PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 19016842-5 2008 We show that harmine not only inhibits the protein-serine/threonine kinase activity of mature DYRK1A, but also its autophosphorylation on tyrosine during translation, indicating that harmine prevents formation of the active enzyme. Harmine 183-190 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 94-100 18938227-6 2008 Phosphorylation of SEPT4 by DYRK1A was inhibited by harmine, which has recently been identified as the most specific inhibitor of DYRK1A. Harmine 52-59 septin 4 Homo sapiens 19-24 18938227-6 2008 Phosphorylation of SEPT4 by DYRK1A was inhibited by harmine, which has recently been identified as the most specific inhibitor of DYRK1A. Harmine 52-59 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 28-34 18938227-6 2008 Phosphorylation of SEPT4 by DYRK1A was inhibited by harmine, which has recently been identified as the most specific inhibitor of DYRK1A. Harmine 52-59 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 130-136 19016842-0 2008 DYRK1A phosphorylates caspase 9 at an inhibitory site and is potently inhibited in human cells by harmine. Harmine 98-105 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 0-6 17039880-0 2006 [Harmine induces apoptosis in human SGC-7901 cells]. Harmine 1-8 sarcoglycan beta Homo sapiens 36-39 19016842-0 2008 DYRK1A phosphorylates caspase 9 at an inhibitory site and is potently inhibited in human cells by harmine. Harmine 98-105 caspase 9 Homo sapiens 22-31 19016842-4 2008 DYRK1A-dependent phosphorylation of Thr125 is also blocked by harmine, confirming the use of this beta-carboline alkaloid as a potent inhibitor of DYRK1A in cells. Harmine 62-69 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 0-6 19016842-4 2008 DYRK1A-dependent phosphorylation of Thr125 is also blocked by harmine, confirming the use of this beta-carboline alkaloid as a potent inhibitor of DYRK1A in cells. Harmine 62-69 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 147-153 19016842-5 2008 We show that harmine not only inhibits the protein-serine/threonine kinase activity of mature DYRK1A, but also its autophosphorylation on tyrosine during translation, indicating that harmine prevents formation of the active enzyme. Harmine 13-20 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 94-100 17850214-3 2007 We have also identified harmine as a potent and specific inhibitor of DYRK1A (dual-specificity tyrosine-phosphorylated and -regulated kinase 1A) in vitro. Harmine 24-31 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 70-76 17850214-3 2007 We have also identified harmine as a potent and specific inhibitor of DYRK1A (dual-specificity tyrosine-phosphorylated and -regulated kinase 1A) in vitro. Harmine 24-31 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 78-143 18562627-1 2008 We previously identified the small molecule harmine as a regulator of peroxisome proliferator activated-receptor gamma (PPARgamma) and adipocyte differentiation. Harmine 44-51 peroxisome proliferator activated receptor gamma Mus musculus 70-118 18562627-1 2008 We previously identified the small molecule harmine as a regulator of peroxisome proliferator activated-receptor gamma (PPARgamma) and adipocyte differentiation. Harmine 44-51 peroxisome proliferator activated receptor gamma Mus musculus 120-129 18562627-3 2008 Inhibitor of DNA biding 2 (Id2) was identified as a gene rapidly induced by harmine but not by PPARgamma agonists. Harmine 76-83 inhibitor of DNA binding 2 Mus musculus 0-25 18562627-3 2008 Inhibitor of DNA biding 2 (Id2) was identified as a gene rapidly induced by harmine but not by PPARgamma agonists. Harmine 76-83 inhibitor of DNA binding 2 Mus musculus 27-30 17488638-0 2007 The small molecule harmine is an antidiabetic cell-type-specific regulator of PPARgamma expression. Harmine 19-26 peroxisome proliferator activated receptor gamma Mus musculus 78-87 17488638-3 2007 This molecule, harmine, is not a ligand for the receptor; rather, it acts as a cell-type-specific regulator of PPARgamma expression. Harmine 15-22 peroxisome proliferator activated receptor gamma Mus musculus 111-120 17488638-4 2007 Administration of harmine to diabetic mice mimics the effects of PPARgamma ligands on adipocyte gene expression and insulin sensitivity. Harmine 18-25 peroxisome proliferator activated receptor gamma Mus musculus 65-74 17488638-6 2007 Molecular studies indicate that harmine controls PPARgamma expression through inhibition of the Wnt signaling pathway. Harmine 32-39 peroxisome proliferator activated receptor gamma Mus musculus 49-58 17088501-8 2006 MAIN OUTCOME MEASURE: Harmine labeled with carbon 11, a radioligand selective for MAO-A and positron emission tomography, was used to measure MAO-A DVS (specific distribution volume), an index of MAO-A density, in different brain regions (prefrontal cortex, anterior cingulate cortex, posterior cingulate cortex, caudate, putamen, thalamus, anterior temporal cortex, midbrain, hippocampus, and parahippocampus). Harmine 22-29 monoamine oxidase A Homo sapiens 82-87 17088501-8 2006 MAIN OUTCOME MEASURE: Harmine labeled with carbon 11, a radioligand selective for MAO-A and positron emission tomography, was used to measure MAO-A DVS (specific distribution volume), an index of MAO-A density, in different brain regions (prefrontal cortex, anterior cingulate cortex, posterior cingulate cortex, caudate, putamen, thalamus, anterior temporal cortex, midbrain, hippocampus, and parahippocampus). Harmine 22-29 monoamine oxidase A Homo sapiens 142-147 17088501-8 2006 MAIN OUTCOME MEASURE: Harmine labeled with carbon 11, a radioligand selective for MAO-A and positron emission tomography, was used to measure MAO-A DVS (specific distribution volume), an index of MAO-A density, in different brain regions (prefrontal cortex, anterior cingulate cortex, posterior cingulate cortex, caudate, putamen, thalamus, anterior temporal cortex, midbrain, hippocampus, and parahippocampus). Harmine 22-29 monoamine oxidase A Homo sapiens 142-147 17039880-1 2006 OBJECTIVE: [corrected] To investigate the effect of apoptosis induced in human SGC-7901 cells by Harmine. Harmine 97-104 sarcoglycan beta Homo sapiens 79-82 17039880-2 2006 METHODS: The effect of Harmine on human SGC-7901 cell survival and apoptosis was determined by MTT assay, light microscopy and flow cytometry. Harmine 23-30 sarcoglycan beta Homo sapiens 40-43 16079787-0 2006 Positron emission tomography quantification of [11C]-harmine binding to monoamine oxidase-A in the human brain. Harmine 53-60 monoamine oxidase A Homo sapiens 72-91 16079787-1 2006 This article describes the kinetic modeling of [(11)C]-harmine binding to monoamine oxidase A (MAO-A) binding sites in the human brain using positron emission tomography (PET). Harmine 55-62 monoamine oxidase A Homo sapiens 74-93 16079787-1 2006 This article describes the kinetic modeling of [(11)C]-harmine binding to monoamine oxidase A (MAO-A) binding sites in the human brain using positron emission tomography (PET). Harmine 55-62 monoamine oxidase A Homo sapiens 95-100 16079787-8 2006 Moclobemide treatment leads to a 64% to 79% MAO-A blockade across brain regions, a result that supports the specificity of [(11)C]-harmine binding to MAO-A. Harmine 131-138 monoamine oxidase A Homo sapiens 150-155 12900293-6 2003 RESULTS: The MAO-A-ligand Harmine expressed specific in vitro binding of 87 +/-21% for MGC and 125 +/- 50% for EPT, compared to reference tissue (rat brain, 100%). Harmine 26-33 monoamine oxidase A Rattus norvegicus 13-18 16149329-1 2005 Harmine, a major alkaloid in ayahuasca (hoasca), is a selective and reversible inhibitor of the enzyme monoamine oxidase-A (MAO-A). Harmine 0-7 monoamine oxidase A Homo sapiens 103-122 16149329-1 2005 Harmine, a major alkaloid in ayahuasca (hoasca), is a selective and reversible inhibitor of the enzyme monoamine oxidase-A (MAO-A). Harmine 0-7 monoamine oxidase A Homo sapiens 124-129 16149329-2 2005 It is also a selective inhibitor of the human cytochrome P450 isozyme 2D6 (CYP 2D6), which metabolizes harmine to a more hydrophilic derivative for eventual excretion. Harmine 103-110 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 46-73 16149329-2 2005 It is also a selective inhibitor of the human cytochrome P450 isozyme 2D6 (CYP 2D6), which metabolizes harmine to a more hydrophilic derivative for eventual excretion. Harmine 103-110 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 75-82 16149329-4 2005 This report broadly describes two subgroups of CYP 2D6 phenotypes--i.e., fast and slow metabolizers of harmine-in 14 experienced male members of the Uniao do Vegetal (UDV) who received a standardized dosage of hoasca. Harmine 103-110 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 47-54 15047157-2 2004 In the present study, harmine was identified from a collection of herbal compounds to be a specific inhibitor of Cdk1/cyclin B, Cdk2/cyclin A, and Cdk5/p25 with IC50 values at low micromoles. Harmine 22-29 cyclin dependent kinase 1 Homo sapiens 113-117 15047157-2 2004 In the present study, harmine was identified from a collection of herbal compounds to be a specific inhibitor of Cdk1/cyclin B, Cdk2/cyclin A, and Cdk5/p25 with IC50 values at low micromoles. Harmine 22-29 cyclin dependent kinase 2 Homo sapiens 128-132 15047157-2 2004 In the present study, harmine was identified from a collection of herbal compounds to be a specific inhibitor of Cdk1/cyclin B, Cdk2/cyclin A, and Cdk5/p25 with IC50 values at low micromoles. Harmine 22-29 cyclin A2 Homo sapiens 133-141 15047157-2 2004 In the present study, harmine was identified from a collection of herbal compounds to be a specific inhibitor of Cdk1/cyclin B, Cdk2/cyclin A, and Cdk5/p25 with IC50 values at low micromoles. Harmine 22-29 cyclin dependent kinase 5 Homo sapiens 147-151 15047157-2 2004 In the present study, harmine was identified from a collection of herbal compounds to be a specific inhibitor of Cdk1/cyclin B, Cdk2/cyclin A, and Cdk5/p25 with IC50 values at low micromoles. Harmine 22-29 cyclin dependent kinase 5 regulatory subunit 1 Homo sapiens 152-155 15047157-4 2004 The CDK inhibition by harmine is competitive with ATP-Mg2+, suggesting that it binds to the ATP-Mg2+-binding pocket of CDKs. Harmine 22-29 cyclin dependent kinase 1 Homo sapiens 119-123 15047157-7 2004 Taken together, harmine is a selective inhibitor of CDKs and cell proliferation. Harmine 16-23 cyclin dependent kinase 1 Homo sapiens 52-56 12649384-2 2003 Cytochromes P450 1A1 (18.5), 1A2 (20), and 2D6 (100) catalyzed the O-demethylation of harmaline, and CYP1A1 (98.5), CYP1A2 (35), CYP2C9 (16), CYP2C19 (30), and CYP2D6 (115) catalyzed that of harmine (relative activities). Harmine 191-198 cytochrome P450, family 1, subfamily a, polypeptide 1 Mus musculus 101-107 12649384-2 2003 Cytochromes P450 1A1 (18.5), 1A2 (20), and 2D6 (100) catalyzed the O-demethylation of harmaline, and CYP1A1 (98.5), CYP1A2 (35), CYP2C9 (16), CYP2C19 (30), and CYP2D6 (115) catalyzed that of harmine (relative activities). Harmine 191-198 cytochrome P450, family 1, subfamily a, polypeptide 2 Mus musculus 116-122 12649384-6 2003 Values for harmine were: CYP1A1, 45.2 and 52.2; CYP1A2, 9.2 and 14.7; CYP2C9, 11.9 and 117; CYP2C19, 21.4 and 121; and CYP2D6, 29.7 and 7.4. Harmine 11-18 cytochrome P450, family 1, subfamily a, polypeptide 1 Mus musculus 25-31 12649384-6 2003 Values for harmine were: CYP1A1, 45.2 and 52.2; CYP1A2, 9.2 and 14.7; CYP2C9, 11.9 and 117; CYP2C19, 21.4 and 121; and CYP2D6, 29.7 and 7.4. Harmine 11-18 cytochrome P450, family 1, subfamily a, polypeptide 2 Mus musculus 48-54 12649384-6 2003 Values for harmine were: CYP1A1, 45.2 and 52.2; CYP1A2, 9.2 and 14.7; CYP2C9, 11.9 and 117; CYP2C19, 21.4 and 121; and CYP2D6, 29.7 and 7.4. Harmine 11-18 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 70-76 12649384-6 2003 Values for harmine were: CYP1A1, 45.2 and 52.2; CYP1A2, 9.2 and 14.7; CYP2C9, 11.9 and 117; CYP2C19, 21.4 and 121; and CYP2D6, 29.7 and 7.4. Harmine 11-18 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 119-125 12649384-7 2003 Inhibition studies using monoclonal antibodies confirmed that CYP1A2 and CYP2D6 were the major isozymes contributing to both harmaline (20% and 50%, respectively) and harmine (20% and 30%) O-demethylations in pooled HLMs. Harmine 167-174 cytochrome P450, family 1, subfamily a, polypeptide 2 Mus musculus 62-68 12649384-7 2003 Inhibition studies using monoclonal antibodies confirmed that CYP1A2 and CYP2D6 were the major isozymes contributing to both harmaline (20% and 50%, respectively) and harmine (20% and 30%) O-demethylations in pooled HLMs. Harmine 167-174 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 73-79 12649384-10 2003 These findings suggest a role for polymorphic CYP2D6 in the pharmacology and toxicology of harmine and harmaline. Harmine 91-98 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 46-52 12445480-5 2002 The inhibitors, D-amphetamine, harmine, tetrindole, and befloxatone all induce similar (but not identical) changes in the spectrum of MAO A, consistent with stacking of inhibitor with the flavin in the active site. Harmine 31-38 monoamine oxidase A Homo sapiens 134-139 12445480-6 2002 D-Amphetamine, harmine, and tetrindole stabilise the semiquinone form of FAD during reduction of MAO A by dithionite and no further reduction of these inhibitor-MAO A complexes has been observed. Harmine 15-22 monoamine oxidase A Homo sapiens 97-102 11890933-5 2002 Mutants defective in excision-resynthesis repair (rad3 and rad1), in error-prone repair (rad6) and in recombinational repair (rad52) showed enhanced sensitivity to harmine and harman, but the ranking of sensitivities was different for the two alkaloids. Harmine 164-171 TFIIH/NER complex ATP-dependent 5'-3' DNA helicase subunit RAD3 Saccharomyces cerevisiae S288C 50-54 11890933-5 2002 Mutants defective in excision-resynthesis repair (rad3 and rad1), in error-prone repair (rad6) and in recombinational repair (rad52) showed enhanced sensitivity to harmine and harman, but the ranking of sensitivities was different for the two alkaloids. Harmine 164-171 ssDNA endodeoxyribonuclease RAD1 Saccharomyces cerevisiae S288C 59-63 11890933-5 2002 Mutants defective in excision-resynthesis repair (rad3 and rad1), in error-prone repair (rad6) and in recombinational repair (rad52) showed enhanced sensitivity to harmine and harman, but the ranking of sensitivities was different for the two alkaloids. Harmine 164-171 E2 ubiquitin-conjugating protein RAD6 Saccharomyces cerevisiae S288C 89-93 11797076-10 2001 Taken together, these results indicate that harmine affects the brain dopamine system probably by acting as a MAO-A inhibitor and not as an inverse agonist for the benzodiazepine receptors. Harmine 44-51 monoamine oxidase A Rattus norvegicus 110-115 9503561-4 1997 MAO-A preferentially deaminates serotonin (5HT) and is selectively inhibited by harmine and clorgyline, while MAO-B preferentially deaminates phenethylamine and benzylamine, and is selectively inhibited by (-)deprenyl as well as low concentrations of pargyline. Harmine 80-87 monoamine oxidase A Homo sapiens 0-5 10404423-2 1999 Such beverages are characterized by the presence of these three harmala alkaloids, where harmine and harmaline reversibly inhibit monoamine oxidase A (MAO-A) while tetrahydroharmine weakly inhibits the uptake of serotonin. Harmine 89-96 monoamine oxidase A Homo sapiens 130-149 10404423-2 1999 Such beverages are characterized by the presence of these three harmala alkaloids, where harmine and harmaline reversibly inhibit monoamine oxidase A (MAO-A) while tetrahydroharmine weakly inhibits the uptake of serotonin. Harmine 89-96 monoamine oxidase A Homo sapiens 151-156 7667371-4 1995 For example, both MDA and BDB produced abnormal body posture that was identical to that reported after administration of hallucinogens such as lysergic acid diethylamide (LSD) and harmine (11). Harmine 180-187 receptor tyrosine kinase like orphan receptor 2 Homo sapiens 26-29 9257326-5 1997 Different approaches for a quantitative determination of MAO-A enzyme binding were attempted and demonstrated an IC50 dose of harmine in the range of 0.05-0.1 mg/kg. Harmine 126-133 monoamine oxidase A Rattus norvegicus 57-62 8990278-6 1997 Harmine, 2-methylharminium, 2,9-dimethylharminium, and harmaline were the most effective inhibitors of the purified MAO A, with low Ki values of 5, 69, 15, and 48 nM, respectively. Harmine 0-7 monoamine oxidase A Homo sapiens 116-121 7667371-6 1995 BDB also produced bursting forward movements, an effect commonly observed after LSD and harmine. Harmine 88-95 receptor tyrosine kinase like orphan receptor 2 Homo sapiens 0-3 34242659-9 2022 TWIST1 inhibitor harmine could significantly suppress the fibrogenesis of keloid fibroblasts. Harmine 17-24 twist family bHLH transcription factor 1 Homo sapiens 0-6 2137718-4 1990 The partially competitive nature of inhibition by one of the more effective pairs, 2-methyl-harmine and harmine, was consistent with uptake of the beta-carbolines by the synaptosomal dopamine uptake system, as was the fact that the accumulation of 2-[14C]methyl-harmine was significantly reduced by low Na+ media and by nomifensine, a potent inhibitor of the dopamine transporter. Harmine 92-99 solute carrier family 6 member 3 Homo sapiens 359-379 33234703-6 2020 An investigation into the mechanism revealed that harmine, when used with LRAs, increased the activity of NFkappaB, MAPK p38, and ERK1/2. Harmine 50-57 mitogen-activated protein kinase 3 Homo sapiens 130-136 33234703-7 2020 Harmine treatment also resulted in reduced expression of HEXIM1, a negative regulator of transcriptional elongation. Harmine 0-7 HEXIM P-TEFb complex subunit 1 Homo sapiens 57-63 34098466-0 2021 Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3beta/DYRK1A dual inhibitors for the treatment of Alzheimer"s disease. Harmine 47-54 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 87-93 34952543-3 2021 Therefore, 18 179 mRNA expression maps (based on the Allen Human Brain Atlas) were correlated with the cerebral distribution volume (VT) of MAO-A assessed in 36 healthy subjects (mean age +- standard deviation: 32.9 +- 8.8 years, 18 female) using (11C)harmine positron emission tomography scans. Harmine 252-259 monoamine oxidase A Homo sapiens 140-145 34098466-0 2021 Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3beta/DYRK1A dual inhibitors for the treatment of Alzheimer"s disease. Harmine 47-54 glycogen synthase kinase 3 alpha Homo sapiens 77-86 34098466-4 2021 In this study, a new series of harmine derivatives were designed, synthesized and evaluated as dual GSK-3beta/DYRK1A inhibitors for their multiple biological activities. Harmine 31-38 glycogen synthase kinase 3 alpha Homo sapiens 100-109 34098466-4 2021 In this study, a new series of harmine derivatives were designed, synthesized and evaluated as dual GSK-3beta/DYRK1A inhibitors for their multiple biological activities. Harmine 31-38 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 110-116 34079546-9 2021 And we also provided evidences that the immunomodulatory capacity of harmine might be attributed to the inhibition of the c-Jun N-terminal kinase (JNK) in wear particle-treated macrophages. Harmine 69-76 mitogen-activated protein kinase 8 Mus musculus 122-145 34205249-5 2021 Of these compounds, synephrine, trigonelline, cytisine, harmine, koumine, peimisine, and hupehenine exhibited in vitro inhibition of alpha-syn-seeded fibril formation. Harmine 56-63 synuclein alpha Homo sapiens 133-142 34384998-0 2021 Cell-based assays and molecular simulation reveal that the anti-cancer harmine is a specific matrix metalloproteinase-3 (MMP-3) inhibitor. Harmine 71-78 matrix metallopeptidase 3 Homo sapiens 93-119 34384998-0 2021 Cell-based assays and molecular simulation reveal that the anti-cancer harmine is a specific matrix metalloproteinase-3 (MMP-3) inhibitor. Harmine 71-78 matrix metallopeptidase 3 Homo sapiens 121-126 34384998-3 2021 We therefore investigated harmine for its effects on MMP-3 and the molecular interaction was also simulated. Harmine 26-33 matrix metallopeptidase 3 Homo sapiens 53-58 34384998-5 2021 These results showed that although harmine stimulation in vitro has very little or no effects on MMP-3 expression by U-87 MG cells, the treatment of harmine decreases MMP-3 activity in a dose dependent manner. Harmine 149-156 matrix metallopeptidase 3 Homo sapiens 97-102 34384998-5 2021 These results showed that although harmine stimulation in vitro has very little or no effects on MMP-3 expression by U-87 MG cells, the treatment of harmine decreases MMP-3 activity in a dose dependent manner. Harmine 149-156 matrix metallopeptidase 3 Homo sapiens 167-172 34384998-7 2021 Using a molecular dynamic simulation approach, we identified the N2, methyl of C1 and benzene ring of harmine interact with Zn2+ (2.4 A), His205 (2.4 A) and His211 (2.4 A) as well as Val163 (2.7 A) at the active site of MMP-3, respectively, and thus conferred a striking specific binding advantage. Harmine 102-109 matrix metallopeptidase 3 Homo sapiens 220-225 34384998-8 2021 Taken altogether, the present study evidences that harmine acts as an MMP-3 inhibitor specially targeting the enzymatic active site and possibly efficiently ameliorates MMP-3-driven malignant and inflammatory diseases. Harmine 51-58 matrix metallopeptidase 3 Homo sapiens 70-75 34384998-8 2021 Taken altogether, the present study evidences that harmine acts as an MMP-3 inhibitor specially targeting the enzymatic active site and possibly efficiently ameliorates MMP-3-driven malignant and inflammatory diseases. Harmine 51-58 matrix metallopeptidase 3 Homo sapiens 169-174 34425477-5 2021 A series of novel benzo(d)imidazo(2,1-b)thiazole derivatives possessing 1,3,4-oxadiazole moiety were designed based on the structure of the first-in-class Twist1 