Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
CHARACTERIZATIONS OF THE UNUSUAL DISSOCIATION PROPERTIES OF MELANOTROPIN PEPTIDES FROM THE MELANOCORTIN RECEPTOR, HMC1R
Autore:
HASKELLLUEVANO C; MIWA H; DICKINSON C; HADLEY ME; HRUBY VJ; YAMADA T; GANTZ I;
Indirizzi:
UNIV ARIZONA,DEPT CHEM TUCSON AZ 85721 UNIV ARIZONA,DEPT CHEM TUCSON AZ 85721 UNIV ARIZONA,DEPT ANAT TUCSON AZ 85721 UNIV MICHIGAN,MED CTR,DEPT INTERNAL MED ANN ARBOR MI 48109 UNIV MICHIGAN,MED CTR,DEPT PEDIAT ANN ARBOR MI 48109 UNIV MICHIGAN,MED CTR,DEPT PHYSIOL ANN ARBOR MI 48109 UNIV MICHIGAN,MED CTR,DEPT SURG ANN ARBOR MI 48109
Titolo Testata:
Journal of medicinal chemistry
fascicolo: 2, volume: 39, anno: 1996,
pagine: 432 - 435
SICI:
0022-2623(1996)39:2<432:COTUDP>2.0.ZU;2-P
Fonte:
ISI
Lingua:
ENG
Soggetto:
MELANOCYTE-STIMULATING HORMONE; ALPHA-MELANOTROPIN; ANALOGS; POTENT; CLONING; DESIGN;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
23
Recensione:
Indirizzi per estratti:
Citazione:
C. Haskellluevano et al., "CHARACTERIZATIONS OF THE UNUSUAL DISSOCIATION PROPERTIES OF MELANOTROPIN PEPTIDES FROM THE MELANOCORTIN RECEPTOR, HMC1R", Journal of medicinal chemistry, 39(2), 1996, pp. 432-435

Abstract

Variation in the degree of prolonged (residual) biological activity of the melanotropin peptides alpha-MSH (alpha-melanocyte-stimulating hormone, Ac-Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-G Pro-Val-NH2) and the superpotent analogues [Nle(4),DPhe(7)]alpha-MSH (MT-I) and [Nle(4),Asp(5),DPhe(7),Lys(10)]alpha-MSH(4-10)-NH2 (MT-II) has stimulated considerable interest regarding this biological phenomena. We have examined the differences in their relative dissociation rates from the melanocortin receptor, hMC1R, to try and correlate peptide dissociation rates with the observations of prolonged biological activity. Interestingly, these studies revealed that alpha-MSH remained 25% bound, MT-I 65% bound, and MT-II 86% bound 6 h after the ligand had been removed from the assay medium. The relative dissociation rate of MT-II was 4 times slower than that for a-MSH and 2 times slower than that for MT-I, which was 2 times slower than that for a-MSH. These data suggest that slow dissociation kinetics (hours) may contribute to the prolonged biological activities observed for both MT-I and MT-II peptides in vitro and in vivo. The prolonged binding, biological activities, and enzymatic stability of MT-I and MT-II make them putative candidates for clinical usessuch as external scintigraphy for the localization of tumors (i.e., melanoma).

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/09/20 alle ore 23:49:11