Recent progress on MAP kinase pathway inhibitors

David E Uehling; Philip A Harris

doi:10.1016/j.bmcl.2015.07.093

Recent progress on MAP kinase pathway inhibitors

Bioorg Med Chem Lett. 2015 Oct 1;25(19):4047-56. doi: 10.1016/j.bmcl.2015.07.093. Epub 2015 Aug 1.

Authors

David E Uehling¹, Philip A Harris²

Affiliations

¹ Department of Drug Discovery, Ontario Institute for Cancer Research, MaRS Centre, 661 University Avenue, Suite 510, Toronto, Ontario M5G 0A3, Canada. Electronic address: david.uehling@oicr.on.ca.
² Pattern Recognition Receptor DPU, GlaxoSmithKline, 1250 S. Collegeville Road, Collegeville, PA 19426-0989, United States.

PMID: 26298497
DOI: 10.1016/j.bmcl.2015.07.093

Abstract

The RAS-RAF-MEK-ERK, or ERK signaling pathway propagates signals through an intracellular signal transduction cascade. Since approximately one third of human cancers are impacted by mutations in the ERK signaling pathway, intensive efforts to develop drugs targeting members of this cascade are ongoing. While efforts to develop drugs aimed at inhibiting RAS are still at an early stage, substantial progress in discovering clinical drugs targeting RAF, MEK, and ERK have been made. This review will highlight the recent progress in this area.

Keywords: B-RAF; ERK; Kinase; MAPK; MEK.

Publication types

Review

MeSH terms

Animals
Dose-Response Relationship, Drug
Humans
MAP Kinase Signaling System / drug effects*
Molecular Structure
Protein Kinase Inhibitors / chemistry
Protein Kinase Inhibitors / pharmacology*
Structure-Activity Relationship

Substances

Protein Kinase Inhibitors