Substrate-based fragment identification for the development of selective, nonpeptidic inhibitors of striatal-enriched protein tyrosine phosphatase

…, M Chatterjee, AC Nairn, PJ Lombroso…

Index: Baguley, Tyler D.; Xu, Hai-Chao; Chatterjee, Manavi; Nairn, Angus C.; Lombroso, Paul J.; Ellman, Jonathan A. Journal of Medicinal Chemistry, 2013 , vol. 56, # 19 p. 7636 - 7650

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Citation Number: 9

Abstract

High levels of striatal-enriched protein tyrosine phosphatase (STEP) activity are observed in a number of neuropsychiatric disorders such as Alzheimer's disease. Overexpression of STEP results in the dephosphorylation and inactivation of many key neuronal signaling molecules, including ionotropic glutamate receptors. Moreover, genetically reducing STEP levels in AD mouse models significantly reversed cognitive deficits and decreased ...