PMID: 25732788Mar 4, 2015Paper

Small-molecule BET inhibitors in clinical and preclinical development and their therapeutic potential

Current Topics in Medicinal Chemistry
Lei YuKe Ding

Abstract

Lysine acetylation is a pivotal mechanism in chromatin processes and the regulation of gene transcription. The acetylated lysine residues of histones are exclusively recognized by bromodomains (BRDs) known as epigenetic reader. Proteins containing BRDs undergo a post-translational modification (PTM) with development of cellular signaling and disease biology. The bromo and extra-terminal (BET) proteins are the second subfamily, which play important roles in cellular proliferation, cell cycle progression and chromatin compaction. Recently, a variety of small molecules have been reported to interact with the BET family proteins and accelerate the validation of BET proteins as druggable targets for treatment of cancers, inflammation and related diseases. In this review, we will summarize the small-molecule inhibitors in clinical and preclinical studies of the BET family bromodomains and their medicinal implications.

Citations

Nov 18, 2015·Journal of Medicinal Chemistry·Frank Anthony RomeroSteven Magnuson
Oct 23, 2016·Drug Discovery Today. Technologies·Wylie S Palmer
Oct 23, 2016·Drug Discovery Today. Technologies·Srimoyee Ghosh, Jose M Lora
Feb 15, 2017·Journal of Medicinal Chemistry·Zhiqing LiuJia Zhou
Apr 24, 2020·Circulation Research·Patricia Cristine BorckJorge Plutzky
Apr 27, 2016·Current Opinion in Clinical Nutrition and Metabolic Care·Dashzeveg Bayarsaihan
Jul 1, 2020·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Jiaqi WangSu Zeng
Apr 13, 2021·Journal of Biomedical Science·Kunal Nepali, Jing-Ping Liou
May 15, 2021·Cold Spring Harbor Molecular Case Studies·Alexandre BazinetFrançois E Mercier
Oct 29, 2017·Advanced Drug Delivery Reviews·Caroline L WilsonLee A Borthwick

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