ArticleChembiochem : a European journal of chemical biology2018
Mechanism of BRAF Activation through Biochemical Characterization of the Recombinant Full-Length Protein.
Article in Chembiochem : a European journal of chemical biology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 50 citations in OpenAlex.
- Dual targeting of interlocked PTK2B and MAPK signaling triggers synergistic ferroptosis via autophagic flux disruption in BRAFCell communication and signaling : CCS · 2026Article
- Divergent CRD-Dependent Mechanisms Govern RAS Isoform-Selective Recruitment of CRAF and ARAF.bioRxiv : the preprint server for biology · 2026Article
- Synonymous Variants of Potential Significance Identified by a 52-Gene Clinical Sequencing Panel in Non-Small Cell Lung Cancer.Genes, chromosomes & cancer · 2026Article
- The paradoxical activity of BRAF inhibitors: potential use in wound healing.Archives of dermatological research · 2025Review
- Spatiotemporal Control of Protein Activity through Optogenetic Allosteric Regulation.Journal of visualized experiments : JoVE · 2024Article
- Exploring Predictive and Prognostic Biomarkers in Colorectal Cancer: A Comprehensive Review.Cancers · 2024Review
- An updated literature on BRAF inhibitors (2018-2023).Molecular diversity · 2024Review
- Hairy cell leukemia - etiopathogenesis, diagnosis and modern therapeutic approach.Biochemia medica · 2024Review
- Ultraviolet Radiation Biological and Medical Implications.Current issues in molecular biology · 2024Review
- Conformational diversity and protein-protein interfaces in drug repurposing in Ras signaling pathway.Scientific reports · 2024Article
- Exploring somatic mutations inFrontiers in pharmacology · 2024Article
- Unveiling the domain-specific and RAS isoform-specific details of BRAF kinase regulation.eLife · 2023Article
- Indeterminate Thyroid Nodules: From Cytology to Molecular Testing.Diagnostics (Basel, Switzerland) · 2023Review
- Co-dependent regulation of p-BRAF and potassium channel KCNMA1 levels drives glioma progression.Cellular and molecular life sciences : CMLS · 2023Article
- Mechanism and inhibition of BRAF kinase.Current opinion in chemical biology · 2022Review
- Targeted Therapy for Melanomas Without BRAF V600 Mutations.Current treatment options in oncology · 2022Review
- Identification of novel natural drug candidates against BRAF mutated carcinoma; An integrative in-silico structure-based pharmacophore modeling and virtual screening process.Frontiers in chemistry · 2022Article
- KNTC1 knockdown suppresses cell proliferation of colon cancer.3 Biotech · 2021Article
- Inhibition of RAF dimers: it takes two to tango.Biochemical Society transactions · 2021Review
- Identification and Characterization of a B-Raf Kinase α-Helix Critical for the Activity of MEK Kinase in MAPK Signaling.Biochemistry · 2020Article
Corrections and comments
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Authors and funding
10 authors at 3 institutions in 1 country.
Funding
Abstract
BRAF kinase plays an important role in mitogen-activated protein kinase (MAPK) signaling and harbors activating mutations in about half of melanomas and in a smaller percentage in many other cancers. Despite its importance, few in vitro studies have been performed to characterize the biochemical properties of full-length BRAF. Herein, a strategy to generate an active, intact form of BRAF protein suitable for in vitro enzyme kinetics is described. It is shown that purified, intact BRAF protein autophosphorylates the kinase activation loop and this can be enhanced by binding the MEK protein substrate through an allosteric mechanism. These studies provide in vitro evidence that BRAF selectively binds to active RAS and that the BRAF/CRAF heterodimer is the most active form, relative to their respective homodimers. Full-length BRAF analysis with small-molecule BRAF inhibitors shows that two drugs, dabrafenib and vemurafenib, can modestly enhance kinase activity of BRAF at low concentration. Taken together, this characterization of intact BRAF contributes to a framework for understanding its role in cell signaling.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.