4.7 Review

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

Journal

DRUG DISCOVERY TODAY
Volume 27, Issue 5, Pages 1464-1473

Publisher

ELSEVIER SCI LTD
DOI: 10.1016/j.drudis.2022.01.012

Keywords

Extracellular regulated protein kinase 1; 2; ERK1; 2 inhibitors; Computer-aided drug design; CADD

Funding

  1. Natural Foundation of Shandong Province [ZR2018BB055]

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In this review, the importance of the ERK1/2 signaling pathway in the treatment of various diseases and the current research on ERK1/2 inhibitors are summarized. The main approaches used to discover ERK inhibitors, including the advantages of computer-aided drug design, are also discussed.
Extracellular signal-regulated kinases 1 and 2 (ERK1/2) are important members of the RAS signaling pathway. They are abnormally expressed in many diseases and, thus, are considered key therapeutic targets of human diseases. In this review, we summarize the importance of the ERK1/2 signaling pathway in the treatment of different diseases and inhibitors of ERK1/2 in clinical or preclinical research. We also discuss the main approaches used to discover ERK inhibitors, including the application and advantages of computer-aided drug design (CADD) approaches.

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