inhibitor harmine. Harmine 172-179 twist family bHLH transcription factor 1 Homo sapiens 155-161 34425477-7 2021 Meanwhile, western blot assay showed that the optimal compound significantly down-regulated Twist1 protein expression in a dose-dependent manner and reduced Twist1 level better than harmine. Harmine 182-189 twist family bHLH transcription factor 1 Homo sapiens 92-98 34425477-7 2021 Meanwhile, western blot assay showed that the optimal compound significantly down-regulated Twist1 protein expression in a dose-dependent manner and reduced Twist1 level better than harmine. Harmine 182-189 twist family bHLH transcription factor 1 Homo sapiens 157-163 34079546-9 2021 And we also provided evidences that the immunomodulatory capacity of harmine might be attributed to the inhibition of the c-Jun N-terminal kinase (JNK) in wear particle-treated macrophages. Harmine 69-76 mitogen-activated protein kinase 8 Mus musculus 147-150 35569122-10 2022 CMap analysis showed that the small molecules scriptaid, torasemide, dexpropranolol, ipratropium bromide, and harmine were potential negative regulators of TGIF1. Harmine 110-117 TGFB induced factor homeobox 1 Homo sapiens 156-161 34078836-11 2021 CONCLUSION: Harmine exposure leads to central neurological symptoms, cardiovascular effects and even death through direct inhibition of the central AChE activity, where the death primarily comes from central neurological symptoms and is cooperated by the secondary cardiovascular collapse. Harmine 12-19 acetylcholinesterase Mus musculus 148-152 35623405-0 2022 Harmine prevents 3-nitropropionic acid-induced neurotoxicity in rats via enhancing NRF2-mediated signaling: Involvement of p21 and AMPK. Harmine 0-7 NFE2 like bZIP transcription factor 2 Rattus norvegicus 83-87 35623405-0 2022 Harmine prevents 3-nitropropionic acid-induced neurotoxicity in rats via enhancing NRF2-mediated signaling: Involvement of p21 and AMPK. Harmine 0-7 KRAS proto-oncogene, GTPase Rattus norvegicus 123-126 35623405-0 2022 Harmine prevents 3-nitropropionic acid-induced neurotoxicity in rats via enhancing NRF2-mediated signaling: Involvement of p21 and AMPK. Harmine 0-7 protein kinase AMP-activated catalytic subunit alpha 2 Rattus norvegicus 131-135 35623405-3 2022 This study aimed at evaluating the prophylactic effects of the dual-specificity tyrosine phosphorylation regulated kinase 1A (DYRK1A) inhibitor "harmine" against 3-NP-indued neurotoxicity and HD-like symptoms. Harmine 145-152 dual specificity tyrosine phosphorylation regulated kinase 1A Rattus norvegicus 63-124 35623405-3 2022 This study aimed at evaluating the prophylactic effects of the dual-specificity tyrosine phosphorylation regulated kinase 1A (DYRK1A) inhibitor "harmine" against 3-NP-indued neurotoxicity and HD-like symptoms. Harmine 145-152 dual specificity tyrosine phosphorylation regulated kinase 1A Rattus norvegicus 126-132 35623405-5 2022 Harmine successfully increased the protein levels of NRF2, AMPK and p21 and the gene expression of Ho-1, Nqo-1 and p62, restored redox homeostasis, and reduced CASPASE-3 level. Harmine 0-7 NFE2 like bZIP transcription factor 2 Rattus norvegicus 53-57 35623405-5 2022 Harmine successfully increased the protein levels of NRF2, AMPK and p21 and the gene expression of Ho-1, Nqo-1 and p62, restored redox homeostasis, and reduced CASPASE-3 level. Harmine 0-7 protein kinase AMP-activated catalytic subunit alpha 2 Rattus norvegicus 59-63 35623405-5 2022 Harmine successfully increased the protein levels of NRF2, AMPK and p21 and the gene expression of Ho-1, Nqo-1 and p62, restored redox homeostasis, and reduced CASPASE-3 level. Harmine 0-7 KRAS proto-oncogene, GTPase Rattus norvegicus 68-71 35623405-5 2022 Harmine successfully increased the protein levels of NRF2, AMPK and p21 and the gene expression of Ho-1, Nqo-1 and p62, restored redox homeostasis, and reduced CASPASE-3 level. Harmine 0-7 heme oxygenase 1 Rattus norvegicus 99-103 35623405-5 2022 Harmine successfully increased the protein levels of NRF2, AMPK and p21 and the gene expression of Ho-1, Nqo-1 and p62, restored redox homeostasis, and reduced CASPASE-3 level. Harmine 0-7 NAD(P)H quinone dehydrogenase 1 Rattus norvegicus 105-110 35623405-5 2022 Harmine successfully increased the protein levels of NRF2, AMPK and p21 and the gene expression of Ho-1, Nqo-1 and p62, restored redox homeostasis, and reduced CASPASE-3 level. Harmine 0-7 KH RNA binding domain containing, signal transduction associated 1 Rattus norvegicus 115-118 35623405-5 2022 Harmine successfully increased the protein levels of NRF2, AMPK and p21 and the gene expression of Ho-1, Nqo-1 and p62, restored redox homeostasis, and reduced CASPASE-3 level. Harmine 0-7 caspase 3 Rattus norvegicus 160-169 35623405-7 2022 This study draws attention to the protective role of harmine against 3-NP-induced motor and cognitive dysfunction that could be mediated via enhancing NRF2-mediated signaling with subsequent amelioration of oxidative stress injury via NRF2 activators, p21 and AMPK, in the striatum, prefrontal cortex, and hippocampus which could offer a promising therapeutic tool to slow the progression of HD. Harmine 53-60 NFE2 like bZIP transcription factor 2 Rattus norvegicus 151-155 35623405-7 2022 This study draws attention to the protective role of harmine against 3-NP-induced motor and cognitive dysfunction that could be mediated via enhancing NRF2-mediated signaling with subsequent amelioration of oxidative stress injury via NRF2 activators, p21 and AMPK, in the striatum, prefrontal cortex, and hippocampus which could offer a promising therapeutic tool to slow the progression of HD. Harmine 53-60 NFE2 like bZIP transcription factor 2 Rattus norvegicus 235-239 35623405-7 2022 This study draws attention to the protective role of harmine against 3-NP-induced motor and cognitive dysfunction that could be mediated via enhancing NRF2-mediated signaling with subsequent amelioration of oxidative stress injury via NRF2 activators, p21 and AMPK, in the striatum, prefrontal cortex, and hippocampus which could offer a promising therapeutic tool to slow the progression of HD. Harmine 53-60 KRAS proto-oncogene, GTPase Rattus norvegicus 252-255 35623405-7 2022 This study draws attention to the protective role of harmine against 3-NP-induced motor and cognitive dysfunction that could be mediated via enhancing NRF2-mediated signaling with subsequent amelioration of oxidative stress injury via NRF2 activators, p21 and AMPK, in the striatum, prefrontal cortex, and hippocampus which could offer a promising therapeutic tool to slow the progression of HD. Harmine 53-60 protein kinase AMP-activated catalytic subunit alpha 2 Rattus norvegicus 260-264 35219102-0 2022 Harmine suppresses collagen production in hepatic stellate cells by inhibiting DYRK1B. Harmine 0-7 dual specificity tyrosine phosphorylation regulated kinase 1B Homo sapiens 79-85 35369706-4 2022 RESULTS: We observed that harmine, an inhibitor of DYRK1a, improved left ventricular ejection fraction (39.5+-1.6% and 29.1+-1.6%, harmine versus placebo, respectively), 2 weeks after I/R MI. Harmine 26-33 dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1a Mus musculus 51-57 35219102-8 2022 Harmine (10 muM) significantly inhibited the increased expression of COL1A1. Harmine 0-7 collagen, type I, alpha 1 Mus musculus 69-75 35244188-5 2022 In addition, DYRK1A knockdown using small interfering RNA transfection or treatment with harmine, a natural alkaloid, significantly reduced the protein expression levels of HIF-1alpha in liver cancer cells under hypoxic conditions in vitro. Harmine 89-96 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 13-19 35219102-11 2022 These results suggest that harmine suppresses COL1A1 expression via inhibiting DYRK1B in HSCs and therefore might be effective for the treatment of liver fibrosis. Harmine 27-34 collagen type I alpha 1 chain Homo sapiens 46-52 35219102-11 2022 These results suggest that harmine suppresses COL1A1 expression via inhibiting DYRK1B in HSCs and therefore might be effective for the treatment of liver fibrosis. Harmine 27-34 dual specificity tyrosine phosphorylation regulated kinase 1B Homo sapiens 79-85 35244188-5 2022 In addition, DYRK1A knockdown using small interfering RNA transfection or treatment with harmine, a natural alkaloid, significantly reduced the protein expression levels of HIF-1alpha in liver cancer cells under hypoxic conditions in vitro. Harmine 89-96 hypoxia inducible factor 1 subunit alpha Homo sapiens 173-183 35244188-11 2022 Co-treatment with harmine and either regorafenib or sorafenib also promoted cell death via the STAT3/HIF-1alpha/AKT signaling pathway under hypoxia using PI staining and western blotting. Harmine 18-25 signal transducer and activator of transcription 3 Homo sapiens 95-100 35244188-11 2022 Co-treatment with harmine and either regorafenib or sorafenib also promoted cell death via the STAT3/HIF-1alpha/AKT signaling pathway under hypoxia using PI staining and western blotting. Harmine 18-25 hypoxia inducible factor 1 subunit alpha Homo sapiens 101-111 35244188-11 2022 Co-treatment with harmine and either regorafenib or sorafenib also promoted cell death via the STAT3/HIF-1alpha/AKT signaling pathway under hypoxia using PI staining and western blotting. Harmine 18-25 AKT serine/threonine kinase 1 Homo sapiens 112-115 3876687-6 1985 In ethanol-withdrawn rats treated with harmine or LON-954 the frequency analysis of tremor revealed a narrow peak frequency at about 12 Hz, which was neither the characteristic frequency of ethanol withdrawal tremor (6 Hz) nor that of harmine or LON-954 (10 Hz). Harmine 39-46 lon peptidase 1, mitochondrial Rattus norvegicus 246-249 35126712-6 2022 Furthermore, DYRK1A inhibitor harmine together with regorafenib provided synergistic anti-liver cancer activity by suppressing cell proliferation. Harmine 30-37 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 13-19 35126712-9 2022 In the present study, AKT was activated in regorafenib-treated cells, and harmine could suppress the activation of AKT and reinforce the anti-cancer effects of regorafenib via regulating AKT in liver cancer cells. Harmine 74-81 AKT serine/threonine kinase 1 Homo sapiens 115-118 35126712-9 2022 In the present study, AKT was activated in regorafenib-treated cells, and harmine could suppress the activation of AKT and reinforce the anti-cancer effects of regorafenib via regulating AKT in liver cancer cells. Harmine 74-81 AKT serine/threonine kinase 1 Homo sapiens 187-190 35126712-10 2022 These data indicated that harmine enhanced the anti-cancer effects of regorafenib on suppressing cell proliferation and inducing apoptosis in liver cancer cells via regulating the activation of AKT, and harmine plus regorafenib may be a potential therapeutic regimen for treating patients with liver cancer. Harmine 26-33 AKT serine/threonine kinase 1 Homo sapiens 194-197 35111758-0 2021 Harmine Alleviated Sepsis-Induced Cardiac Dysfunction by Modulating Macrophage Polarization via the STAT/MAPK/NF-kappaB Pathway. Harmine 0-7 signal transducer and activator of transcription 1 Mus musculus 100-104 35111758-0 2021 Harmine Alleviated Sepsis-Induced Cardiac Dysfunction by Modulating Macrophage Polarization via the STAT/MAPK/NF-kappaB Pathway. Harmine 0-7 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 110-119 35111758-4 2021 In vitro, the expression of the M1 phenotype markers iNOS and COX-2 was increased in RAW 264.7 cells stimulated with lipopolysaccharide (LPS), but this effect was reversed by the harmine intervention. Harmine 179-186 nitric oxide synthase 2, inducible Mus musculus 53-57 35111758-4 2021 In vitro, the expression of the M1 phenotype markers iNOS and COX-2 was increased in RAW 264.7 cells stimulated with lipopolysaccharide (LPS), but this effect was reversed by the harmine intervention. Harmine 179-186 cytochrome c oxidase II, mitochondrial Mus musculus 62-67 35111758-6 2021 Meanwhile, our findings showed that harmine administration effectively attenuated inflammation and apoptosis in H9c2 cells in the proinflammatory environment produced by macrophages, as evidenced by reductions in NLRP3 and cleaved caspase 3 levels and the p-NF-kappaB/NF-kappaB ratio. Harmine 36-43 NLR family, pyrin domain containing 3 Rattus norvegicus 213-218 35111758-6 2021 Meanwhile, our findings showed that harmine administration effectively attenuated inflammation and apoptosis in H9c2 cells in the proinflammatory environment produced by macrophages, as evidenced by reductions in NLRP3 and cleaved caspase 3 levels and the p-NF-kappaB/NF-kappaB ratio. Harmine 36-43 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 258-267 35111758-6 2021 Meanwhile, our findings showed that harmine administration effectively attenuated inflammation and apoptosis in H9c2 cells in the proinflammatory environment produced by macrophages, as evidenced by reductions in NLRP3 and cleaved caspase 3 levels and the p-NF-kappaB/NF-kappaB ratio. Harmine 36-43 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 268-277 35111758-7 2021 The western blot results indicated that the mechanisms underlying harmine-mediated inhibition of M1 polarization might be associated with suppression of STAT1/3, NF-kappaB and MAPK activation. Harmine 66-73 signal transducer and activator of transcription 1 Mus musculus 153-160 35111758-7 2021 The western blot results indicated that the mechanisms underlying harmine-mediated inhibition of M1 polarization might be associated with suppression of STAT1/3, NF-kappaB and MAPK activation. Harmine 66-73 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 162-171 35053488-7 2022 Additionally, we demonstrated that the harmine-targeted suppression of DYRK1A used in conjunction with radiotherapy increases DNA double-strand breaks (DSBs) and impairs homologous repair (HR), resulting in more cancer cell death. Harmine 39-46 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 71-77 34994084-0 2022 Rational Design and Identification of Harmine-Inspired, N-Heterocyclic DYRK1A Inhibitors Employing a Functional Genomic In Vivo Drosophila Model System. Harmine 38-45 minibrain Drosophila melanogaster 71-77 34710745-8 2022 Compound b1 and harmine were more efficient in protecting SH-SY5Y cells against 6-hydroxydopamine-induced cell death, an effect that was previously correlated to Dyrk1A inactivation in cells but not yet verified using chemical inhibitors. Harmine 16-23 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 162-168 522515-2 1979 Isolated intestinal cells catalyzed the cytochrome P-450 dependent metabolism of benzo(a)pyrene, harmine, ethoxyresorufin and ethoxycoumarin. Harmine 97-104 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 40-56 3896805-1 1985 In this study we show that harmine treatment (10 mg/l for 2 or 24 h) of PtK2 cells had a marked effect on the localization of the nucleolar phosphoproteins C23 and B23. Harmine 27-34 protein tyrosine kinase 2 Homo sapiens 72-76 3896805-1 1985 In this study we show that harmine treatment (10 mg/l for 2 or 24 h) of PtK2 cells had a marked effect on the localization of the nucleolar phosphoproteins C23 and B23. Harmine 27-34 nucleolin Homo sapiens 156-159 6279462-1 1982 Inhibition of pineal monoamine oxidase (MAO) activity either by harmine or pargyline in adult male Sprague-Dawley rats housed in a 12 : 12 LD cycle resulted in increase pineal N-acetyltransferase (NAT) activity. Harmine 64-71 monoamine oxidase A Rattus norvegicus 21-38 6279462-1 1982 Inhibition of pineal monoamine oxidase (MAO) activity either by harmine or pargyline in adult male Sprague-Dawley rats housed in a 12 : 12 LD cycle resulted in increase pineal N-acetyltransferase (NAT) activity. Harmine 64-71 monoamine oxidase A Rattus norvegicus 40-43 6310434-0 1983 Cholecystokinin octapeptide (CCK-8), ceruletide and analogues of ceruletide: effects on tremors induced by oxotremorine, harmine and ibogaine. Harmine 121-128 cholecystokinin Mus musculus 0-15 461984-5 1979 One must consider the inhibitory effect of harmine and harmaline on both MAO and N-acetyltransferase when evaluating the effects of these compounds on physiological processes. Harmine 43-50 monoamine oxidase A Rattus norvegicus 73-76 33960660-8 2021 Dual-luciferase reporter assay analyses determined that PDGF-BB was the direct target of AP-1 which was up-regulated by harmine treatment. Harmine 120-127 jun proto-oncogene Mus musculus 89-93 12389-8 1976 The pI curves for inhibition of MAO activity by harmine, pargyline and iproniazid were similar and almost the same pI 50 values for the respective inhibitors were obtained with the two substrates. Harmine 48-55 monoamine oxidase A Rattus norvegicus 32-35 33960660-0 2021 Harmine targets inhibitor of DNA binding-2 and activator protein-1 to promote preosteoclast PDGF-BB production. Harmine 0-7 jun proto-oncogene Mus musculus 47-66 132195-3 1976 Harmine and harmaline were investigated as potentially useful fluorescent inhibitors of (Na+ + K+) activated ATPase. Harmine 0-7 dynein axonemal heavy chain 8 Homo sapiens 109-115 34050242-8 2021 Harmine potently stimulated alpha-cell proliferation and both harmine and HB-EGF increased proliferation of insulin- and glucagon-negative cells, including cytokeratin 19-positive cells. Harmine 62-69 insulin Homo sapiens 108-115 34050242-8 2021 Harmine potently stimulated alpha-cell proliferation and both harmine and HB-EGF increased proliferation of insulin- and glucagon-negative cells, including cytokeratin 19-positive cells. Harmine 62-69 glucagon Homo sapiens 121-129 34050242-8 2021 Harmine potently stimulated alpha-cell proliferation and both harmine and HB-EGF increased proliferation of insulin- and glucagon-negative cells, including cytokeratin 19-positive cells. Harmine 62-69 keratin 19 Homo sapiens 156-170 34030962-0 2021 A natural compound harmine decreases melanin synthesis through regulation of the DYRK1A/NFATC3 pathway. Harmine 19-26 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 81-87 34030962-0 2021 A natural compound harmine decreases melanin synthesis through regulation of the DYRK1A/NFATC3 pathway. Harmine 19-26 nuclear factor of activated T cells 3 Homo sapiens 88-94 34030962-7 2021 Inhibition of DYRK1A, a harmine target, decreased melanin synthesis and tyrosinase expression. Harmine 24-31 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 14-20 34030962-10 2021 Furthermore, harmine also decreased melanin synthesis and tyrosinase expression through regulation of NFATC3 in human primary melanocytes. Harmine 13-20 nuclear factor of activated T cells 3 Homo sapiens 102-108 34030962-11 2021 CONCLUSION: Our results indicate that harmine decreases melanin synthesis through regulation of the DYRK1A/NFATC3 pathway and suggest that the DYRK1A/NFATC3 pathway may be a potential target for the development of depigmenting agents. Harmine 38-45 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 100-106 34030962-11 2021 CONCLUSION: Our results indicate that harmine decreases melanin synthesis through regulation of the DYRK1A/NFATC3 pathway and suggest that the DYRK1A/NFATC3 pathway may be a potential target for the development of depigmenting agents. Harmine 38-45 nuclear factor of activated T cells 3 Homo sapiens 107-113 34030962-11 2021 CONCLUSION: Our results indicate that harmine decreases melanin synthesis through regulation of the DYRK1A/NFATC3 pathway and suggest that the DYRK1A/NFATC3 pathway may be a potential target for the development of depigmenting agents. Harmine 38-45 nuclear factor of activated T cells 3 Homo sapiens 150-156 33960660-4 2021 In this study, we revealed that inhibitor of DNA binding-2 (Id2) and activator protein-1 (AP-1) were important factors implicated in harmine-enhanced preosteoclast PDGF-BB production. Harmine 133-140 inhibitor of DNA binding 2 Mus musculus 32-58 33960660-4 2021 In this study, we revealed that inhibitor of DNA binding-2 (Id2) and activator protein-1 (AP-1) were important factors implicated in harmine-enhanced preosteoclast PDGF-BB production. Harmine 133-140 inhibitor of DNA binding 2 Mus musculus 60-63 33960660-4 2021 In this study, we revealed that inhibitor of DNA binding-2 (Id2) and activator protein-1 (AP-1) were important factors implicated in harmine-enhanced preosteoclast PDGF-BB production. Harmine 133-140 jun proto-oncogene Mus musculus 69-88 33960660-4 2021 In this study, we revealed that inhibitor of DNA binding-2 (Id2) and activator protein-1 (AP-1) were important factors implicated in harmine-enhanced preosteoclast PDGF-BB production. Harmine 133-140 jun proto-oncogene Mus musculus 90-94 33948561-8 2021 Inhibition of ABCB1 was mediated by vardenafil, and TWIST1 expression was reduced by either Harmine or shRNA. Harmine 92-99 twist basic helix-loop-helix transcription factor 1 Mus musculus 52-58 33960660-5 2021 Exposure of RANKL-induced Primary bone marrow macrophages (BMMs), isolated from tibiae and femora of mice, to harmine increased the protein levels of Id2 and AP-1. Harmine 110-117 tumor necrosis factor (ligand) superfamily, member 11 Mus musculus 12-17 33960660-5 2021 Exposure of RANKL-induced Primary bone marrow macrophages (BMMs), isolated from tibiae and femora of mice, to harmine increased the protein levels of Id2 and AP-1. Harmine 110-117 inhibitor of DNA binding 2 Mus musculus 150-153 33960660-5 2021 Exposure of RANKL-induced Primary bone marrow macrophages (BMMs), isolated from tibiae and femora of mice, to harmine increased the protein levels of Id2 and AP-1. Harmine 110-117 jun proto-oncogene Mus musculus 158-162 33960660-6 2021 Knockdown of Id2 by Id2-siRNA reduced the number of preosteoclasts as well as secretion of PDGF-BB in RANKL-stimulated BMMs administrated with harmine. Harmine 143-150 inhibitor of DNA binding 2 Mus musculus 13-16 33960660-6 2021 Knockdown of Id2 by Id2-siRNA reduced the number of preosteoclasts as well as secretion of PDGF-BB in RANKL-stimulated