PTPN11型
蛋白质酪氨酸磷酸酶
靶向治疗
信号转导衔接蛋白
癌症
癌症治疗
癌症研究
化学
磷酸酶
计算生物学
酪氨酸
磷酸化
医学
生物
生物化学
内科学
结直肠癌
克拉斯
作者
Yihui Song,Shu Wang,Min Zhao,Xinyu Yang,Bin Yu
标识
DOI:10.1021/acs.jmedchem.1c02008
摘要
The protein tyrosine phosphatase SHP2 encoded by PTPN11 is a promising therapeutic target for cancer therapy, while the multifaceted roles of SHP2 complicate the drug discovery targeting SHP2. Given the biological significance of SHP2, strategies targeting SHP2 have been developed in recent years. To date, eight SHP2 inhibitors have advanced into clinical trials as mono- or combined therapy for treating solid tumors or adaptive resistant cancers. In this Perspective, we briefly summarize the strategies targeting SHP2 including inhibitors, activators, and proteolysis-targeting chimera (PROTAC) degraders. Besides, targeting the protein-protein interactions between SHP2 and other adaptor proteins is also discussed. Finally, we also highlight the target- and pathway-dependent combination strategies of SHP2 for cancer therapy. This Perspective may provide a timely and updated overview on the strategies targeting SHP2 for cancer therapy.
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