Targeting RAS–RAF–MEK–ERK signaling pathway in human cancer: Current status in clinical trials
Open accessAbstract
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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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)
- PMC
- PMC10066287
- 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
- gold
- doi.org
- Licence
- 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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