1onz

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{{STRUCTURE_1onz| PDB=1onz | SCENE= }}
{{STRUCTURE_1onz| PDB=1onz | SCENE= }}
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'''Oxalyl-aryl-Amino Benzoic acid Inhibitors of PTP1B, compound 8b'''
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===Oxalyl-aryl-Amino Benzoic acid Inhibitors of PTP1B, compound 8b===
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==Overview==
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Protein Tyrosine phosphatase 1B (PTP1B) has been implicated as a key negative regulator of both insulin and leptin signaling pathways. Using an NMR-based screening approach with 15N- and 13C-labeled PTP1B, we have identified 2,3-dimethylphenyloxalylaminobenzoic acid (1) as a general, reversible, and competitive PTPase inhibitor. Structure-based approach guided by X-ray crystallography facilitated the development of 1 into a novel series of potent and selective PTP1B inhibitors occupying both the catalytic site and a portion of the noncatalytic, second phosphotyrosine binding site. Interestingly, oral biovailability has been observed in rats for some compounds. Furthermore, we demonstrated in vivo plasma glucose lowering effects with compound 12d in ob/ob mice.
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{{ABSTRACT_PUBMED_12747781}}
==About this Structure==
==About this Structure==
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[[Category: Oxalyl-aryl-benzoic acid compound with napthyl moiety anchor inhibitor]]
[[Category: Oxalyl-aryl-benzoic acid compound with napthyl moiety anchor inhibitor]]
[[Category: Protein tyrosine phosphatase]]
[[Category: Protein tyrosine phosphatase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 04:05:09 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 03:26:45 2008''

Revision as of 00:26, 28 July 2008

Image:1onz.png

Template:STRUCTURE 1onz

Oxalyl-aryl-Amino Benzoic acid Inhibitors of PTP1B, compound 8b

Template:ABSTRACT PUBMED 12747781

About this Structure

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

Reference

Discovery and structure-activity relationship of oxalylarylaminobenzoic acids as inhibitors of protein tyrosine phosphatase 1B., Liu G, Szczepankiewicz BG, Pei Z, Janowick DA, Xin Z, Hajduk PJ, Abad-Zapatero C, Liang H, Hutchins CW, Fesik SW, Ballaron SJ, Stashko MA, Lubben T, Mika AK, Zinker BA, Trevillyan JM, Jirousek MR, J Med Chem. 2003 May 22;46(11):2093-103. PMID:12747781

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