1jwt
From Proteopedia
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CRYSTAL STRUCTURE OF THROMBIN IN COMPLEX WITH A NOVEL BICYCLIC LACTAM INHIBITOR
Contents |
Overview
Peptidomimetic inhibitors of thrombin lacking the important, Ser195-carbonyl interaction have been prepared. The binding energy lost, after the removal of the activated carbonyl was recaptured through a, series of modifications of the P1 residues of the bicyclic lactam, inhibitors. Selected substituted compounds displayed useful, pharmacological profiles both in vitro and in vivo.
Disease
Known diseases associated with this structure: Dysprothrombinemia OMIM:[176930], Hyperprothrombinemia OMIM:[176930], Hypoprothrombinemia OMIM:[176930]
About this Structure
1JWT is a Single protein structure of sequence from Homo sapiens with BLI as ligand. Active as Thrombin, with EC number 3.4.21.5 Full crystallographic information is available from OCA.
Reference
Novel bicyclic lactam inhibitors of thrombin: potency and selectivity optimization through P1 residues., Levesque S, St-Denis Y, Bachand B, Preville P, Leblond L, Winocour PD, Edmunds JJ, Rubin JR, Siddiqui MA, Bioorg Med Chem Lett. 2001 Dec 17;11(24):3161-4. PMID:11720865
Page seeded by OCA on Mon Nov 12 17:45:21 2007
