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1no6

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{{STRUCTURE_1no6| PDB=1no6 | SCENE= }}
{{STRUCTURE_1no6| PDB=1no6 | SCENE= }}
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'''Potent, Selective Protein Tyrosine Phosphatase 1B Inhibitor Compound 5 Using a Linked-Fragment Strategy'''
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===Potent, Selective Protein Tyrosine Phosphatase 1B Inhibitor Compound 5 Using a Linked-Fragment Strategy===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 12670229 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12670229}}
==About this Structure==
==About this Structure==
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[[Category: Oxamic acid inhibitor bound to p-loop]]
[[Category: Oxamic acid inhibitor bound to p-loop]]
[[Category: Protein tyrosine phosphatase fold]]
[[Category: Protein tyrosine phosphatase fold]]
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Revision as of 10:33, 29 July 2008

Image:1no6.png

Template:STRUCTURE 1no6

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

Template:ABSTRACT PUBMED 12670229

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 Tue Jul 29 13:33:09 2008

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