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Inhibitor Binding Sites in the Protein Tyrosine Phosphatase SHP-2

[ Vol. 20 , Issue. 11 ]

Author(s):

Haonan Zhang, Zhengquan Gao, Chunxiao Meng*, Xiangqian Li* and Dayong Shi*   Pages 1017 - 1030 ( 14 )

Abstract:


Protein tyrosine phosphatase 2 (SHP-2) has long been proposed as a cancer drug target. Several small-molecule compounds with different mechanisms of SHP-2 inhibition have been reported, but none are commercially available. Pool selectivity over protein tyrosine phosphatase 1 (SHP-1) and a lack of cellular activity have hindered the development of selective SHP-2 inhibitors. In this review, we describe the binding modes of existing inhibitors and SHP-2 binding sites, summarize the characteristics of the sites involved in selectivity, and identify the suitable groups for interaction with the binding sites.

Keywords:

PTP, SHP-2, SHP-1, protein tyrosine kinases, PTKs, cancer.

Affiliation:

School of Life Sciences, Shandong University of Technology, Zibo 255049, Shandong Province, School of Life Sciences, Shandong University of Technology, Zibo 255049, Shandong Province, School of Life Sciences, Shandong University of Technology, Zibo 255049, Shandong Province, State Key Laboratory of Microbial Technology, Shandong University, Jinan, 250100, Shandong, State Key Laboratory of Microbial Technology, Shandong University, Jinan, 250100, Shandong



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