BMMs administrated with harmine. Harmine 143-150 inhibitor of DNA binding 2 Mus musculus 20-23 33960660-6 2021 Knockdown of Id2 by Id2-siRNA reduced the number of preosteoclasts as well as secretion of PDGF-BB in RANKL-stimulated BMMs administrated with harmine. Harmine 143-150 tumor necrosis factor (ligand) superfamily, member 11 Mus musculus 102-107 33960660-7 2021 Inhibition of c-Fos or c-Jun (components of AP-1) both reversed the stimulatory effect of harmine on preosteoclast PDGF-BB production. Harmine 90-97 FBJ osteosarcoma oncogene Mus musculus 14-19 33960660-7 2021 Inhibition of c-Fos or c-Jun (components of AP-1) both reversed the stimulatory effect of harmine on preosteoclast PDGF-BB production. Harmine 90-97 jun proto-oncogene Mus musculus 23-28 33960660-7 2021 Inhibition of c-Fos or c-Jun (components of AP-1) both reversed the stimulatory effect of harmine on preosteoclast PDGF-BB production. Harmine 90-97 jun proto-oncogene Mus musculus 44-48 33636211-7 2021 The objectives of the present study were to optimise non-radiolabelled harmine and deprenyl as selective tracers in MAO-A and MAO-B occupancy assays and evaluate MAO occupancy of test compounds in rat brain. Harmine 71-78 monoamine oxidase A Rattus norvegicus 116-121 33636211-11 2021 Pre-treatment with MAO inhibitors resulted in a decrease (maximum, 80-85%) in harmine or an increase (maximum, 85-300%) in L-deprenyl concentrations. Harmine 78-85 monoamine oxidase A Rattus norvegicus 19-22 33713497-7 2021 Similar results were obtained with topical application of harmine, a Harmala alkaloid that leads to degradation of Twist1. Harmine 58-65 twist basic helix-loop-helix transcription factor 1 Mus musculus 115-121 33474722-0 2021 Harmine alleviates atherogenesis by inhibiting disturbed flow-mediated endothelial activation via PTPN14/YAP. Harmine 0-7 protein tyrosine phosphatase, non-receptor type 14 Mus musculus 98-104 33474722-0 2021 Harmine alleviates atherogenesis by inhibiting disturbed flow-mediated endothelial activation via PTPN14/YAP. Harmine 0-7 yes-associated protein 1 Mus musculus 105-108 33474722-4 2021 EXPERIMENTAL APPROACH: Mice of ApoE-/- , LDLR-/- and endothelial cell (EC)-specific overexpression of Yes-associated protein (YAP) in ApoE-/- background were fed a western diet and given harmine for 4 weeks. Harmine 187-194 yes-associated protein 1 Mus musculus 102-124 33474722-4 2021 EXPERIMENTAL APPROACH: Mice of ApoE-/- , LDLR-/- and endothelial cell (EC)-specific overexpression of Yes-associated protein (YAP) in ApoE-/- background were fed a western diet and given harmine for 4 weeks. Harmine 187-194 yes-associated protein 1 Mus musculus 126-129 33474722-4 2021 EXPERIMENTAL APPROACH: Mice of ApoE-/- , LDLR-/- and endothelial cell (EC)-specific overexpression of Yes-associated protein (YAP) in ApoE-/- background were fed a western diet and given harmine for 4 weeks. Harmine 187-194 apolipoprotein E Mus musculus 134-138 33474722-7 2021 KEY RESULTS: Harmine retarded atherogenesis in both ApoE-/- and LDLR-/- mice by inhibiting the endothelial inflammatory response. Harmine 13-20 apolipoprotein E Mus musculus 52-56 33474722-7 2021 KEY RESULTS: Harmine retarded atherogenesis in both ApoE-/- and LDLR-/- mice by inhibiting the endothelial inflammatory response. Harmine 13-20 low density lipoprotein receptor Mus musculus 64-68 33474722-8 2021 Mechanistically, harmine blocked OSS-induced YAP nuclear translocation and EC activation by reducing phosphorylation of YAP at Y357. Harmine 17-24 yes-associated protein 1 Mus musculus 45-48 33474722-8 2021 Mechanistically, harmine blocked OSS-induced YAP nuclear translocation and EC activation by reducing phosphorylation of YAP at Y357. Harmine 17-24 yes-associated protein 1 Mus musculus 120-123 33474722-9 2021 Overexpression of endothelial YAP blunted the beneficial effects of harmine in mice. Harmine 68-75 yes-associated protein 1 Mus musculus 30-33 33474722-11 2021 Moreover, harmine increased PTPN14 expression by stabilizing its protein level and inhibiting its degradation in proteasome. Harmine 10-17 protein tyrosine phosphatase, non-receptor type 14 Mus musculus 28-34 33474722-12 2021 PTPN14 knockdown blocked the effects of harmine on YAPY357 and EC activation. Harmine 40-47 protein tyrosine phosphatase, non-receptor type 14 Mus musculus 0-6 33474722-13 2021 Finally, overexpression of PTPN14 mimicked the effects of harmine and ameliorated atherosclerosis, and knockdown of PTPN14 blunted the atheroprotective effects of harmine and accelerated atherosclerosis, in a partial ligation mouse model. Harmine 58-65 protein tyrosine phosphatase, non-receptor type 14 Mus musculus 27-33 33474722-13 2021 Finally, overexpression of PTPN14 mimicked the effects of harmine and ameliorated atherosclerosis, and knockdown of PTPN14 blunted the atheroprotective effects of harmine and accelerated atherosclerosis, in a partial ligation mouse model. Harmine 163-170 protein tyrosine phosphatase, non-receptor type 14 Mus musculus 116-122 33474722-14 2021 CONCLUSION AND IMPLICATIONS: Harmine alleviated OSS-induced EC activation via a PTPN14/YAPY357 pathway and had a potent athero-protective role. Harmine 29-36 protein tyrosine phosphatase, non-receptor type 14 Mus musculus 80-86 33508300-0 2021 Harmine inhibits the proliferation and migration of glioblastoma cells via the FAK/AKT pathway. Harmine 0-7 protein tyrosine kinase 2 Homo sapiens 79-82 33508300-0 2021 Harmine inhibits the proliferation and migration of glioblastoma cells via the FAK/AKT pathway. Harmine 0-7 AKT serine/threonine kinase 1 Homo sapiens 83-86 33508300-10 2021 Mechanistically, harmine reduced the basal and EGF-enhanced the phosphorylation level of FAK and AKT. Harmine 17-24 protein tyrosine kinase 2 Homo sapiens 89-92 33508300-10 2021 Mechanistically, harmine reduced the basal and EGF-enhanced the phosphorylation level of FAK and AKT. Harmine 17-24 AKT serine/threonine kinase 1 Homo sapiens 97-100 33508300-11 2021 Moreover, harmine inhibited the cell viability of U251-MG and U373-MG cells by downregulating the phosphorylation of the FAK/AKT pathway. Harmine 10-17 protein tyrosine kinase 2 Homo sapiens 121-124 33508300-11 2021 Moreover, harmine inhibited the cell viability of U251-MG and U373-MG cells by downregulating the phosphorylation of the FAK/AKT pathway. Harmine 10-17 AKT serine/threonine kinase 1 Homo sapiens 125-128 33508300-12 2021 Besides, harmine significantly suppressed the migration of U251-MG cells by suppressing the expression of MMP2, MMP9 and VEGF. Harmine 9-16 matrix metallopeptidase 2 Homo sapiens 106-110 33508300-12 2021 Besides, harmine significantly suppressed the migration of U251-MG cells by suppressing the expression of MMP2, MMP9 and VEGF. Harmine 9-16 matrix metallopeptidase 9 Homo sapiens 112-116 33508300-12 2021 Besides, harmine significantly suppressed the migration of U251-MG cells by suppressing the expression of MMP2, MMP9 and VEGF. Harmine 9-16 vascular endothelial growth factor A Homo sapiens 121-125 33508300-14 2021 SIGNIFICANCE: In conclusion, these results suggest that harmine suppresses the proliferation and migration of U251-MG and U373-MG cells by inhibiting the FAK/AKT signaling pathway. Harmine 56-63 protein tyrosine kinase 2 Homo sapiens 154-157 33508300-14 2021 SIGNIFICANCE: In conclusion, these results suggest that harmine suppresses the proliferation and migration of U251-MG and U373-MG cells by inhibiting the FAK/AKT signaling pathway. Harmine 56-63 AKT serine/threonine kinase 1 Homo sapiens 158-161 33785860-6 2022 We further showed that one of the potential underlying mechanism by which harmine alleviates cardiac hypertrophy relied on inhibition of NF-kappaB phosphorylation and the stimulated inflammatory cytokines in pathological ventricular remodeling. Harmine 74-81 nuclear factor kappa B subunit 1 Homo sapiens 137-146 33626096-0 2021 Harmine inhibits breast cancer cell migration and invasion by inducing the degradation of Twist1. Harmine 0-7 twist family bHLH transcription factor 1 Homo sapiens 90-96 33626096-4 2021 Harmine is a beta-carboline alkaloid found in a variety of plants and was recently shown to be able to induce degradation of Twist Family BHLH Transcription Factor 1 (Twist1) in non-small cell lung cancer cells (NSCLC). Harmine 0-7 twist family bHLH transcription factor 1 Homo sapiens 125-165 33626096-4 2021 Harmine is a beta-carboline alkaloid found in a variety of plants and was recently shown to be able to induce degradation of Twist Family BHLH Transcription Factor 1 (Twist1) in non-small cell lung cancer cells (NSCLC). Harmine 0-7 twist family bHLH transcription factor 1 Homo sapiens 167-173 32926882-3 2020 The primary goal of this study was to evaluate the abuse potential of the beta-carbolines harmane, norharmane, and harmine - MAO inhibitors that are found in cigarette smoke - in an intracranial self-simulation (ICSS) model in rats. Harmine 115-122 monoamine oxidase A Rattus norvegicus 125-128 33480316-0 2021 Structure-activity insights of harmine targeting DNA, ROS inducing cytotoxicity with PARP mediated apoptosis against cervical cancer, anti-biofilm formation and in vivo therapeutic study. Harmine 31-38 poly (ADP-ribose) polymerase family, member 1 Mus musculus 85-89 33480316-9 2021 Harmine exhibited G2M arrest with ROS induced effective role in PARP mediated apoptosis as well as anti-inflammatory action on HeLa cells. Harmine 0-7 collagen type XI alpha 2 chain Homo sapiens 64-68 33183209-10 2021 CONCLUSION: Harmine and Harmaline exhibit higher binding affinity towards D2- and D3- dopamine receptors compared to L-DOPA, and PKs and toxicity profile support their potential as drug candidates for PD therapy. Harmine 12-19 dopamine receptor D2 Homo sapiens 74-104 33339338-0 2020 How to Separate Kinase Inhibition from Undesired Monoamine Oxidase A Inhibition-The Development of the DYRK1A Inhibitor AnnH75 from the Alkaloid Harmine. Harmine 145-152 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 103-109 33339338-1 2020 The beta-carboline alkaloid harmine is a potent DYRK1A inhibitor, but suffers from undesired potent inhibition of MAO-A, which strongly limits its application. Harmine 28-35 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 48-54 33339338-1 2020 The beta-carboline alkaloid harmine is a potent DYRK1A inhibitor, but suffers from undesired potent inhibition of MAO-A, which strongly limits its application. Harmine 28-35 monoamine oxidase A Homo sapiens 114-119 33339338-2 2020 We synthesized more than 60 analogues of harmine, either by direct modification of the alkaloid or by de novo synthesis of beta-carboline and related scaffolds aimed at learning about structure-activity relationships for inhibition of both DYRK1A and MAO-A, with the ultimate goal of separating desired DYRK1A inhibition from undesired MAO-A inhibition. Harmine 41-48 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 240-246 33339338-2 2020 We synthesized more than 60 analogues of harmine, either by direct modification of the alkaloid or by de novo synthesis of beta-carboline and related scaffolds aimed at learning about structure-activity relationships for inhibition of both DYRK1A and MAO-A, with the ultimate goal of separating desired DYRK1A inhibition from undesired MAO-A inhibition. Harmine 41-48 monoamine oxidase A Homo sapiens 251-256 33339338-2 2020 We synthesized more than 60 analogues of harmine, either by direct modification of the alkaloid or by de novo synthesis of beta-carboline and related scaffolds aimed at learning about structure-activity relationships for inhibition of both DYRK1A and MAO-A, with the ultimate goal of separating desired DYRK1A inhibition from undesired MAO-A inhibition. Harmine 41-48 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 303-309 33339338-2 2020 We synthesized more than 60 analogues of harmine, either by direct modification of the alkaloid or by de novo synthesis of beta-carboline and related scaffolds aimed at learning about structure-activity relationships for inhibition of both DYRK1A and MAO-A, with the ultimate goal of separating desired DYRK1A inhibition from undesired MAO-A inhibition. Harmine 41-48 monoamine oxidase A Homo sapiens 336-341 33339338-3 2020 Based on evidence from published crystal structures of harmine bound to each of these enzymes, we performed systematic structure modifications of harmine yielding DYRK1A-selective inhibitors characterized by small polar substituents at N-9 (which preserve DYRK1A inhibition and eliminate MAO-A inhibition) and beneficial residues at C-1 (methyl or chlorine). Harmine 146-153 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 163-169 33316942-8 2020 Our results highlight the great potential of this approach for drug repurposing and suggest that harmine and piperlongumine or similar compounds might be useful in the clinic to overcome TRIB2-mediated therapy resistance in cancer patients. Harmine 97-104 tribbles pseudokinase 2 Homo sapiens 187-192 32462403-13 2020 Furthermore, the pharmacological modulation of this protein by different inhibitors (harmine, curcumine, LDN192960, and ID-8) has enabled to clarify DYRK2 functionality. Harmine 85-92 dual specificity tyrosine phosphorylation regulated kinase 2 Homo sapiens 149-154 32761352-0 2020 Human CYP2D6 in the Brain Is Protective Against Harmine-Induced Neurotoxicity: Evidence from Humanized CYP2D6 Transgenic Mice. Harmine 48-55 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 6-12 32761352-0 2020 Human CYP2D6 in the Brain Is Protective Against Harmine-Induced Neurotoxicity: Evidence from Humanized CYP2D6 Transgenic Mice. Harmine 48-55 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 103-109 32761352-3 2020 The beta-carboline harmine, which induces hypothermia and tremor, is metabolized by CYP2D6 to the non-hypothermic/non-tremorgenic harmol. Harmine 19-26 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 84-90 32761352-4 2020 Transgenic mice (TG), expressing human CYP2D6 in addition to their endogenous mouse CYP2D, experience less harmine-induced hypothermia and tremor compared with wild-type mice (WT). Harmine 107-114 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 39-45 32761352-4 2020 Transgenic mice (TG), expressing human CYP2D6 in addition to their endogenous mouse CYP2D, experience less harmine-induced hypothermia and tremor compared with wild-type mice (WT). Harmine 107-114 cytochrome P450, 2d region Mus musculus 39-44 32761352-5 2020 We first sought to elucidate the role of CYP2D in general within the brain in harmine-induced hypothermia and tremor severity. Harmine 78-85 cytochrome P450, 2d region Mus musculus 41-46 32761352-6 2020 A 4-h intracerebroventricular (ICV) pretreatment with the CYP2D inhibitor propranolol increased harmine-induced hypothermia and tremor in TG and increased harmine-induced hypothermia in WT. Harmine 96-103 cytochrome P450, 2d region Mus musculus 58-63 32761352-6 2020 A 4-h intracerebroventricular (ICV) pretreatment with the CYP2D inhibitor propranolol increased harmine-induced hypothermia and tremor in TG and increased harmine-induced hypothermia in WT. Harmine 155-162 cytochrome P450, 2d region Mus musculus 58-63 32761352-7 2020 We next sought to specifically demonstrate that human CYP2D6 expressed in TG brain altered harmine response severity. Harmine 91-98 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 54-60 32761352-8 2020 A 24-h ICV propranolol pretreatment, which selectively and irreversibly inhibits human CYP2D6 in TG brain, increased harmine-induced hypothermia. Harmine 117-124 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 87-93 32761352-10 2020 Human CYP2D6 activity in TG brain was sufficient in vivo to mitigate harmine-induced neurotoxicity. Harmine 69-76 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 6-12 32807492-13 2020 These spheroids also revealed sensitizing potential of DYRK1A inhibitors tested in this study, including Harmine, INDY and L41. Harmine 105-112 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 55-61 32380384-10 2020 Harmine, Clorgyline, Isatin, zonisamide and our title compound including are known with their competitive inhibitory activity on Human monoamine oxidase, commonly named MAO A and B. Harmine 0-7 monoamine oxidase A Homo sapiens 169-180 32425784-0 2020 Harmine Ameliorates Cognitive Impairment by Inhibiting NLRP3 Inflammasome Activation and Enhancing the BDNF/TrkB Signaling Pathway in STZ-Induced Diabetic Rats. Harmine 0-7 NLR family, pyrin domain containing 3 Rattus norvegicus 55-60 32088835-3 2020 The monoamine oxidase A inhibitor drug harmine was suggested to have both antidepressant and anti-inflammatory properties and may, therefore, be a potential candidate for treatment of depression. Harmine 39-46 monoamine oxidase A Rattus norvegicus 4-23 32425784-0 2020 Harmine Ameliorates Cognitive Impairment by Inhibiting NLRP3 Inflammasome Activation and Enhancing the BDNF/TrkB Signaling Pathway in STZ-Induced Diabetic Rats. Harmine 0-7 brain-derived neurotrophic factor Rattus norvegicus 103-107 32425784-0 2020 Harmine Ameliorates Cognitive Impairment by Inhibiting NLRP3 Inflammasome Activation and Enhancing the BDNF/TrkB Signaling Pathway in STZ-Induced Diabetic Rats. Harmine 0-7 neurotrophic receptor tyrosine kinase 2 Rattus norvegicus 108-112 32425784-7 2020 Further study showed that harmine inhibited NLRP3 inflammasome activation, as demonstrated by reduced NLRP3, ASC, cleaved caspase-1, IL-1beta, and IL-18 levels, in the cortex of harmine-treated rats with DM. Harmine 26-33 NLR family, pyrin domain containing 3 Rattus norvegicus 44-49 32425784-7 2020 Further study showed that harmine inhibited NLRP3 inflammasome activation, as demonstrated by reduced NLRP3, ASC, cleaved caspase-1, IL-1beta, and IL-18 levels, in the cortex of harmine-treated rats with DM. Harmine 26-33 NLR family, pyrin domain containing 3 Rattus norvegicus 102-107 32425784-7 2020 Further study showed that harmine inhibited NLRP3 inflammasome activation, as demonstrated by reduced NLRP3, ASC, cleaved caspase-1, IL-1beta, and IL-18 levels, in the cortex of harmine-treated rats with DM. Harmine 26-33 PYD and CARD domain containing Rattus norvegicus 109-112 32425784-7 2020 Further study showed that harmine inhibited NLRP3 inflammasome activation, as demonstrated by reduced NLRP3, ASC, cleaved caspase-1, IL-1beta, and IL-18 levels, in the cortex of harmine-treated rats with DM. Harmine 26-33 caspase 1 Rattus norvegicus 122-131 32425784-7 2020 Further study showed that harmine inhibited NLRP3 inflammasome activation, as demonstrated by reduced NLRP3, ASC, cleaved caspase-1, IL-1beta, and IL-18 levels, in the cortex of harmine-treated rats with DM. Harmine 26-33 interleukin 1 alpha Rattus norvegicus 133-141 32425784-7 2020 Further study showed that harmine inhibited NLRP3 inflammasome activation, as demonstrated by reduced NLRP3, ASC, cleaved caspase-1, IL-1beta, and IL-18 levels, in the cortex of harmine-treated rats with DM. Harmine 26-33 interleukin 18 Rattus norvegicus 147-152 32425784-7 2020 Further study showed that harmine inhibited NLRP3 inflammasome activation, as demonstrated by reduced NLRP3, ASC, cleaved caspase-1, IL-1beta, and IL-18 levels, in the cortex of harmine-treated rats with DM. Harmine 178-185 NLR family, pyrin domain containing 3 Rattus norvegicus 44-49 32425784-9 2020 Moreover, we found that harmine treatment enhanced BDNF and phosphorylated TrkB levels in both the cortex of STZ-induced diabetic rats and HG-treated cells. Harmine 24-31 brain-derived neurotrophic factor Rattus norvegicus 51-55 32425784-9 2020 Moreover, we found that harmine treatment enhanced BDNF and phosphorylated TrkB levels in both the cortex of STZ-induced diabetic rats and HG-treated cells. Harmine 24-31 neurotrophic receptor tyrosine kinase 2 Rattus norvegicus 75-79 32425784-10 2020 These data indicate that harmine mitigates cognitive impairment by inhibiting NLRP3 inflammasome activation and enhancing the BDNF/TrkB signaling pathway. Harmine 25-32 NLR family, pyrin domain containing 3 Rattus norvegicus 78-83 32425784-10 2020 These data indicate that harmine mitigates cognitive impairment by inhibiting NLRP3 inflammasome activation and enhancing the BDNF/TrkB signaling pathway. Harmine 25-32 brain-derived neurotrophic factor Rattus norvegicus 126-130 32425784-10 2020 These data indicate that harmine mitigates cognitive impairment by inhibiting NLRP3 inflammasome activation and enhancing the BDNF/TrkB signaling pathway. Harmine 25-32 neurotrophic receptor tyrosine kinase 2 Rattus norvegicus 131-135 32032735-8 2020 Treatment with another DYRK1A inhibitor, harmine, was capable of correcting neuronal CDKL5-dependent defects; moreover, DYRK1A levels were upregulated in primary Cdkl5-KO neurons in concomitance with increased phosphorylation of Tau, a well-accepted DYRK1A substrate. Harmine 41-48 dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1a Mus musculus 23-29 32032735-8 2020 Treatment with another DYRK1A inhibitor, harmine, was capable of correcting neuronal CDKL5-dependent defects; moreover, DYRK1A levels were upregulated in primary Cdkl5-KO neurons in concomitance with increased phosphorylation of Tau, a well-accepted DYRK1A substrate. Harmine 41-48 cyclin-dependent kinase-like 5 Mus musculus 85-90 32032735-8 2020 Treatment with another DYRK1A inhibitor, harmine, was capable of correcting neuronal CDKL5-dependent defects; moreover, DYRK1A levels were upregulated in primary Cdkl5-KO neurons in concomitance with increased phosphorylation of Tau, a well-accepted DYRK1A substrate. Harmine 41-48 dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1a Mus musculus 120-126 32032735-8 2020 Treatment with another DYRK1A inhibitor, harmine, was capable of correcting neuronal CDKL5-dependent defects; moreover, DYRK1A levels were upregulated in primary Cdkl5-KO neurons in concomitance with increased phosphorylation of Tau, a well-accepted DYRK1A