i bet762 i bet  (MedChemExpress)

Journal: Nucleic Acids Research

Article Title: Chromatin accessibility and pioneer factor FOXA1 restrict glucocorticoid receptor action in prostate cancer

doi: 10.1093/nar/gkad1126

Figure Lengend Snippet: Inhibition of p300’s enzymatic activity hinders cell proliferation and GR transcriptional regulation. ( A ) Depiction of chemical structures of coregulator inhibitors. A-485, p300/CBP histone acetyl transferase (HAT) domain inhibitor; CCS1477, p300/CBP bromodomain inhibitor; I-BET762, bromodomain and extra terminal domain (BET) bromodomain inhibitor; BRM014, BRM/BRG1 ATP domain inhibitor. (B–E) Bar graphs depict KLK3 gene expression analysis in VCaP ENZ 0 ( B ), VCaP ENZ 3w ( C ), 22Rv1 ENZ 0 ( D ), and 22Rv1 ENZ 3w ( E ) cells treated with or without Dex in the presence or absence of 0.1 or 1 μM of indicated inhibitor. Bars represent mean ± SD, n = 3. Statistical significance calculated using one-way ANOVA with Bonferroni post hoc test. (F, G) Line graphs depict change in cell proliferation as function of time in VCaP ( F ) and 22Rv1 ( G ) ENZ 0 and ENZ 3w cells with or without indicated chemical inhibitor treatment. Each data point represents mean ± SD, n = 3. Statistical significance calculated using Two-way ANOVA with Bonferroni post hoc test. * P < 0.05; ** P < 0.01; *** P < 0.001.

Article Snippet: For experiments with the coregulator inhibitors, the cells were treated with 0.1 μM or 1 μM A-485 p300/CBP HAT (Tocris, #6387), CCS1477 p300/CBP bromodomain (MedChemExpress, #HY-111784), I-BET762 BET bromodomain (Sigma, #SML1272), or BRM014 BRM/BRG1 ATP (MedChemExpress, #HY-119374) inhibitors.

Techniques: Inhibition, Activity Assay, Expressing

Journal: Aging Cell

Article Title: Strategies for senolytic drug discovery

doi: 10.1111/acel.13948

Figure Lengend Snippet: Libraries screened for senolytic activity and identified classes of senolytics.

Article Snippet: BET family protein degraders , ARV825, I‐BET151, I‐BET762, JQ1, OTX015, PFI‐1 , TAKEDA drug discovery library ( n = 47,000) , IMR‐90 fibroblasts induced by oncogenic H‐Ras expression , Wakita et al. ( ) .

Techniques: Activity Assay, Drug discovery, Expressing

Journal: Future Science OA

Article Title: Bromodomain and extra-terminal motif inhibitors: a review of preclinical and clinical advances in cancer therapy

doi: 10.4155/fsoa-2018-0115

Figure Lengend Snippet: Clinical trials of bromodomain and extra-terminal inhibitors.

Article Snippet: The safety, tolerability, pharmacokinetics, pharmacodynamics and clinical activity of BET inhibitors are currently being investigated in clinical trials for several cancers, including NMC (OTX015 [NCT02259114, developed by OncoEthix] [ ] and GSK525762/I-BET762 [NCT01587703, developed by GlaxoSmithKline]), refractory AML and elastodynamics syndrome ([NCT02308761], lymphoma [NCT01949883 for CPI-0610, developed by Constellation Pharmaceuticals], MM [NCT02157636 for CPI-0610, developed by Constellation Pharmaceuticals] and hematological malignancies [NCT01713582 for OTX015, developed by OncoEthix]).

Techniques: Clinical Proteomics