机构：[1]Department of Dermatology and Department of Pharmacy, West China Hospital, Sichuan University, Chengdu, Sichuan 610041, P. R. China.四川大学华西医院[2]Laboratory of Dermatology, Clinical Institute of Inflammation and Immunology (CIII), Frontiers Science Center for Disease-related Molecular Network and State Key Laboratory of Biotherapy, West China Hospital, Sichuan University and Collaborative Innovation Center of Biotherapy, Chengdu 610041, China.四川大学华西医院[3]West China School of Public Health, Sichuan University, Chengdu, Sichuan 610041, P. R. China.
In recent years, substantial research has been conducted on molecular mechanisms and inhibitors targeting bromodomains (BRDs) and extra-terminal (BET) family proteins. On this basis, non-BET BRD is gradually becoming a research hot spot. BRDs are abundant in histone acetyltransferase (HAT)-associated activating transcription factors, and BRD-containing HATs have been linked to cancer, inflammation, and viral replication. Therefore, the development of BRD-containing HATs as chemical probes is useful for understanding the specific biological roles of BRDs in diseases and drug discovery. Several types of BRD-containing HATs, including CBP/P300, PCAF/GCN5, and TAF1, are discussed in this context in terms of their structures, functions, and small-molecule inhibitors. Additionally, progress in BRD inhibitors/chemical probes and proteolysis targeting chimeras in terms of drug design, biological activity, and disease application are summarized. These findings provide insights into the development of BRD inhibitors as potential drug candidates for various diseases.
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外文
PubmedID：
中科院(CAS)分区：
出版当年[2023]版：
大类|1 区医学
小类|1 区药物化学
最新[2023]版：
大类|1 区医学
小类|1 区药物化学
第一作者：
第一作者机构：[1]Department of Dermatology and Department of Pharmacy, West China Hospital, Sichuan University, Chengdu, Sichuan 610041, P. R. China.[2]Laboratory of Dermatology, Clinical Institute of Inflammation and Immunology (CIII), Frontiers Science Center for Disease-related Molecular Network and State Key Laboratory of Biotherapy, West China Hospital, Sichuan University and Collaborative Innovation Center of Biotherapy, Chengdu 610041, China.
共同第一作者：
通讯作者：
通讯机构：[1]Department of Dermatology and Department of Pharmacy, West China Hospital, Sichuan University, Chengdu, Sichuan 610041, P. R. China.[2]Laboratory of Dermatology, Clinical Institute of Inflammation and Immunology (CIII), Frontiers Science Center for Disease-related Molecular Network and State Key Laboratory of Biotherapy, West China Hospital, Sichuan University and Collaborative Innovation Center of Biotherapy, Chengdu 610041, China.
推荐引用方式(GB/T 7714)：
Liu Mingxia,Zhang Kaiyao,Li Qinjue,et al.Recent Advances on Small-Molecule Bromodomain-Containing Histone Acetyltransferase Inhibitors[J].Journal of medicinal chemistry.2023,doi:10.1021/acs.jmedchem.2c01638.
APA：
Liu Mingxia,Zhang Kaiyao,Li Qinjue,Pang Haiying,Pan Zhaoping...&He Gu.(2023).Recent Advances on Small-Molecule Bromodomain-Containing Histone Acetyltransferase Inhibitors.Journal of medicinal chemistry,,
MLA：
Liu Mingxia,et al."Recent Advances on Small-Molecule Bromodomain-Containing Histone Acetyltransferase Inhibitors".Journal of medicinal chemistry .(2023)
医学