1xbo

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[[Image:1xbo.jpg|left|200px]]
[[Image:1xbo.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1xbo |SIZE=350|CAPTION= <scene name='initialview01'>1xbo</scene>, resolution 2.50&Aring;
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The line below this paragraph, containing "STRUCTURE_1xbo", 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=IX1:5-(3-{3-[3-HYDROXY-2-(METHOXYCARBONYL)PHENOXY]PROPENYL}PHENYL)-4-(HYDROXYMETHYL)ISOXAZOLE-3-CARBOXYLIC+ACID'>IX1</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, 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_1xbo| PDB=1xbo | SCENE= }}
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|RELATEDENTRY=[[1nl9|1NL9]], [[1nny|1NNY]], [[1no6|1NO6]], [[1nzz|1NZZ]], [[1ony|1ONY]], [[1onz|1ONZ]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1xbo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1xbo OCA], [http://www.ebi.ac.uk/pdbsum/1xbo PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1xbo RCSB]</span>
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}}
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'''PTP1B complexed with Isoxazole Carboxylic Acid'''
'''PTP1B complexed with Isoxazole Carboxylic Acid'''
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[[Category: Xin, Z.]]
[[Category: Xin, Z.]]
[[Category: Zhao, H.]]
[[Category: Zhao, H.]]
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[[Category: isoxazole carboxylic acid]]
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[[Category: Isoxazole carboxylic acid]]
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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 14:49:24 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:47:23 2008''
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Revision as of 11:49, 3 May 2008

Template:STRUCTURE 1xbo

PTP1B complexed with Isoxazole Carboxylic Acid


Overview

Guided by X-ray crystallography, we have extended the structure-activity relationship (SAR) study on an isoxazole carboxylic acid-based PTP1B inhibitor (1) and more potent and equally selective (>20-fold selectivity over the highly homologous T-cell PTPase, TCPTP) PTP1B inhibitors were identified. Inhibitor 7 demonstrated good cellular activity against PTP1B in COS 7 cells.

About this Structure

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

Reference

Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors., Zhao H, Liu G, Xin Z, Serby MD, Pei Z, Szczepankiewicz BG, Hajduk PJ, Abad-Zapatero C, Hutchins CW, Lubben TH, Ballaron SJ, Haasch DL, Kaszubska W, Rondinone CM, Trevillyan JM, Jirousek MR, Bioorg Med Chem Lett. 2004 Nov 15;14(22):5543-6. PMID:15482920 Page seeded by OCA on Sat May 3 14:49:24 2008

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