Current Development Status of MEK Inhibitors
Open accessAbstract
The current development status of mitogen-activated protein kinase kinase (MEK) inhibitors, including the preclinical data and clinical study progress, has been summarized in this review. Different MEK inhibitors, possessing specific physicochemical properties and bioactivity characteristics, may provide different options for patients seeking treatment for cancer. Moreover, the combination of the MEK inhibitors with other therapies—such as chemotherapy, targeted therapy, and immunotherapy—may be a promising approach for clinical use.
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Claims other papers make about this one
Each is checked against this paper’s own text: does it say what the citing paper says it does?
Several clinically approved inhibitors target molecules downstream of KRAS, including RAF, MEK, ERK, PI3K, AKT, and mTOR.
“Several clinically approved inhibitors target molecules downstream of KRAS, including RAF, MEK, ERK, PI3K, AKT, and mTOR [44].”
From KRAS: Biology, Inhibition, and Mechanisms of Inhibitor Resistance (2024) · cites this paper as [44]
Section 3 identifies two approved MEK inhibitors, trametinib and cobimetinib, and §3.1 discusses an approved combination of a MEK inhibitor with a BRAF inhibitor. The paper places RAF, MEK, and ERK in the Ras signaling pathway (§1), but it does not establish that inhibitors targeting ERK, PI3K, AKT, and mTOR are clinically approved; it describes PI3K and ERK inhibitors in an ongoing clinical study (§3.2). (LLM, conf=0.88)
Experimental — accuracy not yet measured
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Cites
Down-Regulation of Na+/K+ATPase Activity by Human Parvovirus B19 Capsid Protein VP1
Almilaji, A., Szteyn, K., Fein, E., Pakladok, T., Muñoz, C., Elvira, B., Towhid, S. T., Alesutan, I., Shumilina, E. V., Bock, C. –., et al. (2013) · Cellular Physiology and Biochemistry · doi:10.1159/000350083 · Cited by 8,675 · see citing works
Mammalian MAP kinase signalling cascades
Chang, L., & Karin, M. (2001) · Nature · doi:10.1038/35065000 · Cited by 5,118 · see citing works
Alessi, D. R., Cuenda, A., Cohen, P., Dudley, D. T., & Saltiel, A. R. (1995) · Journal of Biological Chemistry · doi:10.1074/jbc.270.46.27489 · Cited by 3,396 · see citing works
A synthetic inhibitor of the mitogen-activated protein kinase cascade.
Dudley, D. T., Pang, L., Decker, S. J., Bridges, A. J., & Saltiel, A. R. (1995) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.92.17.7686 · Cited by 2,679 · see citing works
Long, G. V., Stroyakovskiy, D., Gogas, H. J., Levchenko, E., de Braud, F., Larkin, J., Garbe, C., Jouary, T., Hauschild, A., Grob, J., et al. (2015) · The Lancet · doi:10.1016/s0140-6736(15)60898-4 · Cited by 1,397 · see citing works
Planchard, D., Smit, E. F., Groen, H. J. M., Mazières, J., Besse, B., Helland, Å., Giannone, V., D'amelio, A. M., Zhang, P., Mookerjee, B., et al. (2017) · The Lancet Oncology · doi:10.1016/s1470-2045(17)30679-4 · Cited by 1,360 · see citing works
Ascierto, P. A., McArthur, G. A., Dréno, B., Atkinson, V. G., Liszkay, G., Giacomo, A. M. D., Mandalà, M., Демидов, Л. В., Stroyakovskiy, D., Thomas, L., et al. (2016) · The Lancet Oncology · doi:10.1016/s1470-2045(16)30122-x · Cited by 1,022 · see citing works
Planchard, D., Besse, B., Groen, H. J. M., Souquet, P.-J., Quoix, E., Baik, C. S., Barlesi, F., Kim, T. M., Mazieres, J., Novello, S., et al. (2016) · The Lancet Oncology · doi:10.1016/s1470-2045(16)30146-2 · Cited by 888 · see citing works
Ascierto, P. A., Schadendorf, D., Berking, C., Agarwala, S. S., van Herpen, C. M., Queirolo, P., Blank, C. U., Hauschild, A., Beck, J. T., St-Pierre, A., et al. (2013) · The Lancet Oncology · doi:10.1016/s1470-2045(13)70024-x · Cited by 640 · cited 1× · see citing works
“Binimetinib was the first targeted therapy to show activity in patients with NRAS-mutated melanoma and offered a potential option for kinds of cancer with few effective treatments [71,73].”
BackgroundGilmartin, A. G., Bleam, M. R., Groy, A., Moss, K. G., Minthorn, E. A., Kulkarni, S. G., Rominger, C. M., Erskine, S. G., Fisher, K. E., Yang, J., et al. (2011) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-10-2200 · Cited by 590 · see citing works
Infante, J. R., Fecher, L. A., Falchook, G. S., Nallapareddy, S., Gordon, M. S., Becerra, C., DeMarini, D. J., Cox, D. S., Xu, Y., Morris, S. R., et al. (2012) · The Lancet Oncology · doi:10.1016/s1470-2045(12)70270-x · Cited by 552 · see citing works
Dummer, R., Schadendorf, D., Ascierto, P. A., Arance, A. M., Dutriaux, C., Giacomo, A. M. D., Rutkowski, P. L., Vecchio, M. D., Gutzmer, R., Mandalà, M., et al. (2017) · The Lancet Oncology · doi:10.1016/s1470-2045(17)30180-8 · Cited by 501 · see citing works
The clinical development of MEK inhibitors
Zhao, Y., & Adjei, A. A. (2014) · Nature Reviews Clinical Oncology · doi:10.1038/nrclinonc.2014.83 · Cited by 403 · see citing works
Jänne, P. A., van den Heuvel, M. M., Barlesi, F., Cobo, M., Mazieres, J., Crinò, L., Orlov, S., Blackhall, F., Wolf, J., Garrido, P., et al. (2017) · JAMA · doi:10.1001/jama.2017.3438 · Cited by 335 · see citing works
Ma, W., Gilligan, B. M., Yuan, J. D., & Li, T. (2016) · Journal of Hematology & Oncology · doi:10.1186/s13045-016-0277-y · Cited by 328 · see citing works
Banerjee, A., Jakacki, R. I., Onar‐Thomas, A., Wu, S., Nicolaides, T. P., Poussaint, T. Y., Fangusaro, J., Phillips, J. J., Perry, A., Turner, D. C., et al. (2017) · Neuro-Oncology · doi:10.1093/neuonc/now282 · Cited by 320 · see citing works
Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers
Hatzivassiliou, G., Haling, J. R., Chen, H., Song, K. W., Price, S., Heald, R. A., Hewitt, J. F. M., Zak, M., Peck, A., Orr, C., et al. (2013) · Nature · doi:10.1038/nature12441 · Cited by 317 · see citing works
The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901
Barrett, S. D., Bridges, A. J., Dudley, D. T., Saltiel, A. R., Fergus, J. H., Flamme, C. M., Delaney, A. M., Kaufman, M., LePage, S., Leopold, W. R., et al. (2008) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2008.10.054 · Cited by 289 · see citing works
The ups and downs of MEK kinase interactions
Hagemann, C., & Blank, J. L. (2001) · Cellular Signalling · doi:10.1016/s0898-6568(01)00220-0 · Cited by 278 · see citing works
MEK in cancer and cancer therapy
