Discovery of novel heteroaryl alkynes for highly potent KIT^(D816V) cells inhibition to treat gastrointestinal stromal tumors

作     者：Zhicheng Xie Lin Li Yihao Guo Mi Zhang Taiwen Chen Yongpeng Li Xin Li Xi Zhu Yu Zhang Liguang Lou Youhong Hu 

作者机构：State Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China University of Chinese Academy of SciencesBeijing 100049China School of Chinese Materia MedicaNanjing University of Chinese MedicineNanjing 210023China School of Pharmaceutical Science and TechnologyHangzhou Institute for Advanced StudyUCASHangzhou 310024China 

出 版 物：《Acta Pharmaceutica Sinica B》 (药学学报（英文版）)

年 卷 期：2022年第12卷第10期

页      面：4004-4007页

核心收录：

学科分类：1002[医学-临床医学] 100214[医学-肿瘤学] 10[医学] 

基　　金：supported by grants from Shanghai Municipal Science and Technology Major Project(TM202101H012,China) the Science and Technology Commission of Shanghai Municipality(No.18DZ2293200,China) the Yunnan Province Sciences and Technology plan(No.202102AA310026,China) 

主　　题：KIT^(D816V)cells Mutation Drug resistance Gastrointestinal stromal tumors 

摘      要：To the Editor:Gastrointestinal stromal tumors(GIST)is the most popular mesenchymal tumor in the gastrointestinal tract with approximately 80%of GIST harboring gain-of-function mutations at either the extracellular region(exon 9)or the juxtamembrane domain(JMD,exon 11)of KIT,resulting in uncontrolled proliferation and resistance to apotosis1.