1qxk
From Proteopedia
|
Monoacid-Based, Cell Permeable, Selective Inhibitors of Protein Tyrosine Phosphatase 1B
Contents |
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.
Disease
Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[176885], Insulin resistance, susceptibility to OMIM:[176885]
About this Structure
1QXK is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Protein-tyrosine-phosphatase, with EC number 3.1.3.48 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 Thu Feb 21 14:44:50 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. | 429 | Protein tyrosine phosphatase 1b | Ptp1b monoacid-based and cell permeable
