2oae

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[[Image:2oae.gif|left|200px]]
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{{STRUCTURE_2oae| PDB=2oae | SCENE= }}
{{STRUCTURE_2oae| PDB=2oae | SCENE= }}
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'''Crystal structure of rat dipeptidyl peptidase (DPPIV) with thiazole-based peptide mimetic #31'''
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===Crystal structure of rat dipeptidyl peptidase (DPPIV) with thiazole-based peptide mimetic #31===
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==Overview==
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A novel series of pyrrolidine-constrained phenethylamines were developed as dipeptidyl peptidase IV (DPP4) inhibitors for the treatment of type 2 diabetes. The cyclohexene ring of lead-like screening hit 5 was replaced with a pyrrolidine to enable parallel chemistry, and protein co-crystal structural data guided the optimization of N-substituents. Employing this strategy, a &gt;400x improvement in potency over the initial hit was realized in rapid fashion. Optimized compounds are potent and selective inhibitors with excellent pharmacokinetic profiles. Compound 30 was efficacious in vivo, lowering blood glucose in ZDF rats that were allowed to feed freely on a mixed meal.
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(as it appears on PubMed at http://www.pubmed.gov), where 17276063 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17276063}}
==About this Structure==
==About this Structure==
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[[Category: Inhibitor complex]]
[[Category: Inhibitor complex]]
[[Category: Serine-peptidase]]
[[Category: Serine-peptidase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 10:31:13 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 04:31:46 2008''

Revision as of 01:31, 28 July 2008

Image:2oae.png

Template:STRUCTURE 2oae

Crystal structure of rat dipeptidyl peptidase (DPPIV) with thiazole-based peptide mimetic #31

Template:ABSTRACT PUBMED 17276063

About this Structure

2OAE is a Single protein structure of sequence from Rattus norvegicus. Full crystallographic information is available from OCA.

Reference

Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit., Backes BJ, Longenecker K, Hamilton GL, Stewart K, Lai C, Kopecka H, von Geldern TW, Madar DJ, Pei Z, Lubben TH, Zinker BA, Tian Z, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Kempf-Grote AJ, Black-Schaefer C, Sham HL, Trevillyan JM, Bioorg Med Chem Lett. 2007 Apr 1;17(7):2005-12. Epub 2007 Jan 19. PMID:17276063

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