Structural highlights
Evolutionary Conservation
Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.
Publication Abstract from PubMed
Design, synthesis, and SAR are described for a class of DPP-IV inhibitors based on aminobenzo[a]quinolizines with non-aromatic substituents in the S1 specificity pocket. One representative thereof, carmegliptin (8p), was chosen for clinical development. Its X-ray structure in complex with the enzyme and early efficacy data in animal models of type 2 diabetes are also presented.
Discovery of carmegliptin: a potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.,Mattei P, Boehringer M, Di Giorgio P, Fischer H, Hennig M, Huwyler J, Kocer B, Kuhn B, Loeffler BM, Macdonald A, Narquizian R, Rauber E, Sebokova E, Sprecher U Bioorg Med Chem Lett. 2010 Feb 1;20(3):1109-13. Epub 2009 Dec 6. PMID:20031405[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Mattei P, Boehringer M, Di Giorgio P, Fischer H, Hennig M, Huwyler J, Kocer B, Kuhn B, Loeffler BM, Macdonald A, Narquizian R, Rauber E, Sebokova E, Sprecher U. Discovery of carmegliptin: a potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1109-13. Epub 2009 Dec 6. PMID:20031405 doi:10.1016/j.bmcl.2009.12.024
