激酶
酪氨酸激酶
受体酪氨酸激酶
化学
蛋白激酶A
原癌基因蛋白质c-ret
癌症研究
生物
生物化学
受体
神经营养因子
胶质细胞源性神经生长因子
作者
Congcong Jia,Wang Chen,Zijian Feng,Zhaopeng Liu
出处
期刊:Future Medicinal Chemistry
[Newlands Press Ltd]
日期:2021-01-01
卷期号:13 (1): 45-62
被引量:12
标识
DOI:10.4155/fmc-2020-0170
摘要
RET is a proto-oncogene encoding a receptor tyrosine kinase. RET regulates key aspects of cellular proliferation, differentiation and survival. The activation of RET via gene fusions or point mutations is closely related to lung, thyroid and other cancers. This review summarizes the developments of a diversity of small molecule RET protein kinase inhibitors in the past 10 years. These RET inhibitors are classified according to their hinge binder chemotypes as: pyrimidines, including the pyrazolopyrimidines, pyrimidine oxazines, quinazolines, 4-aminopyrimidines and 4-aminopyridines; indolinones; 5-aminopyrazole-4-carboxamides; 3-trifluoromethylanilines; imidazopyridines, imidazopyridazines and pyrazopyridines; nicotinonitriles; pyridones and 1,2,4-triazoles. In each section, the biological activities of the inhibitors, their structure–activity relationships and possible binding modes with the RET kinase are introduced.
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