromodomain containing 4	Homo sapiens	79-83
29649741-3	2018	Both of them can be well docked into the acetyl-lysine (KAc) binding pocket of BRD4, forming key interactions including the critical hydrogen bonds with Asn140 directly and Tyr97 indirectly via a H2O molecule.	4-Quinolinecarbamic acid, 2-butoxy-, 2-(diethylamino)ethyl ester	56-59	bromodomain containing 4	Homo sapiens	79-83
29649741-3	2018	Both of them can be well docked into the acetyl-lysine (KAc) binding pocket of BRD4, forming key interactions including the critical hydrogen bonds with Asn140 directly and Tyr97 indirectly via a H2O molecule.	Hydrogen	133-141	bromodomain containing 4	Homo sapiens	79-83
29649741-3	2018	Both of them can be well docked into the acetyl-lysine (KAc) binding pocket of BRD4, forming key interactions including the critical hydrogen bonds with Asn140 directly and Tyr97 indirectly via a H2O molecule.	Water	196-199	bromodomain containing 4	Homo sapiens	79-83
29796168-4	2018	Here, we aimed to elucidate the anti-cancer effects of JQ1 and the mechanisms underlying BRD4 inhibition in sunitinib-sensitive and -resistant ccRCCs.	Sunitinib	108-117	bromodomain containing 4	Homo sapiens	89-93
29796168-8	2018	Chromatin immunoprecipitation assays revealed that these oncogenes may be promising BRD4 targets, particularly in sunitinib-resistant ccRCC cells.	Sunitinib	114-123	bromodomain containing 4	Homo sapiens	84-88
29796168-9	2018	These results identified SCG5, SPOCD1, RGS19, and ARHGAP22 as potential prognostic markers and showed that BRD4 inhibition may have applications as a potential therapeutic approach in sunitinib-sensitive and -resistant ccRCC.	Sunitinib	184-193	bromodomain containing 4	Homo sapiens	107-111
29343578-0	2018	A New Quinoline BRD4 Inhibitor Targets a Distinct Latent HIV-1 Reservoir for Reactivation from Other "Shock" Drugs.	quinoline	6-15	bromodomain containing 4	Homo sapiens	16-20
29525435-2	2018	Along this line, starting from PLK1-BRD4 dual inhibitor BI-2536, we discovered a new series of dihydroquinoxalin-2(1H)-one with aniline and indoline WPF binders as selective BRD4 inhibitors.	BI 2536	56-63	bromodomain containing 4	Homo sapiens	36-40
29525435-2	2018	Along this line, starting from PLK1-BRD4 dual inhibitor BI-2536, we discovered a new series of dihydroquinoxalin-2(1H)-one with aniline and indoline WPF binders as selective BRD4 inhibitors.	BI 2536	56-63	bromodomain containing 4	Homo sapiens	174-178
29525435-2	2018	Along this line, starting from PLK1-BRD4 dual inhibitor BI-2536, we discovered a new series of dihydroquinoxalin-2(1H)-one with aniline and indoline WPF binders as selective BRD4 inhibitors.	dihydroquinoxalin-2(1h)-one	95-122	bromodomain containing 4	Homo sapiens	36-40
29525435-2	2018	Along this line, starting from PLK1-BRD4 dual inhibitor BI-2536, we discovered a new series of dihydroquinoxalin-2(1H)-one with aniline and indoline WPF binders as selective BRD4 inhibitors.	dihydroquinoxalin-2(1h)-one	95-122	bromodomain containing 4	Homo sapiens	174-178
29525435-2	2018	Along this line, starting from PLK1-BRD4 dual inhibitor BI-2536, we discovered a new series of dihydroquinoxalin-2(1H)-one with aniline and indoline WPF binders as selective BRD4 inhibitors.	aniline	128-135	bromodomain containing 4	Homo sapiens	36-40
29525435-2	2018	Along this line, starting from PLK1-BRD4 dual inhibitor BI-2536, we discovered a new series of dihydroquinoxalin-2(1H)-one with aniline and indoline WPF binders as selective BRD4 inhibitors.	aniline	128-135	bromodomain containing 4	Homo sapiens	174-178