substrate. Harmine 41-48 cyclin-dependent kinase-like 5 Mus musculus 162-167 32032735-8 2020 Treatment with another DYRK1A inhibitor, harmine, was capable of correcting neuronal CDKL5-dependent defects; moreover, DYRK1A levels were upregulated in primary Cdkl5-KO neurons in concomitance with increased phosphorylation of Tau, a well-accepted DYRK1A substrate. Harmine 41-48 dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1a Mus musculus 120-126 32340326-1 2020 Recently, we have shown that harmine induces beta-cell proliferation both in vitro and in vivo, mediated via the DYRK1A-NFAT pathway. Harmine 29-36 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 113-119 32340326-2 2020 We explore structure-activity relationships of the 7-position of harmine for both DYRK1A kinase inhibition and beta-cell proliferation based on our related previous structure-activity relationship studies of harmine in the context of diabetes and beta-cell specific targeting strategies. Harmine 65-72 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 82-88 32340326-5 2020 The DYRK1A inhibitor, compound 1-2b, induced beta-cell proliferation half that of harmine at three times higher concentration. Harmine 82-89 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 4-10 31821176-1 2020 Small molecule inhibitors of Dual Specificity, Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A), including harmine and others, are able to drive human beta cell regeneration. Harmine 112-119 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 29-91 32003560-0 2020 Synthesis and Biological Validation of a Harmine-based, Central Nervous System (CNS)-Avoidant, Selective, Human beta-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. Harmine 41-48 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 197-203 32003560-1 2020 Recently, our group identified that harmine is able to induce beta-cell proliferation both in vitro and in vivo, mediated via the DYRK1A-NFAT pathway. Harmine 36-43 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 130-136 32003560-2 2020 Since, harmine suffers from lack of selectivity, both against other kinases and CNS off-targets, therefore, we sought to expand structure-activity relationships for harmine"s DYRK1A activity, to enhance selectivity for off-targets, while retaining human beta-cell proliferation activity. Harmine 165-172 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 175-181 31901541-5 2020 The Notch, Wnt, Hedgehog and TGF-beta pathways mainly played vital roles in coping with harmine exposure in pupae stage, while the Hippo, Hedgehog and TGF-beta elements were involved in the sex differences. Harmine 88-95 Wnt oncogene analog 2 Drosophila melanogaster 11-14 31901541-5 2020 The Notch, Wnt, Hedgehog and TGF-beta pathways mainly played vital roles in coping with harmine exposure in pupae stage, while the Hippo, Hedgehog and TGF-beta elements were involved in the sex differences. Harmine 88-95 hedgehog Drosophila melanogaster 16-24 31901541-5 2020 The Notch, Wnt, Hedgehog and TGF-beta pathways mainly played vital roles in coping with harmine exposure in pupae stage, while the Hippo, Hedgehog and TGF-beta elements were involved in the sex differences. Harmine 88-95 decapentaplegic Drosophila melanogaster 29-37 31901541-6 2020 Notch, Hippo, Hedgehog, Dpp and Armadillo were proved to be suppressed in the developmental inhibition with fly mutants, while Numb and Punt were increased by harmine. Harmine 159-166 numb Drosophila melanogaster 127-131 30909826-1 2020 The work highlighted interaction of harmalol, harmaline and harmine with human serum albumin by biophysical and biochemical assays. Harmine 60-67 albumin Homo sapiens 79-92 31821176-1 2020 Small molecule inhibitors of Dual Specificity, Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A), including harmine and others, are able to drive human beta cell regeneration. Harmine 112-119 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 93-99 31821176-6 2020 Importantly, other potential kinases, such as the CLK and the GSK3 families, are excluded as important harmine targets. Harmine 103-110 CDC like kinase 1 Homo sapiens 50-53 31776330-8 2019 Finally, direct inhibition of TWIST1 by a small-molecule compound harmine was paralleled by blockade of EndMT in cultured cells and liver fibrosis in mice. Harmine 66-73 twist basic helix-loop-helix transcription factor 1 Mus musculus 30-36 30910851-0 2019 Harmine suppresses bladder tumor growth by suppressing vascular endothelial growth factor receptor 2-mediated angiogenesis. Harmine 0-7 kinase insert domain receptor Homo sapiens 55-100 31572127-10 2019 Knockdown of DYRK1A expression or treatment of the DYRK1A inhibitor harmine attenuated miR-204-5p-induced increase in protein expression of phospho-alpha-Syn or phospho-tau, ER stress, autophagy impairment, and activation of JNK-mediated apoptotic pathway in SH-SY5Y dopaminergic cells or primary cultured dopaminergic neurons. Harmine 68-75 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 51-57 31572127-10 2019 Knockdown of DYRK1A expression or treatment of the DYRK1A inhibitor harmine attenuated miR-204-5p-induced increase in protein expression of phospho-alpha-Syn or phospho-tau, ER stress, autophagy impairment, and activation of JNK-mediated apoptotic pathway in SH-SY5Y dopaminergic cells or primary cultured dopaminergic neurons. Harmine 68-75 membrane associated ring-CH-type finger 8 Homo sapiens 87-90 31572127-10 2019 Knockdown of DYRK1A expression or treatment of the DYRK1A inhibitor harmine attenuated miR-204-5p-induced increase in protein expression of phospho-alpha-Syn or phospho-tau, ER stress, autophagy impairment, and activation of JNK-mediated apoptotic pathway in SH-SY5Y dopaminergic cells or primary cultured dopaminergic neurons. Harmine 68-75 synuclein alpha Homo sapiens 148-157 31572127-10 2019 Knockdown of DYRK1A expression or treatment of the DYRK1A inhibitor harmine attenuated miR-204-5p-induced increase in protein expression of phospho-alpha-Syn or phospho-tau, ER stress, autophagy impairment, and activation of JNK-mediated apoptotic pathway in SH-SY5Y dopaminergic cells or primary cultured dopaminergic neurons. Harmine 68-75 mitogen-activated protein kinase 8 Homo sapiens 225-228 31198408-7 2019 Results: The natural compound harmine, isolated from the plant Peganum harmala, was found to suppress the Muv phenotype of let-60(n1046gf). Harmine 30-37 Ras protein let-60 Caenorhabditis elegans 123-129 31198408-8 2019 In addition, harmine targets the hyper-activation of the Ras/MAPK pathway specifically caused by overexpression or mutated forms of LET-60/Ras and its immediate downstream molecule LIN-45/Raf. Harmine 13-20 Ras protein let-60 Caenorhabditis elegans 132-138 31198408-8 2019 In addition, harmine targets the hyper-activation of the Ras/MAPK pathway specifically caused by overexpression or mutated forms of LET-60/Ras and its immediate downstream molecule LIN-45/Raf. Harmine 13-20 Raf homolog serine/threonine-protein kinase Caenorhabditis elegans 181-187 31454149-3 2019 Meanwhile, the DYRK1A inhibitor harmine could suppress the proliferation of NSCLC cells compared to that of the control. Harmine 32-39 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 15-21 31454149-7 2019 Meanwhile, harmine could also regulate the STAT3/EGFR/Met signalling pathway in human NSCLC cells. Harmine 11-18 signal transducer and activator of transcription 3 Homo sapiens 43-48 31454149-7 2019 Meanwhile, harmine could also regulate the STAT3/EGFR/Met signalling pathway in human NSCLC cells. Harmine 11-18 epidermal growth factor receptor Homo sapiens 49-53 31454149-10 2019 In addition, harmine could enhance the anti-NSCLC activity of AZD9291 by modulating STAT3 pathway. Harmine 13-20 signal transducer and activator of transcription 3 Homo sapiens 84-89 31154274-1 2019 BACKGROUND: beta-Carboline alkaloid harmine (HAR) and harmaline (HAL) are monoamine oxidase (MAO) and acetylcholinesterase (AChE) inhibitors. Harmine 36-43 acetylcholinesterase Rattus norvegicus 102-122 31154274-1 2019 BACKGROUND: beta-Carboline alkaloid harmine (HAR) and harmaline (HAL) are monoamine oxidase (MAO) and acetylcholinesterase (AChE) inhibitors. Harmine 36-43 acetylcholinesterase Rattus norvegicus 124-128 31154274-1 2019 BACKGROUND: beta-Carboline alkaloid harmine (HAR) and harmaline (HAL) are monoamine oxidase (MAO) and acetylcholinesterase (AChE) inhibitors. Harmine 45-48 acetylcholinesterase Rattus norvegicus 102-122 31154274-1 2019 BACKGROUND: beta-Carboline alkaloid harmine (HAR) and harmaline (HAL) are monoamine oxidase (MAO) and acetylcholinesterase (AChE) inhibitors. Harmine 45-48 acetylcholinesterase Rattus norvegicus 124-128 31048127-0 2019 Natural alkaloid harmine promotes degradation of alpha-synuclein via PKA-mediated ubiquitin-proteasome system activation. Harmine 17-24 synuclein alpha Homo sapiens 49-64 31048127-14 2019 PKA inhibitor blocked the effects of harmine in activating UPS, up regulating PSMD1 and promoting <alpha>-syn degradation, indicating that harmine enhances UPS function via PKA activation. Harmine 37-44 proteasome 26S subunit, non-ATPase 1 Homo sapiens 78-83 31354292-7 2019 The AKT/mTOR pathway is involved in mechanisms of gemcitabine resistance in pancreatic cancer cells, our data demonstrated that harmine plus gemcitabine significantly suppressed the AKT/mTOR signaling pathway. Harmine 128-135 AKT serine/threonine kinase 1 Homo sapiens 4-7 31354292-7 2019 The AKT/mTOR pathway is involved in mechanisms of gemcitabine resistance in pancreatic cancer cells, our data demonstrated that harmine plus gemcitabine significantly suppressed the AKT/mTOR signaling pathway. Harmine 128-135 mechanistic target of rapamycin kinase Homo sapiens 8-12 31354292-7 2019 The AKT/mTOR pathway is involved in mechanisms of gemcitabine resistance in pancreatic cancer cells, our data demonstrated that harmine plus gemcitabine significantly suppressed the AKT/mTOR signaling pathway. Harmine 128-135 AKT serine/threonine kinase 1 Homo sapiens 182-185 31354292-7 2019 The AKT/mTOR pathway is involved in mechanisms of gemcitabine resistance in pancreatic cancer cells, our data demonstrated that harmine plus gemcitabine significantly suppressed the AKT/mTOR signaling pathway. Harmine 128-135 mechanistic target of rapamycin kinase Homo sapiens 186-190 30910851-6 2019 To further explore the pharmacological activities of harmine, we tested harmine"s influence on blood vessel formation and found that harmine effectively blocked the microvessel sprouting in rat aortic ring assay when stimulated by vascular endothelial growth factor (VEGF). Harmine 53-60 vascular endothelial growth factor A Rattus norvegicus 231-265 30910851-6 2019 To further explore the pharmacological activities of harmine, we tested harmine"s influence on blood vessel formation and found that harmine effectively blocked the microvessel sprouting in rat aortic ring assay when stimulated by vascular endothelial growth factor (VEGF). Harmine 72-79 vascular endothelial growth factor A Rattus norvegicus 231-265 30910851-6 2019 To further explore the pharmacological activities of harmine, we tested harmine"s influence on blood vessel formation and found that harmine effectively blocked the microvessel sprouting in rat aortic ring assay when stimulated by vascular endothelial growth factor (VEGF). Harmine 72-79 vascular endothelial growth factor A Rattus norvegicus 231-265 30910851-8 2019 Moreover, harmine induced bladder cancer cell apoptosis through triggering the caspase-dependent apoptotic pathway and the downstream vascular endothelial growth factor receptor 2 (VEGFR2) kinase pathway was down-regulated, thus suppressing tumor development signals. Harmine 10-17 kinase insert domain receptor Homo sapiens 134-179 30910851-8 2019 Moreover, harmine induced bladder cancer cell apoptosis through triggering the caspase-dependent apoptotic pathway and the downstream vascular endothelial growth factor receptor 2 (VEGFR2) kinase pathway was down-regulated, thus suppressing tumor development signals. Harmine 10-17 kinase insert domain receptor Homo sapiens 181-187 30910851-9 2019 Herein, our study demonstrated that natural product harmine might have potential in curing human bladder tumor because of its pharmacological function on tumor angiogenesis, trigged by VEGFR2 signaling pathways. Harmine 52-59 kinase insert domain receptor Homo sapiens 185-191 30716318-0 2019 Harmine mitigates LPS-induced acute kidney injury through inhibition of the TLR4-NF-kappaB/NLRP3 inflammasome signalling pathway in mice. Harmine 0-7 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 81-90 30716318-0 2019 Harmine mitigates LPS-induced acute kidney injury through inhibition of the TLR4-NF-kappaB/NLRP3 inflammasome signalling pathway in mice. Harmine 0-7 NLR family, pyrin domain containing 3 Mus musculus 91-96 30716318-0 2019 Harmine mitigates LPS-induced acute kidney injury through inhibition of the TLR4-NF-kappaB/NLRP3 inflammasome signalling pathway in mice. Harmine 0-7 toll-like receptor 4 Mus musculus 76-80 30716318-7 2019 The results showed that pretreatment with harmine (25 or 50 mg/kg) markedly alleviated kidney injury by reducing the release of kidney biomarkers and inflammatory mediators and the formation of malondialdehyde (MDA) and myeloperoxidase (MPO) while increasing superoxide dismutase (SOD) and glutathione (GSH) activities and improving renal histopathological changes. Harmine 42-49 myeloperoxidase Mus musculus 220-235 30716318-7 2019 The results showed that pretreatment with harmine (25 or 50 mg/kg) markedly alleviated kidney injury by reducing the release of kidney biomarkers and inflammatory mediators and the formation of malondialdehyde (MDA) and myeloperoxidase (MPO) while increasing superoxide dismutase (SOD) and glutathione (GSH) activities and improving renal histopathological changes. Harmine 42-49 myeloperoxidase Mus musculus 237-240 30716318-8 2019 In addition, immunohistochemistry staining and western blot analysis indicated that harmine treatment suppressed the expression of toll-like receptor 4 (TLR4) and the phosphorylation of nuclear factor-kappa B (NF-kappaB) p65 and inhibitor of kappaBalpha (IkappaBalpha) while inhibiting the expression of NLRP3, caspase-1 and interleukin-1beta (IL-1beta). Harmine 84-91 toll-like receptor 4 Mus musculus 131-151 30716318-8 2019 In addition, immunohistochemistry staining and western blot analysis indicated that harmine treatment suppressed the expression of toll-like receptor 4 (TLR4) and the phosphorylation of nuclear factor-kappa B (NF-kappaB) p65 and inhibitor of kappaBalpha (IkappaBalpha) while inhibiting the expression of NLRP3, caspase-1 and interleukin-1beta (IL-1beta). Harmine 84-91 toll-like receptor 4 Mus musculus 153-157 30716318-8 2019 In addition, immunohistochemistry staining and western blot analysis indicated that harmine treatment suppressed the expression of toll-like receptor 4 (TLR4) and the phosphorylation of nuclear factor-kappa B (NF-kappaB) p65 and inhibitor of kappaBalpha (IkappaBalpha) while inhibiting the expression of NLRP3, caspase-1 and interleukin-1beta (IL-1beta). Harmine 84-91 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 186-208 30716318-8 2019 In addition, immunohistochemistry staining and western blot analysis indicated that harmine treatment suppressed the expression of toll-like receptor 4 (TLR4) and the phosphorylation of nuclear factor-kappa B (NF-kappaB) p65 and inhibitor of kappaBalpha (IkappaBalpha) while inhibiting the expression of NLRP3, caspase-1 and interleukin-1beta (IL-1beta). Harmine 84-91 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 210-219 30716318-8 2019 In addition, immunohistochemistry staining and western blot analysis indicated that harmine treatment suppressed the expression of toll-like receptor 4 (TLR4) and the phosphorylation of nuclear factor-kappa B (NF-kappaB) p65 and inhibitor of kappaBalpha (IkappaBalpha) while inhibiting the expression of NLRP3, caspase-1 and interleukin-1beta (IL-1beta). Harmine 84-91 v-rel reticuloendotheliosis viral oncogene homolog A (avian) Mus musculus 221-224 30716318-8 2019 In addition, immunohistochemistry staining and western blot analysis indicated that harmine treatment suppressed the expression of toll-like receptor 4 (TLR4) and the phosphorylation of nuclear factor-kappa B (NF-kappaB) p65 and inhibitor of kappaBalpha (IkappaBalpha) while inhibiting the expression of NLRP3, caspase-1 and interleukin-1beta (IL-1beta). Harmine 84-91 nuclear factor of kappa light polypeptide gene enhancer in B cells inhibitor, alpha Mus musculus 255-267 30716318-8 2019 In addition, immunohistochemistry staining and western blot analysis indicated that harmine treatment suppressed the expression of toll-like receptor 4 (TLR4) and the phosphorylation of nuclear factor-kappa B (NF-kappaB) p65 and inhibitor of kappaBalpha (IkappaBalpha) while inhibiting the expression of NLRP3, caspase-1 and interleukin-1beta (IL-1beta). Harmine 84-91 NLR family, pyrin domain containing 3 Mus musculus 304-309 30716318-8 2019 In addition, immunohistochemistry staining and western blot analysis indicated that harmine treatment suppressed the expression of toll-like receptor 4 (TLR4) and the phosphorylation of nuclear factor-kappa B (NF-kappaB) p65 and inhibitor of kappaBalpha (IkappaBalpha) while inhibiting the expression of NLRP3, caspase-1 and interleukin-1beta (IL-1beta). Harmine 84-91 caspase 1 Mus musculus 311-320 30716318-8 2019 In addition, immunohistochemistry staining and western blot analysis indicated that harmine treatment suppressed the expression of toll-like receptor 4 (TLR4) and the phosphorylation of nuclear factor-kappa B (NF-kappaB) p65 and inhibitor of kappaBalpha (IkappaBalpha) while inhibiting the expression of NLRP3, caspase-1 and interleukin-1beta (IL-1beta). Harmine 84-91 interleukin 1 beta Mus musculus 325-342 30716318-8 2019 In addition, immunohistochemistry staining and western blot analysis indicated that harmine treatment suppressed the expression of toll-like receptor 4 (TLR4) and the phosphorylation of nuclear factor-kappa B (NF-kappaB) p65 and inhibitor of kappaBalpha (IkappaBalpha) while inhibiting the expression of NLRP3, caspase-1 and interleukin-1beta (IL-1beta). Harmine 84-91 interleukin 1 beta Mus musculus 344-352 30716318-10 2019 The involved underlying mechanisms of harmine in LPS-induced acute kidney injury might be related to inhibition of the TLR4-NF-kappaB pathway and NLRP3 inflammasome pathway. Harmine 38-45 toll-like receptor 4 Mus musculus 119-123 30716318-10 2019 The involved underlying mechanisms of harmine in LPS-induced acute kidney injury might be related to inhibition of the TLR4-NF-kappaB pathway and NLRP3 inflammasome pathway. Harmine 38-45 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 124-133 30716318-10 2019 The involved underlying mechanisms of harmine in LPS-induced acute kidney injury might be related to inhibition of the TLR4-NF-kappaB pathway and NLRP3 inflammasome pathway. Harmine 38-45 NLR family, pyrin domain containing 3 Mus musculus 146-151 29802995-7 2018 We also examined the effect of severe environmental stress including heat shock, osmotic shock, and exposure to the alkaloid drug harmine on CLK1 alternative splicing in DU145 prostate cancer cells. Harmine 130-137 CDC like kinase 1 Homo sapiens 141-145 30171258-8 2019 We demonstrated that genetic silencing of TWIST1 or treatment with the TWIST1 inhibitor, harmine, resulted in growth inhibition and apoptosis in EGFR-mutant NSCLC. Harmine 89-96 twist family bHLH transcription factor 1 Homo sapiens 71-77 30171258-8 2019 We demonstrated that genetic silencing of TWIST1 or treatment with the TWIST1 inhibitor, harmine, resulted in growth inhibition and apoptosis in EGFR-mutant NSCLC. Harmine 89-96 epidermal growth factor receptor Homo sapiens 145-149 29788780-4 2018 Conclusion & future perspective: The current study delineates the structural requirements for MAO-A selectivity and such information may be helpful in designing selective analogs for kinase, DYRK1A and harmine-based cytotoxics without apparent MAO enzyme inhibition. Harmine 206-213 monoamine oxidase A Homo sapiens 98-103 29423903-0 2018 [11C]Harmine Binding to Brain Monoamine Oxidase A: Test-Retest Properties and Noninvasive Quantification. Harmine 5-12 monoamine oxidase A Homo sapiens 30-49 29977157-0 2018 Harmine, a dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor induces caspase-mediated apoptosis in neuroblastoma. Harmine 0-7 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 11-69 29977157-0 2018 Harmine, a dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor induces caspase-mediated apoptosis in neuroblastoma. Harmine 0-7 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 71-75 29977157-3 2018 Harmine is capable of blocking the activities of dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) family proteins and mitogen-activated protein kinase. Harmine 0-7 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 49-107 29977157-3 2018 Harmine is capable of blocking the activities of dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) family proteins and mitogen-activated protein kinase. Harmine 0-7 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 109-113 29977157-6 2018 The anti-cancer properties of harmine were examined by RealTime-Glo MT cell viability assays, caspase activity assays, PARP cleavage using Western blot analysis, and flow cytometry-based Annexin V detection. Harmine 30-37 caspase 9 Homo sapiens 94-101 29977157-6 2018 The anti-cancer properties of harmine were examined by RealTime-Glo MT cell viability assays, caspase activity assays, PARP cleavage using Western blot analysis, and flow cytometry-based Annexin V detection. Harmine 30-37 collagen type XI alpha 2 chain Homo sapiens 119-123 29977157-6 2018 The anti-cancer properties of harmine were examined by RealTime-Glo MT