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BET inhibitor
BET inhibitors are a class of drugs with anti-cancer, immunosuppressive, and other effects in clinical trials in the United States and Europe and widely used in research. These molecules reversibly bind the bromodomains of Bromodomain and Extra-Terminal motif (BET) proteins BRD2, BRD3, BRD4, and BRDT, and prevent protein-protein interaction between BET proteins and acetylated histones and transcription factors.
== Discovery and development ==
Thienodiazepine BET inhibitors were discovered by scientists at Yoshitomi Pharmaceuticals (now Mitsubishi Tanabe Pharma) in the early 1990s, and their potential both as anti-inflammatories and anti-cancer agents noted. However, these molecules remained largely unknown until 2010 when both the use of JQ1 in NUT midline carcinoma and of I-BET 762 in sepsis were published. Since this time a number of molecules have been described that are capable of targeting BET bromodomains.
BET inhibitors have been described that are able to discriminate between the first and second bromodomains of BET proteins (BD1 vs BD2). However, no BET inhibitor has yet been described that can reliably distinguish between BET family members (BRD2 vs BRD3 vs BRD4 vs BRDT). Only in the research context has targeting individual BET proteins been achieved by mutating them to be more sensitive to a derivative of JQ1 / I-BET 762.〔Baud M.G., Lin-Shiao E., Cardote T., Tallant C., Pschibul A., Chan K.H., Zengerle M., Garcia J.R., Kwan T.T., Ferguson F.M., Ciulli A. (2014) A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes. ''Science''. 2014 Oct 31;346(6209):638-41. PMID 25323695〕
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
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