Design, synthesis, and biological evaluation of Bcr-Abl PROTACs to overcome T315I mutation

Design, synthesis, and biological evaluation of Bcr-Abl PROTACs to overcome T315I mutation

Bcr-Abl threonine 315 to isoleucine 315 (T315I) gatekeeper mutation induced drug resistance remains an unmet clinical challenge for the treatment of chronic myeloid leukemia (CML). Chemical degradation of Bcr-AblT315I protein has become a potential strategy to overcome drug resistance. Herein, we fi...

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Bibliographic Details
Main Authors: Liang Jiang, Yuting Wang, Qian Li, Zhengchao Tu, Sihua Zhu, Sanfang Tu, Zhang Zhang, Ke Ding, Xiaoyun Lu
Format: Article
Language:English
Published: Elsevier 2021-05-01
Series:Acta Pharmaceutica Sinica B
Subjects:
CML
PROTAC
Degradation
T315I mutation
Clinical resistance
Online Access:http://www.sciencedirect.com/science/article/pii/S2211383520307991

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http://www.sciencedirect.com/science/article/pii/S2211383520307991

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