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Updated: Apr 30, 2026

Characterize Disease-related Mutants of RAF Family Kinases by Using a Set of Practical and Feasible Methods
Published on: July 17, 2019
New RAF kinase inhibitors in cancer therapy
Juan Martin-Liberal1, James Larkin
1The Royal Marsden Hospital , Fulham Road SW3 6JJ, London , UK +44 20 7811 8576 ; +44 20 7811 8103 ; james.larkin@rmh.nhs.uk.
Introduction:
Alterations in some key components of the MAPK pathway, such as BRAF, have been found to be related to the development of several malignancies. A number of BRAF inhibitors have been developed in recent years. Two of these compounds, vemurafenib and dabrafenib, have been licensed for the treatment of BRAF-mutant advanced melanoma.
Areas Covered:
This article reviews the antitumour activity and safety of the BRAF inhibitors, vemurafenib and dabrafenib. Moreover, early clinical data available for the most promising new members of this family of drugs as well as the novel therapeutic strategy of dual RAF-MEK inhibition is reviewed. A perspective of the potential role of MAPK inhibition in the treatment of cancer in forthcoming years is also provided.
Expert Opinion:
Inhibition of BRAF has achieved highly successful results in patients affected by BRAF-mutated melanoma and has revolutionised their care. Its efficacy in other malignancies is currently under evaluation in monotherapy and as combination with other agents. Early clinical results of concomitant inhibition of BRAF and MEK suggest that this therapeutic approach is superior to either BRAF or MEK inhibition alone. Identification of BRAF mutations sensitive to treatment is essential for the success of these drugs.
Insights
BRAF inhibitors like vemurafenib and dabrafenib show success in BRAF-mutant melanoma. Dual BRAF-MEK inhibition appears superior, with BRAF mutation identification crucial for treatment success.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- BRAF pathway alterations are linked to various cancers.
- BRAF inhibitors vemurafenib and dabrafenib are approved for BRAF-mutant advanced melanoma.
Purpose of the Study:
- Review the efficacy and safety of vemurafenib and dabrafenib.
- Examine emerging BRAF inhibitors and dual RAF-MEK inhibition strategies.
- Provide a future outlook on MAPK pathway inhibition in cancer treatment.
Main Methods:
- Literature review of antitumour activity and safety data.
- Analysis of early clinical data for new BRAF inhibitors.
- Evaluation of dual RAF-MEK inhibition therapeutic strategies.
Main Results:
- BRAF inhibition has revolutionized BRAF-mutant melanoma treatment.
- Efficacy of BRAF inhibitors in other malignancies is under investigation.
- Dual BRAF-MEK inhibition shows promise, potentially exceeding single-agent therapy.
Conclusions:
- Targeted BRAF inhibition is highly effective for specific melanoma patients.
- Further research is needed to establish efficacy in broader cancer types.
- Identifying specific BRAF mutations is critical for successful targeted therapy.
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