Interaction of site specific hirudin variants with α‐thrombin
- 29 February 1988
- journal article
- Published by Wiley in FEBS Letters
- Vol. 229 (1), 87-90
- https://doi.org/10.1016/0014-5793(88)80803-2
Abstract
The kinetics of complex formation between recombinant hirudin or recombinant hirudin mutants with thrombin were analyzed. In order to elucidate the inhibitor's reactive site peptide bond predetermined amino acid substitutions were introduced at positions of basic amino acid residues by means of site-directed mutagenesis of a hirudin gene. In comparison to recombinant hirudin (K i = 19 pM) only those mutant inhibitors which were modified at amino acid position Lys47 showed a higher K i value for their complexes with thrombin. The observed effects are mainly due to increased k off rate constants.Keywords
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