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Titolo:
Identification of the platelet ADP receptor targeted by antithrombotic drugs
Autore:
Hollopeter, G; Jantzen, HM; Vincent, D; Li, G; England, L; Ramakrishnan, V; Yang, RB; Nurden, P; Nurden, A; Julius, D; Conley, PB;
Indirizzi:
COR Therapeut Inc, S San Francisco, CA 94080 USA COR Therapeut Inc S San Francisco CA USA 94080 an Francisco, CA 94080 USA Univ Calif San Francisco, Dept Mol & Cellular Pharmacol, San Francisco, CA94143 USA Univ Calif San Francisco San Francisco CA USA 94143 rancisco, CA94143 USA Univ Calif San Francisco, Program Neurosci, San Francisco, CA 94143 USA Univ Calif San Francisco San Francisco CA USA 94143 ancisco, CA 94143 USA Hop Cardiol, CNRS, UMR 5533, F-33605 Pessac, France Hop Cardiol Pessac France F-33605 CNRS, UMR 5533, F-33605 Pessac, France
Titolo Testata:
NATURE
fascicolo: 6817, volume: 409, anno: 2001,
pagine: 202 - 207
SICI:
0028-0836(20010111)409:6817<202:IOTPAR>2.0.ZU;2-8
Fonte:
ISI
Lingua:
ENG
Soggetto:
P2Y(1) RECEPTOR; ADENYLATE-CYCLASE; BLOOD-PLATELETS; CLOPIDOGREL; ACTIVATION; AGGREGATION; PROTEINS; CHANNEL; PATHWAY; BINDING;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Agriculture,Biology & Environmental Sciences
Life Sciences
Physical, Chemical & Earth Sciences
Citazioni:
28
Recensione:
Indirizzi per estratti:
Indirizzo: Conley, PB COR Therapeut Inc, S San Francisco, CA 94080 USA COR Therapeut Inc S San Francisco CA USA 94080 o, CA 94080 USA
Citazione:
G. Hollopeter et al., "Identification of the platelet ADP receptor targeted by antithrombotic drugs", NATURE, 409(6817), 2001, pp. 202-207

Abstract

Platelets have a crucial role in the maintenance of normal haemostasis, and perturbations of this system can lead to pathological thrombus formation and vascular occlusion, resulting in stroke, myocardial infarction and unstable angina. ADP released from damaged vessels and red blood cells induces platelet aggregation through activation of the integrin GPIIb-IIIa and subsequent binding of fibrinogen. ADP is also secreted from platelets on activation, providing positive feedback that potentiates the actions of many platelet activators(1). ADP mediates platelet aggregation through its action ontwo G-protein-coupled receptor subtypes(2,3). The P2Y(1) receptor couples to G(q) and mobilizes intracellular calcium ions to mediate platelet shape change and aggregation(4,5). The second ADP receptor required for aggregation (variously called P2Y(ADP), P2Y(AC), P2Ycyc or P2T(AC)) is coupled to the inhibition of adenylyl cyclase through G(i). The molecular identity of the G(i)-linked receptor is still elusive, even though it is the target of efrcacious antithrombotic agents, such as ticlopidine and clopidogrel(6-8) and AR-C66096 (ref. 9). Here we describe the cloning of this receptor, designated P2Y(12), and provide evidence that a patient with a bleeding disorder(10) has a defect in this gene. Cloning of the P2Y12 receptor should facilitate the development of better antiplatelet agents to treat cardiovascular diseases.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 19/01/20 alle ore 11:40:28