New perspectives for targeting RAF kinase in human cancer

PD-1 and PD-L1 Immune Checkpoint Blockade to Treat Breast Cancer

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Improved Survival with Ipilimumab in Patients with Metastatic Melanoma

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Sorafenib in advanced hepatocellular carcinoma

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Mutations of the BRAF gene in human cancer

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Improved survival with vemurafenib in melanoma with BRAF V600E mutation

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A New Era of Systemic Therapy for Hepatocellular Carcinoma with Regorafenib and Lenvatinib

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Pembrolizumab versus Ipilimumab in Advanced Melanoma

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Comprehensive molecular profiling of lung adenocarcinoma

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Sorafenib in Advanced Hepatocellular Carcinoma

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

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Ocular Safety Profile of BRAF and MEK Inhibitors

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How far we have come targeting BRAF-mutant non-small cell lung cancer (NSCLC)

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

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BRAF inhibitors promote intermediate BRAF(V600E) conformations and binary interactions with activated RAS

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

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MAPK inhibitor sensitivity scores predict sensitivity driven by the immune infiltration in pediatric low-grade gliomas

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EV20-mediated delivery of cytotoxic auristatin MMAF exhibits potent therapeutic efficacy in cutaneous melanoma

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Atypical, Non-V600 BRAF Mutations as a Potential Mechanism of Resistance to EGFR Inhibition in Metastatic Colorectal 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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CRAF mutations in lung cancer can be oncogenic and predict sensitivity to combined type II RAF and MEK inhibition

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Paradoxical mitotic exit induced by a small molecule inhibitor of APC/CCdc20

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Mortalin (HSPA9) facilitates BRAF -mutant tumor cell survival by suppressing ANT3-mediated mitochondrial membrane permeability

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

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Design, synthesis, in vitro anticancer evaluation, kinase inhibitory effects, and pharmacokinetic profile of new 1,3,4-triarylpyrazole derivatives possessing terminal sulfonamide moiety

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Progress towards molecular-based management of childhood Langerhans cell histiocytosis

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Immunohistochemical assessment of HRAS Q61R mutations in breast adenomyoepitheliomas

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Approved Small-Molecule ATP-Competitive Kinases Drugs Containing Indole/Azaindole/Oxindole Scaffolds: R&D and Binding Patterns Profiling

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Mechanisms of the JNK/p38 MAPK signaling pathway in drug resistance in ovarian cancer

Ma, Y., Li, C., Shen, Y., Wan-hui, Y., Han, M.-X., Mu, Y.-F., & Han, F. (2025) · Frontiers in Oncology · doi:10.3389/fonc.2025.1533352 · Cited by 38

Engineering Targeting Materials for Therapeutic Cancer Vaccines

Briquez, P. S., Hauert, S., de Titta, A., Gray, L. T., Alpar, A. T., Swartz, M. A., & Hubbell, J. A. (2020) · Frontiers in Bioengineering and Biotechnology · doi:10.3389/fbioe.2020.00019 · Cited by 32

Nuclear receptor tyrosine kinase transport and functions in cancer

Chen, M., Hsu, J. L., & Hung, M. (2020) · Advances in cancer research · doi:10.1016/bs.acr.2020.04.010 · Cited by 33

Characterization and management of ERK inhibitor associated dermatologic adverse events: analysis from a nonrandomized trial of ulixertinib for advanced cancers

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Endoplasmic reticulum stress in melanoma pathogenesis and resistance

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Adaptive Responses as Mechanisms of Resistance to BRAF Inhibitors in Melanoma

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Short-term cellular memory tunes the signaling responses of the chemokine receptor CXCR4

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Silica-based nanomaterials as drug delivery tools for skin cancer (melanoma) treatment

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Intermittent treatment of BRAF V600E melanoma cells delays resistance by adaptive resensitization to drug rechallenge

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Making NSCLC Crystal Clear: How Kinase Structures Revolutionized Lung Cancer Treatment

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B-RAFV600E Inhibitor Dabrafenib Attenuates RIPK3-Mediated Necroptosis and Promotes Functional Recovery after Spinal Cord Injury

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Targeting KRAS in Non-Small Cell Lung Cancer

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RIPK3-MLKL signaling activates mitochondrial CaMKII and drives intrarenal extracellular matrix production during CKD

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Papillary thyroid carcinoma with Hashimoto’s thyroiditis: impact and correlation

Yao, S., & Zhang, H. (2025) · Frontiers in Endocrinology · doi:10.3389/fendo.2025.1512417 · Cited by 31

A Comprehensive Review on the Therapeutic Versatility of Imidazo [2,1-b]thiazoles

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Mechanism and inhibition of BRAF kinase

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Targeting few to help hundreds: JAK, MAPK and ROCK pathways as druggable targets in atypical chronic myeloid leukemia