Neuzillet, C., Tijeras‐Raballand, A., de Mestier, L., Cros, J. F., Faivre, S. J., & Raymond, É. (2013) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2013.10.001 · Cited by 263 · see citing works
Haura, E. B., Ricart, A. D., Larson, T. G., Stella, P. J., Bazhenova, L., Miller, V. A., Cohen, R. B., Eisenberg, P. D., Selaru, P., Wilner, K. D., et al. (2010) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-09-1920 · Cited by 237 · see citing works
Targeting the MAPK pathway in melanoma: Why some approaches succeed and other fail
Inamdar, G. S., Madhunapantula, S. V., & Robertson, G. P. (2010) · Biochemical Pharmacology · doi:10.1016/j.bcp.2010.04.029 · Cited by 223 · see citing works
Recent progress in targeting the Raf/MEK/ERK pathway with inhibitors in cancer drug discovery
THOMPSON, N., & LYONS, J. (2005) · Current Opinion in Pharmacology · doi:10.1016/j.coph.2005.04.007 · Cited by 217 · see citing works
Sakai, T. (2011) · International Journal of Oncology · doi:10.3892/ijo.2011.1015 · Cited by 204 · see citing works
Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate)
Abé, H., Kikuchi, S., Hayakawa, K., Iida, T., Nagahashi, N., Maeda, K., Sakamoto, J., Matsumoto, N., Miura, T., Matsumura, K., et al. (2011) · ACS Medicinal Chemistry Letters · doi:10.1021/ml200004g · Cited by 202 · see citing works
RDEA119/BAY 869766: A Potent, Selective, Allosteric Inhibitor of MEK1/2 for the Treatment of Cancer
Iverson, C., Larson, G., Lai, C., Yeh, L., Dadson, C., Weingarten, P., Appleby, T. C., Vo, T., Maderna, A., Vernier, J., et al. (2009) · Cancer Research · doi:10.1158/0008-5472.can-09-0679 · Cited by 184 · see citing works
Rice, K. D., Aay, N., Anand, N. K., Blazey, C. M., Bowles, O. J., Bussenius, J., Costanzo, S., Curtis, J. K., DeFina, S. C., Dubenko, L. G., et al. (2012) · ACS Medicinal Chemistry Letters · doi:10.1021/ml300049d · Cited by 175 · see citing works
Utility of PD-L1 immunohistochemistry assays for predicting PD-1/PD-L1 inhibitor response
Diggs, L. P., & Hsueh, E. C. (2017) · Biomarker Research · doi:10.1186/s40364-017-0093-8 · Cited by 174 · see citing works
Clinical experience of MEK inhibitors in cancer therapy
Wang, D., Boerner, S. A., Winkler, J. D., & LoRusso, P. M. (2006) · Biochimica et Biophysica Acta (BBA) - Molecular Cell Research · doi:10.1016/j.bbamcr.2006.11.009 · Cited by 171 · see citing works
Dabrafenib and Trametinib, Alone and in Combination for BRAF -Mutant Metastatic Melanoma
Menzies, A. M., & Long, G. V. (2014) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-13-2054 · Cited by 170 · see citing works
Clinical activity and safety of cobimetinib (cobi) and atezolizumab in colorectal cancer (CRC).
Bendell, J. C., Kim, T. W., Goh, B. C., Wallin, J. J., Oh, D., Han, S., Lee, C. B., Hellmann, M. D., Desai, J., Lewin, J. H., et al. (2016) · Journal of Clinical Oncology · doi:10.1200/jco.2016.34.15_suppl.3502 · Cited by 165 · see citing works
Martinez‐García, M., Banerji, U., Albanell, J., Bahleda, R., Dolly, S. O., Kraeber‐Bodéré, F., Rojo, F., Routier, É., Guarin, E., Xu, Z., et al. (2012) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-12-0742 · Cited by 153 · see citing works
Bendell, J. C., Javle, M. M., Bekaii‐Saab, T., Finn, R. S., Wainberg, Z. A., Laheru, D. A., Weekes, C. D., Tan, B. R., Khan, G. N., Zalupski, M. M., et al. (2017) · British Journal of Cancer · doi:10.1038/bjc.2017.10 · Cited by 128 · see citing works
Brown, A. P., Carlson, T., Loi, C., & Graziano, M. J. (2006) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-006-0323-5 · Cited by 127 · see citing works
Dong, Q., Dougan, D. R., Gong, X., Halkowycz, P., Jin, B., Kanouni, T., O’Connell, S. M., Scorah, N., Shi, L., Wallace, M. B., et al. (2011) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2011.01.071 · Cited by 124 · see citing works
MEK Inhibitors in the Treatment of Metastatic Melanoma and Solid Tumors
Grimaldi, A., Simeone, E., Festino, L., Vanella, V., Strudel, M., & Ascierto, P. (2017) · American Journal of Clinical Dermatology · doi:10.1007/s40257-017-0292-y · Cited by 124 · see citing works
Jain, N., Curran, E. K., Iyengar, N. M., Díaz-Flores, E., Kunnavakkam, R., Popplewell, L. L., Kirschbaum, M. H., Karrison, T., Erba, H. P., Green, M., et al. (2013) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-13-1311 · Cited by 116 · see citing works
BRAF inhibitors in cancer therapy
Johansson, C. H., & Brage, S. E. (2013) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2013.11.011 · Cited by 112 · see citing works
Huynh, H. T., Ngo, V. C., Koong, H. N., Poon, D. Y. H., Choo, S. P., Toh, H. C., Thng, C. H., Chow, P. K. H., Ong, H. S., Chung, A. Y. F., et al. (2009) · Journal of Hepatology · doi:10.1016/j.jhep.2009.10.008 · Cited by 99 · see citing works
Lim, H. Y., Heo, J., Choi, H. J., Lin, C.-Y., Yoon, J., Hsu, C., Rau, K., Poon, R. T. P., Yeo, W., Park, J., et al. (2014) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-13-3445 · Cited by 98 · see citing works
Emerging therapeutic agents for lung cancer
Dholaria, B., Hammond, W. A., Shreders, A. J., & Lou, Y. (2016) · Journal of Hematology & Oncology · doi:10.1186/s13045-016-0365-z · Cited by 91 · see citing works
Rosen, L. S., LoRusso, P. M., Ma, W. W., Goldman, J. W., Weise, A. M., Colevas, A. D., Adjei, A. A., Yazji, S., Shen, A., Johnston, S. H., et al. (2016) · Investigational New Drugs · doi:10.1007/s10637-016-0374-3 · Cited by 88 · see citing works
Isshiki, Y., Kohchi, Y., Iikura, H., Matsubara, Y., Asoh, K., Murata, T., Kohchi, M., Mizuguchi, E., Tsujii, S., Hattori, K., et al. (2011) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2011.01.062 · Cited by 80 · see citing works
Combined BRAF and MEK inhibition for the treatment of BRAF-mutated metastatic melanoma
Queirolo, P., Picasso, V., & Spagnolo, F. (2015) · Cancer Treatment Reviews · doi:10.1016/j.ctrv.2015.04.010 · Cited by 74 · see citing works
Dokladda, K., Green, K. A., Pan, D. A., & Hardie, D. G. (2004) · FEBS Letters · doi:10.1016/j.febslet.2004.11.084 · Cited by 74 · see citing works
Boasberg, P. D., Redfern, C. H., Daniels, G. A., Bodkin, D., Garrett, C. R., & Ricart, A. D. (2011) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-011-1620-1 · Cited by 74 · see citing works
The Effects of a Novel MEK Inhibitor PD184161 on MEK-ERK Signaling and Growth in Human Liver Cancer