cell viability assays, caspase activity assays, PARP cleavage using Western blot analysis, and flow cytometry-based Annexin V detection. Harmine 30-37 annexin A5 Homo sapiens 187-196 29977157-7 2018 A molecular interaction model of harmine bound to the DYRK2 family kinase was generated by computational docking using X-ray structures. Harmine 33-40 dual specificity tyrosine phosphorylation regulated kinase 2 Homo sapiens 54-59 29977157-10 2018 Exposure of these NB cell lines to 100 muM of harmine resulted in caspase-3/7 and caspase-9 activation as well as caspase-mediated PARP cleavage and Annexin V-positive stained cells, as early as 24 h after treatment, clearly suggesting apoptosis induction, especially in MYCN-amplified cell lines. Harmine 46-53 caspase 9 Homo sapiens 82-91 29977157-10 2018 Exposure of these NB cell lines to 100 muM of harmine resulted in caspase-3/7 and caspase-9 activation as well as caspase-mediated PARP cleavage and Annexin V-positive stained cells, as early as 24 h after treatment, clearly suggesting apoptosis induction, especially in MYCN-amplified cell lines. Harmine 46-53 caspase 9 Homo sapiens 66-73 29977157-10 2018 Exposure of these NB cell lines to 100 muM of harmine resulted in caspase-3/7 and caspase-9 activation as well as caspase-mediated PARP cleavage and Annexin V-positive stained cells, as early as 24 h after treatment, clearly suggesting apoptosis induction, especially in MYCN-amplified cell lines. Harmine 46-53 MYCN proto-oncogene, bHLH transcription factor Homo sapiens 271-275 29977157-12 2018 Conclusion: Harmine is a known inhibitor of DYRK family kinases. Harmine 12-19 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 44-48 29977157-14 2018 The patient results support our hypothesis that DYRK inhibition by harmine and the subsequent triggering of caspase-mediated apoptosis might present a novel approach to NB therapy. Harmine 67-74 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 48-52 29428472-0 2018 A novel harmine derivative, N-(4-(hydroxycarbamoyl)benzyl)-1-(4- methoxyphenyl)-9H-pyrido[3,4-b]indole-3-carboxamide (HBC), as histone deacetylase inhibitor: in vitro antiproliferation, apoptosis induction, cell cycle arrest, and antimetastatic effects. Harmine 8-15 histone deacetylase 9 Homo sapiens 127-146 29634919-4 2018 In the present study, we determined the crystal structure of the mature form of human DYRK3 in complex with harmine, an ATP competitive inhibitor. Harmine 108-115 dual specificity tyrosine phosphorylation regulated kinase 3 Homo sapiens 86-91 29755345-0 2018 Analogous beta-Carboline Alkaloids Harmaline and Harmine Ameliorate Scopolamine-Induced Cognition Dysfunction by Attenuating Acetylcholinesterase Activity, Oxidative Stress, and Inflammation in Mice. Harmine 49-56 acetylcholinesterase Mus musculus 125-145 29755345-1 2018 The analogous beta-carboline alkaloids, harmaline (HAL) and harmine (HAR), possess a variety of biological properties, including acetylcholinesterase (AChE) inhibitory activity, antioxidant, anti-inflammatory, and many others, and have great potential for treating Alzheimer"s disease (AD). Harmine 60-67 acetylcholinesterase Mus musculus 129-149 29755345-1 2018 The analogous beta-carboline alkaloids, harmaline (HAL) and harmine (HAR), possess a variety of biological properties, including acetylcholinesterase (AChE) inhibitory activity, antioxidant, anti-inflammatory, and many others, and have great potential for treating Alzheimer"s disease (AD). Harmine 60-67 acetylcholinesterase Mus musculus 151-155 29755345-1 2018 The analogous beta-carboline alkaloids, harmaline (HAL) and harmine (HAR), possess a variety of biological properties, including acetylcholinesterase (AChE) inhibitory activity, antioxidant, anti-inflammatory, and many others, and have great potential for treating Alzheimer"s disease (AD). Harmine 69-72 acetylcholinesterase Mus musculus 129-149 29755345-1 2018 The analogous beta-carboline alkaloids, harmaline (HAL) and harmine (HAR), possess a variety of biological properties, including acetylcholinesterase (AChE) inhibitory activity, antioxidant, anti-inflammatory, and many others, and have great potential for treating Alzheimer"s disease (AD). Harmine 69-72 acetylcholinesterase Mus musculus 151-155 29428472-1 2018 This study aims to design and synthesize a novel harmine derivative N-(4-(hydroxycarbamoyl) benzyl)-1-(4-methoxyphenyl)-9H-pyrido [3,4-b]indole-3-carboxamide (HBC) as histone deacetylase (HDAC) inhibitor, and evaluate its antitumor activities and anti-metastasis mechanism. Harmine 49-56 histone deacetylase 9 Homo sapiens 167-186 29428472-1 2018 This study aims to design and synthesize a novel harmine derivative N-(4-(hydroxycarbamoyl) benzyl)-1-(4-methoxyphenyl)-9H-pyrido [3,4-b]indole-3-carboxamide (HBC) as histone deacetylase (HDAC) inhibitor, and evaluate its antitumor activities and anti-metastasis mechanism. Harmine 49-56 histone deacetylase 9 Homo sapiens 188-192 29428472-7 2018 These results demonstrate that novel harmine-based HDAC inhibitor HBC not only exhibited selective HDAC1/6 inhibitory activity and significant in vitro and in vivo antitumor activity, but also possessed DNA binding effect, apoptosis induction, cell cycle arrest effects, and potent anti-metastasis mechanisms, which may hold great promise as therapeutic agent targeting HDAC1/6 for the intervention of human cancers. Harmine 37-44 histone deacetylase 9 Homo sapiens 51-55 29428472-7 2018 These results demonstrate that novel harmine-based HDAC inhibitor HBC not only exhibited selective HDAC1/6 inhibitory activity and significant in vitro and in vivo antitumor activity, but also possessed DNA binding effect, apoptosis induction, cell cycle arrest effects, and potent anti-metastasis mechanisms, which may hold great promise as therapeutic agent targeting HDAC1/6 for the intervention of human cancers. Harmine 37-44 histone deacetylase 1 Homo sapiens 99-104 29428472-7 2018 These results demonstrate that novel harmine-based HDAC inhibitor HBC not only exhibited selective HDAC1/6 inhibitory activity and significant in vitro and in vivo antitumor activity, but also possessed DNA binding effect, apoptosis induction, cell cycle arrest effects, and potent anti-metastasis mechanisms, which may hold great promise as therapeutic agent targeting HDAC1/6 for the intervention of human cancers. Harmine 37-44 histone deacetylase 1 Homo sapiens 99-106 29721090-4 2018 METHODS: The impact of harmine on osteoclastogenesis of RANKL-stimulated RAW264.7 cells was verified by gene expression analysis and tartrate-resistant acid phosphatase (TRAP) staining. Harmine 23-30 tumor necrosis factor (ligand) superfamily, member 11 Mus musculus 56-61 29721090-11 2018 RESULTS: Exposure of RANKL-stimulated RAW264.7 cells to harmine enhanced the formation of preosteoclasts and the production of PDGF-BB. Harmine 56-63 tumor necrosis factor (ligand) superfamily, member 11 Mus musculus 21-26 29721090-12 2018 Harmine augmented the ability of RANKL-stimulated RAW264.7 cells to promote angiogenesis of endothelial cells, whereas the effect was blocked by PDGF-BB inhibition. Harmine 0-7 tumor necrosis factor (ligand) superfamily, member 11 Mus musculus 33-38 29253570-0 2018 Harmine promotes molar root development via SMAD1/5/8 phosphorylation. Harmine 0-7 SMAD family member 1 Homo sapiens 44-51 29179659-7 2018 This phenotype was confirmed with chemical inhibition of DYRK1A using harmine and with primary HPCs cultured as liver organoids. Harmine 70-77 dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1a Mus musculus 57-63 29223449-9 2018 The active compound was isolated by bio-guided purification using thin layer chromatography (TLC) and identified by GC-MS and HPLC-DAD-ESI-MSn as harmine. Harmine 146-153 moesin Homo sapiens 139-142 29510387-11 2018 Mechanistically, in Harmine-treated NSCLC cells, RECK expression and its downstream signaling cascade were dramatically activated. Harmine 20-27 reversion-inducing-cysteine-rich protein with kazal motifs Mus musculus 49-53 29510387-13 2018 CONCLUSION: These findings identify Harmine as a promising activator of RECK signaling for metastatic NSCLC treatment. Harmine 36-43 reversion-inducing-cysteine-rich protein with kazal motifs Mus musculus 72-76 28851812-3 2017 Characterization of the top ranked candidates from the unbiased screen revealed that harmine, a harmala alkaloid, inhibited multiple TWIST1 functions, including single-cell dissemination, suppression of normal branching in 3D epithelial culture, and proliferation of oncogene driver-defined NSCLC cells. Harmine 85-92 twist family bHLH transcription factor 1 Homo sapiens 133-139 29075061-0 2017 Harmine, a Novel DNA Methyltransferase 1 Inhibitor in the Leukemia Cell Line. Harmine 0-7 DNA methyltransferase 1 Homo sapiens 17-40 29075061-4 2017 This study aimed to evaluate the effect of Harmine on DNMT1 (DNA methyl transferase 1) expression in a leukemic cell line. Harmine 43-50 DNA methyltransferase 1 Homo sapiens 54-59 29075061-4 2017 This study aimed to evaluate the effect of Harmine on DNMT1 (DNA methyl transferase 1) expression in a leukemic cell line. Harmine 43-50 DNA methyltransferase 1 Homo sapiens 61-85 29075061-9 2017 Anti proliferative doses of Harmine, has suppressed DNMT1 gene in NB4 cell line. Harmine 28-35 DNA methyltransferase 1 Homo sapiens 52-57 28851812-4 2017 Harmine treatment phenocopied genetic loss of TWIST1 by inducing oncogene-induced senescence or apoptosis. Harmine 0-7 twist family bHLH transcription factor 1 Homo sapiens 46-52 28851812-6 2017 As dimerization is critical for TWIST1 function and stability, the effect of harmine on specific TWIST1 dimers was examined. Harmine 77-84 twist family bHLH transcription factor 1 Homo sapiens 97-103 28851812-8 2017 Harmine preferentially promoted degradation of the TWIST1-E2A heterodimer compared with the TWIST-TWIST1 homodimer, and targeting the TWIST1-E2A heterodimer was required for harmine cytotoxicity. Harmine 0-7 twist family bHLH transcription factor 1 Homo sapiens 51-57 28851812-9 2017 Finally, harmine had activity in both transgenic and patient-derived xenograft mouse models of KRAS-mutant NSCLC. Harmine 9-16 Kirsten rat sarcoma viral oncogene homolog Mus musculus 95-99 28851812-10 2017 These studies identified harmine as a first-in-class TWIST1 inhibitor with marked anti-tumor activity in oncogene-driven NSCLC including EGFR mutant, KRAS mutant and MET altered NSCLC.Implications: TWIST1 is required for oncogene-driven NSCLC tumorigenesis and EMT; thus, harmine and its analogues/derivatives represent a novel therapeutic strategy to treat oncogene-driven NSCLC as well as other solid tumor malignancies. Harmine 25-32 twist family bHLH transcription factor 1 Homo sapiens 53-59 28851812-10 2017 These studies identified harmine as a first-in-class TWIST1 inhibitor with marked anti-tumor activity in oncogene-driven NSCLC including EGFR mutant, KRAS mutant and MET altered NSCLC.Implications: TWIST1 is required for oncogene-driven NSCLC tumorigenesis and EMT; thus, harmine and its analogues/derivatives represent a novel therapeutic strategy to treat oncogene-driven NSCLC as well as other solid tumor malignancies. Harmine 25-32 epidermal growth factor receptor Homo sapiens 137-141 28851812-10 2017 These studies identified harmine as a first-in-class TWIST1 inhibitor with marked anti-tumor activity in oncogene-driven NSCLC including EGFR mutant, KRAS mutant and MET altered NSCLC.Implications: TWIST1 is required for oncogene-driven NSCLC tumorigenesis and EMT; thus, harmine and its analogues/derivatives represent a novel therapeutic strategy to treat oncogene-driven NSCLC as well as other solid tumor malignancies. Harmine 25-32 KRAS proto-oncogene, GTPase Homo sapiens 150-154 28851812-10 2017 These studies identified harmine as a first-in-class TWIST1 inhibitor with marked anti-tumor activity in oncogene-driven NSCLC including EGFR mutant, KRAS mutant and MET altered NSCLC.Implications: TWIST1 is required for oncogene-driven NSCLC tumorigenesis and EMT; thus, harmine and its analogues/derivatives represent a novel therapeutic strategy to treat oncogene-driven NSCLC as well as other solid tumor malignancies. Harmine 25-32 twist family bHLH transcription factor 1 Homo sapiens 198-204 28031411-8 2017 Inhibition of Dyrk1A activity using pharmacologic agents Harmine and INDY compromises viability of spheroids and blocks DREAM assembly. Harmine 57-64 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 14-20 28871225-7 2017 However, when given MK571 and probenecid (the typical MRP2 inhibitor), the PappAB of harmine was increased (1.62- and 1.27-folds), and the efflux ratio was decreased from 1.59 to 0.98 and from 1.59 to 1.19, respectively. Harmine 85-92 ATP binding cassette subfamily C member 2 Homo sapiens 54-58 28871225-8 2017 In addition, the uptake ratio of harmine at 1 muM was >2.65 in the membrane vesicles expressing human MRP2. Harmine 33-40 ATP binding cassette subfamily C member 2 Homo sapiens 105-109 28871225-9 2017 Furthermore, harmine could slightly up-regulate the expression of MRP2, which implying harmine might be the substrate of MRP2. Harmine 13-20 ATP binding cassette subfamily C member 2 Homo sapiens 66-70 28871225-9 2017 Furthermore, harmine could slightly up-regulate the expression of MRP2, which implying harmine might be the substrate of MRP2. Harmine 13-20 ATP binding cassette subfamily C member 2 Homo sapiens 121-125 28871225-9 2017 Furthermore, harmine could slightly up-regulate the expression of MRP2, which implying harmine might be the substrate of MRP2. Harmine 87-94 ATP binding cassette subfamily C member 2 Homo sapiens 66-70 28871225-9 2017 Furthermore, harmine could slightly up-regulate the expression of MRP2, which implying harmine might be the substrate of MRP2. Harmine 87-94 ATP binding cassette subfamily C member 2 Homo sapiens 121-125 28871225-13 2017 MRP2 but MDR1 or BCRP might be involved in the transport of harmine. Harmine 60-67 ATP binding cassette subfamily C member 2 Homo sapiens 0-4 28871225-13 2017 MRP2 but MDR1 or BCRP might be involved in the transport of harmine. Harmine 60-67 ATP binding cassette subfamily B member 1 Homo sapiens 9-13 28871225-13 2017 MRP2 but MDR1 or BCRP might be involved in the transport of harmine. Harmine 60-67 BCR pseudogene 1 Homo sapiens 17-21 28871225-15 2017 All these findings suggested that harmine not only appears be an MRP2 substrate, but also possesses weak metabolic stability, and eventually leads to a low oral bioavailability. Harmine 34-41 ATP binding cassette subfamily C member 2 Homo sapiens 65-69 28314119-8 2017 Screening of a set of harmala alkaloids identified harmine as a potential neurotrophic molecule that significantly stimulated NGF-induced neurite outgrowth in the NS-1 cells. Harmine 51-58 nerve growth factor Rattus norvegicus 126-129 28901502-8 2017 Further study showed that harmine inhibited not only the basal phosphorylation level of extra-cellular signal-regulated kinase 1/2 (ERK1/2) and cyclic adenosine monophosphate response element-binding protein (CREB) but also EGF-induced ERK1/2 and CREB phosphorylation. Harmine 26-33 mitogen-activated protein kinase 1 Homo sapiens 88-130 28901502-8 2017 Further study showed that harmine inhibited not only the basal phosphorylation level of extra-cellular signal-regulated kinase 1/2 (ERK1/2) and cyclic adenosine monophosphate response element-binding protein (CREB) but also EGF-induced ERK1/2 and CREB phosphorylation. Harmine 26-33 mitogen-activated protein kinase 3 Homo sapiens 132-138 28901502-8 2017 Further study showed that harmine inhibited not only the basal phosphorylation level of extra-cellular signal-regulated kinase 1/2 (ERK1/2) and cyclic adenosine monophosphate response element-binding protein (CREB) but also EGF-induced ERK1/2 and CREB phosphorylation. Harmine 26-33 cAMP responsive element binding protein 1 Homo sapiens 209-213 28901502-8 2017 Further study showed that harmine inhibited not only the basal phosphorylation level of extra-cellular signal-regulated kinase 1/2 (ERK1/2) and cyclic adenosine monophosphate response element-binding protein (CREB) but also EGF-induced ERK1/2 and CREB phosphorylation. Harmine 26-33 epidermal growth factor Homo sapiens 224-227 28901502-8 2017 Further study showed that harmine inhibited not only the basal phosphorylation level of extra-cellular signal-regulated kinase 1/2 (ERK1/2) and cyclic adenosine monophosphate response element-binding protein (CREB) but also EGF-induced ERK1/2 and CREB phosphorylation. Harmine 26-33 mitogen-activated protein kinase 3 Homo sapiens 236-242 28901502-8 2017 Further study showed that harmine inhibited not only the basal phosphorylation level of extra-cellular signal-regulated kinase 1/2 (ERK1/2) and cyclic adenosine monophosphate response element-binding protein (CREB) but also EGF-induced ERK1/2 and CREB phosphorylation. Harmine 26-33 cAMP responsive element binding protein 1 Homo sapiens 247-251 28901502-10 2017 In conclusion, our data revealed that harmine inhibited the proliferation and migration of SKOV-3 cells, which might be mediated by ERK/CREB pathway. Harmine 38-45 mitogen-activated protein kinase 1 Homo sapiens 132-135 28901502-10 2017 In conclusion, our data revealed that harmine inhibited the proliferation and migration of SKOV-3 cells, which might be mediated by ERK/CREB pathway. Harmine 38-45 cAMP responsive element binding protein 1 Homo sapiens 136-140 28625859-5 2017 Harmine treatment (20mg/kg) prevented the reductions in brain-derived neurotrophic factor (BDNF) protein levels and hippocampal neurogenesis induced by CUS. Harmine 0-7 brain derived neurotrophic factor Mus musculus 56-89 28625859-5 2017 Harmine treatment (20mg/kg) prevented the reductions in brain-derived neurotrophic factor (BDNF) protein levels and hippocampal neurogenesis induced by CUS. Harmine 0-7 brain derived neurotrophic factor Mus musculus 91-95 28625859-6 2017 In addition, harmine treatment (20mg/kg) increased the protein expression levels of glutamate transporter 1 (GLT-1) and prevented the CUS-induced decreases in glial fibrillary acidic protein (GFAP) protein expressions in the prefrontal cortex and hippocampus, suggesting that restoration of astrocytic functions may be a potential mechanism underlying the antidepressant-like effects of harmine. Harmine 13-20 solute carrier family 1 (glial high affinity glutamate transporter), member 2 Mus musculus 84-107 28625859-6 2017 In addition, harmine treatment (20mg/kg) increased the protein expression levels of glutamate transporter 1 (GLT-1) and prevented the CUS-induced decreases in glial fibrillary acidic protein (GFAP) protein expressions in the prefrontal cortex and hippocampus, suggesting that restoration of astrocytic functions may be a potential mechanism underlying the antidepressant-like effects of harmine. Harmine 13-20 solute carrier family 1 (glial high affinity glutamate transporter), member 2 Mus musculus 109-114 28625859-6 2017 In addition, harmine treatment (20mg/kg) increased the protein expression levels of glutamate transporter 1 (GLT-1) and prevented the CUS-induced decreases in glial fibrillary acidic protein (GFAP) protein expressions in the prefrontal cortex and hippocampus, suggesting that restoration of astrocytic functions may be a potential mechanism underlying the antidepressant-like effects of harmine. Harmine 13-20 glial fibrillary acidic protein Mus musculus 159-190 28625859-6 2017 In addition, harmine treatment (20mg/kg) increased the protein expression levels of glutamate transporter 1 (GLT-1) and prevented the CUS-induced decreases in glial fibrillary acidic protein (GFAP) protein expressions in the prefrontal cortex and hippocampus, suggesting that restoration of astrocytic functions may be a potential mechanism underlying the antidepressant-like effects of harmine. Harmine 13-20 glial fibrillary acidic protein Mus musculus 192-196 28735864-5 2017 Further, we showed that the Ser408 site on GLI1 was not phosphorylated in the presence of the selective DYRK1A inhibitor harmine. Harmine 121-128 GLI family zinc finger 1 Homo sapiens 43-47 28551404-5 2017 As the most abundant compound, harmine inhibited tumor necrosis factor-alpha (TNF-alpha)- and lipopolysaccharides (LPS)-induced NF-kappaB transactivity and nuclear translocation in mouse macrophage RAW 264.7 cells. Harmine 31-38 tumor necrosis factor Mus musculus 78-87 28551404-7 2017 In an LPS-challenged mouse model, harmine markedly averted inflammatory damage of the lung, and decreased serum TNF-alpha, interleukin-1beta (IL-1beta) and IL-6 levels. Harmine 34-41 tumor necrosis factor Mus musculus 112-121 28551404-7 2017 In an LPS-challenged mouse model, harmine markedly averted inflammatory damage of the lung, and decreased serum TNF-alpha, interleukin-1beta (IL-1beta) and IL-6 levels. Harmine 34-41 interleukin 1 beta Mus musculus 123-140 28551404-7 2017 In an LPS-challenged mouse model, harmine markedly averted inflammatory damage of the lung, and decreased serum TNF-alpha, interleukin-1beta (IL-1beta) and IL-6 levels. Harmine 34-41 interleukin 1 beta Mus musculus 142-150 28551404-7 2017 In an LPS-challenged mouse model, harmine markedly averted inflammatory damage of the lung, and decreased serum TNF-alpha, interleukin-1beta (IL-1beta) and IL-6 levels. Harmine 34-41 interleukin 6 Mus musculus 156-160 28264138-2 2017 Harmine, a natural product that selectively inhibits DYRK1A amongst kinases, could serve as a tool compound to better understand the biological processes that arise from DYRK1A inhibition. Harmine 0-7 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 53-59 28264138-2 2017 Harmine, a natural product that selectively inhibits DYRK1A amongst kinases, could serve as a tool compound to better understand the biological processes that arise from DYRK1A inhibition. Harmine 0-7 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 170-176 28264138-3 