RAF inhibitor PLX8394 selectively disrupts BRAF dimers and RAS-independent BRAF-mutant-driven signaling

Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation

Nazarian, R., Shi, H., Wang, Q., Kong, X., Koya, R. C., Lee, H., Chen, Z., Lee, M., Attar, N., Sazegar, H., et al. (2010) · Nature · doi:10.1038/nature09626 · Cited by 2,244

Memorial Sloan Kettering-Integrated Mutation Profiling of Actionable Cancer Targets (MSK-IMPACT)

Cheng, D. T., Mitchell, T. N., Zehir, A., Shah, R. H., Benayed, R., Syed, A., Chandramohan, R., Liu, Z. Y., Won, H. H., Scott, S. N., et al. (2015) · The Journal of Molecular Diagnostics · doi:10.1016/j.jmoldx.2014.12.006 · Cited by 2,119

RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF

Poulikakos, P. I., Zhang, C., Bollag, G. E., Shokat, K. M., & Rosen, N. X. (2010) · Nature · doi:10.1038/nature08902 · Cited by 1,841

Kinase-Dead BRAF and Oncogenic RAS Cooperate to Drive Tumor Progression through CRAF

Heidorn, S. J., Milagre, C. S., Whittaker, S. R., Nourry, A., Niculescu‐Duvaz, I., Dhomen, N. S., Hussain, J., Reis-Filho, J. S., Springer, C. J., Pritchard, C. A., et al. (2010) · Cell · doi:10.1016/j.cell.2009.12.040 · Cited by 1,497

RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E)

Poulikakos, P. I., Persaud, Y., Janakiraman, M., Kong, X., Ng, C., Moriceau, G., Shi, H., Atefi, M., Titz, B., Gabay, M. T., et al. (2011) · Nature · doi:10.1038/nature10662 · Cited by 1,454

Melanoma whole-exome sequencing identifies V600EB-RAF amplification-mediated acquired B-RAF inhibitor resistance

Shi, H., Moriceau, G., Kong, X., Lee, M., Lee, H., Koya, R. C., Ng, C., Chodon, T., Scolyer, R. A., Dahlman, K. B., et al. (2012) · Nature Communications · doi:10.1038/ncomms1727 · Cited by 660

Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS

Yao, Z., Yaeger, R., Rodrik-Outmezguine, V. S., Tao, A., Torres, N. M., Chang, M. T., Drosten, M., Zhao, H., Cecchi, F., Hembrough, T., et al. (2017) · Nature · doi:10.1038/nature23291 · Cited by 562

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

RG7204 (PLX4032), a Selective BRAFV600E Inhibitor, Displays Potent Antitumor Activity in Preclinical Melanoma Models

Yang, H. Y., Higgins, B., Kolinsky, K. D., Packman, K. E., Go, Z., Iyer, R. M., Kolis, S. P., Zhao, S., Lee, R., Grippo, J. F., et al. (2010) · Cancer Research · doi:10.1158/0008-5472.can-10-0646 · Cited by 404

New perspectives for targeting RAF kinase in human cancer

Karoulia, Z., Gavathiotis, E., & Poulikakos, P. I. (2017) · Nature Reviews Cancer · doi:10.1038/nrc.2017.79 · Cited by 404

Design, synthesis and characterisation of a novel type II B-RAF paradox breaker inhibitor

Arora, R., Linders, J. T. M., Aci‐Sèche, S., Verheyen, T., van Heerde, E., Brehmer, D., Chaikuad, A., Knapp, S., & Bonnet, P. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115231 · Cited by 13

Paradox breaker BRAF inhibitors have comparable potency and MAPK pathway reactivation to encorafenib in BRAF mutant colorectal cancer

Pickles, O. J., Drozd, A., Tee, L. J., Beggs, A. D., & Middleton, G. (2020) · Oncotarget · doi:10.18632/oncotarget.27681 · Cited by 13

