Chemical probes and inhibitors of bromodomains outside the BET family

摘要: In the last five years, development of inhibitors bromodomains has emerged as an area intensive worldwide research. Emerging evidence implicated a number non-BET in onset and progression diseases such cancer, HIV infection inflammation. The use small molecule chemical probes been fundamental to pre-clinical evaluation targets. Recent efforts are described highlighting potent, selective cell active bromodomain their therapeutic potential. Over half typical now have reported ligands, but those with atypical binding site residues remain resistant probe discovery efforts.