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Titolo:
Ligand design for alpha, adrenoceptors
Autore:
Bremner, JB; Griffith, R; Coban, B;
Indirizzi:
Univ Wollongong, Dept Chem, Wollongong, NSW 2522, Australia Univ Wollongong Wollongong NSW Australia 2522 ongong, NSW 2522, Australia
Titolo Testata:
CURRENT MEDICINAL CHEMISTRY
fascicolo: 6, volume: 8, anno: 2001,
pagine: 607 - 620
SICI:
0929-8673(200105)8:6<607:LDFAA>2.0.ZU;2-K
Fonte:
ISI
Lingua:
ENG
Soggetto:
PROTEIN-COUPLED RECEPTORS; ALPHA(1)-ADRENOCEPTOR ANTAGONISTS; ALPHA(1B)-ADRENERGIC RECEPTOR; AGONIST BINDING; SELECTIVE ANTAGONIST; SUBTYPE SELECTIVITY; BETA-ADRENOCEPTORS; EXTRACELLULAR LOOP; EFFECTOR PATHWAY; IN-VITRO;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
69
Recensione:
Indirizzi per estratti:
Indirizzo: Bremner, JB Univ Wollongong, Dept Chem, Wollongong, NSW 2522, Australia Univ Wollongong Wollongong NSW Australia 2522 2522, Australia
Citazione:
J.B. Bremner et al., "Ligand design for alpha, adrenoceptors", CURR MED CH, 8(6), 2001, pp. 607-620

Abstract

An area of continuing interest in medicinal chemistry is the design, synthesis and pharmacological evaluation of ligands which bind at adrenoceptor subtypes, which include alpha (1A), alpha (1B), alpha (1D); alpha (2A), alpha (2B), alpha (2C); beta (1), beta (2), beta (3) and possibly beta (4) subtypes. The selective blockade or stimulation of these receptor subtypes is of on-going pharmacological and medicinal interest. However, the design principles for ligand differentiation at these subtypes still need further development. This review focuses on al adrenoceptors with a concentration on literature over the past five years. Structural, physiological and therapeutic aspects of the alpha (1A), alpha (1B) and alpha (1D) subtypes are discussed together with ligands binding to these receptor subtypes. Approaches to al adrenoceptor ligand design based on known ligands and on receptor docking are evaluated. A new combined approach using pharmacophores and receptor docking affords possibilities for deeper insights into achieving small molecule binding selectivity.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/09/20 alle ore 23:32:19