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Titolo:
Discovery of a novel Raf kinase inhibitor
Autore:
Lyons, JF; Wilhelm, S; Hibner, B; Bollag, G;
Indirizzi:
Onyx Pharmaceut, Richmond, CA 94806 USA Onyx Pharmaceut Richmond CA USA 94806 Pharmaceut, Richmond, CA 94806 USA Bayer Corp, W Haven, CT 06516 USA Bayer Corp W Haven CT USA 06516Bayer Corp, W Haven, CT 06516 USA Chiron Corp, Emeryville, CA 94608 USA Chiron Corp Emeryville CA USA 94608Chiron Corp, Emeryville, CA 94608 USA
Titolo Testata:
ENDOCRINE-RELATED CANCER
fascicolo: 3, volume: 8, anno: 2001,
pagine: 219 - 225
SICI:
1351-0088(200109)8:3<219:DOANRK>2.0.ZU;2-H
Fonte:
ISI
Lingua:
ENG
Soggetto:
ONCOGENE ACTIVATION; PROGNOSTIC MARKER; LUNG-CANCER; ADENOCARCINOMA; MUTATION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Citazioni:
19
Recensione:
Indirizzi per estratti:
Indirizzo: Lyons, JF Onyx Pharmaceut, 3031 Res Dr, Richmond, CA 94806 USA Onyx Pharmaceut 3031 Res Dr Richmond CA USA 94806 , CA 94806 USA
Citazione:
J.F. Lyons et al., "Discovery of a novel Raf kinase inhibitor", ENDOCR-R CA, 8(3), 2001, pp. 219-225

Abstract

We discuss the biology of Ras signal transduction and the epidemiology of ras mutations in association with disease as a background for the development of a Raf kinase inhibitor, BAY 43-9006. Knowledge of Ras effector pathways has permitted genetic validation of numerous targets involved in the Rassignaling cascade. A key Ras effector pathway involves the kinase cascade RAF/MEK/ERK (MEK: MAP/ERK kinase; ERK: extracellular signal related kinase). Indeed, we present studies of cell lines stably expressing mutant MEK constructs, which point to Raf kinase as a target for therapeutics with selective anti-tumor activity. Finally, a small molecule drug discovery program based on inhibition of Raf kinase activity is outlined and the initial pre-clinical development process of the Raf kinase inhibitor BAY 43-9006 is discussed.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 01/04/20 alle ore 20:20:33