1ph0

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{{STRUCTURE_1ph0| PDB=1ph0 | SCENE= }}
{{STRUCTURE_1ph0| PDB=1ph0 | SCENE= }}
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'''Non-carboxylic Acid-Containing Inhibitor of PTP1B Targeting the Second Phosphotyrosine Site'''
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===Non-carboxylic Acid-Containing Inhibitor of PTP1B Targeting the Second Phosphotyrosine Site===
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==Overview==
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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.
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{{ABSTRACT_PUBMED_12877578}}
==About this Structure==
==About this Structure==
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[[Category: Protein tyrosine phosphatase 1b]]
[[Category: Protein tyrosine phosphatase 1b]]
[[Category: Salicylic acid moiety at the second site]]
[[Category: Salicylic acid moiety at the second site]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 16:59:49 2008''

Revision as of 13:59, 27 July 2008

Image:1ph0.png

Template:STRUCTURE 1ph0

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

Template:ABSTRACT PUBMED 12877578

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

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