Non-'classical' MEKs: A review of MEK3-7 inhibitors

Bioorg Med Chem Lett. 2020 Jul 1;30(13):127203. doi: 10.1016/j.bmcl.2020.127203. Epub 2020 Apr 23.

Abstract

The MAPK pathways are an enduring area of interest due to their essential roles in cell processes. Increased expression and activity can lead to a multitude of diseases, sparking research efforts in developing inhibitors against these kinases. Though great strides have been made in developing MEK1/2 inhibitors, there is a notable lack of chemical probes for MEK3-7, given their central role in stimuli response, cell growth, and development. This review summarizes the progress that has been made on developing small molecule probes for MEK3-7, the specific disease states in which they have been studied, and their potential to become novel therapeutics.

Keywords: Drug discovery; Kinases; Mitogen-activated protein kinases; Small molecule inhibitors; Structure-activity relationships.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Humans
  • Mitogen-Activated Protein Kinase Kinases / antagonists & inhibitors*
  • Phosphorylation / drug effects
  • Protein Kinase Inhibitors / pharmacology*

Substances

  • Protein Kinase Inhibitors
  • Mitogen-Activated Protein Kinase Kinases