Klein, P. J., Schmidt, C. M., Wiesenauer, C. A., Choi, J. N., Gage, E. A., Yip-Schneider, M., Wiebke, E. A., Wang, Y., Omer, C. A., & Sebolt, J. S. (2006) · Neoplasia · doi:10.1593/neo.05373 · Cited by 73 · see citing works
Identification of coumarin derivatives as a novel class of allosteric MEK1 inhibitors
Han, S., Zhou, V. W., Pan, S., Liu, Y., Hornsby, M. J., McMullan, D., Klock, H. E., Haugen, J., Lesley, S. A., Gray, N. S., et al. (2005) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2005.08.097 · Cited by 73 · see citing works
Leijen, S., Middleton, M. R., Tresca, P., Kraeber‐Bodéré, F., Dieras, V. C., Scheulen, M. E., Gupta, A., López-Valverde, V., Xu, Z., Rueger, R., et al. (2012) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-12-0868 · Cited by 72 · see citing works
Combination Treatment of Patients with BRAF-Mutant Melanoma: A New Standard of Care
Simeone, E., Grimaldi, A. M., Festino, L., Vanella, V., Palla, M., & Ascierto, P. A. (2017) · BioDrugs · doi:10.1007/s40259-016-0208-z · Cited by 67 · see citing works
McCubrey, J. A., Steelman, L. S., Abrams, S. L., Chappell, W. H., Russo, S. M., Ove, R., Milella, M., Tafuri, A., Lunghi, P., Bonati, A., et al. (2010) · Expert Opinion on Emerging Drugs · doi:10.1517/14728210903282760 · Cited by 63 · see citing works
Tai, W. M. D., Yong, W. P., Lim, C., Low, L., Tham, C. K., Koh, T. S., Ng, Q. S., Wang, W., Wang, L. Z., Hartano, S., et al. (2016) · Annals of Oncology · doi:10.1093/annonc/mdw415 · Cited by 61 · see citing works
Laethem, J. V., Riess, H. B., Jassem, J., Haas, M., Martens, U. M., Weekes, C. D., Peeters, M., Ross, P. J., Bridgewater, J. A., Melichar, B., et al. (2016) · Targeted Oncology · doi:10.1007/s11523-016-0469-y · Cited by 59 · see citing works
Haasbach, E., Hartmayer, C., & Planz, O. (2013) · Antiviral Research · doi:10.1016/j.antiviral.2013.03.006 · Cited by 58 · see citing works
Recent progress on MAP kinase pathway inhibitors.
Uehling, D., & Harris, P. (2015) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2015.07.093 · Cited by 55 · see citing works
Paola, R. D., Galuppo, M., Mazzon, E., Paterniti, I., Bramanti, P., & Cuzzocrea, S. (2009) · Pharmacological Research · doi:10.1016/j.phrs.2009.09.008 · Cited by 52 · see citing works
Sullivan, R. J., Gonzalez, R. C., Lewis, K. D., Hamid, O., Infante, J. R., Patel, M. R., Hodi, F. S., Wallin, J. J., Pitcher, B., Cha, E., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2017.35.15_suppl.3063 · Cited by 52 · see citing works
Nivolumab plus ipilimumab in the treatment of advanced melanoma
Tsai, K. K., & DAUD, A. I. (2015) · Journal of Hematology & Oncology · doi:10.1186/s13045-015-0219-0 · Cited by 49 · see citing works
Gandara, D. R., Leighl, N. B., Delord, J., Barlési, F., Bennouna, J., Zalcman, G., Infante, J. R., Reckamp, K. L., Kelly, K. L., Shepherd, F. A., et al. (2016) · Journal of Thoracic Oncology · doi:10.1016/j.jtho.2016.11.2218 · Cited by 49 · see citing works
Cohen, R. B., Aamdal, S., Nyakas, M., Cavallin, M., Green, D., Learoyd, M., Smith, I., & Kurzrock, R. (2013) · European Journal of Cancer · doi:10.1016/j.ejca.2013.01.013 · Cited by 48 · see citing works
MEK inhibitors in oncology: a patent review (2015-Present)
Mahapatra, D. K., Asati, V., & Bharti, S. K. (2017) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2017.1339688 · Cited by 47 · see citing works
Yung, H. W., Wyttenbach, A., & Tolkovsky, A. M. (2004) · Biochemical Pharmacology · doi:10.1016/j.bcp.2004.03.030 · Cited by 39 · see citing works
Adjei, A. A., LoRusso, P. M., Ribas, A., Sosman, J. A., Pavlick, A. C., Dy, G. K., Zhou, X., Gangolli, E. A., Kneissl, M., Faucette, S. R., et al. (2016) · Investigational New Drugs · doi:10.1007/s10637-016-0391-2 · Cited by 38 · see citing works
Cerioni, L., Palomba, L., & Cantoni, O. (2003) · FEBS Letters · doi:10.1016/s0014-5793(03)00675-6 · Cited by 36 · see citing works
Modulation of endochondral ossification by MEK inhibitors PD0325901 and AZD6244 (Selumetinib)
El‐Hoss, J., Kolind, M. P., Jackson, M. T., Deo, N., Mikulec, K., McDonald, M. M., Little, C. B., Little, D. G., & Schindeler, A. (2013) · Bone · doi:10.1016/j.bone.2013.11.013 · Cited by 31 · see citing works
Choo, E. F., Ng, C. M., Berry, L., Belvin, M. P., Lewin‐Koh, N., Merchant, M. A., & Salphati, L. (2012) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-012-1988-6 · Cited by 30 · see citing works
Daouti, S., Higgins, B., Kolinsky, K. D., Packman, K. E., Wang, H., Rizzo, C., Moliterni, J., Huby, N. J. S., Fotouhi, N., Liu, M., et al. (2010) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-09-0601 · Cited by 28 · see citing works
Miller, W. H., Kim, T. M., Lee, C. B., Flaherty, K. T., Reddy, S. A., Jamal, R., Chow, L. Q. M., Rooney, I. A., Pitcher, B., Cha, E., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2017.35.15_suppl.3057 · Cited by 27 · see citing works
BRAF and MEK inhibition for the treatment of advanced BRAF mutant melanoma
Richman, J., Martín-Liberal, J., Diem, S., & Larkin, J. (2015) · Expert Opinion on Pharmacotherapy · doi:10.1517/14656566.2015.1044971 · Cited by 26 · see citing works
Putative allosteric MEK1 and MEK2 inhibitors
Price, S. (2008) · Expert Opinion on Therapeutic Patents · doi:10.1517/13543776.18.6.603 · Cited by 26 · see citing works
Kraeber‐Bodéré, F., Carlier, T., Naegelen, V. M., Shochat, E., Lumbroso, J., Trampal, C., Nagarajah, J., Chua, S. C., Hugonnet, F., Stokkel, M. P. M., et al. (2012) · Journal of Nuclear Medicine · doi:10.2967/jnumed.112.109421 · Cited by 26 · see citing works
Leonard, J. T., Raess, P. W., Dunlap, J. B., Hayes‐Lattin, B., Tyner, J. W., & Traer, E. A. (2016) · Journal of Hematology & Oncology · doi:10.1186/s13045-016-0258-1 · Cited by 25 · see citing works
Beloueche‐Babari, M., Jamin, Y., Arunan, V., Walker‐Samuel, S., Revill, M., Smith, P. D., Halliday, J. L., Waterton, J. C., Barjat, H., Workman, P., et al. (2013) · British Journal of Cancer · doi:10.1038/bjc.2013.456 · Cited by 22 · see citing works
Choo, E. F., Belvin, M. P., Chan, J., Hoeflich, K. P., Orr, C., Robarge, K. D., Yang, X., Zak, M., & Boggs, J. W. (2010) · Xenobiotica · doi:10.3109/00498254.2010.514365 · Cited by 21 · see citing works
Wabnitz, P. A., Mitchell, D., & Wabnitz, D. A. M. (2004) · Pharmaceutical Research · doi:10.1023/b:pham.0000041464.27579.d0 · Cited by 20 · see citing works
MEK inhibitors beyond monotherapy: current and future development.
