Department of Oncology, Nanjing Hospital of Chinese Medicine Affiliated to Nanjing University of Chinese Medicine, Nanjing, China.
Pathol Oncol Res. 2021 Apr 23;27:631095. doi: 10.3389/pore.2021.631095. eCollection 2021.
KRAS mutations have long been considered undruggable. However, a series of direct KRAS mutation inhibitors have been developed since the switch II pocket was discovered recently. This review will summarize progress in the development of direct KRAS G12C mutation inhibitors, current relevant drugs under study and challenges that need to be considered in future research.
KRAS 突变长期以来被认为是不可成药的。然而,自从最近发现开关 II 口袋以来,已经开发出了一系列直接的 KRAS 突变抑制剂。这篇综述将总结直接 KRAS G12C 突变抑制剂的开发进展,目前正在研究的相关药物以及未来研究中需要考虑的挑战。