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Allosteric Inhibitors of SHP2: An Updated Patent Review (2015-2020)

文献类型：期刊论文

作者Wu, Jingwei1; Zhang, Huan2; Zhao, Guilong3,4; Wang, Runling1
刊名CURRENT MEDICINAL CHEMISTRY
出版日期2021
卷号28期号:19页码:3825-3842
关键词SHP2 inhibitor PTPN11 gene allosteric cancer combination therapy clinical trial
ISSN号0929-8673
DOI10.2174/1568011817666200928114851
通讯作者Zhao, Guilong(zhao_guilong@126.com) ; Wang, Runling(grunling@tmu.edu.cn)
英文摘要Srchomology-2-domain-containing PTP 2 (SHP2) is a nonreceptor phosphatase encoded by the PTPN11 gene. Over expression of SHP2 is associated with various human diseases, such as Noonan syndrome, LEOPARD syndrome, and cancers. To overcome the shortcomings of existing orthosteric inhibitors, novel inhibitors targeting the allosteric site of SHP2 with high selectivity and low toxicity are under development. This paper reviews allosteric inhibitors of SHP2 published in patents from 2015 to 2020. The molecules are classified according to the chemical structure of the central core. SHP2 has long been considered as an 'undruggable' protein. Fortunately, a critical breakthrough was made by researchers from Novartis AG Ltd., who identified SHP099 as a highly potent, selective, soluble, and orally bioavailable SHP2 allosteric inhibitor. Currently, there are several allosteric inhibitors of SHP2 in clinical development. However, drug resistance is still a major challenge. The combination of SHP2 allosteric inhibitors and immunotherapy drugs or molecular targeted drugs is emerging as a promising therapeutic strategy against drug resistance.
WOS关键词PROTEIN-TYROSINE PHOSPHATASES ; 1B PTP1B INHIBITORS ; RHEUMATOID-ARTHRITIS ; DOMAIN ; IDENTIFICATION ; ASSOCIATION ; EXPRESSION ; INSIGHTS ; PTPN22 ; DRIVEN
资助项目National Natural Science Foundation of China[81773569]
WOS研究方向Biochemistry & Molecular Biology ; Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000663836500007
出版者BENTHAM SCIENCE PUBL LTD
源URL[http://119.78.100.183/handle/2S10ELR8/296837]  
专题新药研究国家重点实验室
通讯作者Zhao, Guilong; Wang, Runling
作者单位1.Tianjin Med Univ, Sch Pharm, Tianjin Key Lab Technol Enabling Dev Clin Therape, 22 Qixiangtai Rd, Tianjin 300070, Peoples R China
2.Tianjin Med Univ, Dept Pharm, Gen Hosp, Tianjin 300052, Peoples R China
3.Chinese Acad Sci, Inst Drug Discovery & Dev, Zhongshan 528400, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Wu, Jingwei,Zhang, Huan,Zhao, Guilong,et al. Allosteric Inhibitors of SHP2: An Updated Patent Review (2015-2020)[J]. CURRENT MEDICINAL CHEMISTRY,2021,28(19):3825-3842.
APA Wu, Jingwei,Zhang, Huan,Zhao, Guilong,&Wang, Runling.(2021).Allosteric Inhibitors of SHP2: An Updated Patent Review (2015-2020).CURRENT MEDICINAL CHEMISTRY,28(19),3825-3842.
MLA Wu, Jingwei,et al."Allosteric Inhibitors of SHP2: An Updated Patent Review (2015-2020)".CURRENT MEDICINAL CHEMISTRY 28.19(2021):3825-3842.

入库方式： OAI收割

来源：上海药物研究所

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