Intermittent Administration of MEK Inhibitor GDC-0973 plus PI3K Inhibitor GDC-0941 Triggers Robust Apoptosis and Tumor Growth Inhibition

Mutations of the BRAF gene in human cancer

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Quantitative analysis of dose-effect relationships: the combined effects of multiple drugs or enzyme inhibitors

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AKT/PKB signaling: navigating downstream

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Targeting RAS signalling pathways in cancer therapy

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

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Targeting the phosphoinositide 3-kinase pathway in cancer

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Roles of the Raf/MEK/ERK pathway in cell growth, malignant transformation and drug resistance

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Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers

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BRAF mutation predicts sensitivity to MEK inhibition

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The COSMIC (Catalogue of Somatic Mutations in Cancer) database and website

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Cobimetinib and vemurafenib for the treatment of melanoma

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Towards combinatorial targeted therapy in melanoma: From pre-clinical evidence to clinical application (Review)

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Patient-derived xenografts reveal limits to PI3K/mTOR- and MEK-mediated inhibition of bladder cancer

Cirone, P., Andresen, C. J., Eswaraka, J. R., Lappin, P. B., & Bagi, C. M. (2014) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-014-2376-1 · Cited by 37

Preclinical assessment of MEK1/2 inhibitors for neurofibromatosis type 2–associated schwannomas reveals differences in efficacy and drug resistance development

Fuse, M. A., Dinh, C. T., Vitte, J., Kirkpatrick, J. M., Mindos, T., Plati, S. K., Young, J. I., Huang, J., Carlstedt, A., Franco, M. C., et al. (2019) · Neuro-Oncology · doi:10.1093/neuonc/noz002 · Cited by 36

ERK Inhibitor LY3214996-Based Treatment Strategies forRAS-Driven Lung Cancer

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

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Kinetics of RTK activation determine ERK reactivation and resistance to dual BRAF/MEK inhibition in melanoma

Kim, S. S., Carvajal, R. D., Kim, M., & Yang, H. W. (2023) · Cell Reports · doi:10.1016/j.celrep.2023.112570 · Cited by 35

Furthering the design and the discovery of small molecule ATP-competitive mTOR inhibitors as an effective cancer treatment

Lv, X., Ma, X., & Hu, Y. (2013) · Expert Opinion on Drug Discovery · doi:10.1517/17460441.2013.800479 · Cited by 34

A Phase I Study of Alpelisib in Combination with Trastuzumab and LJM716 in Patients with PIK3CA -Mutated HER2-Positive Metastatic Breast Cancer

Jhaveri, K. L., Drago, J. Z., Shah, P. D., Wang, R., Pareja, F. G., Ratzon, F., Iasonos, A. E., Patil, S. N., Rosen, N. X., Fornier, M. N., et al. (2021) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-21-0047 · Cited by 34

Redox effects and cytotoxic profiles of MJ25 and auranofin towards malignant melanoma cells

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Conjunctival Melanoma Targeted Therapy: MAPK and PI3K/mTOR Pathways Inhibition

Zaoui, I. E., Bucher, M., Rimoldi, D., Nicolas, M., Kaya, G., Gobert, R. P., Bedoni, N., Schalenbourg, A., Ezziat, S., Zografos, L., et al. (2019) · Investigative Ophthalmology & Visual Science · doi:10.1167/iovs.18-26508 · Cited by 31

CRISPR screens identify a novel combination treatment targeting BCL-XL and WNT signaling for KRAS/BRAF-mutated colorectal cancers

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PK-PD modeling of combination efficacy effect from administration of the MEK inhibitor GDC-0973 and PI3K inhibitor GDC-0941 in A2058 xenografts

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

Mitogen-activated protein kinase (MEK) inhibitors to treat melanoma alone or in combination with other kinase inhibitors

Faghfuri, E., Nikfar, S., Niaz, K., Faramarzi, M. A., & Abdollahi, M. R. (2018) · Expert Opinion on Drug Metabolism & Toxicology · doi:10.1080/17425255.2018.1432593 · Cited by 28

The MEK1/2 Pathway as a Therapeutic Target in High-Grade Serous Ovarian Carcinoma

Chesnokov, M. S., Khan, I., Park, Y., Ezell, J., Mehta, G., Yousif, A., Hong, L., Buckanovich, R. J., Takahashi, A., & Chefetz, I. (2021) · Cancers · doi:10.3390/cancers13061369 · Cited by 29

Population pharmacokinetics and dosing implications for cobimetinib in patients with solid tumors

