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Titolo:
Molecular manipulation of G-protein-coupled receptors: A new avenue into drug discovery
Autore:
Sautel, M; Milligan, G;
Indirizzi:
Univ Glasgow, Inst Biomed & Life Sci, Div Biochem & Mol Biol, Glasgow G12 8QQ, Lanark, Scotland Univ Glasgow Glasgow Lanark Scotland G12 8QQ ow G12 8QQ, Lanark, Scotland
Titolo Testata:
CURRENT MEDICINAL CHEMISTRY
fascicolo: 9, volume: 7, anno: 2000,
pagine: 889 - 896
SICI:
0929-8673(200009)7:9<889:MMOGRA>2.0.ZU;2-8
Fonte:
ISI
Lingua:
ENG
Soggetto:
B GASTRIN RECEPTOR; CONSTITUTIVELY ACTIVE MUTANTS; BETA(2) ADRENERGIC-RECEPTOR; NEUROPEPTIDE-Y RECEPTOR; 3RD INTRACELLULAR LOOP; D1 DOPAMINE RECEPTOR; BETA(2)-ADRENERGIC RECEPTOR; INVERSE AGONIST; LIGAND-BINDING; STRUCTURAL INSTABILITY;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
71
Recensione:
Indirizzi per estratti:
Indirizzo: Sautel, M INRA, Unite BCM, Domaine Vilvert, F-78352 Jouy En Josas, France INRA Domaine Vilvert Jouy En Josas France F-78352 Josas, France
Citazione:
M. Sautel e G. Milligan, "Molecular manipulation of G-protein-coupled receptors: A new avenue into drug discovery", CURR MED CH, 7(9), 2000, pp. 889-896

Abstract

During the past 10 years or so, associated with the introduction of molecular biology techniques to G protein-coupled receptor (GPCR) research, outstanding progress has been made in understanding the mechanisms of action of these key proteins and their physiological functions. in-vivo manipulation of levels of GPCRs using transgenic and gene knock-out approaches have beenparticularly successful in assessing the roles of specific GPCRs in animalphysiology. Drug discovery is aiming to produce highly specific compounds based on subtle definition of receptor subtypes which can best be studied using heterologous expression of wild type or mutated forms of cDNA or genes encoding these proteins. Furthermore, new therapeutic opportunities may be provided byinvestigation of orphan receptors, the natural ligands for which remain unidentified. Some human diseases have been shown to be associated with rare mutations of GPCRs and the possibility that widely distributed polymorphisms in GPCR genes may allow selective therapeutic strategies for population subgroups is driving the development of the science of pharmacogenetics.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 31/03/20 alle ore 16:25:57