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Molecular Pathways and Mechanisms of BRAF in Cancer Therapy

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Acquired BRAF Rearrangements Induce Secondary Resistance to EGFR therapy in EGFR-Mutated Lung Cancers

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Combinatorial strategies to target RAS-driven cancers

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Expanding the Benefit: Dabrafenib/Trametinib as Tissue-Agnostic Therapy for BRAF V600E–Positive Adult and Pediatric Solid Tumors

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BRAF Inhibitor Resistance in Melanoma: Mechanisms and Alternative Therapeutic Strategies

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The Function of RAS Mutation in Cancer and Advances in its Drug Research

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Targeting KRAS: The Elephant in the Room of Epithelial Cancers

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BRAF Mutations Classes I, II, and III in NSCLC Patients Included in the SLLIP Trial: The Need for a New Pre-Clinical Treatment Rationale

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Clinical mutational profiling and categorization of BRAF mutations in melanomas using next generation sequencing

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Signaling from RAS to RAF: The Molecules and Their Mechanisms

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The Predictive and Prognostic Role of RAS–RAF–MEK–ERK Pathway Alterations in Breast Cancer: Revision of the Literature and Comparison with the Analysis of Cancer Genomic Datasets

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Durable Suppression of Acquired MEK Inhibitor Resistance in Cancer by Sequestering MEK from ERK and Promoting Antitumor T-cell Immunity

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Development of Allosteric BRAF Peptide Inhibitors Targeting the Dimer Interface of BRAF

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Defining and Targeting BRAF Mutations in Solid Tumors

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The Pan-RAF–MEK Nondegrading Molecular Glue NST-628 Is a Potent and Brain-Penetrant Inhibitor of the RAS–MAPK Pathway with Activity across Diverse RAS- and RAF-Driven Cancers

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BRAF Mutations as Actionable Targets: A Paradigm Shift in the Management of Colorectal Cancer and Novel Avenues

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Discovery of Raf Family Is a Milestone in Deciphering the Ras-Mediated Intracellular Signaling Pathway

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Response to the Combination of Osimertinib and Trametinib in a Patient With EGFR-Mutant NSCLC Harboring an Acquired BRAF Fusion

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Targeted therapies in melanoma beyond BRAF: targeting NRAS-mutated and KIT-mutated melanoma

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Targeting CRAF kinase in anti-cancer therapy: progress and opportunities

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BRAFV600E-mutant metastatic NSCLC: disease overview and treatment landscape

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The sixth international RASopathies symposium: Precision medicine—From promise to practice

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A structural perspective on targeting the RTK /Ras/ MAP kinase pathway in cancer

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Identification and characterization of a BRAF fusion oncoprotein with retained autoinhibitory domains

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Epigenetic Mechanisms of Escape from BRAF Oncogene Dependency

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BRAF paradox breakers PLX8394, PLX7904 are more effective against BRAFV600Ε CRC cells compared with the BRAF inhibitor PLX4720 and shown by detailed pathway analysis

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RAS degraders: The new frontier for RAS-driven cancers

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Drug resistance in targeted cancer therapies with RAF inhibitors

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RAF1 amplification drives a subset of bladder tumors and confers sensitivity to MAPK-directed therapeutics

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Mini review: The FDA-approved prescription drugs that target the MAPK signaling pathway in women with breast cancer

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Adult pilocytic astrocytoma in the molecular era: a comprehensive review

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RAS pathway regulation in melanoma

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The future of targeted kinase inhibitors in melanoma

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Prolonged Complete Response With Combined Dabrafenib and Trametinib After BRAF Inhibitor Failure in BRAF-Mutant Glioblastoma

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Lung Cancer Driven by BRAFG469V Mutation Is Targetable by EGFR Kinase Inhibitors

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Mechanism and inhibition of BRAF kinase

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A Next-Generation BRAF Inhibitor Overcomes Resistance to BRAF Inhibition in Patients with BRAF -Mutant Cancers Using Pharmacokinetics-Informed Dose Escalation

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Pan-RAF inhibition induces apoptosis in acute myeloid leukemia cells and synergizes with BCL2 inhibition

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Current Advances and Trends in KRAS Targeted Therapies for Colorectal Cancer

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Classical RAS proteins are not essential for paradoxical ERK activation induced by RAF inhibitors

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Recent advances in targeting protein kinases and pseudokinases in cancer biology

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Emerging actionable targets to treat therapy-resistant colorectal cancers

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Melanomas with concurrent BRAF non-p.V600 and NF1 loss-of-function mutations are targetable by BRAF/MEK inhibitor combination therapy

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BRAF oncogenic mutants evade autoinhibition through a common mechanism