Novel and Potent Small Molecules against Melanoma Harboring BRAF Class I/II/III Mutants for Overcoming Drug Resistance

Kim, N., Shin, I., Lee, J., Jeon, E., Kim, Y., Ryu, S., Ju, E., Cho, W., & Sim, T. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms22073783 · Cited by 13

BRAF V600E-mutated metastatic pediatric Wilms tumor with complete response to targeted RAF/MEK inhibitionPreprint

Odeniyide, P., Shahab, S., Dunn, E. A., Rhee, D. S., Jiang, L., Dome, J. S., Friedman, A. D., Argani, P., & Pratilas, C. A. (2020) · Molecular Case Studies · doi:10.1101/mcs.a004820 · Cited by 14

A comprehensive overview of the molecular features and therapeutic targets in BRAF V600E ‐mutant colorectal cancer

Gu, R., Fang, H., Wang, R., Dai, W., & Cai, G. (2024) · Clinical and Translational Medicine · doi:10.1002/ctm2.1764 · Cited by 14

BRAF Mutations: The Discovery of Allele- and Lineage-Specific Differences

Hanrahan, A. J., & Solit, D. B. (2022) · Cancer Research · doi:10.1158/0008-5472.can-21-3377 · Cited by 13

Melanoma with genetic alterations beyond the BRAF V600 mutation: management and new insights

Awada, G., & Neyns, B. (2022) · Current Opinion in Oncology · doi:10.1097/cco.0000000000000817 · Cited by 11

A patent review of BRAF inhibitors: 2013-2018

Wang, P., Qiu, H., & Zhu, H. (2019) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2019.1640680 · Cited by 11

The first small molecules capable of strongly suppressing proliferation of cancer cells harboring BRAF class I/II/III mutations

Choi, S.-H., Shin, I., Kim, N. D., Nam, Y., & Sim, T. (2020) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2020.07.110 · Cited by 11

Novel insights into the pathogenesis and treatment of NRAS mutant melanoma

Zhao, J. W., Galvez, C., Beckermann, K. E., Johnson, D. B., & Sosman, J. A. (2021) · Expert Review of Precision Medicine and Drug Development · doi:10.1080/23808993.2021.1938545 · Cited by 11

BRAF inhibitors enhance erythropoiesis and treat anemia through paradoxical activation of MAPK signaling

Wu, S., Deng, Y., Sun, H., Liu, X., Zhou, S., Zhao, H., Li, H., Guo, F., Yue, Q., Wu, F., et al. (2024) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-024-02033-6 · Cited by 10

Characterization and inhibitor sensitivity of ARAF, BRAF, and CRAF kinases

Tkacik, E., Jang, D. M., Boxer, K., Ha, B. H., & Eck, M. J. (2025) · Journal of Biological Chemistry · doi:10.1016/j.jbc.2025.110800 · Cited by 10

Inhibition of TGF-β signaling, invasion, and growth of cutaneous squamous cell carcinoma by PLX8394

Siljamäki, E., Riihilä, P., Suwal, U., Nissinen, L. M., Rappu, P., Kallajoki, M. A., Kähäri, V., & Heino, J. (2023) · Oncogene · doi:10.1038/s41388-023-02863-8 · Cited by 10

New perspectives on targeting RAF, MEK and ERK in melanoma

Dumaz, N., & Lebbé, C. (2020) · Current Opinion in Oncology · doi:10.1097/cco.0000000000000708 · Cited by 11

PLX8394, a RAF inhibitor, inhibits enterovirus 71 replication by blocking RAF/MEK/ERK signaling

Wu, C., Zhu, G., Qiu, F., Ren, F., Lin, B., Zhang, D., Yang, Q., & Huang, C. (2023) · Virologica Sinica · doi:10.1016/j.virs.2023.01.006 · Cited by 10

SB202190 Predicts BRAF-Activating Mutations in Primary Colorectal Cancer Organoids via Erk1-2 Modulation

