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

DOI	Resolve DOI: https://doi.org/10.1016/j.bmcl.2005.08.085
Author	Search for: Tolkatchev, Dmitri¹; Search for: Vinogradova, Anna¹; Search for: Ni, Feng¹
Affiliation	National Research Council of Canada. NRC Biotechnology Research Institute
Format	Text, Article
Subject	Enzyme 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	2005
Language	English
NRC number	47477
NPARC number	3538981
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Record identifier	2a5ca9b5-1025-4c74-ba8a-a05425061dfc
Record created	2009-03-01
Record modified	2020-04-07