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Activation Loop Dynamics Are Coupled to Core Motions in Extracellular Signal-Regulated Kinase-2

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Targeting BRAF-mutant non-small cell lung cancer: Current status and future directions

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Development of small-molecule therapeutics and strategies for targeting RAF kinase in BRAF-mutant colorectal cancer

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Immunoproteasome Activation Expands the MHC Class I Immunopeptidome, Unmasks Neoantigens, and Enhances T-cell Anti-Myeloma Activity

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Imidazothiazole-based potent inhibitors of V600E-B-RAF kinase with promising anti-melanoma activity: biological and computational studies

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c-Raf in KRas Mutant Cancers: A Moving Target

McCormick, F. P. (2018) · Cancer Cell · doi:10.1016/j.ccell.2018.01.017 · Cited by 27

Loss of HAT1 expression confers BRAFV600E inhibitor resistance to melanoma cells by activating MAPK signaling via IGF1R

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Anticancer Activity of Euplotin C, Isolated from the Marine Ciliate Euplotes crassus, Against Human Melanoma Cells

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Synergistic inhibition of MEK and reciprocal feedback networks for targeted intervention in malignancy

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Immunomodulatory Properties of BRAF and MEK Inhibitors Used for Melanoma Therapy—Paradoxical ERK Activation and Beyond

Jung, T., Haist, M., Kuske, M., Grabbe, S., & Bros, M. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms22189890 · Cited by 26

Targeting CDC7 sensitizes resistance melanoma cells to BRAFV600E-specific inhibitor by blocking the CDC7/MCM2-7 pathway

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An updated literature on BRAF inhibitors (2018–2023)

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Which Small Molecule? Selecting Chemical Probes for Use in Cancer Research and Target Validation

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Cytotoxicity of combinations of the pan-KRAS inhibitor BAY-293 against primary non-small lung cancer cells

Plangger, A., Rath, B., Hochmair, M. J., Funovics, M. A., & Hamilton, G. (2021) · Translational Oncology · doi:10.1016/j.tranon.2021.101230 · Cited by 24

Small-Molecule Inhibitors and Degraders Targeting KRAS-Driven Cancers

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Recent advances in B-RAF inhibitors as anticancer agents

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Pan-RAS inhibitors: Hitting multiple RAS isozymes with one stone

Coley, A. B., Ward, A., Keeton, A. B., Chen, X., Maxuitenko, Y. Y., Prakash, A., Li, F., Foote, J. B., Buchsbaum, D. J., & Piazza, G. A. (2022) · Advances in cancer research · doi:10.1016/bs.acr.2021.07.009 · Cited by 23

First SAR Study for Overriding NRAS Mutant Driven Acute Myeloid Leukemia

Cho, H., Shin, I., Ju, E., Choi, S.-H., Hur, W., Kim, H., Hong, E., Kim, N. D., Choi, H. G., Gray, N. S., et al. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00882 · Cited by 25

Prime Editing: A Revolutionary Technology for Precise Treatment of Genetic Disorders

Li, M., Lin, Y., Cheng, Q., & Wei, T. (2025) · Cell Proliferation · doi:10.1111/cpr.13808 · Cited by 28

BRAF oncogenic mutants evade autoinhibition through a common mechanism

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Current Insights into the Role of BRAF Inhibitors in Treatment of Melanoma

Kumar, P., Singh, A. K., Kumar, A., & Thareja, S. (2022) · Anti-Cancer Agents in Medicinal Chemistry · doi:10.2174/1871520622666220624164152 · Cited by 24

Realgar‑induced KRAS mutation lung cancer cell death via KRAS/Raf/MAPK mediates ferroptosis

Liu, X., Hai, Y., Dong, J., Xu, L., Hou, W., Su, J., Ren, W., & Liu, D. (2022) · International Journal of Oncology · doi:10.3892/ijo.2022.5447 · Cited by 26

Small-Molecule Screening for Genetic Diseases

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Discovering new biology with drug-resistance alleles

Freedy, A. M., & Liau, B. B. (2021) · Nature Chemical Biology · doi:10.1038/s41589-021-00865-9 · Cited by 25

Non-conducting functions of ion channels: The case of integrin-ion channel complexes

Forzisi, E., & Sesti, F. (2022) · Channels · doi:10.1080/19336950.2022.2108565 · Cited by 24

A Cell-Based MAPK Reporter Assay Reveals Synergistic MAPK Pathway Activity Suppression by MAPK Inhibitor Combination in BRAF -Driven Pediatric Low-Grade Glioma Cells

Usta, D., Sigaud, R., Buhl, J. L., Selt, F., Marquardt, V., Pauck, D., Jansen, J., Pusch, S., Ecker, J., Hielscher, T., et al. (2020) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-19-1021 · Cited by 23

