Related Experiment Video
Updated: Jul 5, 2025

Characterize Disease-related Mutants of RAF Family Kinases by Using a Set of Practical and Feasible Methods
Published on: July 17, 2019
Molecular Targeting of the BRAF Proto-Oncogene/Mitogen-Activated Protein Kinase (MAPK) Pathway across Cancers
Khine S Shan1, Tauseef U Rehman1, Stan Ivanov1
1Memorial Health Care, Division of Hematology and Oncology, Pembroke Pines, FL 33328, USA.
Abstract:
The mitogen-activated protein kinase (MAPK) pathway is essential for cellular proliferation, growth, and survival. Constitutive activation of this pathway by BRAF mutations can cause downstream activation of kinases, leading to uncontrolled cellular growth and carcinogenesis. Therefore, inhibition of BRAF and the downstream substrate MEK has been shown to be effective in controlling tumor growth and proliferation. Over the last decade, several BRAF and MEK inhibitors have been investigated, ranging from primarily melanoma to various cancer types with BRAF alterations. This subsequently led to several Food and Drug Administration (FDA) approvals for BRAF/MEK inhibitors for melanoma, non-small cell lung cancer, anaplastic thyroid cancer, colorectal cancer, histiocytosis neoplasms, and finally, tumor-agnostic indications. Here, this comprehensive review will cover the developments of BRAF and MEK inhibitors from melanomas to tumor-agnostic indications, novel drugs, challenges, future directions, and the importance of those drugs in personalized medicine.
Insights
BRAF and MEK inhibitors are crucial for controlling cancer growth by targeting the MAPK pathway. These targeted therapies have expanded from melanoma to various cancers, including tumor-agnostic approvals, advancing personalized medicine.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- The mitogen-activated protein kinase (MAPK) pathway regulates cell growth and survival.
- BRAF mutations lead to uncontrolled cell proliferation and carcinogenesis.
- Targeting BRAF and MEK is a validated strategy for cancer treatment.
Purpose of the Study:
- To review the development of BRAF and MEK inhibitors.
- To cover their expansion from melanoma to tumor-agnostic indications.
- To discuss novel drugs, challenges, and future directions in personalized cancer medicine.
Main Methods:
- Literature review of BRAF and MEK inhibitors.
- Analysis of clinical trial data and FDA approvals.
- Discussion of therapeutic advancements and personalized medicine applications.
Main Results:
- BRAF/MEK inhibitors are approved for melanoma, lung, thyroid, colorectal cancers, and histiocytosis.
- Tumor-agnostic approvals demonstrate broad efficacy.
- Significant progress has been made in targeted cancer therapy.
Conclusions:
- BRAF and MEK inhibitors represent a significant advancement in oncology.
- Their application has broadened considerably, offering new hope for patients.
- Continued research is vital for optimizing their use in personalized medicine.
More Related Videos
Related Concept Videos
MAPK Signaling Cascades
Targeted Cancer Therapies
There are several types of targeted therapies against...
mTOR Signaling and Cancer Progression
The mTOR pathway or the...
Interactions Between Signaling Pathways
Convergence and divergence, and cross-talk between signaling pathways
Two distinct signaling pathways can converge on a single functional unit, which may either be a single protein or a complex of proteins. The response is either functionally distinct or synergistic between the two pathways but different from the response...
PI3K/mTOR/AKT Signaling Pathway
Mitogens and the Cell Cycle

