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Back Cover: Potent Trivalent Inhibitors of Thrombin through Hybridization of Salivary Sulfopeptides from Hematophagous Arthropods (Angew. Chem. Int. Ed. 10/2021)
Author(s) -
Agten Stijn M.,
Watson Emma E.,
RipollRozada Jorge,
Dowman Luke J.,
Wu Mike C. L.,
Alwis Imala,
Jackson Shaun P.,
Pereira Pedro José Barbosa,
Payne Richard J.
Publication year - 2021
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.202101236
Subject(s) - thrombin , in vivo , peptide , ligation , discovery and development of direct thrombin inhibitors , in vitro , potency , biology , chemistry , biochemistry , microbiology and biotechnology , virology , pharmacology , immunology , genetics , platelet
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.