Work

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

Year: 2010

Type: review

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.

Source: Journal of Hematology & Oncology

DOI: 10.1186/1756-8722-3-8

Authors: Christophe Frémin, Sylvain Meloche

Institutions: Institute for Research in Immunology and Cancer, Université de Montréal

Language: English

Topic: Melanoma and MAPK Pathways

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: gold

Estimated APC paid: $4,990