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Updated: Aug 4, 2025

Reliably Engineering and Controlling Stable Optogenetic Gene Circuits in Mammalian Cells
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Published on: July 6, 2021

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Modulation of ERK5 Activity as a Therapeutic Anti-Cancer Strategy

Duncan C Miller1, Suzannah J Harnor1, Mathew P Martin2

  • 1Cancer Research Horizons Therapeutic Innovation, Newcastle Drug Discovery Group, Newcastle University Centre for Cancer, School of Natural and Environmental Sciences, Newcastle University, Bedson Building, Newcastle upon Tyne NE1 7RU, United Kingdom.

Journal of Medicinal Chemistry
|April 1, 2023
PubMed

Insights

Extracellular signal-regulated kinase 5 (ERK5) shows therapeutic potential in cancer. This review explores ERK5 inhibitors, their complexities, and future drug development for cancer chemotherapy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Extracellular signal-regulated kinase 5 (ERK5) is a key member of the mitogen-activated protein (MAP) kinase pathways.
  • ERK5 pathway dysregulation is implicated in various cancers, suggesting its potential as a therapeutic target.
  • Understanding ERK5's role is crucial for developing effective cancer chemotherapy strategies.

Purpose of the Study:

  • To review the evidence supporting ERK5 as a drug target in cancer.
  • To examine the structural characteristics of ERK5 and its inhibitors.
  • To discuss the complexities of ERK5 pharmacology and future therapeutic opportunities.

Main Methods:

  • Literature review of studies on ERK5 signaling, cancer, and inhibitor development.
  • Analysis of the structural evolution of ERK5 kinase domain inhibitors.
  • Discussion of emerging pharmacological complexities and novel therapeutic approaches.

Main Results:

  • ERK5 is a promising target for cancer chemotherapy.
  • Structurally diverse chemotypes of ERK5 inhibitors have been developed.
  • Paradoxical ERK5 activation by inhibitors presents a pharmacological challenge.
  • Bifunctional degraders of ERK5 show potential for enhanced therapeutic effects.

Conclusions:

  • ERK5 represents a viable target for novel cancer therapeutics.
  • Further research into ERK5 inhibitors and degraders is warranted.
  • Addressing pharmacological complexities is key to successful ERK5-targeted cancer therapy.

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