2h04

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2h04, resolution 2.300Å

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Structural studies of protein tyrosine phosphatase beta catalytic domain in complex with inhibitors

Overview

The sulfamic acid phosphotyrosine mimetic was coupled with a previously, known malonate template to obtain highly selective and potent inhibitors, of HPTPbeta. Potentially hydrolyzable malonate ester functionalities were, replaced with 1,2,4-oxadiazoles without a significant effect on HPTPbeta, potency.

About this Structure

2H04 is a Single protein structure of sequence from Homo sapiens with 4UN as ligand. Active as Protein-tyrosine-phosphatase, with EC number 3.1.3.48 Full crystallographic information is available from OCA.

Reference

Design and synthesis of potent, non-peptidic inhibitors of HPTPbeta., Amarasinghe KK, Evidokimov AG, Xu K, Clark CM, Maier MB, Srivastava A, Colson AO, Gerwe GS, Stake GE, Howard BW, Pokross ME, Gray JL, Peters KG, Bioorg Med Chem Lett. 2006 Aug 15;16(16):4252-6. Epub 2006 Jun 12. PMID:16759857

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