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New progress in leukemia drug research based on the new target of BET BD2

 Last Update: 2022-04-21
 Source: Internet
 Author: User

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Acute Myeloid Leukemia (AML) is a malignant proliferative disease of myeloid primitive progenitor cells of the hematopoietic system

Recently, the team of Xu Yong from the Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences reported a series of BET BD2 inhibitors with high binding activity and high selectivity, which can be used as anti-AML drug candidates .

BET (Bromodomain and Extra-Terminal Domain) family members include BRD2, BRD3, BRD4 and BRDT, each family member has two N-terminal tandem bromodomains (BD1 and BD2)

In this study, a structure-based drug design strategy was adopted, combined with structural biology research to conduct an in-depth discussion of the structure-activity relationship, and finally a compound XY153 (8l) with good drugability was obtained

Xu Yong's team has long been committed to the research of BET small molecule inhibitors and has achieved systematic results (J.

Paper link

Research on anti-leukemia drugs targeting BET BD2 bromodomain

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