1g37

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Image:1g37.gif

Template:STRUCTURE 1g37

CRYSTAL STRUCTURE OF HUMAN ALPHA-THROMBIN COMPLEXED WITH BCH-10556 AND EXOSITE-DIRECTED PEPTIDE


Overview

Bicyclic piperazinone based thrombin inhibitors of general structure 2 were prepared and evaluated in vitro and in vivo. These inhibitors, having in common an electrophilic basic trans-cyclohexylamine P1 residue, displayed high thrombin affinity, high selectivity against trypsin and good in vivo efficacy in the rat arterial thrombosis model.

About this Structure

1G37 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Potent and selective bicyclic lactam inhibitors of thrombin. Part 4: transition state inhibitors., Bachand B, Tarazi M, St-Denis Y, Edmunds JJ, Winocour PD, Leblond L, Siddiqui MA, Bioorg Med Chem Lett. 2001 Feb 12;11(3):287-90. PMID:11212093 Page seeded by OCA on Fri May 2 17:04:54 2008

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