Format

Send to

Choose Destination
See comment in PubMed Commons below
Int J Med Sci. 2012;9(1):51-8. Epub 2011 Nov 18.

The GHS-R blocker D-[Lys3] GHRP-6 serves as CCR5 chemokine receptor antagonist.

Author information

1
Laboratory of Molecular Biology and Immunology, National Institute on Aging, Intramural Program, NIH, 251 Bayview Boulevard, Baltimore, MD 21224, USA.

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.

KEYWORDS:

CCR5; Cancer.; GHRP-6; GHS-R1a; Ghrelin; HIV-1; Inflammation; MIP-1α; MIP-1β; RANTES

PMID:
22211090
PMCID:
PMC3222091
[Indexed for MEDLINE]
Free PMC Article
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Ivyspring International Publisher Icon for PubMed Central
    Loading ...
    Support Center