1qxk

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[[Image:1qxk.gif|left|200px]]
[[Image:1qxk.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1qxk |SIZE=350|CAPTION= <scene name='initialview01'>1qxk</scene>, resolution 2.30&Aring;
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The line below this paragraph, containing "STRUCTURE_1qxk", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=429:2-{4-[2-ACETYLAMINO-3-(4-CARBOXYMETHOXY-3-HYDROXY-PHENYL)-PROPIONYLAMINO]-BUTOXY}-6-HYDROXY-BENZOIC+ACID+METHYL+ESTER'>429</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Protein-tyrosine-phosphatase Protein-tyrosine-phosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.48 3.1.3.48] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= PTPN1 OR PTP1B ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_1qxk| PDB=1qxk | SCENE= }}
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|RELATEDENTRY=[[1nl9|1NL9]], [[1nny|1NNY]], [[1no6|1NO6]], [[1nz7|1NZ7]], [[1ony|1ONY]], [[1pho|1PHO]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1qxk FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1qxk OCA], [http://www.ebi.ac.uk/pdbsum/1qxk PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1qxk RCSB]</span>
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}}
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'''Monoacid-Based, Cell Permeable, Selective Inhibitors of Protein Tyrosine Phosphatase 1B'''
'''Monoacid-Based, Cell Permeable, Selective Inhibitors of Protein Tyrosine Phosphatase 1B'''
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[[Category: Xin, Z.]]
[[Category: Xin, Z.]]
[[Category: Zhang, T.]]
[[Category: Zhang, T.]]
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[[Category: protein tyrosine phosphatase 1b]]
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[[Category: Protein tyrosine phosphatase 1b]]
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[[Category: ptp1b monoacid-based and cell permeable]]
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[[Category: Ptp1b monoacid-based and cell permeable]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 06:49:21 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:20:22 2008''
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Revision as of 03:49, 3 May 2008

Template:STRUCTURE 1qxk

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 Sat May 3 06:49:21 2008

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