2h04

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[[Image:2h04.gif|left|200px]]
[[Image:2h04.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2h04 |SIZE=350|CAPTION= <scene name='initialview01'>2h04</scene>, resolution 2.300&Aring;
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The line below this paragraph, containing "STRUCTURE_2h04", 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=4UN:{4-[2,2-BIS(5-METHYL-1,2,4-OXADIAZOL-3-YL)-3-PHENYLPROPYL]PHENYL}SULFAMIC+ACID'>4UN</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= PTPRB ([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_2h04| PDB=2h04 | SCENE= }}
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|RELATEDENTRY=[[2ho2|2HO2]], [[2ho3|2HO3]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2h04 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2h04 OCA], [http://www.ebi.ac.uk/pdbsum/2h04 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2h04 RCSB]</span>
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}}
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'''Structural studies of protein tyrosine phosphatase beta catalytic domain in complex with inhibitors'''
'''Structural studies of protein tyrosine phosphatase beta catalytic domain in complex with inhibitors'''
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[[Category: Pokross, M E.]]
[[Category: Pokross, M E.]]
[[Category: Walter, R L.]]
[[Category: Walter, R L.]]
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[[Category: drug design]]
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[[Category: Drug design]]
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[[Category: inhibitor]]
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[[Category: Inhibitor]]
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[[Category: phosphatase]]
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[[Category: Phosphatase]]
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[[Category: protein tyrosine phosphatase]]
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[[Category: Protein tyrosine phosphatase]]
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[[Category: sulfamic acid]]
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[[Category: Sulfamic acid]]
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[[Category: wpd-loop]]
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[[Category: Wpd-loop]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 05:42:41 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:23:35 2008''
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Revision as of 02:42, 4 May 2008

Image:2h04.gif

Template:STRUCTURE 2h04

Structural studies of protein tyrosine phosphatase beta catalytic domain in complex with inhibitors


Overview

The sulfamic acid phosphotyrosine mimetic was coupled with a previously known malonate template to obtain highly selective and potent inhibitors of HPTPbeta. Potentially hydrolyzable malonate ester functionalities were replaced with 1,2,4-oxadiazoles without a significant effect on HPTPbeta potency.

About this Structure

2H04 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Design and synthesis of potent, non-peptidic inhibitors of HPTPbeta., Amarasinghe KK, Evidokimov AG, Xu K, Clark CM, Maier MB, Srivastava A, Colson AO, Gerwe GS, Stake GE, Howard BW, Pokross ME, Gray JL, Peters KG, Bioorg Med Chem Lett. 2006 Aug 15;16(16):4252-6. Epub 2006 Jun 12. PMID:16759857 Page seeded by OCA on Sun May 4 05:42:41 2008

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OCA

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