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Titolo:
CHARACTERIZATION OF THE BINDING OF MSH-B, HP-228, GHRP-6 AND 153N-6 TO THE HUMAN MELANOCORTIN RECEPTOR SUBTYPES
Autore:
SCHIOTH HB; MUCENIECE R; WIKBERG JES;
Indirizzi:
UPPSALA UNIV,CTR BIOMED,DEP PHARMACEUT PHARMACOL,BOX 591 S-75124 UPPSALA SWEDEN INST ORGAN SYNTH,PHARMACOL LAB RIGA LATVIA
Titolo Testata:
Neuropeptides
fascicolo: 6, volume: 31, anno: 1997,
pagine: 565 - 571
SICI:
0143-4179(1997)31:6<565:COTBOM>2.0.ZU;2-1
Fonte:
ISI
Lingua:
ENG
Soggetto:
MELANOCYTE-STIMULATING HORMONE; NITRIC-OXIDE SYNTHASE; MOLECULAR-CLONING; RADIOLIGAND BINDING; EXPRESSION; ANALOGS; IDENTIFICATION; MELANOTROPIN; HYPOTHALAMUS; ANTAGONISTS;
Tipo documento:
Article
Natura:
Periodico
Citazioni:
36
Recensione:
Indirizzi per estratti:
Citazione:
H.B. Schioth et al., "CHARACTERIZATION OF THE BINDING OF MSH-B, HP-228, GHRP-6 AND 153N-6 TO THE HUMAN MELANOCORTIN RECEPTOR SUBTYPES", Neuropeptides, 31(6), 1997, pp. 565-571

Abstract

We determined the binding affinities of the MSH analogues MSH-B, HP-228 and 153N-6 and of the enkephalin analogue GHRP-6 on a single eukaryotic cell line transiently expressing the human MC1, MC3, MC4 and MC5 receptors. Moreover, we tested the binding and cAMP response of MSH-B in comparison with alpha-MSH on murine B16 melanoma cells. Our resultsindicate that MSH-B has a potency similar to that of alpha-MSH and that these two peptides induce similar cAMP responses in murine B16 melanoma cells. HP-228 has its highest affinity for the MC1 receptor, For the other receptors, it has slightly higher affinity for the MC5 receptor than for the MC3 and MC4 receptors. 153N-6 was found to be selective for the MC1 receptor. GHRP-6 was found to bind to the MC1 and the MC5 receptors despite its low structural homology with alpha-MSH. [D-Lys(3)]GHRP-6 bound to all the four MC receptors with similar affinities. The structurally related Met-enkephalin and the functionally relatedGHRH, as well as LHRH and somatostatin-14 did not bind to these MC receptors. The low affinity of the GH-releasing/enkephalin peptides may indicate that they do not interact with the MC receptors at pharmacologically relevant concentrations.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 10/07/20 alle ore 18:56:45