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Titolo:
Structure-based design of COX-2 selectivity into flurbiprofen
Autore:
Bayly, CI; Black, WC; Leger, S; Ouimet, N; Ouellet, M; Percival, MD;
Indirizzi:
Merck Frosst Canada Inc, Pointe Claire, PQ H9R 4P8, Canada Merck Frosst Canada Inc Pointe Claire PQ Canada H9R 4P8 Q H9R 4P8, Canada
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
fascicolo: 3, volume: 9, anno: 1999,
pagine: 307 - 312
SICI:
0960-894X(19990208)9:3<307:SDOCSI>2.0.ZU;2-K
Fonte:
ISI
Lingua:
ENG
Soggetto:
ARYL ETHYL KETONES; ALKYL 2-ARYLPROPANOATES; LEAD(IV) ACETATE; CYCLOOXYGENASE-2; INHIBITION; FACILE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
15
Recensione:
Indirizzi per estratti:
Indirizzo: Bayly, CI Merck Frosst Canada Inc, POB 1005, Pointe Claire, PQ H9R 4P8, Canada Merck Frosst Canada Inc POB 1005 Pointe Claire PQ Canada H9R 4P8
Citazione:
C.I. Bayly et al., "Structure-based design of COX-2 selectivity into flurbiprofen", BIOORG MED, 9(3), 1999, pp. 307-312

Abstract

Comparative computer modeling of the X-ray crystal structures of cyclooxygenase isoforms COX-1 and COX-2 has led to the design of COX-2 selectivity into the nonselective inhibitor flurbiprofen. The COX-2 modeling was based on a postulated binding mode for flurbiprofen and took advantage of a small alcove in the COX-2 active site created by different positions of the Leu384 sidechain between COX-I and COX-2. The design hypothesis was tested by synthesis and biological assay of a series of flurbiprofen analogs, culminating in the discovery of several inhibitors having up to 78-fold selectivity for COX-2 over COX-1. (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 20/09/20 alle ore 04:16:24