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

Yuzhen Niu; Hongfang Ji

doi:10.1016/j.drudis.2022.01.012

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

Drug Discov Today. 2022 May;27(5):1464-1473. doi: 10.1016/j.drudis.2022.01.012. Epub 2022 Jan 29.

Authors

Yuzhen Niu¹, Hongfang Ji²

Affiliations

¹ Shandong Provincial Research Center for Bioinformatic Engineering and Technique, School of Life Sciences and Medicine, Shandong University of Technology, Zibo 255000, Shandong, PR China. Electronic address: niuyzh329@sdut.edu.cn.
² Shandong Provincial Research Center for Bioinformatic Engineering and Technique, School of Life Sciences and Medicine, Shandong University of Technology, Zibo 255000, Shandong, PR China. Electronic address: jhf@sdut.edu.cn.

PMID: 35104620
DOI: 10.1016/j.drudis.2022.01.012

Abstract

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.

Keywords: CADD; Computer-aided drug design; ERK1/2; ERK1/2 inhibitors; Extracellular regulated protein kinase 1/2.

Publication types

Review
Research Support, Non-U.S. Gov't

MeSH terms

Drug Design
Enzyme Inhibitors / pharmacology
Extracellular Signal-Regulated MAP Kinases
Humans
MAP Kinase Signaling System*
Phosphorylation
Protein Kinase Inhibitors* / pharmacology
Protein Kinase Inhibitors* / therapeutic use
Signal Transduction

Substances

Enzyme Inhibitors
Protein Kinase Inhibitors
Extracellular Signal-Regulated MAP Kinases