Templeton, I. E., & Musib, L. (2015) · Current opinion in pharmacology (Print) · doi:10.1016/j.coph.2015.05.012 · Cited by 20 · see citing works
Prospects for MEK inhibitors for treating cancer
Martin-Liberal, J., Lagares-Tena, L., & Larkin, J. (2014) · Expert Opinion on Drug Safety · doi:10.1517/14740338.2014.892578 · Cited by 19 · see citing works
Jamieson, D., Griffin, M. J., Sludden, J., Drew, Y., Cresti, N., Swales, K. E., Merriman, M., Allen, R. A., Bevan, P., Buerkle, M., et al. (2016) · European Journal of Cancer · doi:10.1016/j.ejca.2016.08.026 · Cited by 17 · see citing works
Fangusaro, J., Onar‐Thomas, A., Poussaint, T. Y., Wu, S., Ligon, A. H., Lindeman, N. I., Banerjee, A., Packer, R. J., Kilburn, L. B., Pollack, I. F., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2017.35.15_suppl.10504 · Cited by 16 · see citing works
Kwon, B., & Houpt, T. A. (2011) · Neurobiology of Learning and Memory · doi:10.1016/j.nlm.2011.10.005 · Cited by 15 · see citing works
Awada, A. H., Delord, J., Houédé, N., Lebbé, C., Lesimple, T., Schellens, J. H. M., Rottey, S., Kefford, R. F., Rejeb, N., & Raymond, É. (2012) · European Journal of Cancer · doi:10.1016/s0959-8049(12)72401-2 · Cited by 15 · see citing works
Hsueh, E. C., & Gorantla, K. C. (2015) · Experimental Hematology and Oncology · doi:10.1186/s40164-016-0054-1 · Cited by 12 · see citing works
Delord, J., Houédé, N., Awada, A. H., Lebbé, C., Lesimple, T., Schellens, J. H. M., Rottey, S., Kefford, R. F., Rejeb, N., & Raymond, É. (2012) · European Journal of Cancer · doi:10.1016/s0959-8049(12)72413-9 · Cited by 12 · see citing works
Lee, L., Niu, H., Goelzer, P., Rueger, R., Deutsch, J., Busse‐Reid, R., DeSchepper, S., Blotner, S., Barrett, J., Weissgerber, G., et al. (2010) · The Journal of Clinical Pharmacology · doi:10.1177/0091270010361254 · Cited by 11 · see citing works
Wang, W., Zhou, J., Zhao, L., & Chen, S. (2017) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2017.01.135 · Cited by 11 · see citing works
Highly Selective MEK Inhibitors
Lee, C.-S., & Duesbery, N. S. (2010) · Current Enzyme Inhibition · doi:10.2174/157340810793384124 · Cited by 10 · see citing works
Administration, U. S. F. &. D. (2017) · Case Medical Research · doi:10.31525/fda1-ucm564331.htm · Cited by 10 · see citing works
Nakamichi, S., Nokihara, H., Yamamoto, N., Yamada, Y., Fujiwara, Y., Tamura, Y., Wakui, H., Honda, K., Mizugaki, H., Kitazono, S., et al. (2015) · Investigational new drugs · doi:10.1007/s10637-015-0229-3 · Cited by 10 · see citing works
Activity of the MEK inhibitor selumetinib (AZD6244; ARRY-142886) in nasopharyngeal cancer cell lines
Ma, B. B. Y., Lui, V. W. Y., Cheung, C. S. F., Lau, C. P. Y., Ho, K., Hui, E. P., Tsui, S. K., Ng, M. H. L., Cheng, S. H., Ng, P. K., et al. (2012) · Investigational New Drugs · doi:10.1007/s10637-012-9828-4 · Cited by 9 · see citing works
Fangusaro, J., Onar‐Thomas, A., Poussaint, T. Y., Wu, S., Ligon, A. H., Lindeman, N. I., Banerjee, A., Packer, R. J., Kilburn, L. B., Pollack, I. F., et al. (2017) · Neuro-Oncology · doi:10.1093/neuonc/nox083.141 · Cited by 9 · see citing works
Houédé, N., Delord, J., Awada, A. H., Lebbé, C., Lesimple, T., Schellens, J. H. M., Rottey, S., Kefford, R. F., von Richter, O., & Raymond, É. (2012) · European Journal of Cancer · doi:10.1016/s0959-8049(12)72397-3 · Cited by 8 · see citing works
Naing, A., Mita, M. M., Komarnitsky, P. B., Milner, A., von Richter, O., Ogden, J., Piha-Paul, S. A., Fu, S. W., Asatiani, E., & Kurzrock, R. (2012) · European Journal of Cancer · doi:10.1016/s0959-8049(12)72405-x · Cited by 8 · see citing works
Absorption, metabolism and excretion of cobimetinib, an oral MEK inhibitor, in rats and dogs
Takahashi, R., Ma, S., Yue, Q., Kim‐Kang, H., Yi, Y., Ly, J., Boggs, J. W., Fettes, A., McClory, A., Deng, Y., et al. (2016) · Xenobiotica · doi:10.3109/00498254.2016.1157645 · Cited by 8 · see citing works
CInQ-03, a novel allosteric MEK inhibitor, suppresses cancer growth in vitro and in vivo
Kim, D. J., Lee, M., Reddy, K., Li, Y., Lim, D. Y., Xie, H., Lee, S., Yeom, Y. I., Bode, A. M., & Dong, Z. (2013) · Carcinogenesis · doi:10.1093/carcin/bgt015 · Cited by 6 · see citing works
Choo, E. F., Belvin, M. P., Merchant, M. A., Chan, E., Hollingshead, P., Orr, C., Boggs, J. W., Plise, E. G., Robarge, K. D., & Zak, M. (2012) · European Journal of Cancer · doi:10.1016/s0959-8049(12)72299-2 · Cited by 3 · see citing works
Krishnamurthy, A., Dasari, A. N., Lockhart, A. C., Stein, M. N., Sanoff, H. K., Lee, J. J., Hansen, A. R., Bekaii‐Saab, T., Malhotra, U., Rippke, S., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2017.35.4_suppl.609 · Cited by 2 · see citing works
Krishnamurthy, A., Dasari, A. N., Noonan, A. M., Mehnert, J. M., Lockhart, A. C., Stein, M. N., Sanoff, H. K., Lee, J. J., Hansen, A. R., Malhotra, U., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2017.35.15_suppl.2587 · Cited by 2 · see citing works
Flagged first, then by citations
1 of the 98 references couldn’t be matched to a known paper.
