克拉斯
癌症研究
病毒癌基因
突变体
药物发现
癌症
GTP酶
医学
药理学
生物
生物信息学
内科学
结直肠癌
细胞生物学
生物化学
基因
作者
Lala S. Rathod,Pratap S. Dabhade,Santosh N. Mokale
标识
DOI:10.1016/j.drudis.2023.103557
摘要
KRASG12C has been identified as a potential target in the treatment of solid tumors. One of the most often transformed proteins in human cancers is the small Kirsten rat sarcoma homolog (KRAS) subunit of GTPase, which is typically the oncogene driver. KRASG12C is altered to keep the protein in an active GTP-binding form. KRAS has long been considered an 'undrugable' target, but sustained research efforts focusing on the KRASG12C mutant cysteine have achieved promising results. For example, the US Food and Drug Administration (FDA) has passed emergency approval for sotorasib and adagrasib for the treatment of metastatic lung cancer. Such achievements have sparked several original approaches to KRASG12C. In this review, we focus on the design, development, and history of KRASG12C inhibitors.
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