1pyn

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[[Image:1pyn.gif|left|200px]]
[[Image:1pyn.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1pyn |SIZE=350|CAPTION= <scene name='initialview01'>1pyn</scene>, resolution 2.20&Aring;
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The line below this paragraph, containing "STRUCTURE_1pyn", 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=941:2-(4-{2-TERT-BUTOXYCARBONYLAMINO-2-[4-(3-HYDROXY-2-METHOXYCARBONYL-PHENOXY)-BUTYLCARBAMOYL]-ETHYL}-PHENOXY)-MALONIC+ACID'>941</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_1pyn| PDB=1pyn | 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=1pyn FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1pyn OCA], [http://www.ebi.ac.uk/pdbsum/1pyn PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1pyn RCSB]</span>
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}}
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'''DUAL-SITE POTENT, SELECTIVE PROTEIN TYROSINE PHOSPHATASE 1B INHIBITOR USING A LINKED FRAGMENT STRATEGY AND A MALONATE HEAD ON THE FIRST SITE'''
'''DUAL-SITE POTENT, SELECTIVE PROTEIN TYROSINE PHOSPHATASE 1B INHIBITOR USING A LINKED FRAGMENT STRATEGY AND A MALONATE HEAD ON THE FIRST SITE'''
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[[Category: Trevillyan, J M.]]
[[Category: Trevillyan, J M.]]
[[Category: Zhonghua, P.]]
[[Category: Zhonghua, P.]]
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[[Category: malonate-containing inhibitor]]
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[[Category: Malonate-containing inhibitor]]
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[[Category: protein tyrosine phosphatase inhibited with dual site]]
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[[Category: Protein tyrosine phosphatase inhibited with dual site]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 05:39:01 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:06:20 2008''
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Revision as of 02:39, 3 May 2008

Template:STRUCTURE 1pyn

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.

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 Sat May 3 05:39:01 2008

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OCA

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