2qoe

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Image:2qoe.jpg

2qoe, resolution 2.30Å

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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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