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Titolo:
TRUNCATION STUDIES OF ALPHA-MELANOTROPIN PEPTIDES IDENTIFY TRIPEPTIDEANALOGS EXHIBITING PROLONGED AGONIST BIOACTIVITY
Autore:
HASKELLLUEVANO C; SAWYER TK; HENDRATA S; NORTH C; PANAHINIA L; STUM M; STAPLES DJ; CASTRUCCI AMD; HADLEY ME; HRUBY VJ;
Indirizzi:
UNIV ARIZONA,DEPT CHEM TUCSON AZ 85721 UNIV ARIZONA,DEPT CHEM TUCSON AZ 85721 UNIV ARIZONA,DEPT ANAT TUCSON AZ 85721 UPJOHN CO,DEPT BIOPOLYMER CHEM KALAMAZOO MI 49001 UNIV SAO PAULO,INST BIOCIENCIAS,DEPT FISIOL GERAL SAO PAULO BRAZIL
Titolo Testata:
Peptides
fascicolo: 6, volume: 17, anno: 1996,
pagine: 995 - 1002
SICI:
0196-9781(1996)17:6<995:TSOAPI>2.0.ZU;2-P
Fonte:
ISI
Lingua:
ENG
Soggetto:
MELANOCYTE-STIMULATING HORMONE; 5TH MELANOCORTIN RECEPTOR; MINIMAL ACTIVE SEQUENCE; MOLECULAR-CLONING; BIOLOGICAL-ACTIVITY; SKIN BIOASSAY; AMINO-ACIDS; MSH ANALOGS; EXPRESSION; BINDING;
Keywords:
ALPHA-MELANOCYTE STIMULATING HORMONE; ALPHA-MSH; AC-[NLE(4),DPHE(7)]ALPHA-MSH; NDP-MSH; MELANOTROPIN; MELANOTROPIN PHARMACOPHORE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
46
Recensione:
Indirizzi per estratti:
Citazione:
C. Haskellluevano et al., "TRUNCATION STUDIES OF ALPHA-MELANOTROPIN PEPTIDES IDENTIFY TRIPEPTIDEANALOGS EXHIBITING PROLONGED AGONIST BIOACTIVITY", Peptides, 17(6), 1996, pp. 995-1002

Abstract

Systematic analysis of fragment derivatives of the superpotent alpha-MSH analogue, Nle(4)-Glu-His-DPhe(7)-Arg-Trp-Gly-Lys-Pro-Val-NH2 (NDP-MSH), led to the discovery of tripeptide agonists possessing prolongedbioactivity in the frog skin assay. Of particular significance to this discovery was Ac-DPhe-Arg-DTrp-NH2, which was the most potent tripeptide in this series exhibiting sustained melanotropic activity. Different pharmacophore models appear to exist that are dependent on the substructure and stereochemistry of the MSH(6-9) ''active site. '' The tripeptides Ac-DPhe-Arg-Trp-NH2, Ac-DPhe-Arg-DTrp-NH2, and Ac-DPhe-DArg-Trp-NH2 stereochemical combinations require only Phe(7)-Xaa(8)-Trp(9), whereas Ac-DPhe-DArg-DTrp-NH2, Ac-Phe-Arg-DTrp-NH2, and Ac-Phe-Arg-Trp-NH2 additionally require His(6) for minimal biological activity. Ac-DPhe-Arg-DTrp-NH2 represents a novel prototype lead for the developmentof MSH-based peptidomimetic agonists.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/09/20 alle ore 11:16:31