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Titolo:
Model of the BzR binding site: Correlation of data from site-directed mutagenesis and the pharmacophore/receptor model
Autore:
He, XH; Zhang, CC; Cook, JM;
Indirizzi:
Univ Wisconsin, Dept Chem, Milwaukee, WI 53201 USA Univ Wisconsin Milwaukee WI USA 53201 Dept Chem, Milwaukee, WI 53201 USA
Titolo Testata:
MEDICINAL CHEMISTRY RESEARCH
fascicolo: 5, volume: 10, anno: 2001,
pagine: 269 - 308
SICI:
1054-2523(2001)10:5<269:MOTBBS>2.0.ZU;2-U
Fonte:
ISI
Lingua:
ENG
Soggetto:
AMINOBUTYRIC ACID(A) RECEPTORS; GATED ION CHANNELS; NICOTINIC ACETYLCHOLINE-RECEPTOR; GABA-A RECEPTORS; COMPUTER-ASSISTED ANALYSIS; BENZODIAZEPINE BINDING; ALPHA-SUBUNIT; HIGH-AFFINITY; FUNCTIONAL EXPRESSION; MOLECULAR-BIOLOGY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
88
Recensione:
Indirizzi per estratti:
Indirizzo: Cook, JM Univ Wisconsin, Dept Chem, POB 413, Milwaukee, WI 53201 USA Univ Wisconsin POB 413 Milwaukee WI USA 53201 aukee, WI 53201 USA
Citazione:
X.H. He et al., "Model of the BzR binding site: Correlation of data from site-directed mutagenesis and the pharmacophore/receptor model", MED CHEM RE, 10(5), 2001, pp. 269-308

Abstract

A model of the benzodiazepine(Bz) binding site of the GABA(A) receptor hasbeen proposed based on the correlation of data from site-directed mutagenesis to the pharmacophore/receptor model. (Figures 6 and 7). Since the tertiary and quaternary structures of the proteins of the GABA(A) receptor are not known, the present study represents a step toward constituting a detailed model of the BzR site. Attempts are made to employ previous SAR and results of molecular biology to speculate which amino acid residues are responsible for the current structure-affinity results. Much work remains at the molecular level to determine the exact location and function of the amino acids in question.

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Documento generato il 25/01/20 alle ore 01:23:44