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
Institution
Titre
Identification of peptide ligands to the chemokine receptor CCR5 and their maturation by gene shuffling.
Périodique
Molecular Immunology
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
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 11:41
Dernière modification de la notice
20/08/2019 14:37