Transforming bivalent ligands into retractable enzyme inhibitors through polypeptide-protein interactions

From National Research Council Canada

DOIResolve DOI: https://doi.org/10.1016/j.bmcl.2005.08.085
AuthorSearch for: 1; Search for: 1; Search for: 1
Name affiliation
  1. National Research Council of Canada. NRC Biotechnology Research Institute
FormatText, Article
Volume15
Issue23
Pages5120–5123
SubjectEnzyme Inhibitors; Ligands; pharmaceutical; Protein; Thrombin
Abstract
The concept of bivalent polypeptides with controllable flexible linkers is demonstrated through the design of a new generation of 'antidote'-reversible inhibitors of thrombin. These molecules contain two binding moieties, each of which in isolation has only a moderate affinity of binding, which are linked together by a flexible peptide bridge. We show that activities of the potent bivalent inhibitors of thrombin can be reversed by the specific, but much weaker, binding of the linker moiety to protein 'antidotes'
Publication date
LanguageEnglish
NRC number47477
NPARC number3538981
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