3c45
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Revision as of 06:52, 24 April 2008
Human dipeptidyl peptidase IV/CD26 in complex with a fluoroolefin inhibitor
Overview
The synthesis, selectivity, rat pharmacokinetic profile, and drug metabolism profiles of a series of potent fluoroolefin-derived DPP-4 inhibitors (4) are reported. A radiolabeled fluoroolefin 33 was shown to possess a high propensity to form reactive metabolites, thus revealing a potential liability for this class of DPP-4 inhibitors.
About this Structure
3C45 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors., Edmondson SD, Wei L, Xu J, Shang J, Xu S, Pang J, Chaudhary A, Dean DC, He H, Leiting B, Lyons KA, Patel RA, Patel SB, Scapin G, Wu JK, Beconi MG, Thornberry NA, Weber AE, Bioorg Med Chem Lett. 2008 Apr 1;18(7):2409-13. Epub 2008 Feb 26. PMID:18331795 Page seeded by OCA on Thu Apr 24 09:52:01 2008