Costa, D., Venè, R., Coco, S., Longo, L., Tosetti, F., Scabini, S., Mastracci, L., Grillo, F., Poggi, A. D., & Benelli, R. (2023) · Cells · doi:10.3390/cells12040664 · Cited by 11

Atypical (non‐V600E) BRAF mutations in metastatic colorectal cancer in population and real‐world cohorts

Österlund, E., Ristimaki, A. P., Mäkinen, M. J., Kytölä, S. I., Kononen, J., Pfeiffer, P., Soveri, L., Keinänen, M., Sørbye, H., Nunes, L., et al. (2023) · International Journal of Cancer · doi:10.1002/ijc.34733 · Cited by 11

BRAF inhibitors in Melanoma: Structural Insights, Therapeutic Resistance, and Biological Evaluation of Quinazoline Derivatives

Paik, A., Matada, G. S. P., Ghara, A., Pal, R., Pavani, G., & Hemalatha, K. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.117866 · Cited by 9

Dynamic transcriptome analysis reveals signatures of paradoxical effect of vemurafenib on human dermal fibroblasts

Corrales, E., Levit‐Zerdoun, E., Metzger, P., Kowar, S., Ku, M., Brummer, T., & Boerries, M. (2021) · Cell Communication and Signaling · doi:10.1186/s12964-021-00801-3 · Cited by 8

Resistance mechanisms in BRAFV600E paediatric high-grade glioma and current therapeutic approaches

Lehmann, R. J., Rayner, B. S., & Ziegler, D. S. (2022) · Frontiers in Oncology · doi:10.3389/fonc.2022.1031378 · Cited by 9

Prevalence of RAF1 Aberrations in Metastatic Cancer Patients: Real-World Data

Lim, S. H., Jung, J., Hong, J. Y., Kim, S. T., Park, S. H., Park, J. O., Kim, K., & Lee, J. (2023) · Biomedicines · doi:10.3390/biomedicines11123264 · Cited by 9

Mcl-1 mediates intrinsic resistance to RAF inhibitors in mutant BRAF papillary thyroid carcinoma

Cavallo, M. R., Yo, J., Gallant, K. C., Cunanan, C. J., Amirfallah, A., Daniali, M., Sanders, A. B., Aplin, A. E., Pribitkin, E. A., & Hartsough, E. J. (2024) · Cell Death Discovery · doi:10.1038/s41420-024-01945-0 · Cited by 10

BRAF increases endothelial cell stiffness through reorganization of the actin cytoskeleton

Hollósi, A., Pászty, K., Bunta, B., Bozó, T., Kellermayer, M., Debreczeni, M. L., Cervenak, L., Baccarini, M., & Varga, A. (2022) · The FASEB Journal · doi:10.1096/fj.202200344r · Cited by 9

BRAF inhibitor resistance in melanoma: from resistance mechanisms to therapeutic innovations

Shang, Y., Cao, T., Li, J., Li, J., ZHANG, L., Ma, Q., Feng, L., & Zhao, H. (2026) · Molecular Biomedicine · doi:10.1186/s43556-026-00425-4 · Cited by 9

Emerging Tumor-Agnostic Molecular Targets

Bhamidipati, D., & Schram, A. M. (2024) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-23-0725 · Cited by 9

Targeting the Mutational Landscape of Bystander Cells: Drug-Promoted Blood Cancer From High-Prevalence Pre-neoplasias in Patients on BRAF Inhibitors

Simnica, D., Ittrich, H., Bockemeyer, C., Stein, A., & Binder, M. (2020) · Frontiers in Oncology · doi:10.3389/fonc.2020.540030 · Cited by 8

Bioluminescence-based assays for quantifying endogenous protein interactions in live cells

Niles, A. L., Dibble, M., Machleidt, T., Martino, K., Swiatnicki, M., Vu, E. H., & Schwinn, M. K. (2025) · Journal of Biological Chemistry · doi:10.1016/j.jbc.2025.110454 · Cited by 7

