2fjp: Difference between revisions

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[[Image:2fjp.gif|left|200px]]
{{Seed}}
[[Image:2fjp.png|left|200px]]


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{{STRUCTURE_2fjp|  PDB=2fjp  |  SCENE=  }}  
{{STRUCTURE_2fjp|  PDB=2fjp  |  SCENE=  }}  


'''Human dipeptidyl peptidase IV/CD26 in complex with an inhibitor'''
===Human dipeptidyl peptidase IV/CD26 in complex with an inhibitor===




==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.
The line below this paragraph, {{ABSTRACT_PUBMED_16759103}}, adds the Publication Abstract to the page
(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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