ARAF mutations confer resistance to the RAF inhibitor belvarafenib in melanoma

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New response evaluation criteria in solid tumours: revised RECIST guideline (version 1.1)

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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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PHENIX: a comprehensive Python-based system for macromolecular structure solution

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MET Amplification Leads to Gefitinib Resistance in Lung Cancer by Activating ERBB3 Signaling

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A Chromatin-Mediated Reversible Drug-Tolerant State in Cancer Cell Subpopulations

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Signal pathways of melanoma and targeted therapy

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Small molecule inhibitors targeting the cancers

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E3 ligases and deubiquitinating enzymes regulating the MAPK signaling pathway in cancers

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The RASopathies: from pathogenetics to therapeutics

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Molecular Pathways and Mechanisms of BRAF in Cancer Therapy

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Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C

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BRAF — a tumour-agnostic drug target with lineage-specific dependencies

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RAS signaling in carcinogenesis, cancer therapy and resistance mechanisms

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Targeting small GTPases: emerging grasps on previously untamable targets, pioneered by KRAS

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Oncogenic KRAS blockade therapy: renewed enthusiasm and persistent challenges

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Structure and RAF family kinase isoform selectivity of type II RAF inhibitors tovorafenib and naporafenib

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Structural basis for SHOC2 modulation of RAS signalling

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The evolution of BRAF-targeted therapies in melanoma: overcoming hurdles and unleashing novel strategies

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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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Transformer-Based Generative Model Accelerating the Development of Novel BRAF Inhibitors

Yang, L., Yang, G., Bing, Z., Tian, Y., Niu, Y., Yang, L., & Yang, L. (2021) · ACS Omega · doi:10.1021/acsomega.1c05145 · Cited by 49

Harness the functions of gut microbiome in tumorigenesis for cancer treatment

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Mechanistic model of MAPK signaling reveals how allostery and rewiring contribute to drug resistance

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CRAF dimerization with ARAF regulates KRAS-driven tumor growth

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New Approaches to Targeted Therapy in Melanoma

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

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The role of CRAF in cancer progression: from molecular mechanisms to precision therapies

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New prospectives on treatment opportunities in RASopathies

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Drug resistance in targeted cancer therapies with RAF inhibitors

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Targeting RAS mutants in malignancies: successes, failures, and reasons for hope

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Circulating Tumour DNA in Melanoma—Clinic Ready?

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The future of targeted kinase inhibitors in melanoma

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Cooperation between the Hippo and MAPK pathway activation drives acquired resistance to TEAD inhibition

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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

Yaeger, R. D., McKean, M. A., Haq, R., Beck, J. T., Taylor, M. H., Cohen, J. E., Bowles, D. W., Gadgeel, S. M., Mihalcioiu, C. L. D., Papadopoulos, K. P., et al. (2024) · Cancer Discovery · doi:10.1158/2159-8290.cd-24-0024 · Cited by 30

Disrupted molecular glue complex drives RAS inhibitor resistance

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Targeting the SHOC2–RAS interaction in RAS-mutant cancers

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Target deconvolution with matrix-augmented pooling strategy reveals cell-specific drug-protein interactions

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Artificial intelligence in tumor drug resistance: Mechanisms and treatment prospects

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Artificial intelligence and anti-cancer drugs' response

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Mutation profiles in circulating cell‐free DNA predict acquired resistance to olaparib in high‐grade serous ovarian carcinoma

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

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Overloading And unpacKing (OAK) - droplet-based combinatorial indexing for ultra-high throughput single-cell multiomic profiling

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Targeting the ERK mitogen-activated protein kinase cascade for the treatment of KRAS-mutant pancreatic cancer

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Hierarchical Virtual Screening Based on Rocaglamide Derivatives to Discover New Potential Anti-Skin Cancer Agents

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

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ARAF suppresses ERBB3 expression and metastasis in a subset of lung cancers

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Metabolic rewiring directs melanoma immunology

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

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Unique Spectrum of Activating BRAF Alterations in Prostate Cancer

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

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Plasma membrane-associated ARAF condensates fuel RAS-related cancer drug resistance

