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The GHS-R blocker D-[Lys3] GHRP-6 serves as CCR5 chemokine receptor antagonist.
- Source :
-
International journal of medical sciences [Int J Med Sci] 2012; Vol. 9 (1), pp. 51-8. Date of Electronic Publication: 2011 Nov 18. - Publication Year :
- 2012
-
Abstract
- [D-Lys3]-Growth Hormone Releasing Peptide-6 (DLS) is widely utilized in vivo and in vitro as a selective ghrelin receptor (GHS-R) antagonist. This antagonist is one of the most common antagonists utilized in vivo to block GHS-R function and activity. Here, we found that DLS also has the ability to modestly block chemokine function and ligand binding to the chemokine receptor CCR5. The DLS effects on RANTES binding and Erk signaling as well as calcium mobilization appears to be much stronger than its effects on MIP-1α and MIP-1β. CCR5 have been shown to act as major co-receptor for HIV-1 entry into the CD4 positive host cells. To this end, we also found that DLS blocks M-tropic HIV-1 propagation in activated human PBMCs. These data demonstrate that DLS may not be a highly selective GHS-R1a inhibitor and may also effects on other G-protein coupled receptor (GPCR) family members. Moreover, DLS may have some potential clinical applications in blocking HIV infectivity and CCR5-mediated migration and function in various inflammatory disease states.
- Subjects :
- 3T3 Cells
Animals
CCR5 Receptor Antagonists
CD4-Positive T-Lymphocytes metabolism
Calcium metabolism
Chemokine CCL3 metabolism
Chemokine CCL4 metabolism
Extracellular Signal-Regulated MAP Kinases metabolism
HIV Infections virology
HIV-1 growth & development
Humans
Ligands
Mice
Protein Binding
Receptors, Ghrelin antagonists & inhibitors
Receptors, Ghrelin metabolism
Signal Transduction
Chemokine CCL5 metabolism
HIV Infections metabolism
HIV-1 metabolism
Oligopeptides metabolism
Receptors, CCR5 metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1449-1907
- Volume :
- 9
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- International journal of medical sciences
- Publication Type :
- Academic Journal
- Accession number :
- 22211090
- Full Text :
- https://doi.org/10.7150/ijms.9.51