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Titolo:
Understanding channel blocking in the nicotinic acetylcholine receptor
Autore:
Ortells, MO; Barrantes, GE;
Indirizzi:
CONICET, Inst Invest Bioquim, RA-8000 Bahia Blanca, Buenos Aires, Argentina CONICET Bahia Blanca Buenos Aires Argentina RA-8000 enos Aires, Argentina Univ Buenos Aires, Fac Ciencias Exactas & Nat, CONICET, Inst Neurociencia,RA-1428 Buenos Aires, DF, Argentina Univ Buenos Aires Buenos Aires DF Argentina RA-1428 Aires, DF, Argentina
Titolo Testata:
RECEPTORS & CHANNELS
fascicolo: 4, volume: 7, anno: 2001,
pagine: 273 - 288
SICI:
1060-6823(2001)7:4<273:UCBITN>2.0.ZU;2-S
Fonte:
ISI
Lingua:
ENG
Soggetto:
STRUCTURE-BASED DISCOVERY; AFFINITY BINDING-SITE; ION-CHANNEL; NONCOMPETITIVE ANTAGONIST; H-3 CHLORPROMAZINE; DRUG DESIGN; OPEN STATE; HIV-1 PROTEASE; AMINO-ACIDS; INHIBITOR;
Keywords:
automatic docking; channel blockers; hallucinogens; ion channel; local anesthetics; molecular modeling; nicotinic acetylcholine receptor; toxins;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
68
Recensione:
Indirizzi per estratti:
Indirizzo: Ortells, MO CONICET, Inst Invest Bioquim, CC 857, RA-8000 Bahia Blanca, Buenos Aires, Argentina CONICET CC 857 Bahia Blanca Buenos Aires Argentina RA-8000 ina
Citazione:
M.O. Ortells e G.E. Barrantes, "Understanding channel blocking in the nicotinic acetylcholine receptor", RECEPT CHAN, 7(4), 2001, pp. 273-288

Abstract

Ion-channel blockers are molecules that obstruct the path used by ions to cross the membrane through a protein channel. Many of these are local anesthetics, toxins or drugs of abuse, and the knowledge of their mechanism of action at the atomic level is an important step towards the development of new compounds on a structural basis. A molecular model of the transmembrane region of the nicotinic acetylcholine receptor, an important brain and muscle fast signaling protein, was used as a target for docking several channelblockers by means of an automatic docking method. The combination of the independent docking method and molecular models (of the receptor and blockers) reproduced or explained quite accurately experimental data (photoaffinity labeling, site-directed mutagenesis, binding assays). This represents a strong support for the validity of the predictions made for those molecules for which no experimental data is available and also for the models and methods on which are based.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 26/09/20 alle ore 12:11:43