Maintenance of p-eIF2α levels by the eIF2B complex is vital for colorectal cancer

Škapik, I. P., Giacomelli, C., Hahn, S., Deinlein, H., Gallant, P., Diebold, M., Biayna, J., Hendricks, A., Olimski, L., Otto, C., et al. (2025) · The EMBO Journal · doi:10.1038/s44318-025-00381-9 · Cited by 6

Drug repurposing candidates for amyotrophic lateral sclerosis using common and rare genetic variants

Gerring, Z. F., Bhalala, O. G., Fearnley, L. G., Oikari, L. E., White, A. R., Derks, E. M., Watson, R., Yassi, N., Bahlo, M., & Reay, W. R. (2025) · Brain Communications · doi:10.1093/braincomms/fcaf184 · Cited by 6

Biology and Clinical Management of Non-V600 BRAF Alterations in NSCLC

Ortiz‐Cuaran, S., Dupriez, L., Nicq, C., Lindsay, C. R., Mazières, J., Santamarı́a, D., Ambrogio, C., Calvayrac, O., Teixidó, C., Friboulet, L., et al. (2026) · Journal of Thoracic Oncology · doi:10.1016/j.jtho.2025.12.001 · Cited by 6

Impact of protein and small molecule interactions on kinase conformations

Kugler, V., Schwaighofer, S., Feichtner, A., Enzler, F., Fleischmann, J., Strich, S. L., Schwarz, S., Wilson, R., Tschaikner, P., Troppmair, J., et al. (2024) · eLife · doi:10.7554/elife.94755 · Cited by 6

LSD1 inhibition attenuates targeted therapy-induced lineage plasticity in BRAF mutant colorectal cancer

Ladaika, C. A., Chakraborty, A., Masood, A., Hostetter, G. H., Yi, J. M., & O’Hagan, H. M. (2025) · Molecular Cancer · doi:10.1186/s12943-025-02311-z · Cited by 6

Novel GLCCI1-BRAF fusion drives kinase signaling in a case of pheochromocytomatosis

Green, B. L., Grant, R., Richie, C. T., Chatterjee, B., Melo, M. S. D., Barr, F. G., Pacák, K., Agarwal, S. K., & Nilubol, N. (2022) · European Journal of Endocrinology · doi:10.1530/eje-21-0797 · Cited by 6

Design and Synthesis of Novel 2‐Acetamido, 6‐Carboxamide Substituted Benzothiazoles as Potential BRAFV600E Inhibitors – In vitro Evaluation of their Antiproliferative Activity

Batsi, Y., Αντωνοπούλου, Γ., Fotopoulou, T., Koumaki, K., Kritsi, E., Potamitis, C., Goulielmaki, M., Skarmalioraki, S., Papalouka, C., Poulou‐Sidiropoulou, E., et al. (2023) · ChemMedChem · doi:10.1002/cmdc.202300322 · Cited by 6

Advances in the therapy of BRAFV600E metastatic colorectal cancer

Jin, Z., & Sinicrope, F. A. (2019) · Expert Review of Anticancer Therapy · doi:10.1080/14737140.2019.1661778 · Cited by 6

Quest for Clinically Effective RAF Dimer Inhibitors

Xue, J. Y., & Lito, P. (2020) · Journal of Clinical Oncology · doi:10.1200/jco.20.00401 · Cited by 6

Discovery of novel spiro compound as RAF kinase inhibitor with in vitro potency against KRAS mutant cancer

Zhao, P., Wang, X., Zhuang, L., Huang, S. M., Zhou, Y., Yan, Y., Shen, R., Zhang, F., Li, J., Hu, Q., et al. (2022) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2022.128666 · Cited by 5

Basket Trials: Past, Present, and Future

Murciano‐Goroff, Y. R., Uppal, M., Chen, M. F., Harada, G., & Schram, A. M. (2023) · Annual Review of Cancer Biology · doi:10.1146/annurev-cancerbio-061421-012927 · Cited by 6

