Back Cover: Potent Trivalent Inhibitors of Thrombin through Hybridization of Salivary Sulfopeptides from Hematophagous Arthropods (Angew. Chem. Int. Ed. 10/2021)

A novel class of trivalent thrombin inhibitor is reported by Pedro José Barbosa Pereira, Richard J. Payne, and co‐workers in their Research Article on page 5348. These inhibitors were rationally designed by hybridizing native sulfopeptide thrombin inhibitors from three different invertebrates: varie...

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Veröffentlicht in:Angewandte Chemie International Edition 2021-03, Vol.60 (10), p.5570-5570
Hauptverfasser: Agten, Stijn M., Watson, Emma E., Ripoll‐Rozada, Jorge, Dowman, Luke J., Wu, Mike C. L., Alwis, Imala, Jackson, Shaun P., Pereira, Pedro José Barbosa, Payne, Richard J.
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Sprache:eng
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Zusammenfassung:A novel class of trivalent thrombin inhibitor is reported by Pedro José Barbosa Pereira, Richard J. Payne, and co‐workers in their Research Article on page 5348. These inhibitors were rationally designed by hybridizing native sulfopeptide thrombin inhibitors from three different invertebrates: variegin from a bont tick, anophelin from the Anopheles mosquito, and TTI from the tsetse fly. When fused using bidirectional peptide synthesis and peptide ligation technologies the resulting hybrid inhibitors exhibited exquisite potency both in vitro, with femtomolar inhibition constants, and in an in vivo model of thrombosis.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.202101236