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BRAFV600E;K601Q metastatic melanoma patient-derived organoids and docking analysis to predict the response to targeted therapy

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Targeting Lung Cancer With Carvacrol‐Triazole‐Arylidene Hydrazide Hybrids: In Vitro and In Silico Cytotoxicity Assessments

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MITF activity is regulated by a direct interaction with RAF proteins in melanoma cells

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Venetoclax and Cobimetinib in Relapsed/Refractory AML: A Phase 1b Trial

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

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An overview of RAF kinases and their inhibitors (2019–2023)

Hashem, O., Shahin, A. I., Hindawi, M. A. A., Fageeri, M. F., Al-Sbbagh, S. A., Tarazi, H., & El-Gamal, M. I. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116631 · Cited by 14

Targeting the MAPK pathway for NRAS mutant melanoma: from mechanism to clinic

Wang, Y., Xu, G., & Xia, H. (2025) · British Journal of Dermatology · doi:10.1093/bjd/ljaf178 · Cited by 15

Targeting the EGFR/RAS/RAF signaling pathway in anticancer research: a recent update on inhibitor design and clinical trials (2020–2023)

Hajjo, R., Sabbah, D. A., Bardaweel, S. K., & Zhong, H. A. (2024) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2024.2327307 · Cited by 14

Unraveling lipid metabolism reprogramming for overcoming drug resistance in melanoma

Wang, R., Qin, Y., Liu, X., & Wu, J. (2024) · Biochemical Pharmacology · doi:10.1016/j.bcp.2024.116122 · Cited by 13

Head-to-Head Comparison of BRAF/MEK Inhibitor Combinations Proposes Superiority of Encorafenib Plus Trametinib in Melanoma

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Toxoplasma gondii infection regulates apoptosis of host cells via miR-185/ARAF axis

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CRISPR–Drug Combinatorial Screening Identifies Effective Combination Treatments for MTAP -Deleted Cancer

Knoll, N., Masser, S., Bordas, B., Ebright, R. Y., Li, G., Kesar, D., Destefanis, E., Kania, N., Rodriguez, D. J., Jen, J., et al. (2025) · Cancer Research · doi:10.1158/0008-5472.can-25-1464 · Cited by 14

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

RAS and SHOC2 Roles in RAF Activation and Therapeutic Considerations

Bonsor, D. A., & Simanshu, D. K. (2023) · Annual Review of Cancer Biology · doi:10.1146/annurev-cancerbio-062822-030450 · Cited by 13

Combination of bulk RNA sequencing and scRNA sequencing uncover the molecular characteristics of MAPK signaling in kidney renal clear cell carcinoma

Li, X., Guan, H., Ma, C., Dai, Y., Su, J., Chen, X., Yuan, Q., & Wang, J. (2024) · Aging · doi:10.18632/aging.205436 · Cited by 12

Therapeutic Strategies in BRAF V600 Wild-Type Cutaneous Melanoma

Haugh, A. M., & DAUD, A. I. (2024) · American Journal of Clinical Dermatology · doi:10.1007/s40257-023-00841-0 · Cited by 12

Mechanisms of resistance to active state selective tri-complex RAS inhibitorsPreprint

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Allosteric coupling asymmetry mediates paradoxical activation of BRAF by type II inhibitors

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Precision Oncology for Papillary Craniopharyngioma

Blakeley, J. O., & Shannon, K. (2023) · New England Journal of Medicine · doi:10.1056/nejme2305288 · Cited by 11

Exploring Molecular Genetic Alterations and RAF Fusions in Melanoma: A Belvarafenib Expanded Access Program in Patients with RAS/RAF -Mutant Melanoma

Kim, K. H., Cho, S. M., Jeong, Y., Baek, E. S., Lee, C., Ryu, H. J., Noh, Y. S., Hong, Y.-H., Chung, K. Y., Roh, M. R., et al. (2024) · The Oncologist · doi:10.1093/oncolo/oyae018 · Cited by 11

