354 Farnesyl transferase inhibition in circulating peripheral blood mononuclear cells with the novel oral prenyl transferase inhibitor AZD3409 following single and multiple doses in volunteer studies

Wilson, D.L.; Stephens, T C; Bate, Michael; Maulf, Florence Le; McCormack, P. D.; Hughes, Andrew

doi:10.1016/s1359-6349(04)80361-6

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The Erk Pathway As a Target For Cancer Drug Discovery2

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2006

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“…• small molecule inhibitors of RAS farnesylation (AZD-3409 (2), R-115777 (3), and Sch-66336 (4)) [20][21][22][23][24][25][26][27][28][29][30][31][32]. • antisense inhibitors of RAF expression (ISIS-5132) [33][34][35][36].…”

Section: The Erk Pathway As a Target For Cancer Drug Discoverymentioning

confidence: 99%

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Recent Advances in the Research and Development of RAF Kinase Inhibitors

Smith¹,

Dumas²,

Adnane³

et al. 2006

CTMC

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The RAS-RAF-MEK-ERK signaling pathway (ERK pathway) plays a key role in tumorigenesis and cancer progression. Mutations of RAS or B-RAF lead to a constitutive activation of the ERK pathway, which ultimately results in increased cell division, and cell survival. This review article focuses on the recent literature related to ERK pathway inhibitors, with a particular emphasis on RAF kinase inhibitors. Preclinical and clinical data for the RAF kinase inhibitor sorafenib (BAY 43-9006 tosylate), that was recently approved in the US for the treatment of advanced renal cell carcinoma, are also outlined.

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Section: The Erk Pathway As a Target For Cancer Drug Discoverymentioning

confidence: 99%

“…AZD-3409 (2, AstraZeneca) is an orally bioavailable farnesyltransferase inhibitor (FTI) currently in Phase I clinical trials [23][24][25]. The active moiety of AZD-3409 mimics the CAAX box of K-ras4B with functional thiol and carboxylic acid groups on a non-peptide scaffold.…”

Section: The Erk Pathway As a Target For Cancer Drug Discoverymentioning

confidence: 99%