小分子
酪氨酸激酶
受体酪氨酸激酶
肝细胞生长因子
C-Met公司
癌症研究
激酶
生物
药理学
化学
受体
细胞生物学
生物化学
作者
Cilong Chu,Zixuan Rao,Qingshan Pan,Wufu Zhu
标识
DOI:10.1080/13543776.2022.2008356
摘要
c-Met tyrosine kinase receptor is a high-affinity ligand of hepatocyte growth factor (HGF). c-Met is widely expressed in a variety of normal human tissues, but shows abnormally high expression, amplification or mutation in tumour tissues such as lung, gastric and breast cancers. Therefore, the use of c-Met as a target can achieve the inhibition of a series of abnormal physiological processes such as tumourigenesis, development and metastasis. A number of small molecule tyrosine kinase inhibitors targeting c-Met have been successfully marketed.This article reviews recent advances in patented c-Met small molecule inhibitors and their inhibitory activity against various cancer cells from 2018 to date.To date, small molecule inhibitors targeting c-Met have demonstrated impressive therapeutic efficacy in the clinical setting. Most recent patents have focused on addressing the direction of c-Met amplification and overexpression. Despite the great success in the development of selective c-Met inhibitors, the effects of bypass secretion and mutagenesis have led to a need for new c-Met small molecule inhibitors that are safe, efficient, selective and less toxic with novel structures and effective against other targets.
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