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

DOI	Trouver le DOI : https://doi.org/10.1016/j.bmcl.2005.08.085
Auteur	Rechercher : Tolkatchev, Dmitri¹; Rechercher : Vinogradova, Anna¹; Rechercher : Ni, Feng¹
Affiliation	Conseil national de recherches du Canada. Institut de recherche en biotechnologie du CNRC
Format	Texte, Article
Sujet	Enzyme Inhibitors; Ligands; pharmaceutical; Protein; Thrombin
Résumé	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'
Date de publication	2005
Langue	anglais
Numéro du CNRC	47477
Numéro NPARC	3538981
Exporter la notice	Exporter en format RIS
Signaler une correction	Signaler une correction (s'ouvre dans un nouvel onglet)
Identificateur de l’enregistrement	2a5ca9b5-1025-4c74-ba8a-a05425061dfc
Enregistrement créé	2009-03-01
Enregistrement modifié	2020-04-07