1no6

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[[Image:1no6.jpg|left|200px]]
[[Image:1no6.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1no6 |SIZE=350|CAPTION= <scene name='initialview01'>1no6</scene>, resolution 2.40&Aring;
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The line below this paragraph, containing "STRUCTURE_1no6", 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=794:2-[(CARBOXYCARBONYL)(1-NAPHTHYL)AMINO]BENZOIC+ACID'>794</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_1no6| PDB=1no6 | SCENE= }}
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|RELATEDENTRY=[[1nl9|1NL9]], [[1nny|1NNY]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1no6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1no6 OCA], [http://www.ebi.ac.uk/pdbsum/1no6 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1no6 RCSB]</span>
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}}
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'''Potent, Selective Protein Tyrosine Phosphatase 1B Inhibitor Compound 5 Using a Linked-Fragment Strategy'''
'''Potent, Selective Protein Tyrosine Phosphatase 1B Inhibitor Compound 5 Using a Linked-Fragment Strategy'''
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[[Category: Trevillyan, J M.]]
[[Category: Trevillyan, J M.]]
[[Category: Xin, Z.]]
[[Category: Xin, Z.]]
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[[Category: oxamic acid inhibitor bound to p-loop]]
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[[Category: Oxamic acid inhibitor bound to p-loop]]
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[[Category: protein tyrosine phosphatase fold]]
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[[Category: Protein tyrosine phosphatase fold]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 02:46:17 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:33:07 2008''
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Revision as of 23:46, 2 May 2008

Image:1no6.jpg

Template:STRUCTURE 1no6

Potent, Selective Protein Tyrosine Phosphatase 1B Inhibitor Compound 5 Using a Linked-Fragment Strategy


Overview

Protein tyrosine phosphatase 1B (PTP1B) is an enzyme that downregulates the insulin receptor. Inhibition of PTP1B is expected to improve insulin action, and the design of small molecule PTP1B inhibitors to treat type II diabetes has received considerable attention. In this work, NMR-based screening identified a nonselective competitive inhibitor of PTP1B. A second site ligand was also identified by NMR-based screening and then linked to the catalytic site ligand by rational design. X-ray data confirmed that the inhibitor bound with the catalytic site in the native, "open" conformation. The final compound displayed excellent potency and good selectivity over many other phosphatases. The modular approach to drug design described in this work should be applicable for the design of potent and selective inhibitors of other therapeutically relevant protein tyrosine phosphatases.

About this Structure

1NO6 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Discovery of a potent, selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy., Szczepankiewicz BG, Liu G, Hajduk PJ, Abad-Zapatero C, Pei Z, Xin Z, Lubben TH, Trevillyan JM, Stashko MA, Ballaron SJ, Liang H, Huang F, Hutchins CW, Fesik SW, Jirousek MR, J Am Chem Soc. 2003 Apr 9;125(14):4087-96. PMID:12670229 Page seeded by OCA on Sat May 3 02:46:17 2008

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