Exploitation of Castration-Resistant Prostate Cancer Transcription Factor Dependencies by the Novel BET Inhibitor ABBV-075

Competitive inhibitors of acetyl-lysine binding to the bromodomains of the BET (bromodomain and extra terminal) family are being developed for the treatment of solid and hematologic malignancies. The function of BET family member BRD4 at enhancers/superenhancers has been shown to sustain signal-depe...

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Veröffentlicht in:	Molecular cancer research 2017-01, Vol.15 (1), p.35-44
Hauptverfasser:	Faivre, Emily J, Wilcox, Denise, Lin, Xiaoyu, Hessler, Paul, Torrent, Maricel, He, Wei, Uziel, Tamar, Albert, Daniel H, McDaniel, Keith, Kati, Warren, Shen, Yu
Format:	Artikel
Sprache:	eng
Schlagworte:	Alternative splicing Androgen Antagonists - pharmacology Androgen receptors Animals Antiandrogens Antineoplastic Agents - pharmacology Binding Cancer Castration Cell Line, Tumor Cell Proliferation - drug effects Chromatin - metabolism Dihydrotestosterone - pharmacology Drug Resistance, Neoplasm - drug effects Enhancer Elements, Genetic - genetics Enhancers ETS protein Exploitation Fusion protein Gene expression Gene Expression Regulation, Neoplastic - drug effects Gene regulation Humans Inhibition Inhibitors Inhibitory Concentration 50 Ligands Lysine Male Mice Mutation Myc protein Phenotype Phenylthiohydantoin - analogs & derivatives Phenylthiohydantoin - pharmacology Prostate cancer Prostatic Neoplasms, Castration-Resistant - genetics Prostatic Neoplasms, Castration-Resistant - pathology Protein Domains Proteins Pyridones - pharmacology Receptors, Androgen - chemistry Receptors, Androgen - genetics Receptors, Androgen - metabolism Regulatory sequences Resistance factors Ribonucleic acid RNA Signal Transduction - drug effects Solid tumors Sulfonamides - pharmacology Transcription activation Transcription factors Transcription Factors - antagonists & inhibitors Transcription Factors - metabolism Transcription, Genetic - drug effects
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