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D-Phe-Pro-Arg type thrombin inhibitors: unexpected selectivity by modification of the P1 moiety
Udo E W Lange1, Dorit Baucke, Wilfried Hornberger
1BASF AG, D-67056, Ludwigshafen, Germany. wolfgang.hoeffken@basf-ag.de
Bioorganic & Medicinal Chemistry Letters
|June 5, 2003
Abstract:
Synthesis of thrombin inhibitors and their binding mode to thrombin is described. Modification of the P1 moiety leads to an increased selectivity versus trypsin. The observed selectivity is discussed in view of their thrombin-inhibitor complex X-ray structures.