29525435-2	2018	Along this line, starting from PLK1-BRD4 dual inhibitor BI-2536, we discovered a new series of dihydroquinoxalin-2(1H)-one with aniline and indoline WPF binders as selective BRD4 inhibitors.	indoline	140-148	bromodomain containing 4	Homo sapiens	36-40
29525435-2	2018	Along this line, starting from PLK1-BRD4 dual inhibitor BI-2536, we discovered a new series of dihydroquinoxalin-2(1H)-one with aniline and indoline WPF binders as selective BRD4 inhibitors.	indoline	140-148	bromodomain containing 4	Homo sapiens	174-178
29684085-2	2018	Brd4 is recruited to the HIV LTR by interactions with acetyl-histones3 (AcH3) and AcH4.	ach3	72-76	bromodomain containing 4	Homo sapiens	0-4
29684085-2	2018	Brd4 is recruited to the HIV LTR by interactions with acetyl-histones3 (AcH3) and AcH4.	ach4	82-86	bromodomain containing 4	Homo sapiens	0-4
29346775-2	2018	Pharmacological inhibition of BRD4 by BET inhibitors (BETi) has indicated antitumor activity against multiple cancer types.	beti	54-58	bromodomain containing 4	Homo sapiens	30-34
29440272-5	2018	Demonstrating now that iNOS expression in photostressed U87 cells is mediated by NF-kappaB, we hypothesized that (i) recognition of acetylated lysine (acK) on NF-kappaB p65/RelA by bromodomain and extra-terminal (BET) protein Brd4 is crucial; and (ii) by suppressing iNOS expression, a BET inhibitor (JQ1) would attenuate the negative effects of photostress.	Lysine	143-149	bromodomain containing 4	Homo sapiens	226-230
29541371-3	2018	A series of 2,2-dimethyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives were designed and synthesized as selective bromodomain containing protein 4 (BRD4) inhibitors.	2,2-DIMETHYL-2H-BENZO[B][1,4]OXAZIN-3(4H)-ONE	12-57	bromodomain containing 4	Homo sapiens	113-145
29541371-3	2018	A series of 2,2-dimethyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives were designed and synthesized as selective bromodomain containing protein 4 (BRD4) inhibitors.	2,2-DIMETHYL-2H-BENZO[B][1,4]OXAZIN-3(4H)-ONE	12-57	bromodomain containing 4	Homo sapiens	147-151
29483155-4	2018	Here, we report that TICRR physically interacts with the acetyl-histone binding bromodomain (BRD) and extraterminal (BET) proteins BRD2 and BRD4.	acetyl-histone	57-71	bromodomain containing 4	Homo sapiens	140-144
28983974-5	2018	Structural analysis revealed that peptide N-terminus and hydrogen bonds play important roles in the peptide interaction stability and specificity with Brd2 and Brd4.	Hydrogen	57-65	bromodomain containing 4	Homo sapiens	160-164
29180474-7	2018	Loss of H4ac, especially H4K5ac and H4K12ac, disrupted the interaction between BRD4 and H4 by which ascorbate and BETi blocked the binding of BRD4 to acetylated histones.	h4ac	8-12	bromodomain containing 4	Homo sapiens	79-83
29180474-7	2018	Loss of H4ac, especially H4K5ac and H4K12ac, disrupted the interaction between BRD4 and H4 by which ascorbate and BETi blocked the binding of BRD4 to acetylated histones.	h4ac	8-12	bromodomain containing 4	Homo sapiens	142-146
29180474-7	2018	Loss of H4ac, especially H4K5ac and H4K12ac, disrupted the interaction between BRD4 and H4 by which ascorbate and BETi blocked the binding of BRD4 to acetylated histones.	Ascorbic Acid	100-109	bromodomain containing 4	Homo sapiens	79-83
29180474-7	2018	Loss of H4ac, especially H4K5ac and H4K12ac, disrupted the interaction between BRD4 and H4 by which ascorbate and BETi blocked the binding of BRD4 to acetylated histones.	Ascorbic Acid	100-109	bromodomain containing 4	Homo sapiens	142-146
29180474-7	2018	Loss of H4ac, especially H4K5ac and H4K12ac, disrupted the interaction between BRD4 and H4 by which ascorbate and BETi blocked the binding of BRD4 to acetylated histones.	beti	114-118	bromodomain containing 4	Homo sapiens	79-83
