PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 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 32184777-0 2020 BRD4 Inhibition by AZD5153 Promotes Antitumor Immunity via Depolarizing M2 Macrophages. AZD5153 19-26 bromodomain containing 4 Homo sapiens 0-4 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 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 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 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 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 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 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 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 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 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 31523195-11 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 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 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 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 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 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 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 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 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 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 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 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 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 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