Current State of Targeted Therapy in Adult Langerhans Cell Histiocytosis and Erdheim–Chester Disease

He, L., & Cao, X. (2024) · Targeted Oncology · doi:10.1007/s11523-024-01080-x · Cited by 5

Understanding and overcoming innate and acquired MAPK inhibition resistance in anaplastic thyroid cancer

Zeng, P. Y., Meens, J., Karimi, A. H., Pan, H., Cecchini, M. J., Jarycki, L., Ryan, S. E. B., Dawson, A. E., Shaikh, M. H., Palma, D. A., et al. (2026) · Cell Reports Medicine · doi:10.1016/j.xcrm.2026.102820 · Cited by 5

Recent progress in emerging molecular targeted therapies for intrahepatic cholangiocarcinoma

Kim, Y., Song, J., Kim, N., & Sim, T. (2025) · RSC Medicinal Chemistry · doi:10.1039/d4md00881b · Cited by 6

Computational and pharmacophore-based study of Camellia sinensis phytochemicals targeting BRAF in melanoma

Shuvo, M. I. M., Niaz, S. M. R., Jannat, S., Hossain, M. A., Mashhur, N., Ahmed, N., Sohel, M., Hasan, M. I., Ansari, S. A., Humayoo, M., et al. (2025) · Scientific Reports · doi:10.1038/s41598-025-22320-8 · Cited by 5

Looking Beyond the Glioblastoma Mask: Is Genomics the Right Path?

Montella, L., Gaudio, N. D., Bove, G., Cuomo, M., Buonaiuto, M., Costabile, D., Visconti, R., Facchini, G., Altucci, L., Chiariotti, L., et al. (2022) · Frontiers in Oncology · doi:10.3389/fonc.2022.926967 · Cited by 5

Response to osimertinib plus trametinib in a heavily treated epidermal growth factor receptor (EGFR)-positive NSCLC harboring a rare, acquired rapidly accelerated fibrosarcoma B-type (BRAF) p.D594N mutation: a case report

Li, S., Lin, X., Sun, S., Li, S., & Zhou, C. (2022) · Anti-Cancer Drugs · doi:10.1097/cad.0000000000001367 · Cited by 6

BRAF Mutation Class and Clinical Outcomes—Response

Dagogo‐Jack, I., Awad, M. M., & Shaw, A. T. (2019) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-19-0422 · Cited by 5

BRAF Modulates the Interplay Between Cell–Cell and Cell–Extracellular Matrix Adhesions in PECAM-1-Mediated Mechanotransduction

Gráczer, É., Pászty, K., Harsányi, L., Lehoczky, C., Fülöp, A., & Varga, A. (2024) · International Journal of Molecular Sciences · doi:10.3390/ijms252011234 · Cited by 4

Discovery of a highly potent pan-RAF inhibitor IHMT-RAF-128 for cancer treatment

Wang, A., Liu, J., Li, X., Zou, F., Qi, Z., Qi, S., Liu, Q., Wang, Z., Cao, J., Jiang, Z., et al. (2023) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2023.175752 · Cited by 5

Clinicopathogenomic Characteristics of Primary and Metastatic Melanomas With RAF1 and BRAF Fusions

Lezcano, C. M., Kasago, I. S., Tang, H., Febres‐Aldana, C. A., Benhamida, J. K., Shoushtari, A. N., Chen, M. F., & BUSAM, K. J. (2025) · The American Journal of Surgical Pathology · doi:10.1097/pas.0000000000002476 · Cited by 3

Exploring the pathway: clinical utility and open challenges of targeting BRAF alterations in biliary tract cancers and gastrointestinal malignancies

Weiss, L., Zhang, D., Kunz, W. G., Boeck, S. H., Curigliano, G., Subbiah, V., Lordick, F., Brummer, T., Westphalen, C. B., & Bielo, L. B. (2025) · ESMO Gastrointestinal Oncology · doi:10.1016/j.esmogo.2024.100129 · Cited by 4