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

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Implications of glutathione-S transferase P1 in MAPK signaling as a CRAF chaperone: In memory of Dr. Irving Listowsky

Niitsu, Y., Sato, Y., & Takayama, T. (2022) · Proceedings of the Japan Academy Series B · doi:10.2183/pjab.98.005 · Cited by 11

An Efficient Second-Generation Manufacturing Process for the pan-RAF Inhibitor Belvarafenib

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Mechanism of dimer selectivity and binding cooperativity of BRAF inhibitors

Clayton, J., Romany, A., Matenoglou, E., Gavathiotis, E., Poulikakos, P. I., & Shen, J. (2024) · eLife · doi:10.7554/elife.95334.4 · Cited by 11

NOVEL INSIGHTS IN ADVANCED THYROID CARCINOMA: FROM MECHANISMS TO TREATMENTS: Molecular insights into the origin, biology, and treatment of anaplastic thyroid carcinoma

Karimi, A. H., Zeng, P. Y., Cecchini, M. J., Barrett, J. W., Pan, H., Ying, S., Le, N., Mymryk, J. S., Ailles, L., & Nichols, A. C. (2025) · European Thyroid Journal · doi:10.1530/etj-25-0057 · Cited by 11

Melanoma: Pathogenesis and Targeted Therapy

Fu, Y., Liu, J., Mo, Z., Wang, B., Deng, Y., & Jiang, Y. (2026) · MedComm · doi:10.1002/mco2.70566 · Cited by 11

Individualized Treatment Strategy for Cutaneous Melanoma: Where Are We Now and Where Are We Going?

Zeng, H., Liu, F., Zhou, H., & Zeng, C. (2021) · Frontiers in Oncology · doi:10.3389/fonc.2021.775100 · Cited by 9

Preclinical Activity of the Type II RAF Inhibitor Tovorafenib in Tumor Models Harboring Either a BRAF Fusion or an NF1 Loss-of-Function Mutation

Rastogi, S., Perino, S., Lal‐Nag, M., Wang, Y., Blackman, S. C., & Venetsanakos, E. (2025) · Cancer Research Communications · doi:10.1158/2767-9764.crc-24-0451 · Cited by 8

Analysis of the ERK Pathway Cysteinome for Targeted Covalent Inhibition of RAF and MEK Kinases

Romany, A., Liu, R., Zhan, S., Clayton, J., & Shen, J. (2023) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.3c00014 · Cited by 8

Combining single-cell and transcriptomic analysis revealed the immunomodulatory effect of GOT2 on a glutamine-dependent manner in cutaneous melanoma

Song, L., Wei, X., Zhang, X., & Lu, Y. (2023) · Frontiers in Pharmacology · doi:10.3389/fphar.2023.1241454 · Cited by 8

Treatment outcome of NSCLC patients with BRAF mutations: a retrospective, multicentre analysis within the national Network Genomic Medicine (nNGM) Lung Cancer in Germany

Kropf-Sanchen, C., Rasokat, A., Christopoulos, P., Wenzel, C., Wehler, T., Rost, M., Kulhavy, J., Reinmuth, N., Schulz, C. K. J., Scheffler, M., et al. (2025) · ESMO Open · doi:10.1016/j.esmoop.2025.105124 · Cited by 8

Dissecting the MAPK signaling landscape in malignant melanoma: from BRAF and NRAS mutations to precision combination therapies

Fang, X., Wang, S., & Fu, S. (2026) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2025.1723066 · Cited by 9

Peptide inhibitors targeting Ras and Ras-associated protein–protein interactions

Han, D., Li, A., Zhu, L., Zhuang, C., Zhao, Q., & Zou, Y. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116878 · Cited by 7

Current knowledge about immunotherapy resistance for melanoma and potential predictive and prognostic biomarkers

Song, L., Yang, Y., & Tian, X. (2024) · Cancer Drug Resistance · doi:10.20517/cdr.2023.150 · Cited by 5

Belvarafenib penetrates the BBB and shows potent antitumor activity in a murine melanoma brain metastasis model

