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Titolo:
THE STRUCTURE AND ACTIVITY OF MEMBRANE-RECEPTORS - COMPUTATIONAL SIMULATION OF HISTAMINE H-2-RECEPTOR ACTIVATION
Autore:
CAMPILLO M; GIRALDO J; PARDO L;
Indirizzi:
UNIV AUTONOMA BARCELONA,FAC MED,UNITAT BIOESTADIST,LAB MED COMPUTAC BELLATERRA 08193 BARCELONA SPAIN UNIV AUTONOMA BARCELONA,FAC MED,UNITAT BIOESTADIST,LAB MED COMPUTAC BELLATERRA 08193 BARCELONA SPAIN
Titolo Testata:
Journal of molecular structure. Theochem
, volume: 371, anno: 1996,
pagine: 279 - 286
SICI:
0166-1280(1996)371:<279:TSAAOM>2.0.ZU;2-S
Fonte:
ISI
Lingua:
ENG
Soggetto:
PROTEIN-COUPLED RECEPTORS; BETA-ADRENERGIC-RECEPTOR; SITE-DIRECTED MUTAGENESIS; LIGAND-BINDING; MOLECULAR DETERMINANTS; 3-DIMENSIONAL MODELS; REGULATORY PROTEINS; SERINE RESIDUES; AMINO-ACIDS; HISTAMINE-H2-RECEPTOR;
Keywords:
MEMBRANE RECEPTOR; HISTAMINE H-2-RECEPTOR; AB INITIO CALCULATION; G PROTEIN-COUPLED RECEPTOR;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
42
Recensione:
Indirizzi per estratti:
Citazione:
M. Campillo et al., "THE STRUCTURE AND ACTIVITY OF MEMBRANE-RECEPTORS - COMPUTATIONAL SIMULATION OF HISTAMINE H-2-RECEPTOR ACTIVATION", Journal of molecular structure. Theochem, 371, 1996, pp. 279-286

Abstract

A three dimensional molecular model of the transmembrane domain of the Histamine Ha-receptor was constructed, by computer-aided model building techniques, based on the amino acid sequence; topological criteriaguided by inferences from sequence homologies; the electron density projection map of bovine Rhodopsin obtained from electron microscopy; prediction of helix-helix interactions; experimental results from site-directed mutagenesis; and quantum mechanical calculations. In this model, the binding of Histamine to the receptor consists of: i) the ionicinteraction between the protonated side chain amine and the conservedAsp(98), located in transmembrane helix (TMH) 3; ii) the hydrogen bond between the N(3)-H moiety of the imidazole ring and the non conserved Asp(186), located in TMH 5; and iii) the hydrogen bond between the N(1) atom of the imidazole ring and the non conserved Arg(257), locatedin TMB 6. The activation mechanism of the receptor resulting from ligand binding takes the form of a proton transfer from TMH 6 (Arg(257)) to TMH 5 (Asp(186)). This process explains the local changes induced by agonist in the receptor binding site. The structural consequences ofthese changes could mediate the propagation of the extracellular signal, encoded in the structure of the ligand, to the intracellular site.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/11/20 alle ore 06:30:31