29180474-7	2018	Loss of H4ac, especially H4K5ac and H4K12ac, disrupted the interaction between BRD4 and H4 by which ascorbate and BETi blocked the binding of BRD4 to acetylated histones.	beti	114-118	bromodomain containing 4	Homo sapiens	142-146
29563491-5	2018	Both 5-AZA-resistant leukaemia cell lines and clinically 5-AZA-resistant myelodysplastic syndrome and acute myeloid leukaemia specimens have a significant increase in RNA:m5C and NSUN1-/BRD4-associated active chromatin.	Azacitidine	5-10	bromodomain containing 4	Homo sapiens	186-190
29563491-5	2018	Both 5-AZA-resistant leukaemia cell lines and clinically 5-AZA-resistant myelodysplastic syndrome and acute myeloid leukaemia specimens have a significant increase in RNA:m5C and NSUN1-/BRD4-associated active chromatin.	Azacitidine	57-62	bromodomain containing 4	Homo sapiens	186-190
29103140-0	2018	Synthesis and biological evaluation of indazole-4,7-dione derivatives as novel BRD4 inhibitors.	indazole-4,7-dione	39-57	bromodomain containing 4	Homo sapiens	79-83
28783236-5	2017	They were subsequently used to create a suite of AfBPs based on GW841819X (a small molecule inhibitor of BRD4).	GW841819X	64-73	bromodomain containing 4	Homo sapiens	105-109
29348827-6	2017	A high-throughput drug screen confirmed that microtubule inhibitors, topoisomerase inhibitors and anthracyclines are highly cytotoxic in the majority of NMC lines, and that cell lines expressing the BRD4-NUTM1 (exon11:exon2) variant are an order of magnitude more responsive to bromodomain inhibitors (iBETs) on average than those with other BRD4-NUTM1 translocation variants.	Anthracyclines	98-112	bromodomain containing 4	Homo sapiens	342-346
28981843-5	2017	We showed that BRD4 controls RUNX2 by binding to the newly identified ENHs and we demonstrated that the anti-proliferative effects of bromodomain inhibitors (BETi) is associated with RUNX2 transcriptional repression.	beti	158-162	bromodomain containing 4	Homo sapiens	15-19
29077030-6	2017	The RSV Kd value accounted to 6.6 microM in case of BRD4(1).	Resveratrol	4-7	bromodomain containing 4	Homo sapiens	52-56
29077030-7	2017	Molecular docking proposed the binding mode of RSV against BRD4(1) mimicking the acetyl-lysine interactions.	Resveratrol	47-50	bromodomain containing 4	Homo sapiens	59-63
29077030-7	2017	Molecular docking proposed the binding mode of RSV against BRD4(1) mimicking the acetyl-lysine interactions.	N(alpha)-acetyllysine	81-94	bromodomain containing 4	Homo sapiens	59-63
29348827-6	2017	A high-throughput drug screen confirmed that microtubule inhibitors, topoisomerase inhibitors and anthracyclines are highly cytotoxic in the majority of NMC lines, and that cell lines expressing the BRD4-NUTM1 (exon11:exon2) variant are an order of magnitude more responsive to bromodomain inhibitors (iBETs) on average than those with other BRD4-NUTM1 translocation variants.	Anthracyclines	98-112	bromodomain containing 4	Homo sapiens	199-203
29087414-5	2017	Nitroxoline, an FDA-approved antibiotic, was identified to effectively disrupt the interaction between the first bromodomain of BRD4 (bromodomain-containing protein 4) and acetylated H4 peptide with IC50 of 0.98 muM.	nitroxoline	0-11	bromodomain containing 4	Homo sapiens	128-132
29087414-5	2017	Nitroxoline, an FDA-approved antibiotic, was identified to effectively disrupt the interaction between the first bromodomain of BRD4 (bromodomain-containing protein 4) and acetylated H4 peptide with IC50 of 0.98 muM.	nitroxoline	0-11	bromodomain containing 4	Homo sapiens	134-166