Kim, Y.-Y., Park, H., Song, T., Choi, K., Dolton, M., Mao, J., Kim, J., Ahn, Y., Suh, K. H., & Kim, Y. H. (2023) · Clinical & Experimental Metastasis · doi:10.1007/s10585-023-10198-7 · Cited by 6

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

Property-Based Prediction Uncovers Intestinal Excretion as an Elimination Route of Small-Molecule Drugs

Chen, C., Zhao, W., Cao, L., He, M., Khojasteh, S. C., Hop, C. E. C. A., Dragovich, P. S., Wright, M. R., & Zhang, D. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c01251 · Cited by 5

The MEK–RAF molecular glue IK-595 has potent antitumor activity across RAS/MAPK pathway-altered cancers

Haines, E., Burke, M., Catterall, R., de Jesus, V., Hidalgo, D., Li, B., Manna, J., Yang, A., Cavanaugh, J., Wessel, S. R., et al. (2026) · Nature Cancer · doi:10.1038/s43018-025-01081-3 · Cited by 5

Allosteric coupling asymmetry mediates paradoxical activation of BRAF by type II inhibitorsPreprint

Rasmussen, D. M., Semonis, M. M., Greene, J. T., Muretta, J. M., Thompson, A. R., Ramos, S. T., Thomas, D. D., Pomerantz, W. C. K., Freedman, T. S., & Levinson, N. M. (2023) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2023.04.18.536450 · Cited by 5

Combination of the Novel RAF Dimer Inhibitor Brimarafenib With the MEK Inhibitor Mirdametinib Is Effective Against NRAS Mutant Melanoma

Tellenbach, F. L., Seiler, L., Johnson, M. P., Rehrauer, H., Schukla, P., Gómez, J. M. M., Stoffel, C. I., Kamal, A., Dummer, R., Levesque, M. P., et al. (2025) · Pigment Cell & Melanoma Research · doi:10.1111/pcmr.70062 · Cited by 5

Covalent pan-TEAD inhibitors block YAP activity and demonstrate brain penetrance in a Hippo-dependent cancer model

Hagenbeek, T. J., Zbieg, J. R., Smith, R., Paul, S., Gerosa, L., Torrini, C., Guarnaccia, A. D., Ong, C. C., Lacap, J. A., Ning, M., et al. (2026) · Nature Communications · doi:10.1038/s41467-026-74722-5 · Cited by 4

Selective inhibition of BRAF and CRAF sensitizes NF1-deficient malignant peripheral nerve sheath tumors to MEK inhibitors

Wang, J., Sarkar, A., García, N., Zhang, L., Calizo, A., Lisok, A., Campos, K., He, F., Punjaala, N., Marple, T. C., et al. (2025) · Molecular Medicine · doi:10.1186/s10020-025-01353-9 · Cited by 4

Exploring the In Vitro and In Vivo Therapeutic Potential of BRAF and MEK Inhibitor Combination in NRAS-Mutated Melanoma

Niessner, H., Hüsch, A., Kosnopfel, C., Meinhardt, M., Westphal, D., Meier, F., Schilling, B., & Sinnberg, T. (2023) · Cancers · doi:10.3390/cancers15235521 · Cited by 3

Computational Modeling of Drug Response Identifies Mutant-Specific Constraints for Dosing panRAF and MEK Inhibitors in Melanoma

Goetz, A., Shanahan, F., Brooks, L., Lin, E., Mroue, R. M., Cruz, D. D., Hunsaker, T., Czech, B., Dixit, P. D., Segal, U., et al. (2024) · Cancers · doi:10.3390/cancers16162914 · Cited by 3

Rat Sarcoma Virus Family Genes in Acute Myeloid Leukemia: Pathogenetic and Clinical Implications

Khattab, S., Berisha, A., Baran, N., & Piccaluga, P. P. (2025) · Biomedicines · doi:10.3390/biomedicines13010202 · Cited by 4

Targeted therapy for pediatric glioma: RAF(t)ing in the molecular era

Shen, Z.-P., Zhang, Z., Li, N., Xu, L., & Chen, Y. (2025) · World Journal of Pediatrics · doi:10.1007/s12519-025-00889-4 · Cited by 3

