2fjp

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[[Image:2fjp.gif|left|200px]]
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{{STRUCTURE_2fjp| PDB=2fjp | SCENE= }}
{{STRUCTURE_2fjp| PDB=2fjp | SCENE= }}
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'''Human dipeptidyl peptidase IV/CD26 in complex with an inhibitor'''
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===Human dipeptidyl peptidase IV/CD26 in complex with an inhibitor===
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==Overview==
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A series of beta-substituted biarylphenylalanine amides were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-4) for the treatment of type 2 diabetes. Optimization of the metabolic profile of early analogues led to the discovery of (2S,3S)-3-amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1 ,2,4]triazolo[1,5-a]pyridin-6-ylphenyl)butanamide (6), a potent, orally active DPP-4 inhibitor (IC(50) = 6.3 nM) with excellent selectivity, oral bioavailability in preclinical species, and in vivo efficacy in animal models. Compound 6 was selected for further characterization as a potential new treatment for type 2 diabetes.
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The line below this paragraph, {{ABSTRACT_PUBMED_16759103}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 16759103 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16759103}}
==About this Structure==
==About this Structure==
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[[Category: Beta-propeller]]
[[Category: Beta-propeller]]
[[Category: Dimer]]
[[Category: Dimer]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 03:58:41 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 21:36:47 2008''

Revision as of 18:36, 27 July 2008

Template:STRUCTURE 2fjp

Human dipeptidyl peptidase IV/CD26 in complex with an inhibitor

Template:ABSTRACT PUBMED 16759103

About this Structure

2FJP is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1 ,2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes., Edmondson SD, Mastracchio A, Mathvink RJ, He J, Harper B, Park YJ, Beconi M, Di Salvo J, Eiermann GJ, He H, Leiting B, Leone JF, Levorse DA, Lyons K, Patel RA, Patel SB, Petrov A, Scapin G, Shang J, Roy RS, Smith A, Wu JK, Xu S, Zhu B, Thornberry NA, Weber AE, J Med Chem. 2006 Jun 15;49(12):3614-27. PMID:16759103

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