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Recent developments in mitogen activated protein kinase inhibitors as potential anticancer agents

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BRAF/MEK inhibition in NSCLC: mechanisms of resistance and how to overcome it

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From off-to on-target: New BRAF-inhibitor-template-derived compounds selectively targeting mitogen activated protein kinase kinase 4 (MKK4)

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Mutations in the Serine/Threonine Kinase BRAF: Oncogenic Drivers in Solid Tumors

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The anti-cancer drug dabrafenib is not cardiotoxic and inhibits cardiac remodelling and fibrosis in a murine model of hypertension

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Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting V600EBRAF

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BRAF Targeting Across Solid Tumors: Molecular Aspects and Clinical Applications

Mechahougui, H., Gutmans, J., Gouasmi, R., Smekens, L., & Friedlaender, A. (2025) · International Journal of Molecular Sciences · doi:10.3390/ijms26083757 · Cited by 19

Preclinical Characterization of a Next-Generation Brain Permeable, Paradox Breaker BRAF Inhibitor

Wichmann, J., Rynn, C., Friess, T., Petrig-Schaffland, J., Kornacker, M., Handl, C., Emmenegger, J., Eckmann, J., Herting, F., Frances, N., et al. (2021) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-21-2761 · Cited by 18

Targeting RAF dimers in RAS mutant tumors: From biology to clinic

Yin, H., Tang, Q., Xia, H., & Bi, F. (2024) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2024.02.018 · Cited by 18

Targeting Infrequent Driver Alterations in Non-Small Cell Lung Cancer

Nokin, M., Ambrogio, C., Nadal, E., & Santamaría, D. (2020) · Trends in cancer · doi:10.1016/j.trecan.2020.11.005 · Cited by 21

MEK inhibitors in non-V600 BRAF mutations and fusions

Johnson, D. B., Nebhan, C. A., & Noel, M. S. (2020) · Oncotarget · doi:10.18632/oncotarget.27788 · Cited by 18

Analysis of RAS and drug induced homo- and heterodimerization of RAF and KSR1 proteins in living cells using split Nanoluc luciferase

Rohrer, L., Spohr, C., Beha, C., Griffin, R., Braun, S. L., Halbach, S., & Brummer, T. (2023) · Cell Communication and Signaling · doi:10.1186/s12964-023-01146-9 · Cited by 17

Unique Spectrum of Activating BRAF Alterations in Prostate Cancer

Chehrazi‐Raffle, A., Tukachinsky, H., Toye, E., Sivakumar, S., Schrock, A. B., Bergom, H. E., Ebrahimi, H., Pal, S. K., Dorff, T. B., Agarwal, N., et al. (2023) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-23-1393 · Cited by 17

Comparative Genomic Analysis and Clinical Outcomes of BRAF -mutated Advanced Biliary Tract Cancers

Tang, T., Nichetti, F., Kaplan, B., Lonardi, S., Pietrantonio, F., Salvatore, L., Vivaldi, C., Rimassa, L., de Braud, F., Rizzato, M. D., et al. (2023) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-23-1926 · Cited by 17

Structure-based design of potent and selective inhibitors targeting RIPK3 for eliminating on-target toxicity in vitro

Su, H., Chen, G., Xie, H., Li, W., Xiong, M., He, J., Hu, H., Zhao, W., Shao, Q., Li, M., et al. (2025) · Nature Communications · doi:10.1038/s41467-025-59432-8 · Cited by 17

An evaluation of encorafenib for the treatment of melanoma

Carr, M. J., Sun, J. X., Eroglu, Z., & Zager, J. S. (2019) · Expert Opinion on Pharmacotherapy · doi:10.1080/14656566.2019.1694664 · Cited by 16

Applications of personalised signalling network models in precision oncology

Hastings, J. F., O’Donnell, Y. E. I., Fey, D., & Croucher, D. R. (2020) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2020.107555 · Cited by 18

Past and Future Strategies to Inhibit Membrane Localization of the KRAS Oncogene

Haidar, M., & Jacquemin, P. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms222413193 · Cited by 18

Discovery of spiro amide SHR902275: A potent, selective, and efficacious RAF inhibitor targeting RAS mutant cancers

Zhao, P., Zhuang, L., Wang, X., Huang, S. M., Wu, H., Zhou, Y., Yan, Y., Zhang, F., Shen, R., Li, J., et al. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.114040 · Cited by 16

Applying Precision to the Management of BRAF-Mutant Metastatic Colorectal Cancer

Johnson, B., & Kopetz, S. (2020) · Targeted Oncology · doi:10.1007/s11523-020-00747-5 · Cited by 14

Urothelial carcinoma with an NRF1-BRAF rearrangement and response to targeted therapyPreprint

