1pyn

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Template:STRUCTURE 1pyn

DUAL-SITE POTENT, SELECTIVE PROTEIN TYROSINE PHOSPHATASE 1B INHIBITOR USING A LINKED FRAGMENT STRATEGY AND A MALONATE HEAD ON THE FIRST SITE


Overview

A salicylate second site binder was linked to three classes of phosphotyrosine mimetics to produce potent protein tyrosine phosphatase 1B (PTP1B) inhibitors which exhibit significant selectivity against other phosphatases including the most homologous member, TCPTP.

About this Structure

1PYN is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Discovery and SAR of novel, potent and selective protein tyrosine phosphatase 1B inhibitors., Pei Z, Li X, Liu G, Abad-Zapatero C, Lubben T, Zhang T, Ballaron SJ, Hutchins CW, Trevillyan JM, Jirousek MR, Bioorg Med Chem Lett. 2003 Oct 6;13(19):3129-32. PMID:12951078 Page seeded by OCA on Sat May 3 05:39:01 2008

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