Effects of α-melanotropin C-terminal tripeptide analogues on macrophage NO production

Ruta Muceniece, Liga Krigere, Helga Süli-Vargha, Jarl E.S. Wikberg

Research output: Article

11 Citations (Scopus)

Abstract

The C-terminal tripeptide of melanocyte-stimulating hormone, MSH (11-13) (Lys-Pro-Val), possesses strong anti-inflammatory actions, which are mediated via mechanisms that are not fully understood. To shed more light into these mechanisms we have here synthesised and evaluated the activities of L- and D-Val substituted cyclic modifications of MSH (11-13) on nitric oxide (NO) in macrophage RAW 264.7 cells, as well as on binding to melanocortin receptors (MCRs) in B16-F1 and MCR expressing insect cells, and for effects on cAMP. MSH (11-13) and its analogues did neither bind to MCRs nor stimulate cAMP in RAW 264.7 and B16-F1 cells, except H-Lys-Pro-D-Val, which showed a tendency to increase cAMP at high (10-100μM) concentrations. However, all investigated peptides dose dependently inhibited NO in LPS/IFN-γ-stimulated RAW 264.7, cells with a structure activity relationship suggesting the existence of a distinct receptive site. This site appears to be distinct from the MCRs and not linked with cAMP.

Original languageEnglish
Pages (from-to)701-707
Number of pages7
JournalPeptides
Volume24
Issue number5
DOIs
Publication statusPublished - máj. 1 2003

ASJC Scopus subject areas

  • Biochemistry
  • Physiology
  • Endocrinology
  • Cellular and Molecular Neuroscience

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