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Titolo:
Inhibition of adamalysin II and MMPs by phosphonate analogues of snake venom peptides
Autore:
DAlessio, S; Gallina, C; Gavuzzo, E; Giordano, C; Gorini, B; Mazza, F; Paradisi, MP; Panini, G; Pochetti, G; Sella, A;
Indirizzi:
Polifarma Res Ctr, I-00185 Rome, Italy Polifarma Res Ctr Rome Italy I-00185 ifarma Res Ctr, I-00185 Rome, Italy Univ G DAnnunzio, Ist Sci Farm, I-66100 Chieti, Italy Univ G DAnnunzio Chieti Italy I-66100 st Sci Farm, I-66100 Chieti, Italy CNR, Ist Strutturist Chim, I-00016 Monterotondo, Italy CNR Monterotondo Italy I-00016 tturist Chim, I-00016 Monterotondo, Italy Univ Rome La Sapienza, CNR, Ctr Studio Chim Farm, I-00185 Rome, Italy UnivRome La Sapienza Rome Italy I-00185 Chim Farm, I-00185 Rome, Italy Univ Aquila, Dipartimento Chim Ingn Chim & Mat, I-67010 Laquila, Italy Univ Aquila Laquila Italy I-67010 ngn Chim & Mat, I-67010 Laquila, Italy
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY
fascicolo: 2, volume: 7, anno: 1999,
pagine: 389 - 394
SICI:
0968-0896(199902)7:2<389:IOAIAM>2.0.ZU;2-Q
Fonte:
ISI
Lingua:
ENG
Soggetto:
MATRIX METALLOPROTEINASES; GELATINASE-A; COLLAGENASE;
Keywords:
retrobinding pseudopeptide inhibitors; adamalysin II; matrix metalloproteinases;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
27
Recensione:
Indirizzi per estratti:
Indirizzo: Gallina, C UnivPLa Sapienza, Dipartimento Studi Farmaceut, CNR, Ctr StudioChim Farm, Univ La Sapienza P A Moro 5 Rome Italy I-00185 udio Chim Farm,
Citazione:
S. D'Alessio et al., "Inhibition of adamalysin II and MMPs by phosphonate analogues of snake venom peptides", BIO MED CH, 7(2), 1999, pp. 389-394

Abstract

Phosphonate analogues of the peptidomimetic N-(Furan-2-yl)carbonyl-Leu-Trp-OH were prepared with the goal of evaluating the effect of phosphonate forcarboxylate replacement on binding with snake venom metalloproteinases andMMPs, N(Furan-2-yl)carbonyl-Leu-L-Trp(P)-(OH)(2) showed a 75-fold increaseof the inhibiting activity against adamalysin II, a snake venom metalloproteinase structurally related to MMPs and TACE. Both the phosphonate and carboxylate peptidomimetics fit into the active site adopting a retrobinding mode and provide the structural base for a new class of metalloproteinases inhibitors. (C) 1999 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 23/09/20 alle ore 08:32:39