2qoe | pdb_00002qoe
Human Dipeptidyl Peptidase IV in complex with a Triazolopiperazine-based beta amino acid Inhibitor
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| 2qoe, resolution 2.30Å | |||||||||||||
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| Ligands: | NAG, NA and 448 | ||||||||||||
| Gene: | DPP4, ADCP2, CD26 (Homo sapiens) | ||||||||||||
| Activity: | Dipeptidyl-peptidase IV, with EC number 3.4.14.5 | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
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. 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
Page seeded by OCA on Thu Mar 20 18:27:52 2008
