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Updated: Jan 21, 2026

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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Development of ERK1/2 inhibitors as a therapeutic strategy for tumour with MAPK upstream target mutations

Longfei Miao1, Hongqi Tian1

  • 1Tianjin Key Laboratory of Radiation Medicine and Molecular Nuclear Medicine, Institute of Radiation Medicine, Chinese Academy of Medical Science & Peking Union Medical College, Tianjin, China.

Journal of Drug Targeting
|July 26, 2019
PubMed

Insights

Extracellular signal-regulated kinases 1 and 2 (ERK1/2) inhibitors show promise against tumors, but resistance emerges. This review explores ERK1/2 inhibitors as a strategy to overcome resistance and treat cancers with MAPK pathway alterations.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Extracellular signal-regulated kinases 1 and 2 (ERK1/2) are crucial for cell survival and proliferation.
  • Inhibitors targeting the ERK pathway demonstrate antitumor activity, but drug resistance is a significant challenge.
  • Reactivation of ERK1/2 signaling is a common mechanism of acquired resistance to MAPK pathway inhibitors.

Purpose of the Study:

  • To review the mechanisms and types of ERK1/2 inhibitors.
  • To summarize the development status of small-molecule ERK1/2 inhibitors.
  • To discuss future research directions for ERK1/2 inhibitors in cancer therapy.

Main Methods:

  • Literature review of preclinical and clinical studies on ERK1/2 inhibitors.
  • Analysis of drug resistance mechanisms related to ERK1/2 signaling.
  • Exploration of therapeutic strategies involving ERK1/2 inhibition.

Main Results:

  • ERK1/2 inhibitors are effective against tumors with specific MAPK pathway mutations.
  • These inhibitors offer a potential strategy to overcome acquired resistance to other MAPK inhibitors.
  • Ongoing clinical studies are evaluating the efficacy and safety of various small-molecule ERK1/2 inhibitors.

Conclusions:

  • ERK1/2 inhibitors represent a promising therapeutic avenue for various cancers.
  • Overcoming drug resistance through ERK1/2 inhibition requires further investigation.
  • Targeting the ERK pathway holds potential for improved cancer treatment outcomes.
Keywords:
ERK1/2 inhibitorsMAPK pathwayclinicaldrug resistantpreclinicaltumour

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