2017 On the other hand, harmine is also a potent inhibitor of monoamine oxidase A (MAO-A). Harmine 19-26 monoamine oxidase A Homo sapiens 57-76 28264138-3 2017 On the other hand, harmine is also a potent inhibitor of monoamine oxidase A (MAO-A). Harmine 19-26 monoamine oxidase A Homo sapiens 78-83 28322844-2 2017 While harmine is known to inhibit DYRK1A and intercalate into the DNA, tri-substitution was shown previously to modify its activity profile in favor of protein synthesis inhibition. Harmine 6-13 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 34-40 28478808-12 2017 However, high concentration of harmine led to apoptosis characterized by the propidium/Annexin V-positive cell pollution, cell shrunk and the collapse of mitochondrial membrane potential. Harmine 31-38 annexin A5 Homo sapiens 87-96 28250274-8 2017 Treatment with harmine, an inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), which is located in the DS critical region of chromosome 21, and gene knockdown of DYRK1A, upregulated neprilysin in fibroblasts. Harmine 15-22 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 40-101 28250274-8 2017 Treatment with harmine, an inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), which is located in the DS critical region of chromosome 21, and gene knockdown of DYRK1A, upregulated neprilysin in fibroblasts. Harmine 15-22 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 103-109 28270853-4 2017 The in vitro cytotoxicity of harmine evaluated by XTT assay indicated that harmine suppressed the proliferation of TPC-1 cells in a dose- and time-dependent manner. Harmine 29-36 two pore channel 1 Mus musculus 115-120 28270853-4 2017 The in vitro cytotoxicity of harmine evaluated by XTT assay indicated that harmine suppressed the proliferation of TPC-1 cells in a dose- and time-dependent manner. Harmine 75-82 two pore channel 1 Mus musculus 115-120 28270853-5 2017 Moreover, harmine dose-dependently induced apoptosis of TPC-1 cells through regulating the ratio of Bcl-2/Bax. Harmine 10-17 two pore channel 1 Mus musculus 56-61 28270853-5 2017 Moreover, harmine dose-dependently induced apoptosis of TPC-1 cells through regulating the ratio of Bcl-2/Bax. Harmine 10-17 B cell leukemia/lymphoma 2 Mus musculus 100-105 28270853-5 2017 Moreover, harmine dose-dependently induced apoptosis of TPC-1 cells through regulating the ratio of Bcl-2/Bax. Harmine 10-17 BCL2-associated X protein Mus musculus 106-109 28270853-6 2017 The colony forming ability of TPC-1 cells was also time-dependently inhibited by harmine. Harmine 81-88 two pore channel 1 Mus musculus 30-35 28270853-7 2017 The inhibitory effects of harmine on migration and invasion of TPC-1 cells were studied by wound scratching and Transwell assays. Harmine 26-33 two pore channel 1 Mus musculus 63-68 27918874-5 2017 Harmine administration was associated with neuroprotective effects such as reduced excitotoxicity, inflammation, and oxidative stress, and increased brain-derived neurotrophic factor (BDNF) levels. Harmine 0-7 brain derived neurotrophic factor Homo sapiens 149-182 27282658-4 2017 We identify the DYRK1A kinase inhibitor harmine, which phosphorylates Tau that is deregulated in Alzheimer"s disease, as a potentiator of cell death induced by non-toxic doses of doxorubicin. Harmine 40-47 microtubule associated protein tau Homo sapiens 70-73 27282658-5 2017 These observations suggest that harmine or other compounds that target the DYRK1A kinase my offer a new therapeutic opportunity to suppress doxorubicin age-related and dose-dependent cardiotoxicity. Harmine 32-39 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 75-81 27918874-5 2017 Harmine administration was associated with neuroprotective effects such as reduced excitotoxicity, inflammation, and oxidative stress, and increased brain-derived neurotrophic factor (BDNF) levels. Harmine 0-7 brain derived neurotrophic factor Homo sapiens 184-188 26953159-6 2016 Induction of beta-cell proliferation by either 5-IT or harmine, another natural product DYRK1A inhibitor, was suppressed by coincubation with the calcineurin inhibitor FK506, suggesting involvement of DYRK1A and nuclear factor of activated T cells signaling. Harmine 55-62 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 88-94 27957390-6 2016 Harmine has been reported as a potent inhibitor of the dual specificity tyrosine-phosphorylation-regulated kinase (DYRK1A), which regulates cell proliferation and brain development. Harmine 0-7 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 115-121 27957390-8 2016 INDY but not pargyline induced proliferation of hNPCs similarly to harmine, suggesting that inhibition of DYRK1A is a possible mechanism to explain harmine effects upon the proliferation of hNPCs. Harmine 148-155 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 106-112 27957390-9 2016 Our findings show that harmine enhances proliferation of hNPCs and suggest that inhibition of DYRK1A may explain its effects upon proliferation in vitro and antidepressant effects in vivo. Harmine 23-30 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 94-100 27805061-0 2016 Harmine Induces Adipocyte Thermogenesis through RAC1-MEK-ERK-CHD4 Axis. Harmine 0-7 Rac family small GTPase 1 Mus musculus 48-52 27805061-0 2016 Harmine Induces Adipocyte Thermogenesis through RAC1-MEK-ERK-CHD4 Axis. Harmine 0-7 midkine Mus musculus 53-56 27805061-0 2016 Harmine Induces Adipocyte Thermogenesis through RAC1-MEK-ERK-CHD4 Axis. Harmine 0-7 mitogen-activated protein kinase 1 Mus musculus 57-60 27805061-0 2016 Harmine Induces Adipocyte Thermogenesis through RAC1-MEK-ERK-CHD4 Axis. Harmine 0-7 chromodomain helicase DNA binding protein 4 Mus musculus 61-65 27805061-5 2016 In vitro, harmine potently induced the expression of thermogenic genes in both brown and white adipocytes, which was largely abolished by inhibition of RAC1/MEK/ERK pathway. Harmine 10-17 Rac family small GTPase 1 Mus musculus 152-156 27805061-5 2016 In vitro, harmine potently induced the expression of thermogenic genes in both brown and white adipocytes, which was largely abolished by inhibition of RAC1/MEK/ERK pathway. Harmine 10-17 midkine Mus musculus 157-160 27805061-5 2016 In vitro, harmine potently induced the expression of thermogenic genes in both brown and white adipocytes, which was largely abolished by inhibition of RAC1/MEK/ERK pathway. Harmine 10-17 mitogen-activated protein kinase 1 Mus musculus 161-164 27805061-6 2016 Post-transcriptional modification analysis revealed that chromodomain helicase DNA binding protein 4 (CHD4) is a potential downstream target of harmine-mediated ERK activation. Harmine 144-151 chromodomain helicase DNA binding protein 4 Mus musculus 57-100 27805061-6 2016 Post-transcriptional modification analysis revealed that chromodomain helicase DNA binding protein 4 (CHD4) is a potential downstream target of harmine-mediated ERK activation. Harmine 144-151 chromodomain helicase DNA binding protein 4 Mus musculus 102-106 27805061-6 2016 Post-transcriptional modification analysis revealed that chromodomain helicase DNA binding protein 4 (CHD4) is a potential downstream target of harmine-mediated ERK activation. Harmine 144-151 mitogen-activated protein kinase 1 Mus musculus 161-164 27805061-7 2016 CHD4 directly binds the proximal promoter region of Ucp1, which is displaced upon treatment of harmine, thereby serving as a negative modulator of Ucp1. Harmine 95-102 chromodomain helicase DNA binding protein 4 Mus musculus 0-4 27805061-7 2016 CHD4 directly binds the proximal promoter region of Ucp1, which is displaced upon treatment of harmine, thereby serving as a negative modulator of Ucp1. Harmine 95-102 uncoupling protein 1 (mitochondrial, proton carrier) Mus musculus 52-56 27805061-7 2016 CHD4 directly binds the proximal promoter region of Ucp1, which is displaced upon treatment of harmine, thereby serving as a negative modulator of Ucp1. Harmine 95-102 uncoupling protein 1 (mitochondrial, proton carrier) Mus musculus 147-151 27280693-3 2016 Only a few potent and selective ABCG2 inhibitors have been discovered, i.e., fumitremorgin C (FTC), Ko143, and the alkaloid harmine, which contain a tetrahydro-beta-carboline or beta-carboline backbone, respectively. Harmine 124-131 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 32-37 27624103-7 2016 Treatment with the control compound harmine, a Dyrk1a inhibitor, led to a significant increase in Ki-67+ beta-cells, whereas treatment with other compounds had limited to no effect on human beta-cell proliferation. Harmine 36-43 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 47-53 27446381-0 2016 Harmine combined with paclitaxel inhibits tumor proliferation and induces apoptosis through down-regulation of cyclooxygenase-2 expression in gastric cancer. Harmine 0-7 prostaglandin-endoperoxide synthase 2 Homo sapiens 111-127 26953159-6 2016 Induction of beta-cell proliferation by either 5-IT or harmine, another natural product DYRK1A inhibitor, was suppressed by coincubation with the calcineurin inhibitor FK506, suggesting involvement of DYRK1A and nuclear factor of activated T cells signaling. Harmine 55-62 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 201-207 27004568-0 2016 Harmine induces cell cycle arrest and mitochondrial pathway-mediated cellular apoptosis in SW620 cells via inhibition of the Akt and ERK signaling pathways. Harmine 0-7 AKT serine/threonine kinase 1 Homo sapiens 125-128 27004568-12 2016 In conclusion, harmine induces cell cycle arrest and mitochondrial pathway-mediated cellular apoptosis in SW620 cells via inhibition of the Akt and ERK signaling pathways. Harmine 15-22 AKT serine/threonine kinase 1 Homo sapiens 140-143 26348003-12 2015 We demonstrated that harmine significantly reduced HSV-2-induced NF-kappaB activation, as well as IkappaB-alpha degradation and p65 nuclear translocation. Harmine 21-28 nuclear factor kappa B subunit 1 Homo sapiens 65-74 26526348-0 2015 Effects of harmine, an acetylcholinesterase inhibitor, on spatial learning and memory of APP/PS1 transgenic mice and scopolamine-induced memory impairment mice. Harmine 11-18 acetylcholinesterase Mus musculus 23-43 26526348-1 2015 Harmine, a beta-carboline alkaloid present in Peganum harmala with a wide spectrum of pharmacological activities, has been shown to exert strong inhibition against acetylcholinesterase in vitro. Harmine 0-7 acetylcholinesterase Mus musculus 164-184 26526348-4 2015 In addition, whether harmine could penetrate blood brain barrier, interact with and inhibit acetylcholinesterase, and activate downstream signaling network was also investigated. Harmine 21-28 acetylcholinesterase Mus musculus 92-112 26526348-6 2015 Meanwhile, long-term consumption of harmine (20mg/kg) for 10 weeks also slightly benefited the impaired memory of APP/PS1 mice. Harmine 36-43 presenilin 1 Mus musculus 118-121 26526348-8 2015 Molecular docking assay disclosed that harmine molecule could directly dock into the catalytic active site of acetylcholinesterase, which was partially confirmed by its in vivo inhibitory activity on acetylcholinesterase. Harmine 39-46 acetylcholinesterase Mus musculus 110-130 26526348-8 2015 Molecular docking assay disclosed that harmine molecule could directly dock into the catalytic active site of acetylcholinesterase, which was partially confirmed by its in vivo inhibitory activity on acetylcholinesterase. Harmine 39-46 acetylcholinesterase Mus musculus 200-220 26526348-9 2015 Taken together, all these results suggested that harmine could ameliorate impaired memory by enhancement of cholinergic neurotransmission via inhibiting the activity of acetylcholinesterase, which may contribute to its clinical use in the therapy of neurological diseases characterized with acetylcholinesterase deficiency. Harmine 49-56 acetylcholinesterase Mus musculus 169-189 26496827-4 2015 The beta-carboline alkaloid harmine has been demonstrated to exert neuroprotective actions in vivo, and the beneficial effects were specifically due to elevation of GLT-1. Harmine 28-35 solute carrier family 1 member 2 Rattus norvegicus 165-170 26496827-10 2015 In addition, harmine significantly increased the protein expression of GLT-1, and markedly attenuated the expression levels of interleukin-1beta and tumor necrosis factor-alpha, thereby attenuating apoptotic neuronal death in the hippocampus. Harmine 13-20 solute carrier family 1 member 2 Rattus norvegicus 71-76 26496827-10 2015 In addition, harmine significantly increased the protein expression of GLT-1, and markedly attenuated the expression levels of interleukin-1beta and tumor necrosis factor-alpha, thereby attenuating apoptotic neuronal death in the hippocampus. Harmine 13-20 interleukin 1 beta Rattus norvegicus 127-176 26067684-9 2015 Inversely, treatment of MI-induced HF rats with Dyrk1A inhibitor, either harmine or EGCG, improved the symptoms of HF, reversed the molecular changes of Dyrk1A and ASF, and regulated alternative splicing of CaMKIIdelta in HF rats. Harmine 73-80 dual specificity tyrosine phosphorylation regulated kinase 1A Rattus norvegicus 48-54 26067684-9 2015 Inversely, treatment of MI-induced HF rats with Dyrk1A inhibitor, either harmine or EGCG, improved the symptoms of HF, reversed the molecular changes of Dyrk1A and ASF, and regulated alternative splicing of CaMKIIdelta in HF rats. Harmine 73-80 dual specificity tyrosine phosphorylation regulated kinase 1A Rattus norvegicus 153-159 26622726-0 2015 Paclitaxel combined with harmine inhibits the migration and invasion of gastric cancer cells through downregulation of cyclooxygenase-2 expression. Harmine 25-32 prostaglandin-endoperoxide synthase 2 Homo sapiens 119-135 25998054-5 2015 Importantly, both Treg cells generated using the DYRK1A inhibitor harmine and direct administration of harmine itself potently attenuate inflammation in multiple experimental models of systemic autoimmunity and mucosal inflammation. Harmine 66-73 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 49-55 26192590-4 2015 Here we characterized a series of novel harmine analogs with minimal or absent MAO-A inhibitory activity. Harmine 40-47 monoamine oxidase A Homo sapiens 79-84 25068731-1 2015 In our study, a series of new harmine derivatives has been prepared by cycloaddition reaction using various arylnitrile oxides and evaluated in vitro against acetylcholinesterase and 5-lipoxygenase enzymes, MCF7 and HCT116 cancer cell lines. Harmine 30-37 acetylcholinesterase (Cartwright blood group) Homo sapiens 158-178 25068731-3 2015 The greatest activity against acetylcholinesterase (IC50 = 10.4 microM) was obtained for harmine 1 and cytotoxic activities (IC50 = 0.2 microM) for compound 3a. Harmine 89-96 acetylcholinesterase (Cartwright blood group) Homo sapiens 30-50 26382920-5 2015 Our further study found that Harmine, a natural compound, negatively regulates HR but not NHEJ by interfering Rad51 recruitment, resulting in severe cytotoxicity in hepatoma cells. Harmine 29-36 RAD51 recombinase Homo sapiens 110-115 25751815-0 2015 A high-throughput chemical screen reveals that harmine-mediated inhibition of DYRK1A increases human pancreatic beta cell replication. Harmine 47-54 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 78-84 25617675-2 2015 Harmine nanosuspensions were transformed into harmine solid nanocrystals (HAR-SNC) via different stress of solidification process including freezing, lyophilization and spray-drying. Harmine 0-7 lymphatic vessel endothelial hyaluronan receptor 1 Homo sapiens 74-77 25617675-2 2015 Harmine nanosuspensions were transformed into harmine solid nanocrystals (HAR-SNC) via different stress of solidification process including freezing, lyophilization and spray-drying. Harmine 46-53 lymphatic vessel endothelial hyaluronan receptor 1 Homo sapiens 74-77 25238961-0 2014 Harmine mediated neuroprotection via evaluation of glutamate transporter 1 in a rat model of global cerebral ischemia. Harmine 0-7 solute carrier family 1 member 2 Rattus norvegicus 51-74 25250831-1 2015 Harmine is a naturally occurring monoamine oxidase inhibitor that has recently been shown to selectively inhibit the dual-specificity tyrosine-(Y)-phosphorylation-regulated kinase 1A (DYRK1A). Harmine 0-7 dual specificity tyrosine phosphorylation regulated kinase 1A Rattus norvegicus 117-182 25250831-1 2015 Harmine is a naturally occurring monoamine oxidase inhibitor that has recently been shown to selectively inhibit the dual-specificity tyrosine-(Y)-phosphorylation-regulated kinase 1A (DYRK1A). Harmine 0-7 dual specificity tyrosine phosphorylation regulated kinase 1A Rattus norvegicus 184-190 25238961-4 2014 Preclinical findings implicate that Harmine present neuroprotection effects in a rat model of amyotrophic lateral sclerosis disease, and the beneficial effects were specifically due to up-regulation of GLT-1. Harmine 36-43 solute carrier family 1 member 2 Rattus norvegicus 202-207 24176842-0 2014 Harmine induces apoptosis and inhibits tumor cell proliferation, migration and invasion through down-regulation of cyclooxygenase-2 expression in gastric cancer. Harmine 0-7 prostaglandin-endoperoxide synthase 2 Homo sapiens 115-131 24154665-4 2014 MAO-A VT (an index of MAO-A density) was measured using [(11)C]harmine positron emission tomography (PET) in 42 subjects with MDEs secondary to major depressive disorder and 37 healthy controls. Harmine 63-70 monoamine oxidase A Homo sapiens 0-5 24154665-4 2014 MAO-A VT (an index of MAO-A density) was measured using [(11)C]harmine positron emission tomography (PET) in 42 subjects with MDEs secondary to major depressive disorder and 37 healthy controls. Harmine 63-70 monoamine oxidase A Homo sapiens 22-27 24898155-0 2014 Greater monoamine oxidase a binding in perimenopausal age as measured with carbon 11-labeled harmine positron emission tomography. Harmine 93-100 monoamine oxidase A Homo sapiens 8-27 24176842-9 2014 In addition, harmine significantly inhibited the expression of COX-2, PCNA, Bcl-2 and MMP-2 as well as increased Bax expression in gastric cancer cells. Harmine 13-20 prostaglandin-endoperoxide synthase 2 Homo sapiens 63-68 24176842-9 2014 In addition, harmine significantly inhibited the expression of COX-2, PCNA, Bcl-2 and MMP-2 as well as increased Bax expression in gastric cancer cells. Harmine 13-20 proliferating cell nuclear antigen Homo sapiens 70-74 24176842-9 2014 In addition, harmine significantly inhibited the expression of COX-2, PCNA, Bcl-2 and MMP-2 as well as increased Bax expression in gastric cancer cells. Harmine 13-20 BCL2 apoptosis regulator Homo sapiens 76-81 24176842-9 2014 In addition, harmine significantly inhibited the expression of COX-2, PCNA, Bcl-2 and MMP-2 as well as increased Bax expression in gastric cancer cells. Harmine 13-20 matrix metallopeptidase 2 Homo sapiens 86-91 24176842-9 2014 In addition, harmine significantly inhibited the expression of COX-2, PCNA, Bcl-2 and MMP-2 as well as increased Bax expression in gastric cancer cells. Harmine 13-20 BCL2 associated X, apoptosis regulator Homo sapiens 113-116 24176842-10 2014 These results collectively indicate that harmine induces apoptosis and inhibits proliferation, migration and invasion of human gastric cancer cells, which may be mediated by down-regulation of COX-2 expression. Harmine 41-48 prostaglandin-endoperoxide synthase 2 Homo sapiens 193-198 25087965-2 2014 We previously reported that the harmala alkaloid, harmine, lengthens the circadian period of Bmal1 transcription in NIH 3T3 fibroblasts. Harmine 50-57 aryl hydrocarbon receptor nuclear translocator like Homo sapiens 93-98 25087965-4 2014 Harmine significantly lengthened the period of PER2::LUC expression in embryonic fibroblasts, in neuronal cells differentiated from neuronal progenitor cells and in SCN slices obtained from PER2::LUC mice. Harmine 0-7 period circadian clock 2 Mus musculus 47-51 25087965-4 2014 Harmine significantly lengthened the period of PER2::LUC expression in embryonic fibroblasts, in neuronal cells differentiated from neuronal progenitor cells and in SCN slices obtained from PER2::LUC mice. Harmine 0-7 period circadian clock 2 Mus musculus 190-194 25087965-5 2014 Although harmine did not induce the transient mRNA expression of clock genes such as Per1, Per2 and Bmal1 in embryonic fibroblasts, it significantly extended the half-life of PER2::LUC protein in neuronal cells and SCN slices. Harmine 9-16 period circadian regulator 2 Homo sapiens 175-179 24109558-6 2013 Our data indicate that harmine exhibits a pronounced cytotoxicity and induces an anti-proliferation state in MCF-7 cells which is accompanied by a significant inhibition of telomerase activity and an induction of an accelerated senescence phenotype by over-expressing elements of the p53/p21 pathway. Harmine 23-30 tumor protein p53 Homo sapiens 284-287 25287872-6 2013 Treatment with harmine reversed the increase in citrate synthase activity in the prefrontal cortex. Harmine 15-22 citrate synthase Rattus norvegicus 48-64 24109558-6 2013 Our data indicate that harmine exhibits a pronounced cytotoxicity and induces an anti-proliferation state in MCF-7 cells which is accompanied by a significant inhibition of telomerase activity and an induction of an accelerated senescence phenotype by over-expressing elements of the p53/p21 pathway. Harmine 23-30 H3 histone pseudogene 16 Homo sapiens 288-291 23403377-1 2013 Positron emission tomography (PET) imaging of monoamine oxidases (MAO-A: [(11)C]harmine, [(11)C]clorgyline, and [(11)C]befloxatone; MAO-B: [(11)C]deprenyl-D2) has been actively pursued given clinical importance of MAOs in human neuropsychiatric disorders. Harmine 80-87 monoamine oxidase A Homo sapiens 66-71 23360763-3 2013 In the former case one of the new compounds, C624 (naphto [1,2-b]benzofuran-5,9-diol) displays a potency comparable to that of the first-in-class DYRK1A inhibitor, harmine, lacking however the drawback of drastically