1qxk
From Proteopedia
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| , resolution 2.30Å | |||||||
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| Ligands: | |||||||
| Gene: | PTPN1 OR PTP1B (Homo sapiens) | ||||||
| Activity: | Protein-tyrosine-phosphatase, with EC number 3.1.3.48 | ||||||
| Related: | 1NL9, 1NNY, 1NO6, 1NZ7, 1ONY, 1PHO
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Monoacid-Based, Cell Permeable, Selective Inhibitors of Protein Tyrosine Phosphatase 1B
Overview
Monoacid-based PTP1B inhibitors with improved physiochemical properties have been investigated. A (2-hydroxy-phenoxy) acetic acid-based phosphotyrosyl mimetic has been linked with an optimized second arylphosphate binding site ligand to produce compound 20 with low micromolar potency against PTP1B, good selectivity over TCPTP (20-fold) and high cell permeability in the Caco-2 system.
About this Structure
1QXK is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B., Xin Z, Liu G, Abad-Zapatero C, Pei Z, Szczepankiewicz BG, Li X, Zhang T, Hutchins CW, Hajduk PJ, Ballaron SJ, Stashko MA, Lubben TH, Trevillyan JM, Jirousek MR, Bioorg Med Chem Lett. 2003 Nov 17;13(22):3947-50. PMID:14592481
Page seeded by OCA on Sun Mar 30 23:20:22 2008
Categories: Homo sapiens | Protein-tyrosine-phosphatase | Single protein | Abad-Zapatero, C. | Ballaron, S J. | Hajduk, P J. | Hutchins, C W. | Jirousek, M R. | Li, X. | Liu, G. | Lubben, T H. | Pei, Z. | Stashko, M A. | Szczepankiewick, B G. | Trevillyan, J M. | Xin, Z. | Zhang, T. | Protein tyrosine phosphatase 1b | Ptp1b monoacid-based and cell permeable
