Recent advancement in targeting the KRAS-G12C mutant for cancer therapy / 药学学报
Acta Pharmaceutica Sinica
; (12): 374-382, 2021.
Article
in Zh
| WPRIM
| ID: wpr-873780
Responsible library:
WPRO
ABSTRACT
RAS, as a well-known proto-oncogene, is the most frequently mutated oncogene in human cancers, yet tremendous efforts over the past 30 years have failed to develop effective therapies for RAS-mutant cancer. Recently, specifically targeting the KRAS-G12C mutant, a frequently occurring KRAS mutation in human cancers, has shown promise in conquering KRAS-mutant cancers, and has inspired interest in this direction. We herein review the very recent progress achieved in the development of covalent inhibitors towards KRAS-G12C mutant, in combinational therapies and in proteolysis-targeting chimeras (PROTACs)-based approaches to disrupt KRAS-G12C protein. We provide insights for drug discovery against KRAS-G12C-mutated tumors and discuss the potential challenges in this field.
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Index:
WPRIM
Language:
Zh
Journal:
Acta Pharmaceutica Sinica
Year:
2021
Type:
Article