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Through the Looking Glass: Time-lapse Microscopy and Longitudinal Tracking of Single Cells to Study Anti-cancer Therapeutics
06:00

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Drugging ERK1/2 in Cancer: A Glimpse of Small-Molecule Inhibitors

Zhiqi Peng1,2, Yuqi Fu2, Yanmei Chen1,2

  • 1Department of Urology, Institute of Precision Drug Innovation and Cancer Center, Second Affiliated Hospital of Dalian Medical University, Dalian, China.

Medicinal Research Reviews
|July 22, 2026
PubMed

Insights

Extracellular signal-regulated kinases 1 and 2 (ERK1/2) are key in cancer. This review covers ERK1/2 signaling, its role in tumorigenesis, and emerging targeted therapies for precision oncology.

Area of Science:

  • Molecular Biology
  • Oncology
  • Pharmacology

Background:

  • Extracellular signal-regulated kinases 1 and 2 (ERK1/2) are central components of the mitogen-activated protein kinase (MAPK) pathway.
  • Aberrant ERK1/2 signaling is a hallmark of various cancers, including melanoma, pancreatic, and colorectal cancers, driving tumorigenesis.

Purpose of the Study:

  • To provide a comprehensive review of ERK1/2 research, encompassing historical milestones, signaling networks, and therapeutic strategies.
  • To explore novel therapeutic modalities for targeting ERK1/2 in precision oncology.

Main Methods:

  • Literature review of historical milestones in ERK1/2 research.
  • Detailed analysis of the ERK1/2 signaling network, including upstream regulators (RAS, RAF, MEK) and downstream effectors.
  • Overview of current and emerging therapeutic approaches targeting ERK1/2.

Main Results:

  • ERK1/2 signaling is a critical regulator of tumorigenesis, frequently dysregulated in major cancers.
  • Therapeutic strategies include single-target and dual-target small-molecule inhibitors, combination therapies, and innovative approaches like PROTACs, AUTACs, and ADCs.
  • These therapies aim to overcome resistance and enhance efficacy in cancer treatment.

Conclusions:

  • ERK1/2-targeted therapies hold significant potential in the field of precision oncology.
  • Integrating mechanistic understanding with clinical development is crucial for advancing ERK1/2-directed cancer treatments.
  • Novel therapeutic modalities offer promising avenues for selective modulation of ERK1/2 activity.
Keywords:
ERK1/2MAPK signaling pathwaycancer therapydrug discoverysmall‐molecule inhibitor

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