期刊论文

Huang, W.;Hao, G.-F.;Yang, G.-F.

英文

European Journal of Medicinal Chemistry

0223-5234

2022

237

114406

10.1016/j.ejmech.2022.114406

This work was supported by the National Key Research and Development Program of China ( 2021YFD1700102 ), the National Natural Science Foundation of China ( 32125033 and 31960548 ). Program of Introducing Talents of Discipline to Universities of China (111 Program, D20023), the Key Research and Development Program of Hubei Province , China ( 2020BCB042 ), and the Science and Technology Program of Wuhan (No. 2019020701011460 ).

本校为第一机构

Mutation-induced resistance to targeted drug treatment poses a serious threat to successful chemotherapy. Multiple mutations underlying drug resistance remain a largely unsolved scientific issue. Tropomyosin receptor kinases (TRKs) are promising therapeutic targets for several malignant human cancers, but they have become less effective due to multiple resistance mutations. Thus, TRKs are representative cases to explore the problem of multiple resistance mutations. Here, we proposed a conformational adjustment strategy of drug design to overcom...