Research works printed but not linked: 2
- [49]Pheneger J. Wallace E. Marlow A. Hurley B. Lyssikatos J. Bendele A.M. Lee P.A. Characterization of ARRY-438162, a Potent MEK Inhibitor in Combination with Methotrexate or Ibuprofen in In Vivo Models of Arthritis Proceedings of the 2006 Annual Scientific Meeting Boston, MA, USA 20–24 October 2006 794
- [50]Wallace E. Lyssikatos J. Blake J. Marlow A. Greschuk J. Yeh T. Callejo M. Marsh V. Poch G. Otten J. AZD8330 (ARRY-424704): Preclinical evaluation of a potent, selective MEK 1/2 inhibitor currently in phase I trials Proceedings of the AACR Denver, CO, USA 18–22 April 2009 Volume 69
Cited by
Sorted by citations
RAF-MEK-ERK pathway in cancer evolution and treatment
Ullah, R., Yin, Q., Snell, A. H., & Wan, L. (2022) · Seminars in Cancer Biology · doi:10.1016/j.semcancer.2021.05.010 · Cited by 553 · see citing works
Targeting Aberrant RAS/RAF/MEK/ERK Signaling for Cancer Therapy
Degirmenci, U., Wang, M., & Hu, J. (2020) · Cells · doi:10.3390/cells9010198 · Cited by 541 · see citing works
Tyrosine kinase inhibitors for solid tumors in the past 20 years (2001–2020)
Huang, L., Jiang, S., & Shi, Y. (2020) · Journal of Hematology & Oncology · doi:10.1186/s13045-020-00977-0 · Cited by 467 · see citing works
Five-Year Analysis of Adjuvant Dabrafenib plus Trametinib in Stage III Melanoma
Dummer, R., Hauschild, A., Santinami, M., Atkinson, V. G., Mandalà, M., Kirkwood, J. M., Chiarion‐Sileni, V., Larkin, J., Nyakas, M., Dutriaux, C., et al. (2020) · New England Journal of Medicine · doi:10.1056/nejmoa2005493 · Cited by 407 · see citing works
MEK inhibitors for the treatment of non-small cell lung cancer
Han, J., Liu, Y., Yang, S., Wu, X., Li, H., & Wang, Q. (2021) · Journal of Hematology & Oncology · doi:10.1186/s13045-020-01025-7 · Cited by 291 · see citing works
Targeting the PI3K/AKT/mTOR and RAF/MEK/ERK pathways for cancer therapy
Li, Q., Li, Z., Luo, T. L., & Shi, H. (2022) · Molecular Biomedicine · doi:10.1186/s43556-022-00110-2 · Cited by 274 · see citing works
Central serous chorioretinopathy: An update on risk factors, pathophysiology and imaging modalities
Kaye, R., Chandra, S., Sheth, J. U., Boon, C. J. F., Sivaprasad, S., & Lotery, A. J. (2020) · Progress in Retinal and Eye Research · doi:10.1016/j.preteyeres.2020.100865 · Cited by 258 · see citing works
Tolerability of BRAF/MEK inhibitor combinations: adverse event evaluation and management
Heinzerling, L., Eigentler, T., Fluck, M., Hassel, J. C., Heller-Schenck, D., Leipe, J., Pauschinger, M., Vogel, A., Zimmer, L., & Gutzmer, R. (2019) · ESMO Open · doi:10.1136/esmoopen-2019-000491 · Cited by 236 · see citing works
MEK inhibitor resistance mechanisms and recent developments in combination trials
Kun, E., Tsang, Y. T. M., Ng, C. W., Gershenson, D. M., & Wong, K. (2020) · Cancer Treatment Reviews · doi:10.1016/j.ctrv.2020.102137 · Cited by 189 · see citing works
The current understanding on the impact of KRAS on colorectal cancer
Meng, M., Zhong, K., Jiang, T., Liu, Z., Kwan, H. Y., & Su, T. (2021) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2021.111717 · Cited by 171 · see citing works
Perspective of mesenchymal transformation in glioblastoma
Kim, Y., Varn, F. S., Park, S., Yoon, B. W., Park, H. R., Lee, C., Verhaak, R. G. W., & Paek, S. H. (2021) · Acta Neuropathologica Communications · doi:10.1186/s40478-021-01151-4 · Cited by 146 · see citing works
A review: FDA-approved fluorine-containing small molecules from 2015 to 2022
Sheikhi, N., Bahraminejad, M., Saeedi, M., & Mirfazli, S. S. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115758 · Cited by 141 · see citing works
Navigating the ERK1/2 MAPK Cascade
Martín-Vega, A., & Cobb, M. H. (2023) · Biomolecules · doi:10.3390/biom13101555 · Cited by 124 · see citing works
Ocular Adverse Events Associated with Mek Inhibitors
Méndez-Martínez, S., Calvo, P., Ruiz-Moreno, O., Pardiñas Barón, N., Leciñena Bueno, J., Gil Ruiz, M. D. R., & Pablo, L. (2019) · Retina · doi:10.1097/iae.0000000000002451 · Cited by 117 · see citing works
Synthetically Lethal Interactions of ATM, ATR, and DNA-PKcs
Kantidze, O. L., Velichko, A. K., Luzhin, A. V., Petrova, N. V., & Razin, S. V. (2018) · Trends in cancer · doi:10.1016/j.trecan.2018.09.007 · Cited by 111 · see citing works
BRAF and MEK Inhibitors and Their Toxicities: A Meta-Analysis
Garutti, M., Bergnach, M., Polesel, J., Palmero, L., Pizzichetta, M. A., & Puglisi, F. (2022) · Cancers · doi:10.3390/cancers15010141 · Cited by 96 · see citing works
Allosteric MEK inhibitors act on BRAF/MEK complexes to block MEK activation
Pino, G. L. G., Li, K., Park, E., Schmoker, A. M., Ha, B. H., & Eck, M. J. (2021) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.2107207118 · Cited by 95 · see citing works
MAPK Pathway: a Potential Target for the Treatment of Non-small-cell Lung Carcinoma
Pradhan, R., Singhvi, G., Dubey, S. K., Gupta, G., & Dua, K. (2019) · Future Medicinal Chemistry · doi:10.4155/fmc-2018-0468 · Cited by 90 · see citing works
CD73's Potential as an Immunotherapy Target in Gastrointestinal Cancers
Harvey, J. B., Phan, L. H., Villarreal, O. E., & Bowser, J. L. (2020) · Frontiers in Immunology · doi:10.3389/fimmu.2020.00508 · Cited by 87 · see citing works
BRAF in malignant melanoma progression and metastasis: potentials and challenges.
