A dimerization-dependent mechanism drives RAF catalytic activation

Coot : model-building tools for molecular graphics

Emsley, P., & Cowtan, K. (2004) · Acta Crystallographica Section D Biological Crystallography · doi:10.1107/s0907444904019158 · Cited by 30,571

Mutations of the BRAF gene in human cancer

Davies, H., Bignell, G. R., Cox, C., Stephens, P., Edkins, S., Clegg, S., Teague, J., Woffendin, H., Garnett, M. J., Bottomley, W., et al. (2002) · Nature · doi:10.1038/nature00766 · Cited by 10,674

Targeting the Raf-MEK-ERK mitogen-activated protein kinase cascade for the treatment of cancer

Roberts, P. J., & Der, C. J. (2007) · Oncogene · doi:10.1038/sj.onc.1210422 · Cited by 2,788

An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor

Zhang, X., Gureasko, J., Shen, K., Cole, P. A., & Kuriyan, J. (2006) · Cell · doi:10.1016/j.cell.2006.05.013 · Cited by 1,650

KSR is a scaffold required for activation of the ERK/MAPK module

Roy, F., Laberge, G., Douziech, M., Ferland-McCollough, D., & Therrien, M. (2002) · Genes & Development · doi:10.1101/gad.962902 · Cited by 217

Inhibition of Mutated, Activated BRAF in Metastatic Melanoma

Flaherty, K. T., Puzanov, I., Kim, K. B., Ribas, A., McArthur, G. A., Sosman, J. A., O'Dwyer, P. J., Lee, R. J., Grippo, J. F., Nolop, K., et al. (2010) · New England Journal of Medicine · doi:10.1056/nejmoa1002011 · Cited by 3,103

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

Targeting RAS–ERK signalling in cancer: promises and challenges

Samatar, A. A., & Poulikakos, P. I. (2014) · Nature Reviews Drug Discovery · doi:10.1038/nrd4281 · Cited by 1,163

Targeting the RAS/RAF/MAPK pathway for cancer therapy: from mechanism to clinical studies

Bahar, M. E., Kim, H. J., & Kim, D. R. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01705-z · Cited by 888

Regulation of RAF protein kinases in ERK signalling

Lavoie, H., & Therrien, M. (2015) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm3979 · Cited by 702

Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design

Ostrem, J. M. L., & Shokat, K. M. (2016) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2016.139 · Cited by 641

MEK1 and MEK2 inhibitors and cancer therapy: the long and winding road

Caunt, C. J., Sale, M. J., Smith, P. D., & Cook, S. J. (2015) · Nature Reviews Cancer · doi:10.1038/nrc4000 · Cited by 606

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

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

Melanoma: from mutations to medicine

Tsao, H., Chin, L., Garraway, L. A., & Fisher, D. E. (2012) · Genes & Development · doi:10.1101/gad.191999.112 · Cited by 496

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

Ras-GTP dimers activate the Mitogen-Activated Protein Kinase (MAPK) pathway

Nan, X., Tamgüney, T. M., Collisson, E. A., Lin, L.-J., Pitt, C., Galeas, J., Lewis, S., Gray, J. W., McCormick, F., & Chu, S. (2015) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1509123112 · Cited by 273

Inhibition of RAS function through targeting an allosteric regulatory site

Spencer-Smith, R., Koide, A., Zhou, Y., Eguchi, R. R., Sha, F., Gajwani, P., Santana, D., Gupta, A., Jacobs, M., Herrero-Garcia, E., et al. (2017) · Nature Chemical Biology · doi:10.1038/nchembio.2231 · Cited by 283

PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

He, M., Cao, C., Ni, Z., Liu, Y., Song, P., Hao, S., He, Y., Sun, X., & Rao, Y. (2022) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-022-00999-9 · Cited by 283

Targeting RAS–RAF–MEK–ERK signaling pathway in human cancer: Current status in clinical trials

Song, Y., Bi, Z., Liu, Y., Qin, F., Wei, Y., & Wei, X. (2023) · Genes & Diseases · doi:10.1016/j.gendis.2022.05.006 · Cited by 212

GTP-Dependent K-Ras Dimerization

Muratcioglu, S., Chavan, T. S., Freed, B. C., Jang, H., Khavrutskii, L., Freed, R. N., Dyba, M. A., Stefanisko, K., Tarasov, S. G., Gursoy, A., et al. (2015) · Structure · doi:10.1016/j.str.2015.04.019 · Cited by 202

