Identification of peptide ligands to the chemokine receptor CCR5 and their maturation by gene shuffling.

Détails

ID Serval
serval:BIB_40146D7DD41B
Type
Article: article d'un périodique ou d'un magazine.
Collection
Publications
Titre
Identification of peptide ligands to the chemokine receptor CCR5 and their maturation by gene shuffling.
Périodique
Molecular Immunology
Auteur(s)
Vyroubalova E.C., Hartley O., Mermod N., Fisch I.
ISSN
0161-5890 (Print)
ISSN-L
0161-5890
Statut éditorial
Publié
Date de publication
04/2006
Volume
43
Numéro
10
Pages
1573-1578
Langue
anglais
Notes
Publication types: Journal Article ; Research Support, Non-U.S. Gov't
Publication Status: ppublish
Résumé
The determination of protein-protein interactions and their role in diverse pathophysiological processes is a promising approach to the identification of molecules of therapeutic potential. This paper describes the identification of peptidic CCR5 receptor ligands as potential drug leads against HIV-1 infection using in vitro evolution based on phage display. A phage-displayed peptide library was used to select for anti-CCR5 peptide. Further in vitro evolution of the peptide by exon shuffling was performed to identify peptides with optimized characteristics for CCR5 receptor. This peptide inhibited HIV coreceptor activity in a cell fusion assay with an IC50 of 5 microM. It did not exhibit either agonistic or antagonistic activity on CCR5 in the concentration range used. To our knowledge, this is a first report that describes the identification of peptide ligands specific to the CCR5 receptor from a phage-displayed library and the maturation of the selected peptide sequence by gene shuffling.
Mots-clé
Animals, Anti-HIV Agents/chemistry, Anti-HIV Agents/pharmacology, CHO Cells, Cells, Cultured, Cricetinae, Cricetulus, DNA Shuffling, Directed Molecular Evolution, Drug Design, Humans, Ligands, Membrane Fusion/drug effects, Peptide Library, Peptides/chemistry, Peptides/genetics, Receptors, CCR5/agonists, Receptors, CCR5/antagonists & inhibitors
Pubmed
Web of science
Création de la notice
24/01/2008 10:41
Dernière modification de la notice
20/08/2019 13:37
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