Isaacson, A. L., Guseva, N. V., Bossler, A., & Ma, D. (2019) · Molecular Case Studies · doi:10.1101/mcs.a003848 · Cited by 15

Rapid response to monotherapy with MEK inhibitor trametinib for a lung adenocarcinoma patient harboring primary SDN1-BRAF fusion: A case report and literature review

Yu, Y., Yu, M., Li, Y., Zhou, X., Tian, T., Du, Y., Tu, Z., & Huang, M. (2022) · Frontiers in Oncology · doi:10.3389/fonc.2022.945620 · Cited by 14

Novel RAF ‐directed approaches to overcome current clinical limits and block the RAS / RAF node

Scardaci, R., Berlinska, E., Scaparone, P., Michelina, S. V., Garbo, E., Novello, S., Santamarı́a, D., & Ambrogio, C. (2024) · Molecular Oncology · doi:10.1002/1878-0261.13605 · Cited by 14

Exploring Small-Molecule Inhibitors Targeting MAPK Pathway Components: Focus on ERK, MEK1, and MEK2 Kinases in Cancer Treatment

Mukherjee, T., Mohanty, S., Kaur, J., Das, M., Adhikary, K., Chatterjee, P., & Maiti, R. (2024) · Chemical Biology Letters · doi:10.62110/sciencein.cbl.2024.v11.659 · Cited by 15

Tumor-Agnostic Genomic and Clinical Analysis of BRAF Fusions Identifies Actionable Targets

Chen, M. F., Yang, S., Tao, J. J., Desîlets, A., Diamond, E. L., Wilhelm, C., Rosen, E. Y., Gong, Y., Mullaney, K. A., Torrisi, J. M., et al. (2024) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-23-3981 · Cited by 14

Multi‐sample measurement of hyperpolarized pyruvate‐to‐lactate flux in melanoma cells

Lees, H., Millan, M., Ahamed, F., Eskandari, R., Granlund, K. L., Jeong, S., & Keshari, K. R. (2020) · NMR in Biomedicine · doi:10.1002/nbm.4447 · Cited by 14

Recent Developments in Targeting RAS Downstream Effectors for RAS-Driven Cancer Therapy

Tatlı, Ö., & Doğanay, G. D. (2021) · Molecules · doi:10.3390/molecules26247561 · Cited by 14

Identification of Synergistic Drug Combinations to Target KRAS-Driven Chemoradioresistant Cancers Utilizing Tumoroid Models of Colorectal Adenocarcinoma and Recurrent Glioblastoma

Gupta, K., Jones, J. C., Farias, V., Mackeyev, Y., Singh, P. K., Quiñones‐Hinojosa, A., & Krishnan, S. (2022) · Frontiers in Oncology · doi:10.3389/fonc.2022.840241 · Cited by 12

Development of a potent small‐molecule degrader against oncogenic BRAFV600E protein that evades paradoxical MAPK activation

Ohoka, N., Suzuki, M., Uchida, T., Tsukumo, Y., Yoshida, M., Inoué, T., Ohki, H., & Naito, M. (2022) · Cancer Science · doi:10.1111/cas.15401 · Cited by 13

Abstract PR-1: Acquired resistance to RAF inhibitors is mediated by splicing isoforms of BRAF(V600E) that dimerize in a RAS-independent manner.

Poulikakos, P. I. (2011) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.targ-11-pr-1 · Cited by 2

Abstract IA7: Novel mechanisms of resistance in BRAF-mutant melanoma

Poulikakos, P. I. (2012) · Clinical Cancer Research · doi:10.1158/1078-0432.mechres-ia7

Abstract LB-419: An in-frame deletion in the N-terminal regulatory domain of BRAF(V600E) causes resistance to the RAF inhibitor PLX4032

Poulikakos, P. I., Persaud, Y., Gabay, M. T., Janakiraman, M., Joseph, E. W., Pratilas, C. A., Chapman, P. B., Rosen, N. X., & Solit, D. B. (2011) · Cancer Research · doi:10.1158/1538-7445.am2011-lb-419 · Cited by 1

BRAF Mutants Evade ERK-Dependent Feedback by Different Mechanisms that Determine Their Sensitivity to Pharmacologic Inhibition

Yao, Z., Torres, N. M., Tao, A., Gao, Y., Luo, L., Li, Q., de Stanchina, E., Abdel-Wahab, O., Solit, D. B., Poulikakos, P. I., et al. (2015) · Cancer Cell · doi:10.1016/j.ccell.2015.08.001 · Cited by 543

New RAF inhibitor with broad activity

Crunkhorn, S. (2015) · Nature Reviews Drug Discovery · doi:10.1038/nrd4778