Pharmacological inhibitors of the ERK signaling pathway: application as anticancer drugs.
The ERK signaling pathway, also known as the p42/p44 MAP kinase pathway, is a major determinant in the control of cell growth, cell differentiation and cell survival. This pathway, which operates downstream of Ras, is often up-regulated in human tumors and as such represents an attractive target for anticancer therapy. In this chapter we review the rationale for targeting the components of the ERK pathway, either alone or in association with cytotoxic anticancer agents. We present the most advanced inhibitors of this pathway and discuss their specificity and mechanism of action.
Laboratory of Cell Regulation, Department of Pharmaceutical Sciences, Graduate School of Biomedical Sciences, Nagasaki University, 1-14, Bunkyo-machi, Nagasaki 852-8521, Japan.
Michiaki
M
Kohno
Jacques
J
Pouyssegur
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects* / Q000502:physiology; D004354:Drug Screening Assays, Antitumor / Q000639:trends; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D020928:Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology*; D015398:Signal Transduction / Q000187:drug effects / Q000502:physiology; D018631:ras Proteins / Q000378:metabolism
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D020928:Mitogen-Activated Protein Kinases; D018631:ras Proteins