可药性
磷酸酶
激酶
癌症
蛋白磷酸酶2
磷酸化
抑制器
药物发现
原癌基因酪氨酸蛋白激酶Src
生物
PTPN11型
癌症研究
计算生物学
生物化学
遗传学
基因
结直肠癌
克拉斯
作者
Julia P. Vainonen,Majid Momeny,Jukka Westermarck
出处
期刊:Science Translational Medicine
[American Association for the Advancement of Science (AAAS)]
日期:2021-04-07
卷期号:13 (588)
被引量:55
标识
DOI:10.1126/scitranslmed.abe2967
摘要
The phosphorylation status of oncoproteins is regulated by both kinases and phosphatases. Kinase inhibitors are rarely sufficient for successful cancer treatment, and phosphatases have been considered undruggable targets for cancer drug development. However, innovative pharmacological approaches for targeting phosphatases have recently emerged. Here, we review progress in the therapeutic targeting of oncogenic Src homology region 2 domain-containing phosphatase-2 (SHP2) and tumor suppressor protein phosphatase 2A (PP2A) and select other druggable oncogenic and tumor suppressor phosphatases. We describe the modes of action for currently available small molecules that target phosphatases, their use in drug combinations, and advances in clinical development toward future cancer therapies.
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