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Updated: Feb 5, 2026

Characterize Disease-related Mutants of RAF Family Kinases by Using a Set of Practical and Feasible Methods
Published on: July 17, 2019
Recent advances of RAF (rapidly accelerated fibrosarcoma) inhibitors as anti-cancer agents
Usama M Ammar1, Mohammed S Abdel-Maksoud2, Chang-Hyun Oh3
1Center for Biomaterials, Korea Institute of Science & Technology (KIST), Seoul, Seongbuk-gu, 02792, Republic of Korea; Department of Biomolecular Science, University of Science & Technology (UST), Daejeon, Yuseong-gu, 34113, Republic of Korea; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Ahram Canadian University, Giza, 12566, Egypt.
Abstract:
Frequent oncogenic mutations have been identified in MAPK (mitogen-activated protein kinase) signaling pathway components. As a result, MAPK pathway is associated with human cancer initiation, in particular RAF (rapidly accelerated fibrosarcoma) component. The mutation in RAF component leads to auto-activation of MAPK signaling pathway, stimulating the uncontrolled cell growth and proliferation. In last few years, diverse chemical scaffolds have been identified as RAF inhibitors. Most of these scaffolds show potent anti-cancer activity. The present review highlights the recent investigations of RAF inhibitors during the last five years.
Insights
RAF pathway mutations drive cancer by promoting uncontrolled cell growth. Recent research focuses on diverse RAF inhibitors, showing potent anti-cancer activity, with this review highlighting investigations over the past five years.
Area of Science:
- Oncology
- Molecular Biology
- Medicinal Chemistry
Background:
- The mitogen-activated protein kinase (MAPK) signaling pathway is frequently altered in cancer.
- Mutations in RAF components of the MAPK pathway lead to its auto-activation, driving uncontrolled cell proliferation.
- RAF signaling is a critical target for anti-cancer drug development.
Purpose of the Study:
- To review recent investigations of RAF inhibitors over the last five years.
- To highlight the development of diverse chemical scaffolds targeting the RAF component.
- To summarize the anti-cancer activity of identified RAF inhibitors.
Main Methods:
- Literature review of scientific publications from the last five years.
- Analysis of studies reporting on RAF inhibitors and their chemical scaffolds.
- Evaluation of reported anti-cancer activities and mechanisms of action.
Main Results:
- Numerous chemical scaffolds targeting RAF have been identified.
- Many of these RAF inhibitors demonstrate significant anti-cancer potency.
- Recent research has expanded the landscape of RAF-targeted therapies.
Conclusions:
- RAF inhibitors represent a promising therapeutic strategy for cancers driven by MAPK pathway mutations.
- Continued investigation into novel chemical scaffolds is crucial for advancing RAF-targeted cancer treatments.
- The development of effective RAF inhibitors holds potential for controlling tumor growth and proliferation.
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