Article
PCC0208023, a potent SHP2 allosteric inhibitor, imparts an antitumor effect against KRAS mutant colorectal cancer.
Toxicology and applied pharmacology - 1 Jul 2020
Chen Xiao, Zou Fangxia, Hu Zhengping, Du Guangying, Yu Pengfei, Wang Wenyan, Wang Hongbo, Ye Liang, Tian Jingwei
Abstract excerpt
The non-receptor tyrosine phosphatase SHP2, encoded by PTPN11, plays an indispensable role in tumors driven by oncogenic KRAS mutations, which frequently occur in colorectal cancer. Here, PCC0208023, a potent SHP2 allosteric inhibitor, was synthesized to evaluate its inhibitory effects against the SHP2 enzyme, and the KRAS mutant colorectal cancer in vitro and in vivo, and its impart on the RAS/MAPK pathway....
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