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Inhibition of Mutated, Activated BRAF in Metastatic Melanoma

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The Discovery of Exarafenib (KIN-2787): Overcoming the Challenges of Pan-RAF Kinase Inhibition

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Expert consensus on the diagnosis and treatment of solid tumors with BRAF mutations

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Hydroxynaphthalenecarboxamides and substituted piperazinylpropandiols, two new series of BRAF inhibitors. A theoretical and experimental study

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Transcriptomic and functional studies reveal miR-431-5p as a tumour suppressor in pancreatic ductal adenocarcinoma cells

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The GSK3 kinase and LZTR1 protein regulate the stability of Ras family proteins and the proliferation of pancreatic cancer cells

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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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OPN3 Regulates Melanogenesis in Human Congenital Melanocytic Nevus Cells through Functional Interaction with BRAFV600E

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Antitumor Effects of Pan-RAF Inhibitor LY3009120 Against Lung Cancer Cells Harboring Oncogenic BRAF Mutation

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

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RAF-independent MEK mutations drive refractory histiocytic neoplasms but respond to ERK inhibition

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Triple Blockade of Oncogenic RAS Signaling Using KRAS and MEK Inhibitors in Combination with Irradiation in Pancreatic Cancer

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Signalling in pancreatic cancer: from pathways to therapy

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Emerging Tumor-Agnostic Molecular Targets

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RNF43 Inactivation Enhances the B‐RAF/MEK Signaling and Creates a Combinatory Therapeutic Target in Cancer Cells

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Context Matters—Why We Need to Change From a One Size Fits all Approach to Made-to-Measure Therapies for Individual Patients With Pancreatic Cancer

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

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RAS-independent ERK activation by constitutively active KSR3 in non-chordate metazoa

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Occult polyclonality of preclinical pancreatic cancer models drives in vitro evolution

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BRAF L485–P490 deletion mutant metastatic melanoma sensitive to BRAF and MEK inhibition: A case report and literature review

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Deletion Mutations Keep Kinase Inhibitors in the Loop

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

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Knockdown of 15-bp Deletion-Type v-raf Murine Sarcoma Viral Oncogene Homolog B1 mRNA in Pancreatic Ductal Adenocarcinoma Cells Repressed Cell Growth In Vitro and Tumor Volume In Vivo

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

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Unexpected Widespread Bone Metastases from a BRAF K601N Mutated Follicular Thyroid Carcinoma within a Previously Resected Multinodular Goiter

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Implementing Massive Parallel Sequencing into Biliary Samples Obtained through Endoscopic Retrograde Cholangiopancreatography for Diagnosing Malignant Bile Duct Strictures

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Clinical phenotype of adult-onset systemic histiocytosis harboring BRAF in-frame deletions

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Current and emerging treatment options for BRAFV600-mutant melanoma

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Genomic Alterations in Langerhans Cell Histiocytosis

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Over-expressed, N-terminally truncated BRAF is detected in the nucleus of cells with nuclear phosphorylated MEK and ERK

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Occult polyclonality of preclinical pancreatic cancer models drives in vitro evolutionPreprint

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In silico repurposing of clinically approved drugs as potential BRAF inhibitors: a pharmacophore-based virtual screening and experimental investigation

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Custom pyrosequencing assay to detect short BRAF deletions in Langerhans cell histiocytic lesions

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The Activation of MEK1 by Enhanced Homodimerization Drives TumorigenesisPreprint

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Disseminated Langerhans cell histiocytosis in a 51-year-old man with cutaneous involvement and multiple endocrinopathies

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Evaluating the therapeutic potential of the PAK1 and TBK1 kinases in pancreatic ductal adenocarcinoma

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Stellenwert der BRAF-Inhibition bei soliden Tumoren wie dem kolorektalen Karzinom

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BRAF Landscape and Its Implications among Patients with Pediatric Low-Grade Gliomas: A Comprehensive Review of the Literature

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SH003 enhances the anti-cancer effects of Dabrafenib on lung cancer harboring BRAF G469A mutation by inhibiting the MAPK signaling pathwayPreprint

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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. (2024) · eLife · doi:10.7554/elife.95481.1

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

Recent progress in small-molecule targeted therapies for melanoma treatment

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Oncogenic KRAS-driven type I interferon signalling primes pancreatic cancer for necroptosis

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Langerhans cell histiocytosis: molecular mechanisms underlying pathogenesis and emerging targeted therapeutics

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Unveiling BRAF Mutations in Non-small Cell Lung Cancer: State of the Art and Future Perspectives

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Spatial modulation of RAF by RAF/MEK glue enables full-dose combination with pan-RAF inhibitor and potent RAS-mutant tumor-selective MAPK and growth inhibition

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BindingDB Entry 50015972: Novel N-(4-thiocyanatophenyl)-1H-1,2,3-triazole-4-carboxamides exhibit selective cytotoxic activity at nanomolar doses towards human leukemic T-cells.

BindingDB (2023) · UC San Diego · doi:10.7270/q2d50rwt

BindingDB Entry 50002350: Current Insights of BRAF Inhibitors in Cancer.

BindingDB (2020) · UC San Diego · doi:10.7270/q2j968zt

BindingDB Entry 50020999: RIPK1 inhibitors: A key to unlocking the potential of necroptosis in drug development.

BindingDB (2025) · UC San Diego · doi:10.7270/q2hx1j85

BindingDB Entry 50021636: The Discovery of Exarafenib (KIN-2787): Overcoming the Challenges of Pan-RAF Kinase Inhibition.

BindingDB (2025) · UC San Diego · doi:10.7270/q23f4v9x

Abstract 2142: Novel oncogenic BRaf deletions functioning as BRaf homodimer and sensitive to inhibition by LY3009120, a pan Raf and Raf dimer inhibitor

Chen, S.-H., Buchanan, S. G., Zhang, Y., Horn, R. D. V., Yin, T., Yadav, V., Wong, S. S., Huber, L., Henry, J. R., Conti, I., et al. (2015) · Cancer Research · doi:10.1158/1538-7445.am2015-2142

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

Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers

Peng, S.-B., Henry, J. R., Kaufman, M. D., Lu, W.-P., Smith, B. D., Vogeti, S., Rutkoski, T. J., Wise, S., Chun, L., Zhang, Y., et al. (2015) · Cancer Cell · doi:10.1016/j.ccell.2015.08.002 · Cited by 303

Abstract DDT02-02: Identification of LY3009120 as a pan inhibitor of Raf isoforms and dimers with minimal paradoxical activation and activities against BRaf or Ras mutant tumor cells

Peng, S.-B., Henry, J. R., Kaufman, M. D., Lu, W.-P., Smith, B. D., Vogeti, S., Wise, S., Zhang, Y., Horn, R. D. V., Zhang, X., et al. (2014) · Cancer Research · doi:10.1158/1538-7445.am2014-ddt02-02 · Cited by 2

Abstract 4374: Activation mechanism of oncogenic C-helix shifting mutations in BRAF, EGFR, and HER2

Foster, S. A., Whalen, D. M., Özen, A., Wongchenko, M. J., Yin, J., Yen, I., Schaefer, G., Mayfield, J. D., Chmielecki, J., Stephens, P. J., et al. (2016) · Cancer Research · doi:10.1158/1538-7445.am2016-4374