Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N‑Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype - Wellaway, Christopher R; Bamborough, Paul; Bernard, Sharon G; Chung, Chun-wa; Craggs, Peter D; Cutler, Leanne; Demont, Emmanuel H; Evans, John P; Gordon, Laurie; Karamshi, Bhumika; Lewis, Antonia J; Lindon, Matthew J; et al. (Journal of medicinal chemistry, 2020)
Keywords: Animals; Anti-Inflammatory Agents - chemistry; Anti-Inflammatory Agents - metabolism; Anti-Inflammatory Agents - pharmacology; Binding Sites; Cell Cycle Proteins - antagonists & inhibitors; Cell Cycle Proteins - classification; Cell Cycle Proteins - metabolism; Cell Line, Tumor; Chemistry, Medicinal; Cytokines - metabolism; Drug Design; Half-Life; Humans; Leukocytes, Mononuclear - cytology; Leukocytes, Mononuclear - drug effects; Leukocytes, Mononuclear - metabolism; Life Sciences & Biomedicine; Male; Mice; Molecular Dynamics Simulation; Pharmacology & Pharmacy; Phylogeny; Protein Domains; Quinolones - chemistry; Quinolones - metabolism; Quinolones - pharmacology; Science & Technology; Transcription Factors - antagonists & inhibitors; Transcription Factors - classification; Transcription Factors - metabolism; POTENT; PROTEIN; CHROMATIN; SMALL-MOLECULE; OPTIMIZATION; IDENTIFICATION; RVX-208; DISCOVERY; FAMILY; BRD4