1q1m

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[[Image:1q1m.jpg|left|200px]]
[[Image:1q1m.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1q1m |SIZE=350|CAPTION= <scene name='initialview01'>1q1m</scene>, resolution 2.60&Aring;
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The line below this paragraph, containing "STRUCTURE_1q1m", 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=234:5-{2-FLUORO-5-[3-(3-HYDROXY-2-METHOXYCARBONYL-PHENOXY)-PROPENYL]-PHENYL}-ISOXAZOLE-3-CARBOXYLIC+ACID'>234</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_1q1m| PDB=1q1m | 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=1q1m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1q1m OCA], [http://www.ebi.ac.uk/pdbsum/1q1m PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1q1m RCSB]</span>
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}}
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'''A Highly Efficient Approach to a Selective and Cell Active PTP1B inhibitors'''
'''A Highly Efficient Approach to a Selective and Cell Active PTP1B inhibitors'''
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[[Category: Xin, Z.]]
[[Category: Xin, Z.]]
[[Category: Zhao, H.]]
[[Category: Zhao, H.]]
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[[Category: inhibitors with isoxazole-salicylate pharmacophore]]
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[[Category: Inhibitors with isoxazole-salicylate pharmacophore]]
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[[Category: protein tyrosine phosphatase 1b]]
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[[Category: Protein tyrosine phosphatase 1b]]
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[[Category: ptp1b]]
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[[Category: Ptp1b]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 05:45:19 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:07:37 2008''
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Revision as of 02:45, 3 May 2008

Image:1q1m.jpg

Template:STRUCTURE 1q1m

A Highly Efficient Approach to a Selective and Cell Active PTP1B inhibitors


Overview

Using an NMR-based fragment screening and X-ray crystal structure-based assembly, starting with millimolar ligands for both the catalytic site and the second phosphotyrosine binding site, we have identified a small-molecule inhibitor of protein tyrosine phosphatase 1B with low micromolar inhibition constant, high selectivity (30-fold) over the highly homologous T-cell protein tyrosine phosphatase, and good cellular activity in COS-7 cells.

About this Structure

1Q1M is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Fragment screening and assembly: a highly efficient approach to a selective and cell active protein tyrosine phosphatase 1B inhibitor., Liu G, Xin Z, Pei Z, Hajduk PJ, Abad-Zapatero C, Hutchins CW, Zhao H, Lubben TH, Ballaron SJ, Haasch DL, Kaszubska W, Rondinone CM, Trevillyan JM, Jirousek MR, J Med Chem. 2003 Sep 25;46(20):4232-5. PMID:13678400 Page seeded by OCA on Sat May 3 05:45:19 2008

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OCA

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