Understanding cancer drug resistance with Sleeping Beauty functional genomic screens: Application to MAPK inhibition in cutaneous melanoma

Zhu, E. Y., Schillo, J. L., Murray, S., Riordan, J. D., & Dupuy, A. J. (2023) · iScience · doi:10.1016/j.isci.2023.107805 · Cited by 4

Characterizing the Molecular Mechanism of the Lethal C423D Mutation in FgMyoI: A Molecular Perspective

Bao, Y., Jia, F., Li, M., Xu, R., Xie, Y., Zhang, F., & Guo, J. (2024) · Journal of Agricultural and Food Chemistry · doi:10.1021/acs.jafc.3c08648 · Cited by 3

Targeting Hyperactive Ras Signaling in Pediatric CancerPreprint

Levinson, A. L., Shannon, K., & Huang, B. J. (2024) · Cold Spring Harbor Perspectives in Medicine · doi:10.1101/cshperspect.a041572 · Cited by 3

In Vivo Efficacy of ABHD17 Inhibition Validates the Palmitoylation Cycle as a Therapeutic Target in NRAS -Mutant CancerPreprint

Decker, M., Huang, B. J., Ware, T. B., Boone, C. D., Tang, M., Ybarra, J., Sale, M. J., Francois, R. A., Ballapuram, A. C., Taran, K. A., et al. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.03.20.644389 · Cited by 3

Unveiling Common Transcriptomic Features between Melanoma Brain Metastases and Neurodegenerative Diseases

Soler-Sáez, I., Karz, A., Hidalgo, M. R., Gómez-Cabañes, B., López‐Cerdán, A., Català-Senent, J. F., Prutisto-Chang, K., Eskow, N. M., Izar, B., Redmer, T., et al. (2024) · Journal of Investigative Dermatology · doi:10.1016/j.jid.2024.09.005 · Cited by 3

Phase I Clinical Trial Evaluating Safety, Tolerability, and Early Activity of Exarafenib (KIN-2787), a Highly Selective Pan-RAF Inhibitor, in BRAF -Altered Solid Tumors or NRAS -Mutant Melanoma

Gambardella, V., McKean, M. A., Kim, R., Kato, S., Cassier, P. A., Mehnert, J. M., Chmielowski, B., Gaudy‐Marqueste, C., Chen, C. T., Planchard, D., et al. (2026) · JCO oncology advances. · doi:10.1200/oa-25-00114 · Cited by 2

Dual inhibition of BRAF for cancer treatment: advances and therapeutic potential

Ren, C., Zhang, M., Liu, J., Zhang, L., Guan, X., Pu, S., & Li, J. (2025) · Future Medicinal Chemistry · doi:10.1080/17568919.2025.2575748 · 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

Protomer Selectivity of RAF Inhibitors Within the RAS/RAF SignalosomePreprint

Vasta, J. D., Michaud, A., Zimprich, C., Thomas, M., Wilkinson, J., Crapster, J. A., & Robers, M. B. (2022) · Research Square · doi:10.21203/rs.3.rs-2175742/v1 · Cited by 2

Abstract 36: ARAF mutations confer resistance to RAF dimer inhibitors in NRAS and BRAF mutant melanoma

Malek, S. (2021) · Cancer Research · doi:10.1158/1538-7445.am2021-36

ARAF Mutations Limit Response to RAF Dimer Inhibition

(2021) · Cancer Discovery · doi:10.1158/2159-8290.cd-rw2021-069 · Cited by 4

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

Abstract A012: Emergence of MEK1 mutations in RAF or RAS-mutant solid tumors following treatment with a combination of selective type II RAF inhibitor belvarafenib and MEK inhibitor cobimetinib

Hilz, S., Chen, M., Nowicka, M., Chakravarthy, H., Moshref, M., Gerosa, L., Eng‐Wong, J., Chou, C. K., Noh, Y. S., Hong, Y.-H., et al. (2024) · Cancer Research · doi:10.1158/1538-7445.canevol23-a012

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

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