Targeting the p300/NONO axis sensitizes melanoma cells to BRAF inhibitors

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MKK4 Inhibitors—Recent Development Status and Therapeutic Potential

Katzengruber, L., Sander, P., & Laufer, S. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms24087495 · Cited by 22

Targeted Therapy for Colorectal Cancers With Non-V600 BRAF Mutations: Perspectives for Precision Oncology

Dankner, M. (2018) · JCO Precision Oncology · doi:10.1200/po.18.00195 · Cited by 23

Mortalin depletion induces MEK/ERK-dependent and ANT/CypD-mediated death in vemurafenib-resistant B-RafV600E melanoma cells

Wu, P., Hong, S., & Park, J. (2021) · Cancer Letters · doi:10.1016/j.canlet.2020.12.044 · Cited by 22

The paradox-breaking panRAF plus SRC family kinase inhibitor, CCT3833, is effective in mutant KRAS-driven cancers

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Biphasic Mathematical Model of Cell–Drug Interaction That Separates Target-Specific and Off-Target Inhibition and Suggests Potent Targeted Drug Combinations for Multi-Driver Colorectal Cancer Cells

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Mutation-oriented profiling of autoinhibitory kinase conformations predicts RAF inhibitor efficacies

Mayrhofer, J. E., Enzler, F., Feichtner, A., Röck, R., Fleischmann, J., Raffeiner, A., Tschaikner, P., Ogris, E., Huber, R. G., Hartl, M., et al. (2020) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.2012150117 · Cited by 18

Signaling pathways, microenvironment, and targeted treatments in Langerhans cell histiocytosis

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Response and resistance to BRAFV600E inhibition in gliomas: Roadblocks ahead?

Capogiri, M., Micheli, A. J. D., Lassaletta, Á., Muñoz, D. P., Coppé, J., Mueller, S., & Stücklin, A. G. (2023) · Frontiers in Oncology · doi:10.3389/fonc.2022.1074726 · Cited by 21

Tumor Cell Resistance to the Inhibition of BRAF and MEK1/2

Chen, W., & Park, J. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms241914837 · Cited by 21

Small molecule inhibitor agerafenib effectively suppresses neuroblastoma tumor growth in mouse models via inhibiting ERK MAPK signaling

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Selective CRAF Inhibition Elicits Transactivation

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High‐Throughput Miniaturized Synthesis of PROTAC‐Like Molecules

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A brief history of RAS and the RAS Initiative

McCormick, F. P. (2022) · Advances in cancer research · doi:10.1016/bs.acr.2021.07.003 · Cited by 20

Spectrum of BRAF Aberrations and Its Potential Clinical Implications: Insights From Integrative Pan-Cancer Analysis

Yi, Q., Peng, J., Xu, Z., Liang, Q., Cai, Y., Peng, B., He, Q., & Yan, Y. (2022) · Frontiers in Bioengineering and Biotechnology · doi:10.3389/fbioe.2022.806851 · Cited by 21

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

Roa, P., Bremer, N. V., Foglizzo, V., & Cocco, E. (2024) · Cancers · doi:10.3390/cancers16061215 · Cited by 26

Melatonin synergizes BRAF‐targeting agent dabrafenib for the treatment of anaplastic thyroid cancer by inhibiting AKT/hTERT signalling

Liao, Y., Gao, Y., Chang, A., Li, Z., Wang, H., Cao, J., Gu, W., & Tang, R. (2020) · Journal of Cellular and Molecular Medicine · doi:10.1111/jcmm.15854 · Cited by 21

Clinical Translation of Combined MAPK and Autophagy Inhibition in RAS Mutant Cancer

Lee, J. J., Jain, V., & Amaravadi, R. K. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms222212402 · Cited by 20

Co-mutations of epidermal growth factor receptor and BRAF in Chinese non-small cell lung cancer patients

Peng, P., Lv, G., Hu, J., Wang, K., Lv, J., & Guo, G. F. (2021) · Annals of Translational Medicine · doi:10.21037/atm-21-3570 · Cited by 17

Protomer selectivity of type II RAF inhibitors within the RAS/RAF complex

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A patent review of RAF kinase inhibitors (2010–2018)

Man, R., Zhang, Y., Jiang, A.-Q., & Zhu, H. (2019) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2019.1651842 · Cited by 19

Pan-RAF Inhibition Shows Anti-Leukemic Activity in RAS-Mutant Acute Myeloid Leukemia Cells and Potentiates the Effect of Sorafenib in Cells with FLT3 Mutation

Khoury, J. D., Tashakori, M., Yang, H. Y., Loghavi, S., Wang, Y., Wang, J., Piya, S., & Borthakur, G. M. (2020) · Cancers · doi:10.3390/cancers12123511 · 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