inhibiting monoamine oxidase-A (MAO-A) as harmine does. Harmine 164-171 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 146-152 23509697-0 2013 Harmine and harmaline downregulate TCDD-induced Cyp1a1 in the livers and lungs of C57BL/6 mice. Harmine 0-7 cytochrome P450, family 1, subfamily a, polypeptide 1 Mus musculus 48-54 23116713-6 2013 Therefore, this study screened a compound library and identified the beta-carboline alkaloid harmine as a novel inducer of CCN2 in human chondrocytic HCS-2/8 cells and osteoarthritic articular chondrocytes. Harmine 93-100 cellular communication network factor 2 Homo sapiens 123-127 23116713-9 2013 The chondroprotective effect of harmine was investigated under inflammatory condition by stimulation with TNFalpha, and harmine was shown to ameliorate TNFalpha-induced decrease in expression of CCN2 and cartilage markers. Harmine 32-39 tumor necrosis factor Homo sapiens 106-114 23116713-9 2013 The chondroprotective effect of harmine was investigated under inflammatory condition by stimulation with TNFalpha, and harmine was shown to ameliorate TNFalpha-induced decrease in expression of CCN2 and cartilage markers. Harmine 32-39 tumor necrosis factor Homo sapiens 152-160 23116713-9 2013 The chondroprotective effect of harmine was investigated under inflammatory condition by stimulation with TNFalpha, and harmine was shown to ameliorate TNFalpha-induced decrease in expression of CCN2 and cartilage markers. Harmine 32-39 cellular communication network factor 2 Homo sapiens 195-199 23116713-9 2013 The chondroprotective effect of harmine was investigated under inflammatory condition by stimulation with TNFalpha, and harmine was shown to ameliorate TNFalpha-induced decrease in expression of CCN2 and cartilage markers. Harmine 120-127 tumor necrosis factor Homo sapiens 152-160 23116713-9 2013 The chondroprotective effect of harmine was investigated under inflammatory condition by stimulation with TNFalpha, and harmine was shown to ameliorate TNFalpha-induced decrease in expression of CCN2 and cartilage markers. Harmine 120-127 cellular communication network factor 2 Homo sapiens 195-199 22923366-6 2013 This increase was abolished when CBS-deficient and Dyrk1A-transgenic mice were treated with harmine, an inhibitor of Dyrk1A kinase activity, which emphasizes the role of Dyrk1A activity on ERK and Akt activation. Harmine 92-99 dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1a Mus musculus 51-57 22923366-6 2013 This increase was abolished when CBS-deficient and Dyrk1A-transgenic mice were treated with harmine, an inhibitor of Dyrk1A kinase activity, which emphasizes the role of Dyrk1A activity on ERK and Akt activation. Harmine 92-99 dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1a Mus musculus 117-123 22923366-6 2013 This increase was abolished when CBS-deficient and Dyrk1A-transgenic mice were treated with harmine, an inhibitor of Dyrk1A kinase activity, which emphasizes the role of Dyrk1A activity on ERK and Akt activation. Harmine 92-99 dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1a Mus musculus 117-123 22923366-6 2013 This increase was abolished when CBS-deficient and Dyrk1A-transgenic mice were treated with harmine, an inhibitor of Dyrk1A kinase activity, which emphasizes the role of Dyrk1A activity on ERK and Akt activation. Harmine 92-99 mitogen-activated protein kinase 1 Mus musculus 189-192 22923366-6 2013 This increase was abolished when CBS-deficient and Dyrk1A-transgenic mice were treated with harmine, an inhibitor of Dyrk1A kinase activity, which emphasizes the role of Dyrk1A activity on ERK and Akt activation. Harmine 92-99 thymoma viral proto-oncogene 1 Mus musculus 197-200 23509697-1 2013 We previously demonstrated that Peganum harmala L. extract and its main active constituents, harmine and harmaline inhibit the 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD)-mediated induction of the carcinogen-activating enzyme, Cyp1a1, in vitro. Harmine 93-100 cytochrome P450, family 1, subfamily a, polypeptide 1 Mus musculus 226-232 23509697-3 2013 Therefore, the aim of this study is to examine the effect of harmine and harmaline on TCDD-mediated induction of Cyp1a1 in mice livers and lungs. Harmine 61-68 cytochrome P450, family 1, subfamily a, polypeptide 1 Mus musculus 113-119 23509697-9 2013 The effect of harmine and harmaline on TCDD-mediated induction of Cyp1a1 mRNA, protein, and activity levels was determined using real-time PCR, Western blot analysis, and 7-ethoxyresurofin as a substrate, respectively. Harmine 14-21 cytochrome P450, family 1, subfamily a, polypeptide 1 Mus musculus 66-72 23509697-10 2013 Our results showed that harmine and harmaline significantly decreased the TCDD-mediated induction of Cyp1a1 in both the livers and lungs. Harmine 24-31 cytochrome P450, family 1, subfamily a, polypeptide 1 Mus musculus 101-107 23509697-11 2013 We concluded that harmine and harmaline are promising candidate to inhibit TCDD-mediated induction of Cyp1a1 in mice hepatic and extrahepatic tissues. Harmine 18-25 cytochrome P450, family 1, subfamily a, polypeptide 1 Mus musculus 102-108 23076833-2 2013 Harmine is an inhibitor of monoamine oxidase A (MAO-A) and interacts in vitro with several pharmacological targets which modulate dopamine (DA) neurotransmission. Harmine 0-7 monoamine oxidase A Rattus norvegicus 27-46 23076833-2 2013 Harmine is an inhibitor of monoamine oxidase A (MAO-A) and interacts in vitro with several pharmacological targets which modulate dopamine (DA) neurotransmission. Harmine 0-7 monoamine oxidase A Rattus norvegicus 48-53 22186668-2 2012 We measured the effect of changes in MAO-A substrate on MAO-A binding in regions implicated in affective and neurodegenerative disease with [(11)C]-harmine positron emission tomography in healthy volunteers. Harmine 146-155 monoamine oxidase A Homo sapiens 56-61 22770529-2 2012 Harmine is known for its anticancer properties and is a DYRK1A inhibitor. Harmine 0-7 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 56-62 22335895-3 2012 Based on information obtained from a structure-activity relationship study previously conducted for an acridine series of haspin inhibitors in conjunction with in silico docking using a recently disclosed crystal structure of the kinase, harmine analogs were designed that resulted in significantly increased haspin kinase inhibitory potency. Harmine 238-245 histone H3 associated protein kinase Mus musculus 122-128 22335895-3 2012 Based on information obtained from a structure-activity relationship study previously conducted for an acridine series of haspin inhibitors in conjunction with in silico docking using a recently disclosed crystal structure of the kinase, harmine analogs were designed that resulted in significantly increased haspin kinase inhibitory potency. Harmine 238-245 histone H3 associated protein kinase Mus musculus 309-315 22335895-4 2012 The harmine derivatives also demonstrated less activity towards DYRK2 compared to the acridine series. Harmine 4-11 dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 2 Mus musculus 64-69 22877698-4 2012 However, when applied over the same concentration range, harmine significantly inhibited C-shapes elicited by cocaine, with a concentration of 0.1 muM producing almost 90% inhibition. Harmine 57-64 latexin Homo sapiens 147-150 22877698-6 2012 When tested in the presence of the glutamate transporter inhibitor dihydrokainate (DHK) (0.1, 1 muM), harmine (0.1 muM) efficacy against cocaine-induced C-shapes was significantly reduced. Harmine 102-109 latexin Homo sapiens 96-99 22877698-6 2012 When tested in the presence of the glutamate transporter inhibitor dihydrokainate (DHK) (0.1, 1 muM), harmine (0.1 muM) efficacy against cocaine-induced C-shapes was significantly reduced. Harmine 102-109 latexin Homo sapiens 115-118 22335895-2 2012 High throughput screening of approximately 140,000 compounds identified the beta-carbolines harmine and harmol as moderately potent haspin kinase inhibitors. Harmine 92-99 histone H3 associated protein kinase Mus musculus 132-138 22001777-0 2012 Transcriptional and posttranslational inhibition of dioxin-mediated induction of CYP1A1 by harmine and harmol. Harmine 91-98 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 81-87 21401525-6 2012 Furthermore, EMSA (electrophoretic mobility-shift assay) and Western-blot analysis showed that harmine enhanced the transactivating function of RORalpha (retinoid-related orphan receptor alpha), probably by increasing its nuclear translocation. Harmine 95-102 RAR related orphan receptor A Homo sapiens 144-152 21401525-6 2012 Furthermore, EMSA (electrophoretic mobility-shift assay) and Western-blot analysis showed that harmine enhanced the transactivating function of RORalpha (retinoid-related orphan receptor alpha), probably by increasing its nuclear translocation. Harmine 95-102 RAR related orphan receptor A Homo sapiens 154-192 21401525-7 2012 Exogenous expression of RORalpha also caused a long period, confirming the phenotype indicated by harmine. Harmine 98-105 RAR related orphan receptor A Homo sapiens 24-32 21401525-8 2012 These results suggest that harmine extends the circadian period by enhancing RORalpha function and that harmine is a new candidate that contributes to the control of period length in mammalian cells. Harmine 27-34 RAR related orphan receptor A Homo sapiens 77-85 22001777-2 2012 We previously demonstrated that harmine inhibits the dioxin-mediated induction of Cyp1a1 activity in murine hepatoma cells. Harmine 32-39 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 82-88 22001777-3 2012 Therefore, the aim of this study is to determine the effect of harmine and its main metabolite, harmol, on the dioxin-mediated induction of CYP1A1 in human HepG2 and murine Hepa 1c1c7 hepatoma cells. Harmine 63-70 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 140-146 22001777-4 2012 Our results showed that harmine and harmol significantly inhibited the dioxin-mediated induction of CYP1A1 at mRNA, protein, and activity levels in a concentration-dependent manner in human and murine hepatoma cells. Harmine 24-31 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 100-106 22001777-5 2012 Moreover, harmine and harmol inhibited the AhR-dependent luciferase activity and the activation and transformation of AhR using the electrophoretic mobility shift assay. Harmine 10-17 aryl hydrocarbon receptor Homo sapiens 43-46 22001777-5 2012 Moreover, harmine and harmol inhibited the AhR-dependent luciferase activity and the activation and transformation of AhR using the electrophoretic mobility shift assay. Harmine 10-17 aryl hydrocarbon receptor Homo sapiens 118-121 21570953-9 2011 The bone morphogenetic protein (BMP) antagonist noggin and its receptor kinase inhibitors dorsomorphin and LDN-193189 attenuated harmine-promoted ALP activity. Harmine 129-136 noggin Mus musculus 48-54 23300602-6 2012 Harmine also prevented p53 degradation in the presence of cycloheximide and activated nuclear accumulation of p53 followed by increasing its transcriptional activity in endothelial cells. Harmine 0-7 transformation related protein 53, pseudogene Mus musculus 23-26 23300602-6 2012 Harmine also prevented p53 degradation in the presence of cycloheximide and activated nuclear accumulation of p53 followed by increasing its transcriptional activity in endothelial cells. Harmine 0-7 transformation related protein 53, pseudogene Mus musculus 110-113 23300602-9 2012 Our results suggested a novel mechanism and bioactivity of harmine, which inhibited tumor growth by activating the p53 signaling pathway and blocking angiogenesis in endothelial cells. Harmine 59-66 transformation related protein 53, pseudogene Mus musculus 115-118 22558087-0 2012 JKA97, a novel benzylidene analog of harmine, exerts anti-cancer effects by inducing G1 arrest, apoptosis, and p53-independent up-regulation of p21. Harmine 37-44 tumor protein p53 Homo sapiens 111-114 22558087-0 2012 JKA97, a novel benzylidene analog of harmine, exerts anti-cancer effects by inducing G1 arrest, apoptosis, and p53-independent up-regulation of p21. Harmine 37-44 H3 histone pseudogene 16 Homo sapiens 144-147 21463543-0 2011 Monoamine oxidase A inhibitor occupancy during treatment of major depressive episodes with moclobemide or St. John"s wort: an [11C]-harmine PET study. Harmine 132-139 monoamine oxidase A Homo sapiens 0-19 23300602-0 2012 A natural small molecule harmine inhibits angiogenesis and suppresses tumour growth through activation of p53 in endothelial cells. Harmine 25-32 transformation related protein 53, pseudogene Mus musculus 106-109 23300602-4 2012 Here, we identified harmine (beta-carboline alkaloid) as a novel activator of p53 signaling involved in inhibition of angiogenesis and tumor growth. Harmine 20-27 transformation related protein 53, pseudogene Mus musculus 78-81 23300602-5 2012 Harmine induced p53 phosphorylation and disrupted the p53-MDM2 interaction. Harmine 0-7 transformation related protein 53, pseudogene Mus musculus 16-19 23300602-5 2012 Harmine induced p53 phosphorylation and disrupted the p53-MDM2 interaction. Harmine 0-7 transformation related protein 53, pseudogene Mus musculus 54-57 23300602-5 2012 Harmine induced p53 phosphorylation and disrupted the p53-MDM2 interaction. Harmine 0-7 transformed mouse 3T3 cell double minute 2 Mus musculus 58-62 21433154-4 2011 Harmine, harmol and harmane exhibited noncompetitive inhibition on the activity of CYP3A4 with K(i) values of 16.76, 5.13 and 1.66 muM, respectively. Harmine 0-7 latexin Homo sapiens 131-134 21433154-6 2011 Harmaline, harmine and harmol showed typical competitive inhibition on the activity of CYP2D6 with K(i) values of 20.69, 36.48 and 47.11 muM, respectively. Harmine 11-18 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 87-93 21433154-6 2011 Harmaline, harmine and harmol showed typical competitive inhibition on the activity of CYP2D6 with K(i) values of 20.69, 36.48 and 47.11 muM, respectively. Harmine 11-18 latexin Homo sapiens 137-140 21504804-3 2011 Orphan ligand library screening using this system identified the beta-carboline derivative harmine, which is a highly potent inhibitor of dual-specificity tyrosine-phosphorylation regulated kinase 1A (DYRK1A), to be an NFAT regulator in osteoclasts. Harmine 91-98 dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1a Mus musculus 138-199 21504804-3 2011 Orphan ligand library screening using this system identified the beta-carboline derivative harmine, which is a highly potent inhibitor of dual-specificity tyrosine-phosphorylation regulated kinase 1A (DYRK1A), to be an NFAT regulator in osteoclasts. Harmine 91-98 dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1a Mus musculus 201-207 21504804-4 2011 RAW264.7 cells highly expressed DYRK1A protein, and in vitro phosphorylation assay demonstrated that harmine directly inhibited the DYRK1A-mediated phosphorylation (in-activation) of NFATc1. Harmine 101-108 dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1a Mus musculus 32-38 21504804-4 2011 RAW264.7 cells highly expressed DYRK1A protein, and in vitro phosphorylation assay demonstrated that harmine directly inhibited the DYRK1A-mediated phosphorylation (in-activation) of NFATc1. Harmine 101-108 dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1a Mus musculus 132-138 21504804-4 2011 RAW264.7 cells highly expressed DYRK1A protein, and in vitro phosphorylation assay demonstrated that harmine directly inhibited the DYRK1A-mediated phosphorylation (in-activation) of NFATc1. Harmine 101-108 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 183-189 21504804-5 2011 Harmine promoted the dephosphorylation (activation) of NFATc1 in RAW264.7 cells within 24h, and it significantly increased the expression of NFATc1 in RAW264.7 cells and mouse primary bone marrow macrophages (BMMs) both in the presence and absence of RANKL stimulation. Harmine 0-7 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 55-61 21504804-5 2011 Harmine promoted the dephosphorylation (activation) of NFATc1 in RAW264.7 cells within 24h, and it significantly increased the expression of NFATc1 in RAW264.7 cells and mouse primary bone marrow macrophages (BMMs) both in the presence and absence of RANKL stimulation. Harmine 0-7 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 141-147 21504804-5 2011 Harmine promoted the dephosphorylation (activation) of NFATc1 in RAW264.7 cells within 24h, and it significantly increased the expression of NFATc1 in RAW264.7 cells and mouse primary bone marrow macrophages (BMMs) both in the presence and absence of RANKL stimulation. Harmine 0-7 tumor necrosis factor (ligand) superfamily, member 11 Mus musculus 251-256 21504804-6 2011 Although harmine promoted NFATc1 expression and stimulated target genes for osteoclastogenesis, cell-cell fusion and the formation of TRAP-positive multinucleated osteoclasts from RAW264.7 cells and BMMs was significantly inhibited by harmine treatment. Harmine 9-16 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 26-32 21504804-7 2011 Meanwhile, harmine remarkably promoted the expression of inhibitor of DNA binding/differentiation-2 (Id2), which is a negative regulator for osteoclastogenesis, in RAW264.7 cells and BMMs. Harmine 11-18 inhibitor of DNA binding 2 Mus musculus 101-104 21504804-8 2011 An Id2-null-mutant showed slightly increased osteoclast formation from BMMs, and the harmine-mediated inhibition of osteoclast formation was abolished in the BMMs of Id2-null-mutant mice. Harmine 85-92 inhibitor of DNA binding 2 Mus musculus 3-6 21504804-8 2011 An Id2-null-mutant showed slightly increased osteoclast formation from BMMs, and the harmine-mediated inhibition of osteoclast formation was abolished in the BMMs of Id2-null-mutant mice. Harmine 85-92 inhibitor of DNA binding 2 Mus musculus 166-169 21504804-9 2011 These results suggest that harmine is a potent activator of NFATc1 that interferes with the function of DYRK1A in osteoclast precursors and also up-regulates Id2 protein, which may dominantly inhibit expression pathways associated with cell-cell fusion, thereby leading to the disruption of the fusion events mediating osteoclastogenesis. Harmine 27-34 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 60-66 21504804-9 2011 These results suggest that harmine is a potent activator of NFATc1 that interferes with the function of DYRK1A in osteoclast precursors and also up-regulates Id2 protein, which may dominantly inhibit expression pathways associated with cell-cell fusion, thereby leading to the disruption of the fusion events mediating osteoclastogenesis. Harmine 27-34 dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1a Mus musculus 104-110 21504804-9 2011 These results suggest that harmine is a potent activator of NFATc1 that interferes with the function of DYRK1A in osteoclast precursors and also up-regulates Id2 protein, which may dominantly inhibit expression pathways associated with cell-cell fusion, thereby leading to the disruption of the fusion events mediating osteoclastogenesis. Harmine 27-34 inhibitor of DNA binding 2 Mus musculus 158-161 21504804-10 2011 The small molecule harmine is therefore expected to provide an experimental tool for investigating signaling cascades in osteoclastogenesis, especially those centered on DYRK1A-mediated NFATc1 and Id2 regulation. Harmine 19-26 dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1a Mus musculus 170-176 21504804-10 2011 The small molecule harmine is therefore expected to provide an experimental tool for investigating signaling cascades in osteoclastogenesis, especially those centered on DYRK1A-mediated NFATc1 and Id2 regulation. Harmine 19-26 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 186-192 21504804-10 2011 The small molecule harmine is therefore expected to provide an experimental tool for investigating signaling cascades in osteoclastogenesis, especially those centered on DYRK1A-mediated NFATc1 and Id2 regulation. Harmine 19-26 inhibitor of DNA binding 2 Mus musculus 197-200 21570953-12 2011 Furthermore, BMP-responsive and Runx2-responsive reporters were activated by harmine treatment. Harmine 77-84 runt related transcription factor 2 Mus musculus 32-37 21570953-13 2011 Taken together, these results indicate that harmine enhances osteoblast differentiation probably by inducing the expressions of BMPs and activating BMP and Runx2 pathways. Harmine 44-51 runt related transcription factor 2 Mus musculus 156-161 20810002-7 2011 MAOA binding was measured with [11C]harmine positron emission tomography (PET) in prefrontal brain regions and personality traits were measured with the NEO Personality Inventory Revised (NEO PI-R). Harmine 36-43 monoamine oxidase A Homo sapiens 0-4 21034752-9 2011 We next tested its efficacy in both wild type animals and in an ALS animal model of disease and demonstrated that harmine effectively increased GLT-1 protein and glutamate transporter activity in vivo. Harmine 114-121 solute carrier family 1 member 2 Homo sapiens 144-149 21838142-3 2011 Results show harmine in form of base and salt in water and in mixture of DMSO and water has the hightest inhibition activity on ACHE using eserine as reference substance. Harmine 13-20 acetylcholinesterase (Cartwright blood group) Homo sapiens 128-132 21838142-4 2011 Harmalol in form of salt in water and harmine in form of base and salt in mixture of DMSO and water has the hightest activity on BUCHE. Harmine 38-45 butyrylcholinesterase Homo sapiens 129-134 21034752-7 2011 When screening a library of 1040 FDA approved compounds and natural products, we identified harmine, a naturally occurring beta-carboline alkaloid, as one of the top hits for activating the EAAT2 promoter. Harmine 92-99 solute carrier family 1 member 2 Homo sapiens 190-195 21034752-8 2011 We further tested harmine in our in vitro cell culture systems and confirmed its ability to