Targeting Oncogenic Driver Mutations in Lung Cancer

Lee, M. H., Rous, F. A., Borczuk, A., Liu, S. V., Gadgeel, S. M., & Halmos, B. (2023) · Cambridge University Press eBooks · doi:10.1017/9781009336123 · Cited by 2

Comprehensive evaluation of cell death-related genes as novel diagnostic biomarkers for breast cancer

Shi, X., Ding, H., Tao, J., Zhu, Y., Zhang, X., He, G., Yang, J., Wu, X., Liu, X., & Yu, X. (2023) · Heliyon · doi:10.1016/j.heliyon.2023.e21341 · Cited by 3

Comprehensive Landscape of BRAF Variant Classes, Clonalities, and Co-Mutations in Metastatic Colorectal Cancer Using ctDNA Profiling

Johnson, B., Morris, V. K., Wang, X., Dasari, A. N., Raghav, K. P. S., Shen, J. P., Lee, M. S., Huey, R. W., Parseghian, C. M., Willis, J. A., et al. (2024) · Cancers · doi:10.3390/cancers16040737 · Cited by 2

[Progress of BRAF Gene Alteration in Non-small Cell Lung Cancer].

Deng, L., Yang, Y., & Huang, J. (2024) · PubMed Central · doi:10.3779/j.issn.1009-3419.2024.101.01 · Cited by 2

Disruption of the pro-oncogenic c-RAF–PDE8A complex represents a differentiated approach to treating KRAS–c-RAF dependent PDAC

Cooke, S. F., Wright, T. A., Sin, Y. Y., Ling, J., Kyurkchieva, E., Phanthaphol, N., Mcskimming, T., Herbert, K. J., Rebus, S., Biankin, A. V., et al. (2024) · Scientific Reports · doi:10.1038/s41598-024-59451-3 · Cited by 2

BRAF Gene Fusions in Melanoma

Odintsov, I., Davis, D., Pissaloux, D., Tirode, F., de la Fouchardière, A., & Hanna, J. (2025) · The American Journal of Surgical Pathology · doi:10.1097/pas.0000000000002370 · Cited by 2

An Unusual Case of Acquired AGK-BRAF Gene Fusion in Metastatic EGFR-mutant Lung Adenocarcinoma: A Case Report

Chang, C.-C., Hsieh, M., & Hsu, W. (2025) · Journal of Cancer Research and Practice · doi:10.4103/ejcrp.ejcrp-d-24-00023 · Cited by 2

Inhibiting the Extracellular Signal-regulated Kinase 1/2 (ERK1/2) Cascade in Cancer and the Heart: for Better or Worse, in Sickness and Health?

Clerk, A., Amadi, S. U., Smith, S. J., & Sugden, P. H. (2024) · International Journal of Drug Discovery and Pharmacology · doi:10.53941/ijddp.2024.100006 · Cited by 2

RAF conformational autoinhibition and 14-3-3 proteins promote paradoxical activationPreprint

Mendiratta, G., Abbott, K., Li, Y.-C., Yu, J., Huang, J., Shokhirev, M. N., McFall, T., Wahl, G. M., & Stites, E. C. (2019) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/849489 · Cited by 2

An amino-terminal BRAF deletion accounting for acquired resistance to RAF/EGFR inhibition in colorectal cancerPreprint

Tung, J. K., Neishaboori, N., Haraldsdóttir, S., & Suarez, C. J. (2020) · Molecular Case Studies · doi:10.1101/mcs.a005140 · Cited by 2

Characterization and inhibitor sensitivity of ARAF, BRAF, and CRAF complexesPreprint

Tkacik, E., Jang, D. M., Boxer, K., Ha, B. H., & Eck, M. J. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.08.14.670349 · Cited by 2

Endolysosomal Sequestration Effects Controlled Release of BRAF Paradox Breaker Nanoparticles

