دورية أكاديمية
Discovery of non-covalent dipeptidyl peptidase IV inhibitors which induce a conformational change in the active site.
| العنوان: | Discovery of non-covalent dipeptidyl peptidase IV inhibitors which induce a conformational change in the active site. |
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| المؤلفون: | Sheehan SM; Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285, USA. SHEEHAN_SCOTT@LILLY.COM, Mest HJ, Watson BM, Klimkowski VJ, Timm DE, Cauvin A, Parsons SH, Shi Q, Canada EJ, Wiley MR, Ruehter G, Evers B, Petersen S, Blaszczak LC, Pulley SR, Margolis BJ, Wishart GN, Renson B, Hankotius D, Mohr M, Zechel JC, Michael Kalbfleisch J, Dingess-Hammond EA, Boelke A, Weichert AG |
| المصدر: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Mar 15; Vol. 17 (6), pp. 1765-8. Date of Electronic Publication: 2006 Dec 24. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Print ISSN: 0960-894X (Print) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Oxford : Elsevier Science Ltd Original Publication: Oxford ; New York : Pergamon Press, c1991- |
| مواضيع طبية MeSH: | Dipeptidyl-Peptidase IV Inhibitors*, Protease Inhibitors/*chemical synthesis , Protease Inhibitors/*pharmacology, Animals ; Binding Sites ; Computer Simulation ; Crystallography, X-Ray ; Dipeptidyl Peptidase 4/blood ; Drug Evaluation, Preclinical ; Hydrogen Bonding ; Male ; Models, Molecular ; Molecular Conformation ; Protease Inhibitors/chemistry ; Rats ; Rats, Wistar ; Spectrometry, Fluorescence |
| مستخلص: | A series of non-covalent inhibitors of the serine protease dipeptidyl peptidase IV (DPP-IV) were found to adopt a U-shaped binding conformation in X-ray co-crystallization studies. Remarkably, Tyr547 undergoes a 70 degrees side-chain rotation to accommodate the inhibitor and allows access to a previously unexposed area of the protein backbone for hydrogen bonding. |
| المشرفين على المادة: | 0 (Dipeptidyl-Peptidase IV Inhibitors) 0 (Protease Inhibitors) EC 3.4.14.5 (Dipeptidyl Peptidase 4) |
| تواريخ الأحداث: | Date Created: 20070124 Date Completed: 20070529 Latest Revision: 20101118 |
| رمز التحديث: | 20231215 |
| DOI: | 10.1016/j.bmcl.2006.12.074 |
| PMID: | 17239592 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 0960-894X |
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| DOI: | 10.1016/j.bmcl.2006.12.074 |