Cited by 212Melanoma and MAPK PathwaysProtein Kinase Regulation and GTPase SignalingProtein Tyrosine Phosphatases

Targeting RAS–RAF–MEK–ERK signaling pathway in human cancer: Current status in clinical trials

Open access
Song, Yanlin, Bi, Zhenfei, Liu, Yu, Qin, Furong, Wei, Yuquan, Wei, Xiawei·2023·Genes & Diseases

Abstract

Molecular target inhibitors have been regularly approved by Food and Drug Administration (FDA) for tumor treatment, and most of them intervene in tumor cell proliferation and metabolism. The RAS-RAF-MEK-ERK pathway is a conserved signaling pathway that plays vital roles in cell proliferation, survival, and differentiation. The aberrant activation of the RAS-RAF-MEK-ERK signaling pathway induces tumors. About 33% of tumors harbor RAS mutations, while 8% of tumors are driven by RAF mutations. Great efforts have been dedicated to targeting the signaling pathway for cancer treatment in the past decades. In this review, we summarized the development of inhibitors targeting the RAS-RAF-MEK-ERK pathway with an emphasis on those used in clinical treatment. Moreover, we discussed the potential combinations of inhibitors that target the RAS-RAF-MEK-ERK signaling pathway and other signaling pathways. The inhibitors targeting the RAS-RAF-MEK-ERK pathway have essentially modified the therapeutic strategy against various cancers and deserve more attention in the current cancer research and treatment.

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Crossref · 10.1016/j.gendis.2022.05.006

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204 of 204 references verified0 citation errors · 0 not checkable

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  • Aberrant activation of the RAS/MAPK pathway contributes to the development and progression of MM and other cancers.

    “The aberrant activation of RAS/MAPK pathway contributes to the development and progression of MM and other cancers [87, 88].”

    From Multiple myeloma: signaling pathways and targeted therapy (2024) · cites this paper as [88]

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Authors
Song, Y., Bi, Z., Liu, Y., Qin, F., Wei, Y., & Wei, X.
Affiliations
Sichuan University (CN)
Corresponding author
Wei, Xiawei
Venue
Genes & Diseases
Publisher
Elsevier BV
Published
2023-01
Volume
10
Issue
1
Pages
76-88
ISSN
2352-3042 (ISSN-L)
OpenAlex
W4280552157
Cited by
212
References
206
Citations by year
2026: 52 · 2025: 77 · 2024: 58 · 2023: 23 · 2022: 2
FWCI
4.17
Type
journal article
Language
en
Open access
Locations
  • Genes & Diseases (publishedVersion, cc-by-nc-nd)
  • PubMed Central (publishedVersion)
  • PubMed (publishedVersion)
  • DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
Funders
  • National Outstanding Youth Science Fund Project of National Natural Science Foundation of China (32122052)
  • Key Research and Development Program of Sichuan Province (2020YFS0553)
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Melanoma and MAPK Pathways
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Kinase Regulation and GTPase Signaling
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Tyrosine Phosphatases
Keywords
RAS/MAPK pathway, targeted cancer therapy, RAS inhibitors, RAF inhibitors, MEK inhibitors, ERK inhibitor, combination therapy, RAS mutations, RAF mutations, clinical trials, tumor cell proliferation

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