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Autor:
Andre Boelke, Emily Jane Canada, Brian Morgan Watson, Valentine J. Klimkowski, Michael Mohr, Qing Shi, David E. Timm, Shon Roland Pulley, Andreas Gerhard Weichert, Hans-Juergen Mest, J. Michael Kalbfleisch, Elizabeth A. Dingess-Hammond, Johann-Christian Zechel, Gerd Ruehter, Brandon J. Margolis, Soenke Petersen, Michael Robert Wiley, Graham N. Wishart, Annick J. Cauvin, Beatrice Renson, Stephen Parsons, Larry C. Blaszczak, Dirk Hankotius, Britta Evers, Scott Martin Sheehan
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(6)
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 acco