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Titolo:
Characterization of the human cysteinyl leukotriene CysLT(1) receptor
Autore:
Lynch, KR; ONeill, GP; Liu, QY; Im, DS; Sawyer, N; Metters, KM; Coulombe, N; Abramovitz, M; Figueroa, DJ; Zeng, ZZ; Connolly, BM; Bai, C; Austin, CP; Chateauneuf, A; Stocco, R; Greig, GM; Kargman, S; Hooks, SB; Hosfield, E; Williams, DL; Ford-Hutchinson, AW; Caskey, CT; Evans, JF;
Indirizzi:
Univ Virginia, Hlth Sci Ctr, Dept Pharmacol, Charlottesville, VA 22908 USAUniv Virginia Charlottesville VA USA 22908 Charlottesville, VA 22908 USA Merck8,rosst Canada & Co, Dept Biochem & Mol Biol, Pointe Claire, PQ H9R 4P Merck Frosst Canada & Co Pointe Claire PQ Canada H9R 4P8 laire, PQ H9R 4P Merck & Co Inc, Dept Pharmacol, W Point, PA 19486 USA Merck & Co Inc W Point PA USA 19486 Dept Pharmacol, W Point, PA 19486 USA Merck & Co Inc, Dept Human Genet, W Point, PA 19486 USA Merck & Co Inc W Point PA USA 19486 pt Human Genet, W Point, PA 19486 USA
Titolo Testata:
NATURE
fascicolo: 6738, volume: 399, anno: 1999,
pagine: 789 - 793
SICI:
0028-0836(19990624)399:6738<789:COTHCL>2.0.ZU;2-X
Fonte:
ISI
Lingua:
ENG
Soggetto:
DOUBLE-BLIND TRIAL; GUINEA-PIG LUNG; CHRONIC ASTHMA; ANTAGONIST; MONTELUKAST; POTENT; PHARMACOLOGY; MULTICENTER; EXPRESSION; RESPONSES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Agriculture,Biology & Environmental Sciences
Life Sciences
Physical, Chemical & Earth Sciences
Citazioni:
28
Recensione:
Indirizzi per estratti:
Indirizzo: Evans, JF Univ Virginia, Hlth Sci Ctr, Dept Pharmacol, Charlottesville, VA22908 USA Univ Virginia Charlottesville VA USA 22908 sville, VA 22908 USA
Citazione:
K.R. Lynch et al., "Characterization of the human cysteinyl leukotriene CysLT(1) receptor", NATURE, 399(6738), 1999, pp. 789-793

Abstract

The cysteinyl leukotrienes-leukotriene C-4(LTC4), leukotriene D-4(LTD4) and leukotriene E-4(LTE4)-are important mediators of human bronchial asthma(1-3). Pharmacological studies have determined that cysteinyl leukotrienes activate at least two receptors, designated CysLT(1) and CysLT(2) (refs 4-6). The CysLT(1)-selective antagonists, such as montelukast (Singulair)(7-10),zafirlukast (Accolate)(11) and pranlukast (Onon)(12), are important in thetreatment of asthma. Previous biochemical characterization of CysLT(1) antagonists and the CysLT(1) receptor has been in membrane preparations from tissues enriched for this receptor(13). Here we report the molecular and pharmacological characterization of the cloned human CysLT(1) receptor. We describe the functional activation (calcium mobilization) of this receptor by LTD4 and LTC4, and competition for radiolabelled LTD4 binding to this receptor by the cysteinyl leukotrienes and three structurally distinct classes of CysLT(1)-receptor antagonists. We detected CysLT(1)-receptor messenger RNA in spleen, peripheral blood leukocytes and lung. In normal human lung, expression of the CysLT(1)-receptor mRNA was confined to smooth muscle cells and tissue macrophages. Finally, we mapped the human CysLT(1)-receptor geneto the X chromosome.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 24/11/20 alle ore 21:54:04