increase EAAT2/GLT1 gene expression and functional glutamate uptake activity. Harmine 18-25 solute carrier family 1 member 2 Homo sapiens 101-106 21034752-8 2011 We further tested harmine in our in vitro cell culture systems and confirmed its ability to increase EAAT2/GLT1 gene expression and functional glutamate uptake activity. Harmine 18-25 solute carrier family 1 member 2 Homo sapiens 107-111 21573099-0 2011 beta-carboline compounds, including harmine, inhibit DYRK1A and tau phosphorylation at multiple Alzheimer"s disease-related sites. Harmine 36-43 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 53-59 21573099-0 2011 beta-carboline compounds, including harmine, inhibit DYRK1A and tau phosphorylation at multiple Alzheimer"s disease-related sites. Harmine 36-43 microtubule associated protein tau Homo sapiens 64-67 21573099-1 2011 Harmine, a beta-carboline alkaloid, is a high affinity inhibitor of the dual specificity tyrosine phosphorylation regulated kinase 1A (DYRK1A) protein. Harmine 0-7 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 72-133 21573099-1 2011 Harmine, a beta-carboline alkaloid, is a high affinity inhibitor of the dual specificity tyrosine phosphorylation regulated kinase 1A (DYRK1A) protein. Harmine 0-7 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 135-141 21573099-5 2011 Here we test the ability of harmine, and numerous additional beta-carboline compounds, to inhibit the DYRK1A dependent phosphorylation of tau protein on serine 396, serine 262/serine 356 (12E8 epitope), and threonine 231 in cell culture assays and in vitro phosphorylation assays. Harmine 28-35 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 102-108 21573099-5 2011 Here we test the ability of harmine, and numerous additional beta-carboline compounds, to inhibit the DYRK1A dependent phosphorylation of tau protein on serine 396, serine 262/serine 356 (12E8 epitope), and threonine 231 in cell culture assays and in vitro phosphorylation assays. Harmine 28-35 microtubule associated protein tau Homo sapiens 138-141 21183355-1 2011 Previous studies have shown that harmine is a reversible inhibitor of human monoamine oxidase A (MAO-A). Harmine 33-40 monoamine oxidase A Homo sapiens 76-95 21429205-8 2011 Furthermore, RT-PCR analysis showed that harmine induced apoptosis in B16F-10 melanoma cells by up-regulating Bax and activating Caspase-3, 9 and p53 and down-regulating Bcl-2. Harmine 41-48 BCL2-associated X protein Mus musculus 110-113 21429205-8 2011 Furthermore, RT-PCR analysis showed that harmine induced apoptosis in B16F-10 melanoma cells by up-regulating Bax and activating Caspase-3, 9 and p53 and down-regulating Bcl-2. Harmine 41-48 caspase 3 Mus musculus 129-138 21429205-8 2011 Furthermore, RT-PCR analysis showed that harmine induced apoptosis in B16F-10 melanoma cells by up-regulating Bax and activating Caspase-3, 9 and p53 and down-regulating Bcl-2. Harmine 41-48 transformation related protein 53, pseudogene Mus musculus 146-149 21429205-8 2011 Furthermore, RT-PCR analysis showed that harmine induced apoptosis in B16F-10 melanoma cells by up-regulating Bax and activating Caspase-3, 9 and p53 and down-regulating Bcl-2. Harmine 41-48 B cell leukemia/lymphoma 2 Mus musculus 170-175 21429205-9 2011 Harmine also up-regulated Caspase-8 and Bid, indicating that harmine affected both extrinsic and intrinsic pathways of apoptosis. Harmine 0-7 caspase 8 Mus musculus 26-35 21429205-9 2011 Harmine also up-regulated Caspase-8 and Bid, indicating that harmine affected both extrinsic and intrinsic pathways of apoptosis. Harmine 0-7 BH3 interacting domain death agonist Mus musculus 40-43 21429205-9 2011 Harmine also up-regulated Caspase-8 and Bid, indicating that harmine affected both extrinsic and intrinsic pathways of apoptosis. Harmine 61-68 caspase 8 Mus musculus 26-35 21185805-0 2011 Harmine is an ATP-competitive inhibitor for dual-specificity tyrosine phosphorylation-regulated kinase 1A (Dyrk1A). Harmine 0-7 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 44-105 21185805-0 2011 Harmine is an ATP-competitive inhibitor for dual-specificity tyrosine phosphorylation-regulated kinase 1A (Dyrk1A). Harmine 0-7 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 107-113 21185805-3 2011 In this study, we show that harmine functions as an ATP-competitive inhibitor against Dyrk1A. Harmine 28-35 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 86-92 21185805-4 2011 Our conclusion is supported by kinetic analysis of harmine inhibition as well as by the characterization of a Dyrk1A mutation conferring significant resistance to harmine. Harmine 163-170 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 110-116 21185805-6 2011 The V306A mutation offers harmine resistance by differentially altering Dyrk1A affinity for harmine and ATP. Harmine 26-33 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 72-78 21185805-6 2011 The V306A mutation offers harmine resistance by differentially altering Dyrk1A affinity for harmine and ATP. Harmine 92-99 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 72-78 21185805-9 2011 Our results reveal that harmine inhibits Dyrk1A activity by interacting with residues in the ATP-binding pocket and displacing ATP. Harmine 24-31 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 41-47 21185805-10 2011 Our results also suggest that harmine will be a good lead compound for further designing of selective ATP-competitive Dyrk1A inhibitors through exploration of the ATP-binding pocket of Dyrk1A. Harmine 30-37 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 118-124 21185805-10 2011 Our results also suggest that harmine will be a good lead compound for further designing of selective ATP-competitive Dyrk1A inhibitors through exploration of the ATP-binding pocket of Dyrk1A. Harmine 30-37 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 185-191 21047508-4 2011 We found that harmine, a beta-carboline alkaloid, inhibited multinucleated osteoclast formation induced by receptor activator of nuclear factor-kappaB ligand (RANKL) in RAW264.7 cells. Harmine 14-21 tumor necrosis factor (ligand) superfamily, member 11 Mus musculus 107-157 21047508-4 2011 We found that harmine, a beta-carboline alkaloid, inhibited multinucleated osteoclast formation induced by receptor activator of nuclear factor-kappaB ligand (RANKL) in RAW264.7 cells. Harmine 14-21 tumor necrosis factor (ligand) superfamily, member 11 Mus musculus 159-164 21047508-6 2011 Furthermore, harmine prevented RANKL-induced bone resorption in both cell and bone tissue cultures. Harmine 13-20 tumor necrosis factor (ligand) superfamily, member 11 Mus musculus 31-36 21047508-9 2011 In mechanistic studies, we found that harmine inhibited the RANKL-induced expression of c-Fos and subsequent expression of nuclear factor of activated T cells (NFAT) c1, which is a master regulator of osteoclastogenesis. Harmine 38-45 tumor necrosis factor (ligand) superfamily, member 11 Mus musculus 60-65 21047508-9 2011 In mechanistic studies, we found that harmine inhibited the RANKL-induced expression of c-Fos and subsequent expression of nuclear factor of activated T cells (NFAT) c1, which is a master regulator of osteoclastogenesis. Harmine 38-45 FBJ osteosarcoma oncogene Mus musculus 88-93 21047508-11 2011 These results indicate that harmine inhibits osteoclast formation via downregulation of c-Fos and NFATc1 induced by RANKL and represses bone resorption. Harmine 28-35 FBJ osteosarcoma oncogene Mus musculus 88-93 21047508-11 2011 These results indicate that harmine inhibits osteoclast formation via downregulation of c-Fos and NFATc1 induced by RANKL and represses bone resorption. Harmine 28-35 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 98-104 21047508-11 2011 These results indicate that harmine inhibits osteoclast formation via downregulation of c-Fos and NFATc1 induced by RANKL and represses bone resorption. Harmine 28-35 tumor necrosis factor (ligand) superfamily, member 11 Mus musculus 116-121 21183355-1 2011 Previous studies have shown that harmine is a reversible inhibitor of human monoamine oxidase A (MAO-A). Harmine 33-40 monoamine oxidase A Homo sapiens 97-102 21183355-2 2011 Moreover, the crystal structure of human MAO-A in complex with harmine has been recently solved. Harmine 63-70 monoamine oxidase A Homo sapiens 41-46 21183355-3 2011 This crystal structure shows that close to the methoxy group of the harmine moiety, a lipophilic pocket is left vacant within the binding site of human MAO-A. Harmine 68-75 monoamine oxidase A Homo sapiens 152-157 21183355-7 2011 The results show that O-alkylated compounds with lipophilic groups like cyclohexyl, phenyl and aliphatic chains increase the inhibition of MAO-A compared to harmine. Harmine 157-164 monoamine oxidase A Homo sapiens 139-144 21183355-11 2011 However, several compounds show a better inhibition on MAO-B compared to harmine. Harmine 73-80 monoamine oxidase B Homo sapiens 55-60 20219660-14 2010 Among various constituents of Banisteriopsis caapi, harmine (7), harmaline (6) and tetrahydroharmine (5) are responsible for MAO-A inhibition, while two major proanthocyanidines, epicatechin (8) and procyanidine B2 (9) produce antioxidant effects. Harmine 52-59 monoamine oxidase A Homo sapiens 125-130 20686906-0 2010 Chronic administration of harmine elicits antidepressant-like effects and increases BDNF levels in rat hippocampus. Harmine 26-33 brain-derived neurotrophic factor Rattus norvegicus 84-88 20686906-7 2010 Brain-derived neurotrophic factor (BDNF) hippocampal levels were assessed in imipramine and harmine-treated rats by ELISA sandwich assay. Harmine 92-99 brain-derived neurotrophic factor Rattus norvegicus 0-33 20686906-8 2010 Interestingly, chronic administration of harmine at the higher doses (10 and 15 mg/kg), but not imipramine, increased BDNF protein levels in rat hippocampus. Harmine 41-48 brain-derived neurotrophic factor Rattus norvegicus 118-122 21372424-3 2011 A harmala alkaloid, harmine, an opium alkaloid, papaverine, and Lycoris alkaloids, lycorine and lycoricidinol, showed TNF-alpha suppressive activities stronger than or comparable to that of a reference polyphenol, butein, in RAW264 cells (IC(50)=4, 10, 2.1, 0.02, and 8 microM, respectively). Harmine 20-27 tumor necrosis factor Mus musculus 118-127 21372424-6 2011 In addition, harmine was found to suppress interleukin-6 (IL-6) production in RAW264 cells. Harmine 13-20 interleukin 6 Mus musculus 43-56 21372424-6 2011 In addition, harmine was found to suppress interleukin-6 (IL-6) production in RAW264 cells. Harmine 13-20 interleukin 6 Mus musculus 58-62 21372424-10 2011 In conclusion, some herbal alkaloids like harmine, in spite of lacking antioxidative property, have potential as anti-inflammatory agents that strongly suppress TNF-alpha and NO production by a unique mechanism. Harmine 42-49 tumor necrosis factor Mus musculus 161-170 21967457-5 2011 Higher expression levels of pro-metastatic genes such as matrix metalloproteinase-9 (MMP-9), extracellular signal[en]regulated kinase (ERK), and vascular endothelial factors (VEGFs), all of which play important roles in cancer cell migration and invasion, were observed in the metastatic group compared with normal, but were all down-regulated by treatment with harmine. Harmine 362-369 matrix metallopeptidase 9 Mus musculus 57-83 21967457-7 2011 In conclusion, harmine exerts anti-metastatic activity and this effect could be linked to the metastasis-related signaling pathway that includes ERK, VEGF, and MMPs. Harmine 15-22 vascular endothelial growth factor A Mus musculus 150-154 21967457-7 2011 In conclusion, harmine exerts anti-metastatic activity and this effect could be linked to the metastasis-related signaling pathway that includes ERK, VEGF, and MMPs. Harmine 15-22 matrix metallopeptidase 9 Mus musculus 160-164 20858484-0 2010 Harmine inhibits tumour specific neo-vessel formation by regulating VEGF, MMP, TIMP and pro-inflammatory mediators both in vivo and in vitro. Harmine 0-7 vascular endothelial growth factor A Mus musculus 68-72 20858484-0 2010 Harmine inhibits tumour specific neo-vessel formation by regulating VEGF, MMP, TIMP and pro-inflammatory mediators both in vivo and in vitro. Harmine 0-7 tissue inhibitor of metalloproteinase 1 Mus musculus 79-83 20858484-5 2010 A drastic elevation in serum pro-angiogenic factors such as vascular endothelial growth factor (VEGF), nitric oxide (NO) and pro-inflammatory cytokines in angiogenesis induced animals was significantly decreased by harmine treatment. Harmine 215-222 vascular endothelial growth factor A Mus musculus 60-94 20858484-5 2010 A drastic elevation in serum pro-angiogenic factors such as vascular endothelial growth factor (VEGF), nitric oxide (NO) and pro-inflammatory cytokines in angiogenesis induced animals was significantly decreased by harmine treatment. Harmine 215-222 vascular endothelial growth factor A Mus musculus 96-100 20858484-6 2010 At the same time harmine increased anti-tumour factors like interleukin-2 (IL-2) and tissue inhibitor metalloprotease (TIMP). Harmine 17-24 interleukin 2 Mus musculus 60-73 20858484-6 2010 At the same time harmine increased anti-tumour factors like interleukin-2 (IL-2) and tissue inhibitor metalloprotease (TIMP). Harmine 17-24 interleukin 2 Mus musculus 75-79 20858484-6 2010 At the same time harmine increased anti-tumour factors like interleukin-2 (IL-2) and tissue inhibitor metalloprotease (TIMP). Harmine 17-24 tissue inhibitor of metalloproteinase 1 Mus musculus 85-117 20858484-6 2010 At the same time harmine increased anti-tumour factors like interleukin-2 (IL-2) and tissue inhibitor metalloprotease (TIMP). Harmine 17-24 tissue inhibitor of metalloproteinase 1 Mus musculus 119-123 20858484-7 2010 Moreover nuclear factor (NF)-kappaB and other transcription factors like CREB, ATF-2 involved in tumour development and angiogenesis were also inhibited by harmine. Harmine 156-163 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 9-35 20858484-7 2010 Moreover nuclear factor (NF)-kappaB and other transcription factors like CREB, ATF-2 involved in tumour development and angiogenesis were also inhibited by harmine. Harmine 156-163 cAMP responsive element binding protein 1 Mus musculus 73-77 20858484-7 2010 Moreover nuclear factor (NF)-kappaB and other transcription factors like CREB, ATF-2 involved in tumour development and angiogenesis were also inhibited by harmine. Harmine 156-163 activating transcription factor 2 Mus musculus 79-84 20858484-11 2010 Production of other factors by tumour cells which are involved in angiogenesis like cyclooxygenase (COX-2), inducible nitric oxide synthase (iNOS) and matrix metalloproteases (MMPs) were also decrease by the treatment with harmine. Harmine 223-230 cytochrome c oxidase II, mitochondrial Mus musculus 100-105 20858484-11 2010 Production of other factors by tumour cells which are involved in angiogenesis like cyclooxygenase (COX-2), inducible nitric oxide synthase (iNOS) and matrix metalloproteases (MMPs) were also decrease by the treatment with harmine. Harmine 223-230 nitric oxide synthase 2, inducible Mus musculus 108-139 21150338-5 2010 The SOD and CAT activities increased with acute and chronic treatments with imipramine and harmine, compared to control group in prefrontal cortex and hippocampus. Harmine 91-98 catalase Rattus norvegicus 12-15 19796173-0 2009 Harmine specifically inhibits protein kinase DYRK1A and interferes with neurite formation. Harmine 0-7 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 45-51 19772900-6 2010 Interestingly, treatment with harmine reversed anhedonia, the increase of adrenal gland weight, normalized ACTH circulating levels and BDNF protein levels. Harmine 30-37 brain-derived neurotrophic factor Rattus norvegicus 135-139 20036304-8 2010 Inhibition of MAO-A by seed extracts was quantitatively attributed to harmaline and harmine whereas inhibition by root extracts came from harmine with no additional interferences. Harmine 84-91 monoamine oxidase A Homo sapiens 14-19 19548284-6 2010 Harmine reduced resistance to the anticancer drugs mitoxantrone and camptothecin mediated by BCRP and might be an interesting new reversal agent. Harmine 0-7 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 93-97 19632287-0 2009 Acute harmine administration induces antidepressive-like effects and increases BDNF levels in the rat hippocampus. Harmine 6-13 brain-derived neurotrophic factor Rattus norvegicus 79-83 19632287-3 2009 The present study aims to compare the behavioral effects and the BDNF hippocampus levels of acute administration of harmine and imipramine in rats. Harmine 116-123 brain-derived neurotrophic factor Rattus norvegicus 65-69 19632287-5 2009 Afterwards, hippocampal BDNF protein levels were assessed in imipramine- and harmine-treated rats by ELISA-sandwich assay. Harmine 77-84 brain-derived neurotrophic factor Rattus norvegicus 24-28 19632287-7 2009 Acute administration of harmine at the higher dose, but not imipramine, increased BDNF protein levels in the rat hippocampus. Harmine 24-31 brain-derived neurotrophic factor Rattus norvegicus 82-86 19586613-4 2009 This response does not require ERK1/2 or ERK5, but it is diminished by ablation of DYRK1A expression by siRNA or chemical inhibition of DYRK1A by harmine. Harmine 146-153 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 83-89 19586613-4 2009 This response does not require ERK1/2 or ERK5, but it is diminished by ablation of DYRK1A expression by siRNA or chemical inhibition of DYRK1A by harmine. Harmine 146-153 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 136-142 19796173-4 2009 Comparative in vitro assays of four kinases of the DYRK family showed that harmine inhibited substrate phosphorylation by DYRK1A more potently than it inhibited substrate phosphorylation by the closely related kinase DYRK1B [half maximal inhibitory concentrations (IC(50)) of 33 nm versus 166 nm, respectively] and by the more distant members of the family, DYRK2 and DYRK4 (1.9 microm and 80 microm, respectively). Harmine 75-82 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 51-55 19796173-4 2009 Comparative in vitro assays of four kinases of the DYRK family showed that harmine inhibited substrate phosphorylation by DYRK1A more potently than it inhibited substrate phosphorylation by the closely related kinase DYRK1B [half maximal inhibitory concentrations (IC(50)) of 33 nm versus 166 nm, respectively] and by the more distant members of the family, DYRK2 and DYRK4 (1.9 microm and 80 microm, respectively). Harmine 75-82 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 122-128 19796173-4 2009 Comparative in vitro assays of four kinases of the DYRK family showed that harmine inhibited substrate phosphorylation by DYRK1A more potently than it inhibited substrate phosphorylation by the closely related kinase DYRK1B [half maximal inhibitory concentrations (IC(50)) of 33 nm versus 166 nm, respectively] and by the more distant members of the family, DYRK2 and DYRK4 (1.9 microm and 80 microm, respectively). Harmine 75-82 dual specificity tyrosine phosphorylation regulated kinase 1B Homo sapiens 217-223 19796173-4 2009 Comparative in vitro assays of four kinases of the DYRK family showed that harmine inhibited substrate phosphorylation by DYRK1A more potently than it inhibited substrate phosphorylation by the closely related kinase DYRK1B [half maximal inhibitory concentrations (IC(50)) of 33 nm versus 166 nm, respectively] and by the more distant members of the family, DYRK2 and DYRK4 (1.9 microm and 80 microm, respectively). Harmine 75-82 dual specificity tyrosine phosphorylation regulated kinase 2 Homo sapiens 358-363 19796173-4 2009 Comparative in vitro assays of four kinases of the DYRK family showed that harmine inhibited substrate phosphorylation by DYRK1A more potently than it inhibited substrate phosphorylation by the closely related kinase DYRK1B [half maximal inhibitory concentrations (IC(50)) of 33 nm versus 166 nm, respectively] and by the more distant members of the family, DYRK2 and DYRK4 (1.9 microm and 80 microm, respectively). Harmine 75-82 dual specificity tyrosine phosphorylation regulated kinase 4 Homo sapiens 368-373 19796173-5 2009 Much higher concentrations of harmine were required to suppress tyrosine autophosphorylation of the translational intermediate of DYRK1A in a bacterial in vitro translation system (IC(50) = 1.9 microm). Harmine 30-37 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 130-136 19796173-6 2009 Importantly, harmine inhibited the phosphorylation of a specific substrate by DYRK1A in cultured cells with a potency similar to that observed in vitro (IC(50) = 48 nm), without negative effects on the viability of the cells. Harmine 13-20 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 78-84 19796173-9 2009 In summary, our data show that harmine inhibits DYRK1A substrate phosphorylation more potently than it inhibits tyrosine autophosphorylation, and provide evidence for a role of DYRK1A in the regulation of neurite formation. Harmine 31-38 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 48-54 19796173-9 2009 In summary, our data show that harmine inhibits DYRK1A substrate phosphorylation more potently than it inhibits tyrosine autophosphorylation, and provide evidence for a role of DYRK1A in the regulation of neurite formation. Harmine 31-38 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 177-183 19844572-7 2009 Moreover, these effects were abolished by treatment with harmine, the most potent and specific inhibitor of Dyrk1a. Harmine 57-64 dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1a Mus musculus 108-114 19372220-7 2009 Similarly, treatment of cardiomyocytes with harmine, a specific inhibitor of DYRK1A, revealed cardiomyocyte hypertrophy on morphological and molecular level. Harmine 44-51 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 77-83