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Updated: Mar 19, 2026

Characterize Disease-related Mutants of RAF Family Kinases by Using a Set of Practical and Feasible Methods
Published on: July 17, 2019
Therapeutic Approaches to RAS Mutation
Aaron J Scott1, Christopher H Lieu, Wells A Messersmith
1From the Division of Medical Oncology, University of Colorado Denver Anschutz Medical Campus, and University of Colorado Cancer Center, Aurora, CO.
Abstract:
The study of oncogenic RAS mutations has led to crucial discoveries regarding cancer molecular biology and behavior and has been integral in shaping the era of targeted cancer therapy. RAS mutations are one of the most common oncogenic drivers in human cancer, and intense efforts to find a clinically effective inhibitor are ongoing. Despite these efforts, targeting RAS mutations has remained elusive, so much so that some have termed oncogenic RAS mutations as "undruggable." In this review, we will summarize current understanding of RAS biology, explore strategies to inhibit RAS oncoproteins and its downstream effectors, and discuss recently described complexities that have shed new light on this pursuit.
Insights
Targeting oncogenic RAS mutations, common in cancer, remains challenging. This review explores RAS biology, inhibition strategies, and new complexities in developing effective cancer therapies.
Area of Science:
- Oncology
- Molecular Biology
- Cancer Genetics
Background:
- Oncogenic RAS mutations are key drivers in human cancers.
- These mutations have significantly advanced cancer molecular biology understanding and targeted therapy development.
- Despite progress, effective inhibitors for RAS mutations remain elusive, earning them the "undruggable" moniker.
Purpose of the Study:
- To review current knowledge of RAS biology.
- To explore strategies for inhibiting RAS oncoproteins and their downstream targets.
- To discuss recent complexities influencing the development of RAS-targeted cancer therapies.
Main Methods:
- Literature review of RAS biology and targeted therapy research.
- Analysis of current and emerging strategies for RAS oncoprotein inhibition.
- Discussion of recent findings and complexities in the field.
Main Results:
- RAS mutations are prevalent oncogenic drivers.
- Targeting RAS has been historically difficult, necessitating novel approaches.
- Recent discoveries are providing new insights into RAS biology and potential therapeutic avenues.
Conclusions:
- Understanding RAS biology is crucial for cancer treatment.
- Developing effective RAS inhibitors is an ongoing, complex challenge.
- Emerging strategies and complexities offer new hope for targeting RAS-mutated cancers.
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