Alqathama, A. A. (2020) · PubMed Central · Cited by 86 · see citing works
New Directions in the Therapy of Glioblastoma
Szklener, K., Mazurek, M., Wieteska, M., Wacławska, M., Bilski, M., & Mańdziuk, S. (2022) · Cancers · doi:10.3390/cancers14215377 · Cited by 84 · see citing works
Ram, T., Singh, A. K., Kumar, A., Singh, H., Pathak, P., Grishina, M., Khalilullah, H., Jaremko, M., Emwas, A.-H. M., Verma, A., et al. (2023) · RSC Medicinal Chemistry · doi:10.1039/d3md00145h · Cited by 83 · see citing works
Understanding the role of dopamine in cancer: past, present and future
Grant, C. E., Flis, A. L., & Ryan, B. M. (2022) · Carcinogenesis · doi:10.1093/carcin/bgac045 · Cited by 82 · see citing works
MAPK Signaling Pathway in Oral Squamous Cell Carcinoma: Biological Function and Targeted Therapy
Cheng, Y.-X., Chen, J., Shi, Y.-X., Fang, X.-D., & Tang, Z. (2022) · Cancers · doi:10.3390/cancers14194625 · Cited by 70 · see citing works
Self-citationMitochondria: The metabolic switch of cellular oncogenic transformation
Tan, Y. Q., Zhang, X., Zhang, S., Zhu, T., Garg, M., Lobie, P. E., & Pandey, V. (2021) · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer · doi:10.1016/j.bbcan.2021.188534 · Cited by 75 · see citing works
Protein–Protein Interactions: Emerging Oncotargets in the RAS-ERK Pathway
García-Gómez, R., Bustelo, X. R., & Crespo, P. (2018) · Trends in Cancer · doi:10.1016/j.trecan.2018.07.002 · Cited by 72 · see citing works
Fernández‐Ruiz, M., Meije, Y., Manuel, O., Akan, H., Carratalà, J., Aguado, J. M., & Delaloye, J. (2018) · Clinical Microbiology and Infection · doi:10.1016/j.cmi.2018.01.029 · Cited by 72 · see citing works
Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader
Wei, J., Hu, J., Wang, L., Xie, L., Jin, M. S., Chen, X., Liu, J., & Jin, J. J. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b01528 · Cited by 67 · see citing works
Covalent Docking Identifies a Potent and Selective MKK7 Inhibitor
Shraga, A., Olshvang, E., Davidzohn, N., Khoshkenar, P., Germain, N., Shurrush, K. A., Carvalho, S., Avram, L., Albeck, S., Unger, T., et al. (2018) · Cell chemical biology · doi:10.1016/j.chembiol.2018.10.011 · Cited by 66 · see citing works
Murali, I., Kasar, S. N., Naeem, A. S., Tyekucheva, S., Khalsa, J. K., Thrash, E. M., Itchaki, G., Livitz, D. G., Leshchiner, I., Dong, S., et al. (2021) · Blood · doi:10.1182/blood.2020006765 · Cited by 64 · see citing works
KRAS: Biology, Inhibition, and Mechanisms of Inhibitor Resistance
Ash, L. J., Busia-Bourdain, O., Okpattah, D., Kamel, A., Liberchuk, A., & Wolfe, A. L. (2024) · Current Oncology · doi:10.3390/curroncol31040150 · Cited by 59 · see citing works
“Sotorasib administration led to the tumor infiltration of CD8 T-cells, macrophages, and dendritic cells, which were further amplified by the combination with anti-PD-1 therapy.”
BackgroundSynthetic Lethality through the Lens of Medicinal Chemistry
Myers, S. H., Ortega, J. A., & Cavalli, A. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00766 · Cited by 60 · see citing works
Chun, Y. S., Kim, M., Lee, S., Kim, M. J., Hong, T.-J., Jeon, J. K., Ganbat, D., Kim, H. T., Kim, S. S., Kam, T., et al. (2022) · Molecular Psychiatry · doi:10.1038/s41380-022-01713-5 · Cited by 56 · see citing works
Inhibition of autophagy and MEK promotes ferroptosis in Lkb1-deficient Kras-driven lung tumors
Bhatt, V. D., Lan, T., Wang, W., Kong, J., Lopes, E. C., Wang, J., Khayati, K., Raju, A., Rangel, M., Lopez, E., et al. (2023) · Cell Death and Disease · doi:10.1038/s41419-023-05592-8 · Cited by 57 · see citing works
Precision drugging of the MAPK pathway in head and neck cancer
Ngan, H.-L., Law, C.-H., Choi, Y., Chan, J., & Lui, V. W. (2022) · npj Genomic Medicine · doi:10.1038/s41525-022-00293-1 · Cited by 51 · see citing works
Design, Synthesis, and Biological Evaluation of MEK PROTACs
Vollmer, S., Cunoosamy, D. M., Lv, H., Feng, H., Li, X., Nan, Z., Yang, W., & Perry, M. W. D. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00810 · Cited by 53 · see citing works
A mass spectrometry-based proteome map of drug action in lung cancer cell lines
Ruprecht, B., Bernardo, J. D., Wang, Z., Mo, X., Ursu, O., Christopher, M., Fernandez, R. B., Zheng, L., Dill, B. D., Wang, H., et al. (2020) · Nature Chemical Biology · doi:10.1038/s41589-020-0572-3 · Cited by 53 · see citing works
Wang, X., Xiao, T., Chen, P., Jiang, P., Li, W., Chang, H., Wei, C., Lai, X., Zhang, H., Pan, Y., et al. (2024) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-024-01986-y · Cited by 48 · see citing works
Neuwelt, A. J., Kimball, A. K., Johnson, A. M., Arnold, B. W., Bullock, B., Kaspar, R. E., Kleczko, E. K., Kwak, J., Wu, M., Heasley, L. E., et al. (2020) · Journal for ImmunoTherapy of Cancer · doi:10.1136/jitc-2019-000441 · Cited by 46 · see citing works
Jain, A. S., Prasad, A., Pradeep, S., Dharmashekar, C., Achar, R. R., Silina, E. V., Stupin, V. A., Amachawadi, R. G. G., Prasad, S. K., Pruthvish, R., et al. (2021) · Frontiers in Oncology · doi:10.3389/fonc.2021.741326 · Cited by 50 · see citing works
KRAS targeting antibody synergizes anti-cancer activity of gemcitabine against pancreatic cancer
Kang, Y. W., Lee, J. E., Jung, K. H., Son, M. K., Shin, S., Kim, S., Fang, Z., YAN, H. H., Park, J. H., Han, B., et al. (2018) · Cancer Letters · doi:10.1016/j.canlet.2018.09.013 · Cited by 46 · see citing works
Llauradó, M., Dawson, A., Hoenisch, J., Kim, H. H., Bamford, S., Salamanca, C. M., DiMattia, G. E., Shepherd, T. G., Cremona, M., Hennessy, B. T., et al. (2019) · Cancer Cell International · doi:10.1186/s12935-019-0725-1 · Cited by 46 · see citing works
PHGDH as a mechanism for resistance in metabolically-driven cancers
Rathore, R., Schutt, C. R., & Tine, B. A. V. (2020) · Cancer Drug Resistance · doi:10.20517/cdr.2020.46 · Cited by 46 · see citing works
Research progress on KRAS mutations in colorectal cancer
Cefalì, M., Epistolio, S., Palmarocchi, M. C., Frattini, M., & Dosso, S. D. (2021) · Journal of Cancer Metastasis and Treatment · doi:10.20517/2394-4722.2021.61 · Cited by 47 · see citing works
Small molecule inhibitors in pancreatic cancer
Sun, J., Russell, C. C., Scarlett, C. J., & McCluskey, A. (2020) · RSC Medicinal Chemistry · doi:10.1039/c9md00447e · Cited by 45 · see citing works
A Comprehensive Review of Various Therapeutic Strategies for the Management of Skin Cancer
Dachani, S. R., Kaleem, M., Mujtaba, M. A., Mahajan, N. M., Ali, S. A., Almutairy, A. F., Mahmood, D., Anwer, M. K., Ali, M. D., & Kumar, S. (2024) · ACS Omega · doi:10.1021/acsomega.3c09780 · Cited by 44 · see citing works