29083896-0	2017	Filling Blank Spots on the Map: Identification of Ligand Binding Modes and Interacting Water Molecules for Brd4-BD1 by WaterLOGSY Titrations.	Water	87-92	bromodomain containing 4	Homo sapiens	107-111
28945351-11	2017	Serine 1 phosphorylation inhibited binding of the BRD4 N-terminal bromodomain to polyacetylated H4 tails by >5-fold, whereas methylation had no effect.	Serine	0-6	bromodomain containing 4	Homo sapiens	50-54
28945351-12	2017	Furthermore, binding of BRDT and BRD4 N-terminal bromodomains to H4K5acetyl was enhanced 1.4-9.5-fold by any neighboring acylation of lysine 8, indicating a secondary H4K8acyl binding site that is more permissive of non-acetyl acylations than previously appreciated.	lysine 8	134-142	bromodomain containing 4	Homo sapiens	33-37
29228703-7	2017	Remarkably, SF2523 was more efficient than Wortmannin (the PI3K inhibitor) and JQ1 (the BRD4 specific inhibitor) in killing RCC cells.	SF2523	12-18	bromodomain containing 4	Homo sapiens	88-92
28481868-4	2017	PIN1 directly binds to phosphorylated threonine (T) 204 of BRD4 as revealed by peptide binding and crystallographic studies and enhances BRD4"s stability by inhibiting its ubiquitination.	Threonine	38-47	bromodomain containing 4	Homo sapiens	59-63
28586718-0	2017	Discovery of a series of dihydroquinoxalin-2(1H)-ones as selective BET inhibitors from a dual PLK1-BRD4 inhibitor.	dihydroquinoxalin-2(1h)-ones	25-53	bromodomain containing 4	Homo sapiens	99-103
28586718-2	2017	Interestingly, some kinase inhibitors have been demonstrated to be potent bromodomain inhibitors, especially the PLK1 inhibitor BI-2536 and the JAK2 inhibitor TG101209, which can bind to BRD4 with IC50 values of 0.025 muM and 0.13 muM, respectively.	BI 2536	128-135	bromodomain containing 4	Homo sapiens	187-191
28586718-2	2017	Interestingly, some kinase inhibitors have been demonstrated to be potent bromodomain inhibitors, especially the PLK1 inhibitor BI-2536 and the JAK2 inhibitor TG101209, which can bind to BRD4 with IC50 values of 0.025 muM and 0.13 muM, respectively.	TG101209	159-167	bromodomain containing 4	Homo sapiens	187-191
28481868-5	2017	PIN1 also catalyses the isomerization of proline 205 of BRD4 and induces its conformational change, which promotes its interaction with CDK9 and increases BRD4"s transcriptional activity.	Proline	41-48	bromodomain containing 4	Homo sapiens	56-60
27494802-2	2017	The lysine residues of Bromodomain-1 (BD1) of Brd4 undergo epsilon-N-Acetylation posttranslational modifications to control transcription of genes.	Lysine	4-10	bromodomain containing 4	Homo sapiens	46-50
28042144-2	2017	Although the BET-protein inhibitor (BETi) OTX015 caused accumulation of BRD4, treatment with equimolar concentrations of ARV-825 caused sustained and profound depletion (>90%) of BRD4 and induced significantly more apoptosis in cultured and patient-derived (PD) CD34+ post-MPN sAML cells, while relatively sparing the CD34+ normal hematopoietic progenitor cells.	beti	36-40	bromodomain containing 4	Homo sapiens	72-76
28805822-5	2017	Transcriptome and BRD4 cistrome analyses reveal enhanced expression of the GTPase RAC1 and cholesterol-biosynthesis-associated genes together with activation of AKT-mTORC1 signaling as a consequence of BRD4 stabilization.	Cholesterol	91-102	bromodomain containing 4	Homo sapiens	18-22
28805822-5	2017	Transcriptome and BRD4 cistrome analyses reveal enhanced expression of the GTPase RAC1 and cholesterol-biosynthesis-associated genes together with activation of AKT-mTORC1 signaling as a consequence of BRD4 stabilization.	Cholesterol	91-102	bromodomain containing 4	Homo sapiens	202-206
