| Structural highlights
1qxk is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
| | Ligands: |
| | Related: | 1nl9, 1nny, 1no6, 1nz7, 1ony, 1pho |
| Gene: | PTPN1 OR PTP1B (Homo sapiens) |
| Activity: | Protein-tyrosine-phosphatase, with EC number 3.1.3.48 |
| Resources: | FirstGlance, OCA, RCSB, PDBsum |
Evolutionary Conservation
Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.
Publication Abstract from PubMed
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.
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[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ 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. Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B. Bioorg Med Chem Lett. 2003 Nov 17;13(22):3947-50. PMID:14592481
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