BRAF inhibitors and their immunological effects in malignant melanoma

Adams, R., Coumbe, J. E. M., Coumbe, B. G. T., Thomas, J., Willsmore, Z., Dimitrievska, M., Yasuzawa-Parker, M., Hoyle, M., Ingar, S., Geh, J. L. C., et al. (2022) · Expert Review of Clinical Immunology · doi:10.1080/1744666x.2022.2044796 · 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

Diagnostic molecular techniques in haematology: recent advances

Koutsi, A., & Vervesou, E. (2018) · Annals of Translational Medicine · doi:10.21037/atm.2018.05.30 · Cited by 20

The MEK/ERK Module Is Reprogrammed in Remodeling Adult Cardiomyocytes

Kubin, T., Çetinkaya, A., Kubin, N., Bramlage, P., Sen-Hild, B., Gajawada, P., Akintürk, H., Schönburg, M., Schaper, W. K. A., Choi, Y., et al. (2020) · International Journal of Molecular Sciences · doi:10.3390/ijms21176348 · 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

Synthesis, biological evaluation and molecular docking studies of novel 1,2,3-triazole-quinazolines as antiproliferative agents displaying ERK inhibitory activity

Nunes, P. S. G., da Silva, G. F., Nascimento, S., Mantoani, S. P., de Andrade, P., Bernardes, E. S., Kawano, D. F., Leopoldino, A. M., & Carvalho, I. (2021) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2021.104982 · Cited by 18

Discovery of BRAF/HDAC Dual Inhibitors Suppressing Proliferation of Human Colorectal Cancer Cells

Li, Y., Huang, Y., Cheng, H., Xu, F. L., Qi, R., Dai, B., Yang, Y., Tu, Z., Peng, L., & Zhang, Z. (2022) · Frontiers in Chemistry · doi:10.3389/fchem.2022.910353 · Cited by 17

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

BRAF Δβ3-αC in-frame deletion mutants differ in their dimerization propensity, HSP90 dependence, and druggability

Lauinger, M., Christen, D., Klar, R. F. U., Roubaty, C., Heilig, C. E., Stumpe, M., Knox, J. J., Radulovich, N., Tamblyn, L., Xie, I. Y., et al. (2023) · Science Advances · doi:10.1126/sciadv.ade7486 · Cited by 17

Rigosertib promotes anti-tumor immunity via autophagic degradation of PD-L1 in colorectal cancer cells

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RAF and MEK Inhibitors in Non-Small Cell Lung Cancer

Adamopoulos, C., Papavassiliou, K. A., Poulikakos, P. I., & Papavassiliou, A. G. (2024) · International Journal of Molecular Sciences · doi:10.3390/ijms25094633 · Cited by 18

Advance of Seriniquinone Analogues as Melanoma Agents

Hammons, J. C., Trzoss, L., Jimenez, P. C., Hirata, A. S., Costa-Lotufo, L. V., Clair, J. J. L., & Fenical, W. (2019) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.8b00391 · Cited by 17

Interstitial Deletions Generating Fusion Genes

Panagopoulos, I., & Heim, S. (2021) · Cancer Genomics & Proteomics · doi:10.21873/cgp.20251 · Cited by 21

Recent advances in the understanding of the molecular pathogenesis and targeted therapy options in Langerhans cell histiocytosis

Suh, J. K., Kang, S. H., Kim, H., Im, H. J., & Koh, K. (2021) · Blood Research · doi:10.5045/br.2021.2021013 · Cited by 17

300 INVITED RAF Inhibitors

Nicolantonio, F. P. (2011) · European Journal of Cancer · doi:10.1016/s0959-8049(11)70515-9

Targeting RAF kinases for cancer therapy: BRAF-mutated melanoma and beyond

Holderfield, M. T., Deuker, M. M., McCormick, F. P., & McMahon, M. (2014) · Nature reviews. Cancer · doi:10.1038/nrc3760 · Cited by 850

Current Insights of BRAF Inhibitors in Cancer

Agianian, B., & Gavathiotis, E. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b01306 · Cited by 103

Abstract 1225: A unified model of RAF inhibitor action determines inhibitor activity in BRAF-dependent tumors

Karoulia, Z., Wu, Y., Ahmed, T. A., Xin, Q., Bollard, J., Krepler, C., Wu, X., Zhang, C., Bollag, G. E., Herlyn, M., et al. (2017) · Cancer Research · doi:10.1158/1538-7445.am2017-1225

Tumor adaptation and resistance to RAF inhibitors

Lito, P., Rosen, N., & Solit, D. B. (2013) · Nature Medicine · doi:10.1038/nm.3392 · Cited by 585