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Titolo:
Non-competitive GABA antagonists: probing the mechanisms of their selectivity for insect versus mammalian receptors
Autore:
Ozoe, Y; Akamatsu, M;
Indirizzi:
Shimane Univ, Fac Life & Environm Sci, Dept Life Sci & Biotechnol, Matsue,Shimane 6908504, Japan Shimane Univ Matsue Shimane Japan 6908504 , Matsue,Shimane 6908504, Japan Kyoto Univ, Grad Sch Agr, Div Environm Sci & Technol, Kyoto 6068502, JapanKyoto Univ Kyoto Japan 6068502 ironm Sci & Technol, Kyoto 6068502, Japan
Titolo Testata:
PEST MANAGEMENT SCIENCE
fascicolo: 10, volume: 57, anno: 2001,
pagine: 923 - 931
SICI:
1526-498X(200110)57:10<923:NGAPTM>2.0.ZU;2-6
Fonte:
ISI
Lingua:
ENG
Soggetto:
GATED CHLORIDE CHANNEL; AMINOBUTYRIC-ACID RECEPTORS; DROSOPHILA-MELANOGASTER; NONCOMPETITIVE ANTAGONIST; RESISTANT DROSOPHILA; CYSTEINE MUTANTS; BLOCKING ACTIONS; BINDING-SITES; H-3 EBOB; PICROTOXIN;
Keywords:
gamma-aminobutyric acid receptors; non-competitive antagonists; insecticides; selectivity;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Agriculture,Biology & Environmental Sciences
Citazioni:
40
Recensione:
Indirizzi per estratti:
Indirizzo: Ozoe, Y Shimane Univ, Fac Life & Environm Sci, Dept Life Sci & Biotechnol,Matsue,Shimane 6908504, Japan Shimane Univ Matsue Shimane Japan 6908504 ,Shimane 6908504, Japan
Citazione:
Y. Ozoe e M. Akamatsu, "Non-competitive GABA antagonists: probing the mechanisms of their selectivity for insect versus mammalian receptors", PEST MAN SC, 57(10), 2001, pp. 923-931

Abstract

A great variety of non-competitive antagonists of ionotropic gamma -aminobutyric acid (GABA) receptors have been reported. While they are structurally diverse, there are common features in their structures. Thus, it was hypothesized that they bind to an identical site in different or overlapping orientations, and this hypothesis was validated by three-dimensional structure-activity relationship (3D-QSAR) analysis using receptor-binding data. Meanwhile, although most antagonists are highly toxic to both vertebrates and invertebrates, several classes of antagonists, such as nor-diterpene lactone picrodendrins, phenyl heterocyclic compounds and disubstituted bicyclophosphorothionates, were found to exhibit selectivity for housefly versus rat GABA receptors. To probe their selectivity mechanisms, the 3D-QSAR method was applied to the three classes of antagonists. This revealed several important differences that might be related to the selectivity of antagonists between the structures of the non-competitive antagonist-binding sites of housefly and rat GABA receptors. (C) 2001 Society of Chemical Industry.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 19/01/20 alle ore 11:57:13