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Titolo:
SELECTIVITY OF [PHE-I-7], [ALA(6)], AND [D-ALA(4),GLN(5),TYR(6)] SUBSTITUTED ACTH(4-10) ANALOGS FOR THE MELANOCORTIN RECEPTORS
Autore:
SCHIOTH HB; MUCENIECE R; WIKBERG JES;
Indirizzi:
UPPSALA UNIV,DEPT PHARMACEUT PHARMACOL,BIOMED CTR,BOX 591 S-75124 UPPSALA SWEDEN
Titolo Testata:
Peptides
fascicolo: 5, volume: 18, anno: 1997,
pagine: 761 - 763
SICI:
0196-9781(1997)18:5<761:SO[[A[>2.0.ZU;2-P
Fonte:
ISI
Lingua:
ENG
Soggetto:
ALPHA-MSH ANALOGS; MOLECULAR-CLONING; EXPRESSION; ALANINE; BINDING;
Keywords:
MELANOCORTIN RECEPTOR SUBTYPES; MSH; ACTH; LIGAND BINDING; BIM 22015;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
19
Recensione:
Indirizzi per estratti:
Citazione:
H.B. Schioth et al., "SELECTIVITY OF [PHE-I-7], [ALA(6)], AND [D-ALA(4),GLN(5),TYR(6)] SUBSTITUTED ACTH(4-10) ANALOGS FOR THE MELANOCORTIN RECEPTORS", Peptides, 18(5), 1997, pp. 761-763

Abstract

We tested [Ala(6)]ACTH(4-10) and [Phe-I-7]ACTH(4-10) (putative MC receptor antagonists), [D-Ala(4),Gln(5),Tyr(6)] ACTH(4-10) (BIM22015), and ACTH(4-10) with radioligand binding using transiently expressed human MC1, MC3, MC4, and MC5 receptors. [Phe-I-7]ACTH(4-1O) had higher affinity for the MC3 MC4, and MC5 receptors but lower for the MC1 compared to ACTH(4-10). [Ala(6)]ACTH(4-10) did not bind the MC1 receptor but had highest affinity for the MC4 receptor. The data indicate that the His(6) has a specially important role in binding to the MC1 receptor. The BIM 22015 did not bind to these MC receptor subtypes, which indicates that the neurotrophic and myotrophic properties that are attributed to this peptide are mediated by some other receptor. (C) 1997 Elsevier Science Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 11/07/20 alle ore 03:09:06