Hu, J., Wei, J., Yim, H., Wang, L., Xie, L., Jin, M. S., Kabir, M., Qin, L., Chen, X., Liu, J., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01609 · Cited by 43 · see citing works
Chao, M., Chang, L.-H., Tu, H., Chang, C.-D., Lai, M.-J., Chen, Y.-Y., Liou, J., Teng, C., & Pan, S. (2019) · Clinical Epigenetics · doi:10.1186/s13148-019-0681-6 · Cited by 43 · see citing works
Current Perspectives and Novel Strategies of NRAS-Mutant Melanoma
García-Álvarez, A., Ortiz, C., & Muñoz-Couselo, E. (2021) · OncoTargets and Therapy · doi:10.2147/ott.s278095 · Cited by 34 · see citing works
HDAC inhibitors with potential to overcome drug resistance in castration-resistant prostate cancer
Biersack, B., Nitzsche, B., & Höpfner, M. (2022) · Cancer Drug Resistance · doi:10.20517/cdr.2021.105 · Cited by 41 · see citing works
Ekiz, H. A., Lai, S.-C. A., Gundlapalli, H., Haroun, F., Williams, M. A., & Welm, A. L. (2018) · OncoImmunology · doi:10.1080/2162402x.2018.1480286 · Cited by 37 · see citing works
The coding and non-coding transcriptional landscape of subependymal giant cell astrocytomas
Bongaarts, A., van Scheppingen, J., Korotkov, A., Mijnsbergen, C., Anink, J. J., Jansen, F. E., Spliet, W. G. M., den Dunnen, W. F. A., Gruber, V., Scholl, T. O., et al. (2019) · Brain · doi:10.1093/brain/awz370 · Cited by 37 · see citing works
Laure, M., Hamza, H., Koch-Heier, J., Quernheim, M., Müller, C., Schreiber, A., Müller, G., Pleschka, S., Ludwig, S., & Planz, O. (2020) · Antiviral Research · doi:10.1016/j.antiviral.2020.104806 · Cited by 37 · see citing works
BRAF and MEK Targeted Therapies in Pediatric Central Nervous System Tumors
Talloa, D., Triarico, S., Agresti, P., Mastrangelo, S., Attinà, G., Romano, A., Maurizi, P., & Ruggiero, A. (2022) · Cancers · doi:10.3390/cancers14174264 · Cited by 34 · see citing works
Arbidol: The current demand, strategies, and antiviral mechanisms
Kang, Y., Shi, Y., & Xu, S. (2023) · Immunity Inflammation and Disease · doi:10.1002/iid3.984 · Cited by 34 · see citing works
Decoding allosteric landscapes: computational methodologies for enzyme modulation and drug discovery
Zhu, R., Wu, C., Zha, J., Lu, S., & Zhang, J. (2025) · RSC Chemical Biology · doi:10.1039/d4cb00282b · Cited by 34 · see citing works
The role of the p90 ribosomal S6 kinase family in prostate cancer progression and therapy resistance
Cronin, R., Brooke, G. N., & Prischi, F. (2021) · Oncogene · doi:10.1038/s41388-021-01810-9 · Cited by 32 · see citing works
Options of Therapeutics and Novel Delivery Systems of Drugs for the Treatment of Melanoma
Wang, H., Tran, T., Duong, K. T., Nguyen, T. B., & Le, U. M. (2022) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.2c00775 · Cited by 34 · see citing works
Wu, S., Xu, H., Wu, X., Liu, P., Shi, Y., Pang, P., Deng, L., Zhou, G., & Chen, X. (2019) · Phytomedicine · doi:10.1016/j.phymed.2019.152895 · Cited by 31 · see citing works
Uitdehaag, J. C. M., Kooijman, J. J., de Roos, J. A. D. M., Prinsen, M. B. W., Dylus, J., Willemsen‐Seegers, N., Kawase, Y., Sawa, M., de Man, J., van Gerwen, S. J. C., et al. (2018) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-18-0877 · Cited by 30 · see citing works
Galvin, R. T., Watson, A. L., Largaespada, D. A., Ratner, N., Osum, S. H., & Moertel, C. L. (2021) · Current Oncology Reports · doi:10.1007/s11912-021-01032-y · Cited by 30 · see citing works
Rabiee, B., Anwar, K. N., Shen, X., Putra, I., Liu, M., Jung, R., Afsharkhamseh, N., Rosenblatt, M. I., Fishman, G. A., Liu, X., et al. (2020) · Science Translational Medicine · doi:10.1126/scitranslmed.aaz4894 · Cited by 28 · see citing works
Lee, H., Lee, J., & Kim, H. (2019) · Pharmacological Research · doi:10.1016/j.phrs.2019.104466 · Cited by 28 · see citing works
Yue, W., Deng, X., Wang, Z., Jiang, M., Hu, R., Duan, Y., Wang, Q., Cui, J., & Fang, Y. (2023) · Immunity & Ageing · doi:10.1186/s12979-023-00354-8 · Cited by 27 · see citing works
Zhang, J., Joshua, A. M., Li, Y., O’Meara, C. H., Morris, M. J., & Khachigian, L. M. (2024) · Cancer Letters · doi:10.1016/j.canlet.2024.216633 · Cited by 27 · see citing works
Suman, I., Šimić, L., Jurešić, G. Č., Buljević, S., Klepac, D., & Domitrović, R. (2024) · Cell Death Discovery · doi:10.1038/s41420-024-01872-0 · Cited by 26 · see citing works
Li, Y., Dong, Q., & Cui, Y. (2019) · Cancer Biology and Medicine · doi:10.20892/j.issn.2095-3941.2019.0137 · Cited by 25 · see citing works
Recent applications of computational methods to allosteric drug discovery
Govindaraj, R. G., Thangapandian, S., Schauperl, M., Denny, R. A., & Diller, D. (2023) · Frontiers in Molecular Biosciences · doi:10.3389/fmolb.2022.1070328 · Cited by 30 · see citing works
Feichtenschlager, V., Zheng, Y. J., Ho, W. W.-S., Chen, L.-N., Callanan, C., Chen, C., Lee, A., Ortiz, J., Rappersberger, K., & Ortiz‐Urda, S. (2023) · Oncotarget · doi:10.18632/oncotarget.28447 · Cited by 26 · see citing works
Huestis, M. P., Cruz, D. D., DiPasquale, A. G., Durk, M. R., Eigenbrot, C. W., Gibbons, P., Gobbi, A., Hunsaker, T., La, H., Leung, D. H., et al. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c02085 · Cited by 26 · see citing works
A review on tyrosine kinase inhibitors for targeted breast cancer therapy
Sankarapandian, V., Rajendran, R. L., Miruka, C. O., Poornima, S., Maran, B. A. V., Krishnamoorthy, R., Gangadaran, P., & Ahn, B. (2024) · Pathology - Research and Practice · doi:10.1016/j.prp.2024.155607 · Cited by 25 · see citing works
Advanced Acral Melanoma Therapies: Current Status and Future Directions
Zhang, Y., Lan, S., & Wu, D. (2022) · Current Treatment Options in Oncology · doi:10.1007/s11864-022-01007-6 · Cited by 26 · see citing works
Wang, X., Luo, Z., Chen, J., Chen, Y., Ji, D., Li, F., Chen, L., Zhao, Q., Hu, P., Sun, P., et al. (2023) · BMC Medicine · doi:10.1186/s12916-022-02669-7 · Cited by 25 · see citing works
Lee, J., Lim, B., Pearson, T., Choi, K. C., Fuson, J. A., Bartholomeusz, C., Paradiso, L. J., Myers, T. J., Tripathy, D., & Ueno, N. T. (2019) · Breast Cancer Research and Treatment · doi:10.1007/s10549-019-05166-3 · Cited by 24 · see citing works
Booth, A. E. C., Hopkins, A. M., Rowland, A., Kichenadasse, G., Smith, J. R., & Sorich, M. J. (2020) · Therapeutic Advances in Medical Oncology · doi:10.1177/1758835920944359 · Cited by 24 · see citing works
