RVX-297- a novel BD2 selective inhibitor of BET bromodomains

• Published in: Biochemical and biophysical research communications Vol. 477; no. 1; pp. 62 - 67
• Main Authors: Kharenko, Olesya A., Gesner, Emily M., Patel, Reena G., Norek, Karen, White, Andre, Fontano, Eric, Suto, Robert K., Young, Peter R., McLure, Kevin G., Hansen, Henrik C.
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 12.08.2016
• Subjects: 60 APPLIED LIFE SCIENCES; BD1 and BD2 domains; BET; BET inhibitors; binding properties; Binding Sites; BRD; Bromodomains; CALORIMETRY; CARDIOVASCULAR DISEASES; CLINICAL TRIALS; CRYSTAL STRUCTURE; CRYSTALLOGRAPHY; Crystallography, X-Ray; epigenetics; HISTONES; ITC; LYSINE; MOLECULES; pharmacokinetics; Quinazolinones - pharmacology; RVX-297; Selectivity; THERMODYNAMIC PROPERTIES; THERMODYNAMICS; TITRATION; TRANSCRIPTION; TRANSCRIPTION FACTORS; Transcription Factors - antagonists & inhibitors; Transcription Factors - chemistry; X RADIATION; X-ray diffraction; BET; BD1 and BD2 domains; BRD; Bromodomains; ITC; Selectivity; RVX-297; BET inhibitors; Crystal structure

Bromodomains are epigenetic readers that specifically bind to the acetyl lysine residues of histones and transcription factors. Small molecule BET bromodomain inhibitors can disrupt this interaction which leads to potential modulation of several disease states. Here we describe the binding propertie...