27494802-4	2017	In this study, an attempt has been made to screen compounds from flavonoids and extended flavonoids libraries targeting acetylated lysine (KAc) binding site of BD1 of Brd4 using docking and molecular dynamics simulations.	Flavonoids	65-75	bromodomain containing 4	Homo sapiens	167-171
27494802-4	2017	In this study, an attempt has been made to screen compounds from flavonoids and extended flavonoids libraries targeting acetylated lysine (KAc) binding site of BD1 of Brd4 using docking and molecular dynamics simulations.	Flavonoids	89-99	bromodomain containing 4	Homo sapiens	167-171
27494802-4	2017	In this study, an attempt has been made to screen compounds from flavonoids and extended flavonoids libraries targeting acetylated lysine (KAc) binding site of BD1 of Brd4 using docking and molecular dynamics simulations.	Lysine	131-137	bromodomain containing 4	Homo sapiens	167-171
27494802-8	2017	We have identified a flavonoid which shows docking and Glide e-model score comparatively much higher than those of already reported known inhibitors against Brd4.	Flavonoids	21-30	bromodomain containing 4	Homo sapiens	157-161
27494802-9	2017	The protein-ligand complex with top-ranked flavonoid was used for dynamics simulation study for 50 ns in order to validate its stability inside the active site of Brd4 receptor.	Flavonoids	43-52	bromodomain containing 4	Homo sapiens	163-167
28484091-0	2017	Ubenimex enhances Brd4 inhibition by suppressing HEXIM1 autophagic degradation and suppressing the Akt pathway in glioma cells.	ubenimex	0-8	bromodomain containing 4	Homo sapiens	18-22
28549889-2	2017	We have previously developed inhibitors of BRD4, which recognizes acetylated lysine residue on histones and recruits transcription elongation factor to the transcription start site, while inhibitors of histone deacetylase (HDAC), which catalyzes the removal of acetyl groups on histones, are already in clinical use for cancer treatment.	Lysine	77-83	bromodomain containing 4	Homo sapiens	43-47
28549889-4	2017	Here, we describe the design and synthesis of N6-[2-(7-hydroxyamino-7-oxoheptyloxy)benzoyl]adenine (5d) as a BRD4/HDAC dual inhibitor.	n6-[2-(7-hydroxyamino-7-oxoheptyloxy)benzoyl]adenine	46-98	bromodomain containing 4	Homo sapiens	109-113
28369619-8	2017	BRD4, a well-characterized acetyllysine reader, has been shown to play a major role in regulating transcription of selected subsets of genes.	N-epsilon-Acetyl-L-lysine	27-39	bromodomain containing 4	Homo sapiens	0-4
28955774-3	2017	Here we report urea-induced equilibrium unfolding experiments monitored by circular dichroism (CD) and fluorescence on two structurally similar BRDs: BRD2(2) and BRD4(1), showing that BRD4(1) is more stable than BRD2(2).	Urea	15-19	bromodomain containing 4	Homo sapiens	162-166
28955774-3	2017	Here we report urea-induced equilibrium unfolding experiments monitored by circular dichroism (CD) and fluorescence on two structurally similar BRDs: BRD2(2) and BRD4(1), showing that BRD4(1) is more stable than BRD2(2).	Urea	15-19	bromodomain containing 4	Homo sapiens	184-188
28032455-0	2017	In silico design and bioevaluation of selective benzotriazepine BRD4 inhibitors with potent antiosteoclastogenic activity.	benzotriazepine	48-63	bromodomain containing 4	Homo sapiens	64-68
28626565-5	2017	Using bromodomain-containing protein 4 (BRD4) as a paradigm, we engineer an "aromatic cage" of the bromodomain to introduce 4-azido-l-phenylalanine (pAzF) without compromising its ability to recognize acetylated lysine residues in histone proteins.	4-azidophenylalanine	124-147	bromodomain containing 4	Homo sapiens	6-38
