2qoe

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==Overview==
==Overview==
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Various beta-amino amides containing triazolopiperazine heterocycles have, been prepared and evaluated as potent, selective, orally active dipeptidyl, peptidase IV (DPP-4) inhibitors. These compounds display excellent oral, bioavailability and good overall pharmacokinetic profiles in preclinical, species. Moreover, in vivo efficacy in an oral glucose tolerance test in, lean mice is demonstrated.
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Various beta-amino amides containing triazolopiperazine heterocycles have been prepared and evaluated as potent, selective, orally active dipeptidyl peptidase IV (DPP-4) inhibitors. These compounds display excellent oral bioavailability and good overall pharmacokinetic profiles in preclinical species. Moreover, in vivo efficacy in an oral glucose tolerance test in lean mice is demonstrated.
==About this Structure==
==About this Structure==
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[[Category: transmembrane]]
[[Category: transmembrane]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 12:23:41 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:40:55 2008''

Revision as of 16:40, 21 February 2008

Image:2qoe.jpg

2qoe, resolution 2.30Å

Drag the structure with the mouse to rotate

Human Dipeptidyl Peptidase IV in complex with a Triazolopiperazine-based beta amino acid Inhibitor

Overview

Various beta-amino amides containing triazolopiperazine heterocycles have been prepared and evaluated as potent, selective, orally active dipeptidyl peptidase IV (DPP-4) inhibitors. These compounds display excellent oral bioavailability and good overall pharmacokinetic profiles in preclinical species. Moreover, in vivo efficacy in an oral glucose tolerance test in lean mice is demonstrated.

About this Structure

2QOE is a Single protein structure of sequence from Homo sapiens with , and as ligands. Active as Dipeptidyl-peptidase IV, with EC number 3.4.14.5 Full crystallographic information is available from OCA.

Reference

Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors., Kowalchick JE, Leiting B, Pryor KD, Marsilio F, Wu JK, He H, Lyons KA, Eiermann GJ, Petrov A, Scapin G, Patel RA, Thornberry NA, Weber AE, Kim D, Bioorg Med Chem Lett. 2007 Nov 1;17(21):5934-9. Epub 2007 Aug 23. PMID:17827003

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