TAILIEUCHUNG - Báo cáo khoa học: B1–Proteases as Molecular Targets of Drug Development B1-001 DPP-IV structure and inhibitor design

The incretin hormones GLP-1 and GIP are released from the gut during meals, and serve as enhancers of glucose stimulated insu-lin release from the beta cells. Furthermore, GLP-1 also stimu-lates beta cell growth and insulin biosynthesis, inhibits glucagon secretion, reduces free fatty acids and delays gastric emptying. GLP-1 has therefore been suggested as a potentially new treat-ment for type 2 diabetes. | Abstracts B1-Proteases as Molecular Targets of Drug Development B1-001 DPP-IV structure and inhibitor design H. B. Rasmussen1 S. Branner1 N. Wagtmann3 J. R. Bjelke1 and A. B. Kanstrup2 1Protein Engineering Novo Nordisk A S Bagsvaerd Denmark 2Medicinal Chemistry Novo Nordisk A S Maaloev Denmark 3Discovery Biology Novo Nordisk A S Maaloev DENMARK. E-mail hbrm@ The incretin hormones GLP-1 and GIP are released from the gut during meals and serve as enhancers of glucose stimulated insu lin release from the beta cells. Furthermore GLP-1 also stimulates beta cell growth and insulin biosynthesis inhibits glucagon secretion reduces free fatty acids and delays gastric emptying. GLP-1 has therefore been suggested as a potentially new treatment for type 2 diabetes. However GLP-1 is very rapidly degraded in the bloodstream by the enzyme dipeptidyl peptidase IV DPP-IV EC . A very promising approach to harvest the beneficial effect of GLP-1 in the treatment of diabetes is to inhibit the DPP-IV enzyme thereby enhancing the levels of endogenously intact circulating GLP-1. The three dimensional structure of human DPP-IV in complex with various inhibitors 138 Abstracts creates a better understanding of the specificity and selectivity of this enzyme and allows for further exploration and design of new therapeutic inhibitors. The majority of the currently known DPP-IV inhibitors consist of an alpha amino acid pyrrolidine core to which substituents have been added to optimize affinity potency enzyme selectivity oral bioavailability and duration of action. Various compound series and their SAR relative to alpha amino acids will be presented. B1-002 MEROPS the peptidase database N. D. Rawlings F. R. Morton and A. J. Barrett Bioinformatics Wellcome Trust Sanger Institute Hinxton Cambridgeshire UK. E-mail ndr@ Peptidases also known proteases or proteinases and their inhibitors are of major importance to human health. The MEROPS database is a comprehensive

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