Chen, C., Perea, A. M., Sridharan, R., & Heller, D. A. (2025) · ACS Nano · doi:10.1021/acsnano.5c09100 · Cited by 1

Sustained Response to Pan-BRAF Inhibitor Plixorafenib (FORE8394, PLX8394) in a Young Adult With Neurodegenerative Langerhans Cell Histiocytosis

Yi, J. S., McCarthy, K. S., Mazur, K. A., Kudlaty, R., Armstrong, T., Desai, N. K., Shepherd, S. P., Zinn, D., Velazquez, J., Scull, B., et al. (2025) · JCO Precision Oncology · doi:10.1200/po-25-00225 · Cited by 1

Small-molecule drug discovery in malignant melanoma: current status and prospective developments

Miao, X., Liu, Y., Li, C., Wu, J., Li, Y., Li, Z., Li, J., Sun, Y., & Han, J. (2025) · Medicinal Chemistry Research · doi:10.1007/s00044-025-03515-0 · Cited by 1

MEK interactions tune RAF kinase sensitivity to conformation-selective inhibition

Stoddard, E. G., Perera, B. G. K., Fang, L., Brush, D. S., Zhong, Y., Potter, Z. E., Simon, J. J., Golkowski, M. G., & Maly, D. J. (2026) · Nature Chemical Biology · doi:10.1038/s41589-026-02212-2 · Cited by 3

Tumor‐agnostic inhibitors in oncology: A new phase for precision medicine

Li, M., & Hsieh, H. (2020) · Journal of the Chinese Chemical Society · doi:10.1002/jccs.202000377 · Cited by 1

Kinases in motion: impact of protein and small molecule interactions on kinase conformationsPreprint

Kugler, V., Schwaighofer, S., Feichtner, A., Enzler, F., Fleischmann, J., Strich, S. L., Schwarz, S., Wilson, R., Tschaikner, P., Troppmair, J., et al. (2024) · eLife · doi:10.7554/elife.94755.2 · Cited by 1

Inhibition of fatty acid synthase enhances therapeutic efficacy and delays acquired resistance to BRAF-targeted therapy in colorectal cancer

Geisen, M. E., Tessmann, J. W., Kelson, C. O., He, D., Wang, C., Faisal, A. S. M., Beswick, E. J., Baca, Y., Rock, S., Kolesar, J. M., et al. (2026) · Neoplasia · doi:10.1016/j.neo.2026.101283

1P1-N-096 神経筋システムにおいて感覚運動ニューロンが構成する運動調節機構のモデリング(デジタルヒューマン2,生活を支援するロボメカ技術のメガインテグレーション)

内原, 匡., 大武, 美., & Nakamura, Y. (2005) · The Proceedings of JSME annual Conference on Robotics and Mechatronics (Robomec)

Kinases in motion: impact of protein and small molecule interactions on kinase conformationsPreprint

Kugler, V., Schwaighofer, S., Feichtner, A., Enzler, F., Fleischmann, J., Strich, S. L., Schwarz, S., Wilson, R., Tschaikner, P., Troppmair, J., et al. (2024) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2024.01.11.575270

Kinases in motion: impact of protein and small molecule interactions on kinase conformationsPreprint

Kugler, V., Schwaighofer, S., Feichtner, A., Enzler, F., Fleischmann, J., Strich, S. L., Schwarz, S., Wilson, R., Tschaikner, P., Troppmair, J., et al. (2024) · eLife · doi:10.7554/elife.94755.1

Reviewer #2 (Public Review): Kinases in motion: impact of protein and small molecule interactions on kinase conformations

(2024) · eLife · doi:10.7554/elife.94755.1.sa0

Uncovering the mechanistic basis of intracellular Raf inhibitor sensitivity reveals synergistic cotreatment strategiesPreprint

Stoddard, E. G., Fang, L., Zhong, Y., Potter, Z. E., Brush, D. S., Simon, J. J., Golkowski, M. G., & Maly, D. J. (2024) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2024.09.18.613772

