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The design of potent, selective, non-covalent, peptide thrombin inhibitors utilizing imidazole as a S1 binding element by Michael R. Wiley; Leonard C. Weir; Steven L. Briggs; Nickolay Y. Chirgadze; David Clawson; Donetta S. Gifford-Moore; Aaron L. Schacht; Gerald F. Smith; Vasu Vasudevan; Larry L. Zornes; Valentine J. Klimkowski is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is The design of potent, selective, non-covalent, peptide thrombin inhibitors utilizing imidazole as a S1 binding element about?

Modeling of neutral or mildly basic functional groups in the S1 site of thrombin led to the targeting of imidazole as a S 1 binding element and correctly predicted the optimal chain length for connecting this group with the $2 and $3 binding elements. Derivatives of 4-(3-aminopropyl)-imidazole can be selective inhibitors of thrombin demonstrating potent anticoagulant activity.

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Author

Michael R. Wiley; Leonard C. Weir; Steven L. Briggs; Nickolay Y. Chirgadze; David Clawson; Donetta S. Gifford-Moore; Aaron L. Schacht; Gerald F. Smith; Vasu Vasudevan; Larry L. Zornes; Valentine J. Klimkowski

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)

Published

1999

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)