A potent and selective small-molecule inhibitor for the lymphoid-specific tyrosine phosphatase (LYP), a target associated with autoimmune diseases

…, S Liu, A Menon, S Stanford, E Oppong…

Index: He, Yantao; Liu, Sijiu; Menon, Ambili; Stanford, Stephanie; Oppong, Emmanuel; Gunawan, Andrea M.; Wu, Li; Wu, Dennis J.; Barrios, Amy M.; Bottini, Nunzio; Cato, Andrew C. B.; Zhang, Zhong-Yin Journal of Medicinal Chemistry, 2013 , vol. 56, # 12 p. 4990 - 5008

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Citation Number: 23

Abstract

Lymphoid-specific tyrosine phosphatase (LYP), a member of the protein tyrosine phosphatase (PTP) family of signaling enzymes, is associated with a broad spectrum of autoimmune diseases. Herein we describe our structure-based lead optimization efforts within a 6-hydroxy-benzofuran-5-carboxylic acid series culminating in the identification of compound 8b, a potent and selective inhibitor of LYP with a K i value of 110 nM and more ...