Targeting BRAF kinase fusions with pan-RAF and vertical MAPK inhibitionPreprint

Turner, J. A., MacBeth, M. L., Bagby, S. M., Whitty, P. A., Hartman, S. J., Simmons, D. M., Yacob, B. W., Pitts, T. M., Robinson, W. A., & Couts, K. L. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.02.06.636895

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Tkacik, E., Jang, D. M., Boxer, K., Ha, B. H., & Eck, M. J. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.64898/2025.12.15.694443

Additional file 3 of 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., Halbach, S., & Brummer, T. (2023) · Figshare · doi:10.6084/m9.figshare.23519961

Additional file 1 of 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., Halbach, S., & Brummer, T. (2023) · Figshare · doi:10.6084/m9.figshare.23519955

Additional file 4 of 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., Halbach, S., & Brummer, T. (2023) · Figshare · doi:10.6084/m9.figshare.23519964

Additional file 2 of 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., Halbach, S., & Brummer, T. (2023) · Figshare · doi:10.6084/m9.figshare.23519958

Preclinical exploration and current clinical applications of immunotherapeutic strategies for hepatocellular carcinoma

Yu, H., Wen, X., Cui, M. H., & Liu, S. (2026) · Frontiers in Immunology · doi:10.3389/fimmu.2026.1769251

In vitro reconstitutions suggest a general model for paradoxical activation of ARAF, BRAF, and CRAF by diverse RAF inhibitor types that does not rely on negative allosteryPreprint

Tkacik, E., Jang, D. M., Boxer, K., Ha, B. H., & Eck, M. J. (2026) · eLife · doi:10.7554/elife.110344

In vitro reconstitutions suggest a general model for paradoxical activation of ARAF, BRAF, and CRAF by diverse RAF inhibitor types that does not rely on negative allosteryPreprint

Tkacik, E., Jang, D. M., Boxer, K., Ha, B. H., & Eck, M. J. (2026) · eLife · doi:10.7554/elife.110344.1

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Tardif, N. (2019) · theses.fr (ABES) · doi:10.70675/3578ec97z89f3z41dfz8a68zf1d1d099db63

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Estrada, C. (2020) · theses.fr (ABES) · doi:10.70675/e84b4f6az1676z4c2dz80e4zd8668460d3c5

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Vidal-Cruchez, O. (2021) · theses.fr (ABES) · doi:10.70675/0c0e4622zadcfz40b9zb89ez6f22a14b8866

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Brandstetter, J., Goldstein, L., Schreiber, T., Palme, R., Lindner, T., Joksch, M., Krause, B., Vollmar, B., & Kumstel, S. (2026) · PLoS ONE · doi:10.1371/journal.pone.0347843

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A pathway-dependency framework for acquired resistance to targeted therapy in EGFR-mutant, KRAS G12C-mutant, and BRAF V600E-mutant NSCLC

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BindingDB Entry 50013684: From off-to on-target: New BRAF-inhibitor-template-derived compounds selectively targeting mitogen activated protein kinase kinase 4 (MKK4).

BindingDB (2022) · UC San Diego · doi:10.7270/q2mw2mxg

BindingDB Entry 50017162: Discovery of novel spiro compound as RAF kinase inhibitor with in vitro potency against KRAS mutant cancer.

BindingDB (2023) · UC San Diego · doi:10.7270/q29w0kjk

BindingDB Entry 50010954: Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting

BindingDB (2021) · UC San Diego · doi:10.7270/q2vx0m3g

BindingDB Entry 50015127: Discovery of spiro amide SHR902275: A potent, selective, and efficacious RAF inhibitor targeting RAS mutant cancers.

BindingDB (2023) · UC San Diego · doi:10.7270/q25h7m5p

BindingDB Entry 50020772: Design, synthesis and characterisation of a novel type II B-RAF paradox breaker inhibitor.

BindingDB (2024) · UC San Diego · doi:10.7270/q2jw8kcj

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

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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

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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