Targeting Protein-Protein Interaction by Small Molecules

Jin, L., Wang, W., & Fang, G. (2014) · Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev-pharmtox-011613-140028 · Cited by 195

RAS: Striking at the Core of the Oncogenic Circuitry

Gimple, R. C., & Wang, X. (2019) · Frontiers in Oncology · doi:10.3389/fonc.2019.00965 · Cited by 174

Structural basis for the action of the drug trametinib at KSR-bound MEK

Khan, Z. M., Real, A. M., Marsiglia, W. M., Chow, A., Duffy, M. E., Yerabolu, J. R., Scopton, A. P., & Dar, A. C. (2020) · Nature · doi:10.1038/s41586-020-2760-4 · Cited by 178

Oncogenic BRAF Deletions That Function as Homodimers and Are Sensitive to Inhibition by RAF Dimer Inhibitor LY3009120

Chen, S.-H., Zhang, Y., Van Horn, R. D., Yin, T., Buchanan, S., Yadav, V., Mochalkin, I., Wong, S. S., Yue, Y. G., Huber, L., et al. (2016) · Cancer Discovery · doi:10.1158/2159-8290.cd-15-0896 · Cited by 171

Pharmacological targeting of RAS: recent success with direct inhibitors

O’Bryan, J. P. (2019) · Pharmacological Research · doi:10.1016/j.phrs.2018.10.021 · Cited by 153

Molecular Pathways and Mechanisms of BRAF in Cancer Therapy

Poulikakos, P. I., Sullivan, R. J., & Yaeger, R. (2022) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-21-2138 · Cited by 145

Allostery: Allosteric Cancer Drivers and Innovative Allosteric Drugs

Nussinov, R., Zhang, M., Maloney, R., Liu, Y., Tsai, C.-J., & Jang, H. (2022) · Journal of Molecular Biology · doi:10.1016/j.jmb.2022.167569 · Cited by 66

K-Ras prenylation as a potential anticancer target

Baranyi, M., Buday, L., & Hegedűs, B. (2020) · Cancer and Metastasis Reviews · doi:10.1007/s10555-020-09902-w · Cited by 62

KRASQ61H Preferentially Signals through MAPK in a RAF Dimer-Dependent Manner in Non–Small Cell Lung Cancer

Zhou, Z.-W., Ambrogio, C., Bera, A. K., Li, Q., Li, X.-X., Li, L., Son, J., Gondi, S., Li, J., Campbell, E., et al. (2020) · Cancer Research · doi:10.1158/0008-5472.can-20-0448 · Cited by 60

Cryo-EM structure of a RAS/RAF recruitment complex

Park, E., Rawson, S., Schmoker, A., Kim, B.-W., Oh, S., Song, K., Jeon, H., & Eck, M. J. (2023) · Nature Communications · doi:10.1038/s41467-023-40299-6 · Cited by 51

Drug resistance resulting from kinase dimerization is rationalized by thermodynamic factors describing allosteric inhibitor effects

Kholodenko, B. N. (2015) · Cell Reports · doi:10.1016/j.celrep.2015.08.014 · Cited by 49

KSR induces RAS‐independent MAPK pathway activation and modulates the efficacy of KRAS inhibitors

Paniagua, G., Jacob, H. K. C., Brehey, O., García‐Alonso, S., Lechuga, C. G., Pons, T., Musteanu, M., Guerra, C., Drosten, M., & Barbacid, M. (2022) · Molecular Oncology · doi:10.1002/1878-0261.13213 · Cited by 34

Dynamic Protein Allosteric Regulation and Disease

Nussinov, R., Tsai, C.-J., & Jang, H. (2019) · Advances in Experimental Medicine and Biology · doi:10.1007/978-981-13-8719-7_2 · Cited by 18

Interplay of PKA and Rac: Fine-tuning of Rac localization and signaling

Bachmann, V. A., Bister, K., & Stefan, E. (2013) · Small GTPases · doi:10.4161/sgtp.27281 · Cited by 14

Unveiling the Domain-Specific and RAS Isoform-Specific Details of BRAF Regulation

Trebino, T., Markusic, B., Nan, H., Banerjee, S., & Wang, Z. (2023) · doi:10.1101/2023.04.24.538112 · Cited by 1

Unveiling the Domain-Specific and RAS Isoform-Specific Details of BRAF Regulation

(2023) · doi:10.7554/elife.88836.2 · Cited by 1