28535045-6	2017	An additional series of dihydropyridopyrimidines was synthesized to exploit the proximity of a channel near the ZA loop of Brd4, leading to compounds with submicromolar affinity and cellular target engagement.	dihydropyridopyrimidines	24-48	bromodomain containing 4	Homo sapiens	123-127
28195723-2	2017	Disrupting the protein-protein interactions between BRD4 and acetyl-lysine has been shown to effectively block cell proliferation in cancer, cytokine production in acute inflammation, and so forth.	N(alpha)-acetyllysine	61-74	bromodomain containing 4	Homo sapiens	52-56
28378926-0	2017	Translational Modeling of Drug-Induced Myelosuppression and Effect of Pretreatment Myelosuppression for AZD5153, a Selective BRD4 Inhibitor.	AZD5153	104-111	bromodomain containing 4	Homo sapiens	125-129
28626565-5	2017	Using bromodomain-containing protein 4 (BRD4) as a paradigm, we engineer an "aromatic cage" of the bromodomain to introduce 4-azido-l-phenylalanine (pAzF) without compromising its ability to recognize acetylated lysine residues in histone proteins.	4-azidophenylalanine	124-147	bromodomain containing 4	Homo sapiens	40-44
28378926-1	2017	In this work, we evaluate the potential risk of thrombocytopenia in man for a BRD4 inhibitor, AZD5153, based on the platelet count decreases from a Han Wistar rat study.	AZD5153	94-101	bromodomain containing 4	Homo sapiens	78-82
28626565-5	2017	Using bromodomain-containing protein 4 (BRD4) as a paradigm, we engineer an "aromatic cage" of the bromodomain to introduce 4-azido-l-phenylalanine (pAzF) without compromising its ability to recognize acetylated lysine residues in histone proteins.	pazf	149-153	bromodomain containing 4	Homo sapiens	6-38
28626565-5	2017	Using bromodomain-containing protein 4 (BRD4) as a paradigm, we engineer an "aromatic cage" of the bromodomain to introduce 4-azido-l-phenylalanine (pAzF) without compromising its ability to recognize acetylated lysine residues in histone proteins.	pazf	149-153	bromodomain containing 4	Homo sapiens	40-44
28626565-5	2017	Using bromodomain-containing protein 4 (BRD4) as a paradigm, we engineer an "aromatic cage" of the bromodomain to introduce 4-azido-l-phenylalanine (pAzF) without compromising its ability to recognize acetylated lysine residues in histone proteins.	Lysine	212-218	bromodomain containing 4	Homo sapiens	6-38
28626565-5	2017	Using bromodomain-containing protein 4 (BRD4) as a paradigm, we engineer an "aromatic cage" of the bromodomain to introduce 4-azido-l-phenylalanine (pAzF) without compromising its ability to recognize acetylated lysine residues in histone proteins.	Lysine	212-218	bromodomain containing 4	Homo sapiens	40-44
28626565-7	2017	Applying IBPP, we uncovered novel acetylated interacting partners of BRD4, such as transcription factors, expanding on its previously unappreciated role in diverse biological processes.	ibpp	9-13	bromodomain containing 4	Homo sapiens	69-73
28347667-3	2017	Through AlphaScreen-based high-throughput screening assay, a novel small molecular inhibitor was identified, and named DCBD-005, which inhibited the binding between BRD4-BD1 and acetylated lysines with an IC50 value of 0.81+-0.03muM.	dcbd-005	119-127	bromodomain containing 4	Homo sapiens	165-173
28347667-6	2017	These results indicated that this novel BRD4-BD1 inhibitor DCBD-005 is promising to be developed into a drug candidate in the treatment of BRD4-related diseases.	dcbd-005	59-67	bromodomain containing 4	Homo sapiens	40-48
28336808-2	2017	Using the chemical scaffold of the JAK2 inhibitor TG101348, we developed and characterized single agents which potently and simultaneously inhibit BRD4 and a specific set of oncogenic tyrosine kinases including JAK2, FLT3, RET, and ROS1.	Fedratinib	50-58	bromodomain containing 4	Homo sapiens	147-151
