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Titolo:
PHOSPHORUS-CONTAINING PEPTIDES AS MIXED INHIBITORS OF ENDOPEPTIDASE-3.4.24.15 AND ENDOPEPTIDASE-3.4.24.16 - EFFECT ON NEUROTENSIN DEGRADATION IN-VITRO AND IN-VIVO
Autore:
VINCENT B; DIVE V; YIOTAKIS A; SMADJA C; MALDONADO R; VINCENT JP; CHECLER F;
Indirizzi:
UNIV NICE SOPHIA ANTIPOLIS,INST PHARMACOL MOLEC & CELLULAIRE,CNRS,UPR441,660 ROUTE LUCIOLES F-06560 VALBONNE FRANCE UNIV NICE SOPHIA ANTIPOLIS,INST PHARMACOL MOLEC & CELLULAIRE,CNRS,UPR441 F-06560 VALBONNE FRANCE CEN SACLAY,STRUCT PROT SOLUT LAB GIF SUR YVETTE FRANCE UNIV ATHENS,DEPT ORGAN CHEM,ORGAN CHEM LAB GR-15771 ATHENS GREECE UER SCI PHARMACEUT & BIOL,INSERM,U266,DEPT CHIM ORGAN,CNRS,UA498 F-75006 PARIS FRANCE
Titolo Testata:
British Journal of Pharmacology
fascicolo: 6, volume: 115, anno: 1995,
pagine: 1053 - 1063
SICI:
0007-1188(1995)115:6<1053:PPAMIO>2.0.ZU;2-Z
Fonte:
ISI
Lingua:
ENG
Soggetto:
BRAIN SYNAPTIC-MEMBRANES; ENKEPHALIN DEGRADING ENZYMES; RAT-BRAIN; ANALGESIC RESPONSES; POTENT INHIBITOR; PZ-PEPTIDASE; METALLOENDOPEPTIDASE; INACTIVATION; PURIFICATION; INVOLVEMENT;
Keywords:
NEUROTENSIN; DEGRADATION; PEPTIDASES; ENDOPEPTIDASE 3.4.24.15; ENDOPEPTIDASE 3.4.24.16; PHOSPHORUS PEPTIDES; INHIBITORS; ILEUM CONTRACTION; CULTURED NEURONS; ANALGESIA;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
33
Recensione:
Indirizzi per estratti:
Citazione:
B. Vincent et al., "PHOSPHORUS-CONTAINING PEPTIDES AS MIXED INHIBITORS OF ENDOPEPTIDASE-3.4.24.15 AND ENDOPEPTIDASE-3.4.24.16 - EFFECT ON NEUROTENSIN DEGRADATION IN-VITRO AND IN-VIVO", British Journal of Pharmacology, 115(6), 1995, pp. 1053-1063

Abstract

1 We have examined several phosphorus-containing peptides as potential mixed inhibitors of two neurotensin-degrading zinc metallopeptidases, endopeptidase 3.4.24.15 and endopeptidase 3.4.24.16. 2 Among a series of 13 phosphonamide peptides, 2-naphtyl)ethylphosphonyl-glycyl-prolyl-norleucine (phosphodiepryl 08) was found to inhibit potently the hydrolysis of neurotensin by purified endopeptidase 3.4.24.15 and 3.4.24.16 with an identical K-i value of 0.4 nM. 3 Phosphodiepryl 08 displayed a strong selectivity towards the two peptidases since it failed to inhibit several other zinc-containing peptidases such as endopeptidase 3.4.24.11, angiotensin-converting enzyme, aminopeptidase M, leucine aminopeptidase and carboxypeptidases A and B. 4 The protective effect ofphosphodiepryl 08 on neurotensin degradation was examined in vitro and in vivo in central and peripheral bioassays. 5 Phosphodiepryl 08 virtually abolished neurotensin degradation by 4-day-old plated pure cultured neurones from mouse embryos and greatly potentiated neurotensin-induced antinociception in the mouse hot plate test. 6 In the periphery, phosphodiepryl 08 inhibited neurotensin degradation by membranes prepared from isolated longitudinal smooth muscle of guinea-pig ileum andgreatly potentiated the neurotensin-induced contraction of the same longitudinal smooth muscle preparation. 7 Our study indicates that phosphodiepryl 08 behaves as a potent and selective mixed inhibitor of endopeptidase 3.4.24.15 and 3.4.24.16 and can be used as a powerful agentto prevent neurotensin degradation, in vitro and in vive, in central and peripheral assays.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 06/04/20 alle ore 21:45:00