2h02 | pdb_00002h02

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

File:2h02.gif


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2h02, resolution 2.300Å
Ligands: 2UN
Gene: PTPRB (Homo sapiens)
Activity: Protein-tyrosine-phosphatase, with EC number 3.1.3.48
Related: 2HO3, 2HO4


Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



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

2H02 is a Single protein structure of sequence from Homo sapiens. 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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