1ph0

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[[Image:1ph0.jpg|left|200px]]
[[Image:1ph0.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1ph0 |SIZE=350|CAPTION= <scene name='initialview01'>1ph0</scene>, resolution 2.20&Aring;
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The line below this paragraph, containing "STRUCTURE_1ph0", 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=418:2-{4-[2-(S)-ALLYLOXYCARBONYLAMINO-3-{4-[(2-CARBOXY-PHENYL)-OXALYL-AMINO]-PHENYL}-PROPIONYLAMINO]-BUTOXY}-6-HYDROXY-BENZOIC+ACID+METHYL+ESTER'>418</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_1ph0| PDB=1ph0 | SCENE= }}
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|RELATEDENTRY=[[1onz|1ONZ]], [[1ony|1ONY]], [[1nl9|1NL9]], [[1nny|1NNY]], [[1n06|1N06]], [[1nz7|1NZ7]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1ph0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1ph0 OCA], [http://www.ebi.ac.uk/pdbsum/1ph0 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1ph0 RCSB]</span>
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}}
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'''Non-carboxylic Acid-Containing Inhibitor of PTP1B Targeting the Second Phosphotyrosine Site'''
'''Non-carboxylic Acid-Containing Inhibitor of PTP1B Targeting the Second Phosphotyrosine Site'''
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[[Category: Szczepankiewicz, B.]]
[[Category: Szczepankiewicz, B.]]
[[Category: Xin, Z.]]
[[Category: Xin, Z.]]
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[[Category: oxalyl-aryl-benzoic acid compound inhibitor]]
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[[Category: Oxalyl-aryl-benzoic acid compound inhibitor]]
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[[Category: protein tyrosine phosphatase 1b]]
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[[Category: Protein tyrosine phosphatase 1b]]
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[[Category: salicylic acid moiety at the second site]]
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[[Category: Salicylic acid moiety at the second site]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 05:04:34 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:59:32 2008''
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Revision as of 02:04, 3 May 2008

Image:1ph0.jpg

Template:STRUCTURE 1ph0

Non-carboxylic Acid-Containing Inhibitor of PTP1B Targeting the Second Phosphotyrosine Site


Overview

Protein tyrosine phosphatase (PTPase) 1B (PTP1B) has been implicated as a key negative regulator of both insulin and leptin signaling cascades. We identified several salicylic acid-based ligands for the second phosphotyrosine binding site of PTP1B using a NMR-based screening. Structure-based linking with a catalytic site-directed oxalylarylaminobenzoic acid-based pharmacophore led to the identification of a novel series of potent PTP1B inhibitors exhibiting 6-fold selectivity over the highly homologous T-cell PTPase (TCPTP) and high selectivity over other phosphatases.

About this Structure

1PH0 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Selective protein tyrosine phosphatase 1B inhibitors: targeting the second phosphotyrosine binding site with non-carboxylic acid-containing ligands., Liu G, Xin Z, Liang H, Abad-Zapatero C, Hajduk PJ, Janowick DA, Szczepankiewicz BG, Pei Z, Hutchins CW, Ballaron SJ, Stashko MA, Lubben TH, Berg CE, Rondinone CM, Trevillyan JM, Jirousek MR, J Med Chem. 2003 Jul 31;46(16):3437-40. PMID:12877578 Page seeded by OCA on Sat May 3 05:04:34 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

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