28347667-3	2017	Through AlphaScreen-based high-throughput screening assay, a novel small molecular inhibitor was identified, and named DCBD-005, which inhibited the binding between BRD4-BD1 and acetylated lysines with an IC50 value of 0.81+-0.03muM.	Lysine	189-196	bromodomain containing 4	Homo sapiens	165-173
28347667-6	2017	These results indicated that this novel BRD4-BD1 inhibitor DCBD-005 is promising to be developed into a drug candidate in the treatment of BRD4-related diseases.	dcbd-005	59-67	bromodomain containing 4	Homo sapiens	40-44
28347667-5	2017	Moreover, the crystal structure of compound DCBD-005 with the BRD4-BD1 was determined at 1.72A resolution, which revealed the binding mechanism of the leading compound, and also provided solid basis for further structure-based optimization.	Dichlorobutadiene	44-48	bromodomain containing 4	Homo sapiens	62-70
28314513-0	2017	Design, synthesis and biological evaluation of 7-methylimidazo[1,5-a]pyrazin-8(7H)-one derivatives as BRD4 inhibitors.	2-methyl-6-(4-methoxyphenyl)-3,7-dihydroimidazo(1,2-alpha)pyrazin-3-one	47-86	bromodomain containing 4	Homo sapiens	102-106
28314513-2	2017	In this paper, we synthesized a series of 7-methylimidazo[1,5-a]pyrazin-8(7H)-one derivatives as potent BRD4 inhibitors and evaluated their BRD4 inhibitory activities in vitro and anti-proliferation effects on tumor cells.	2-methyl-6-(4-methoxyphenyl)-3,7-dihydroimidazo(1,2-alpha)pyrazin-3-one	42-81	bromodomain containing 4	Homo sapiens	104-108
28314513-2	2017	In this paper, we synthesized a series of 7-methylimidazo[1,5-a]pyrazin-8(7H)-one derivatives as potent BRD4 inhibitors and evaluated their BRD4 inhibitory activities in vitro and anti-proliferation effects on tumor cells.	2-methyl-6-(4-methoxyphenyl)-3,7-dihydroimidazo(1,2-alpha)pyrazin-3-one	42-81	bromodomain containing 4	Homo sapiens	140-144
28281917-0	2017	BRD4 inhibitor IBET upregulates p27kip/cip protein stability in neuroendocrine tumor cells.	molibresib	15-19	bromodomain containing 4	Homo sapiens	0-4
28281917-5	2017	In contrast, an inhibitor (IBET) to an epigenetic regulator, Brd4 that binds acetylated histones and upregulates transcription of multiple genes including protooncogene c-Myc, potently inhibited the NET cells.	molibresib	27-31	bromodomain containing 4	Homo sapiens	61-65
28203693-8	2017	In Ty-82 cells, we also identified a complex genomic rearrangement involving the BRD4-NUT rearrangement underlying the simple t(15;19) karyotype.	Thr-Tyr	3-5	bromodomain containing 4	Homo sapiens	81-85
28249162-5	2017	Mechanistically, BETi decreased Brd4 occupancy at the Cd274 locus without any change in Myc occupancy, resulting in transcriptional pausing and rapid loss of Cd274 mRNA production.	beti	17-21	bromodomain containing 4	Homo sapiens	32-36
28077651-7	2017	In vivo, poly(I C)-induced neutrophilia and mucosal chemokine production are blocked by a small-molecule BRD4 bromodomain inhibitor.	Poly I-C	9-18	bromodomain containing 4	Homo sapiens	105-109
28073847-1	2017	Purpose: AZD5153 is a novel BRD4/BET inhibitor with a distinctive bivalent bromodomain binding mode.	AZD5153	9-16	bromodomain containing 4	Homo sapiens	28-32
28137841-2	2017	Here, we report on the biological activity, the structural basis, and therapeutic effects of the family of multitargeted compounds that simultaneously disrupt functions of two critical MYC-mediating factors through inhibiting the acetyllysine binding of BRD4 and the kinase activity of PI3K.	N-epsilon-Acetyl-L-lysine	230-242	bromodomain containing 4	Homo sapiens	254-258