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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
Summary
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.
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