1pyn | pdb_00001pyn
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| 1pyn, resolution 2.20Å | |||||||||||||
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| Ligands: | 941 | ||||||||||||
| Gene: | PTPN1 OR PTP1B (Homo sapiens) | ||||||||||||
| Activity: | Protein-tyrosine-phosphatase, with EC number 3.1.3.48 | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
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.
Disease
Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[176885], Insulin resistance, susceptibility to OMIM:[176885]
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 Thu Mar 20 13:30:41 2008
