Format

Send to:

Choose Destination
See comment in PubMed Commons below
J Hematol Oncol. 2010 Feb 11;3:8. doi: 10.1186/1756-8722-3-8.

From basic research to clinical development of MEK1/2 inhibitors for cancer therapy.

Author information

  • 1Institut de Recherche en Immunologie et Cancérologie and Department of Pharmacology, Université de Montréal, Montreal, Quebec H3C 3J7, Canada.

Abstract

The Ras-dependent Raf/MEK/ERK1/2 mitogen-activated protein (MAP) kinase signaling pathway is a major regulator of cell proliferation and survival. Not surprisingly, hyperactivation of this pathway is frequently observed in human malignancies as a result of aberrant activation of receptor tyrosine kinases or gain-of-function mutations in RAS or RAF genes. Components of the ERK1/2 pathway are therefore viewed as attractive candidates for the development of targeted therapies of cancer. In this article, we briefly review the basic research that has laid the groundwork for the clinical development of small molecules inhibitors of the ERK1/2 pathway. We then present the current state of clinical evaluation of MEK1/2 inhibitors in cancer and discuss challenges ahead.

PMID:
20149254
[PubMed - indexed for MEDLINE]
PMCID:
PMC2830959
Free PMC Article
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for BioMed Central Icon for PubMed Central
    Loading ...
    Write to the Help Desk