Smith, M. P., Ferguson, H. R., Ferguson, J., Zindy, E., Kowalczyk, K., Kedward, T., Bates, C., Parsons, J., Watson, J., Chandler, S., et al. (2021) · bioRxiv · doi:10.15252/embj.2020107182 · Cited by 22 · see citing works
Directing T-Cell Immune Responses for Cancer Vaccination and Immunotherapy
Smith, P. L., Piadel, K., & Dalgleish, A. G. (2021) · Vaccines · doi:10.3390/vaccines9121392 · Cited by 23 · see citing works
Advances in Immunosuppressive Agents Based on Signal Pathway
Xu, Z., & Chu, M. (2022) · Frontiers in Pharmacology · doi:10.3389/fphar.2022.917162 · Cited by 24 · see citing works
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 23 · see citing works
Ludwig, S., Pleschka, S., & Planz, O. (2023) · Current Opinion in Virology · doi:10.1016/j.coviro.2023.101304 · Cited by 23 · see citing works
Hoffman, T. E., Nangia, V., Ill, C. R., Passanisi, V. J., Armstrong, C., Yang, C., & Spencer, S. L. (2023) · Science Signaling · doi:10.1126/scisignal.ade8744 · Cited by 22 · see citing works
Biswas, B., Huang, Y., Craik, D. J., & Wang, C. K. L. (2024) · Chemical Science · doi:10.1039/d4sc01088d · Cited by 23 · see citing works
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 · see citing works
Biondini, M., Kiepas, A., El–Houjeiri, L., Annis, M. G., Hsu, B. E., Fortier, A.-M., Morin, G., Martina, J. A., Sirois, I., Aguilar‐Mahecha, A., et al. (2022) · Oncogene · doi:10.1038/s41388-022-02206-z · Cited by 22 · see citing works
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 · see citing works
Genome-Based Classification and Therapy of Prostate Cancer
Angeles, A. K., Bauer, S., Ratz, L., Klauck, S. M., & Sültmann, H. (2018) · Diagnostics · doi:10.3390/diagnostics8030062 · Cited by 22 · see citing works
Hybrids of MEK inhibitor and NO donor as multitarget antitumor drugs
Wang, C., Xi, D., Wang, H., Niu, Y., Liang, L., Xu, F., Peng, Y., & Xu, P. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112271 · Cited by 22 · see citing works
Exploring azetidine containing heterocycles: From green synthesis to applications
Jaiswal, S., Arya, N., Kishore, D., Dwivedi, J., & Sharma, S. K. (2025) · Tetrahedron · doi:10.1016/j.tet.2025.134491 · Cited by 21 · see citing works
Fragment-Based Discovery of Novel Allosteric MEK1 Binders
Fruscia, P. D., Edfeldt, F., Shamovsky, I. L., Collie, G. W., Aagaard, A., Barlind, L., Börjesson, U., Hansson, E. L., Lewis, R. J., Nilsson, M., et al. (2021) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.0c00563 · Cited by 21 · see citing works
Colorectal Cancer, Liver Metastases and Biotherapies
Osei‐Bordom, D., Kamarajah, S. K., & Christou, N. (2021) · Biomedicines · doi:10.3390/biomedicines9080894 · Cited by 21 · see citing works
A benzoxazole compound as a novel MEK inhibitor for the treatment of RAS/RAF mutant cancer
Cheng, Y., Wang, X., Xia, X., Zhang, W. Y., & Tian, H. (2019) · International Journal of Cancer · doi:10.1002/ijc.32119 · Cited by 20 · see citing works
Self-citationClinical 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 · see citing works
A superior loading control for the cellular thermal shift assay
Delport, A., & Hewer, R. (2022) · Scientific Reports · doi:10.1038/s41598-022-10653-7 · Cited by 19 · see citing works
Systemic MEK inhibition enhances the efficacy of 5-aminolevulinic acid-photodynamic therapy
Chelakkot, V. S., Som, J., Yoshioka, E., Rice, C. P. J., Rutihinda, S. G., & Hirasawa, K. (2019) · British Journal of Cancer · doi:10.1038/s41416-019-0586-3 · Cited by 19 · see citing works
Non-‘classical’ MEKs: A review of MEK3-7 inhibitors
Kwong, A. J., & Scheidt, K. A. (2020) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2020.127203 · Cited by 19 · see citing works
Koshrovski‐Michael, S., Ajamil, D. R., Dey, P., Kleiner, R., Tevet, S., Epshtein, Y., Buzhor, M. G., Khoury, R., Pozzi, S., Shenbach‐Koltin, G., et al. (2024) · Science Advances · doi:10.1126/sciadv.adr4762 · Cited by 18 · see citing works
Wiwatchaitawee, K., Mekkawy, A. I., Quarterman, J. C., Naguib, Y. W., Ebeid, K., Geary, S. M., & Salem, A. K. (2021) · Drug Delivery and Translational Research · doi:10.1007/s13346-021-01065-7 · Cited by 18 · see citing works
Preclinical characterization of tunlametinib, a novel, potent, and selective MEK inhibitor
Liu, Y., Cheng, Y., Huang, G., Xia, X., Wang, X., & Tian, H. (2023) · Frontiers in Pharmacology · doi:10.3389/fphar.2023.1271268 · Cited by 18 · see citing works
Self-citationEffect of NFX-179 MEK inhibitor on cutaneous neurofibromas in persons with neurofibromatosis type 1
Sarin, K. Y., Bradshaw, M. H., O'Mara, C., Shahryari, J., Kincaid, J., Kempers, S. E., Tu, J. H., Dhawan, S., DuBois, J. C., Wilson, D., et al. (2024) · Science Advances · doi:10.1126/sciadv.adk4946 · Cited by 18 · see citing works
MEK inhibitors: a promising targeted therapy for cardiovascular disease
Mohammed, K. A. K., Madeddu, P. R., & Avolio, E. (2024) · Frontiers in Cardiovascular Medicine · doi:10.3389/fcvm.2024.1404253 · Cited by 18 · see citing works
- Authors
- Cheng, Y., & Tian, H.
- Affiliations
- Chinese Academy of Medical Sciences & Peking Union Medical College (CN)
- Corresponding author
- Tian, Hongqi
- Venue
- Molecules
- Publisher
- MDPI AG
- Published
- 2017-09-26
- Volume
- 22
- Issue
- 10
- Pages
- 1551
- ISSN
- 1420-3049 (ISSN-L)
- PMC
- PMC6151813
- OpenAlex
- W2758375389
- Cited by
- 291
- References
- 98
- Citations by year
- 2026: 22 · 2025: 22 · 2024: 47 · 2023: 62 · 2022: 39 · 2021: 34 · 2020: 30 · 2019: 21 · 2018: 14
- FWCI
- 1.66
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- Locations
- Molecules (publishedVersion, cc-by)
- Europe PMC (PubMed Central) (publishedVersion, other-oa)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Funders
- Chinese Academy of Medical Sciences (2017-I2M-3-019, 2017-)
- Peking Union Medical College
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Melanoma and MAPK Pathways
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Tyrosine Phosphatases
- Health Sciences › Medicine › Pathology and Forensic Medicine › Cancer Mechanisms and Therapy
- Keywords
- MEK inhibitors, MEK, cancer therapy, combination therapy, chemotherapy, targeted therapy, immunotherapy, preclinical drug development, clinical trials, drug development
- MeSH terms
- Animals, Antineoplastic Agents, Clinical Trials as Topic, Drug Evaluation, Preclinical, Humans, Signal Transduction, ras Proteins, Mitogen-Activated Protein Kinase Kinases, Protein Kinase Inhibitors, Extracellular Signal-Regulated MAP Kinases, raf Kinases, Drug Discovery, Molecular Targeted Therapy
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
