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Current developments in extracellular-regulated protein kinase (ERK1/2) inhibitors

Yuzhen Niu1, Hongfang Ji1

  • 1Shandong Provincial Research Center for Bioinformatic Engineering and Technique, School of Life Sciences and Medicine, Shandong University of Technology, Zibo 255000, Shandong, PR China.

Drug Discovery Today
|February 1, 2022
PubMed

Insights

Extracellular signal-regulated kinases 1 and 2 (ERK1/2) are key targets for treating diseases due to their abnormal expression. This review covers ERK1/2

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Extracellular signal-regulated kinases 1 and 2 (ERK1/2) are crucial components of the RAS signaling pathway.
  • Abnormal ERK1/2 expression is implicated in various human diseases, highlighting their therapeutic potential.

Purpose of the Study:

  • To review the significance of the ERK1/2 signaling pathway in disease treatment.
  • To discuss current clinical and preclinical ERK1/2 inhibitors.
  • To explore ERK inhibitor discovery methods, including computer-aided drug design (CADD).

Main Methods:

  • Literature review of ERK1/2 signaling in disease.
  • Analysis of existing ERK1/2 inhibitors in research and clinical trials.
  • Evaluation of CADD methodologies for ERK inhibitor development.

Main Results:

  • ERK1/2 pathway dysregulation is a common feature across multiple diseases.
  • Several ERK1/2 inhibitors are under investigation for therapeutic applications.
  • CADD offers efficient and advantageous approaches for identifying novel ERK inhibitors.

Conclusions:

  • The ERK1/2 pathway is a validated therapeutic target for diverse diseases.
  • Targeting ERK1/2 with inhibitors shows promise in preclinical and clinical settings.
  • CADD is a valuable tool for accelerating the discovery of effective ERK inhibitors.
Keywords:
CADDComputer-aided drug designERK1/2ERK1/2 inhibitorsExtracellular regulated protein kinase 1/2

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