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Selumetinib for the Treatment of Metastatic Uveal Melanoma: Past and Future Perspectives

Komatsubara, K. M., Manson, D. K., & Carvajal, R. D. (2016) · Future Oncology · doi:10.2217/fon-2015-0075 · Cited by 28

Targeting BRAF-mutant non-small cell lung cancer: Current status and future directions

Riudavets, M., Cascetta, P., & Planchard, D. (2022) · Lung Cancer · doi:10.1016/j.lungcan.2022.05.014 · Cited by 30

Ku80 promotes melanoma growth and regulates antitumor effect of melatonin by targeting HIF1-α dependent PDK-1 signaling pathway

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From basic researches to new achievements in therapeutic strategies of KRAS-driven cancers

Saliani, M., Jalal, R., & Ahmadian, M. R. (2019) · Cancer Biology and Medicine · doi:10.20892/j.issn.2095-3941.2018.0530 · Cited by 27

Selective Eradication of Colon Cancer Cells Harboring PI3K and/or MAPK Pathway Mutations in 3D Culture by Combined PI3K/AKT/mTOR Pathway and MEK Inhibition

Atanasova, V. S., Riedl, A., Strobl, M. M., Flandorfer, J., Unterleuthner, D., Weindorfer, C., Neuhold, P., Stang, S., Hengstschläger, M., Bergmann, M. M., et al. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms24021668 · Cited by 27

In pursuit of synergy: An investigation of the PI3K/mTOR/MEK co-targeted inhibition strategy in NSCLC

Heavey, S., Cuffe, S. D., Finn, S. P., Young, V., Ryan, R. J., Nicholson, S. A., Leonard, N. A., McVeigh, N., Barr, M. P., O'Byrne, K. J., et al. (2016) · Oncotarget · doi:10.18632/oncotarget.12755 · Cited by 27

Phase I trial of MEK 1/2 inhibitor pimasertib combined with mTOR inhibitor temsirolimus in patients with advanced solid tumors

Mita, M., Fu, S., Piha-Paul, S. A., Janku, F., Mita, A., Natale, R., Guo, W., Zhao, C., Kurzrock, R., & Naing, A. (2017) · Investigational New Drugs · doi:10.1007/s10637-017-0442-3 · Cited by 26

Synthesis and biological evaluation of novel N -(piperazin-1-yl)alkyl-1 H -dibenzo[ a , c ]carbazole derivatives of dehydroabietic acid as potential MEK inhibitors

Chen, H., Qiao, C., Miao, T., Li, A., Wang, W., & Gu, W. (2019) · Journal of Enzyme Inhibition and Medicinal Chemistry · doi:10.1080/14756366.2019.1655407 · Cited by 26

Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3 H )-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor

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

Cross-species Proteomics Reveals Specific Modulation of Signaling in Cancer and Stromal Cells by Phosphoinositide 3-kinase (PI3K) Inhibitors

Rajeeve, V., Vendrell, I., Wilkes, E. H., Torbett, N. E., & Cutillas, P. R. (2014) · Molecular & Cellular Proteomics · doi:10.1074/mcp.m113.035204 · Cited by 25

Upstream mitogen-activated protein kinase (MAPK) pathway inhibition: MEK inhibitor followed by a BRAF inhibitor in advanced melanoma patients

Goldinger, S. M., Zimmer, L., Schulz, C., Ugurel, S., Höeller, C., Kaehler, K. C., Schadendorf, D., Hassel, J. C., Becker, J., Hauschild, A., et al. (2013) · European Journal of Cancer · doi:10.1016/j.ejca.2013.09.014 · Cited by 25

Synergistic inhibition of MEK and reciprocal feedback networks for targeted intervention in malignancy

Li, Y., Dong, Q., & Cui, Y. (2019) · Cancer Biology and Medicine · doi:10.20892/j.issn.2095-3941.2019.0137 · Cited by 25

Discovery of Cobimetinib as a novel A-FABP inhibitor using machine learning and molecular docking-based virtual screening

Yang, S., Li, S., & Chang, J. (2022) · RSC Advances · doi:10.1039/d2ra01057g · Cited by 25

Cobimetinib Plus Vemurafenib: A Review in BRAF V600 Mutation-Positive Unresectable or Metastatic Melanoma

Keating, G. M. (2016) · Drugs · doi:10.1007/s40265-016-0562-7 · Cited by 26

From Microbial Switches to Metabolic Sensors: Rewiring the Gut–Brain Kynurenine Circuit

Tanaka, M., & Vécsei, L. (2025) · Biomedicines · doi:10.3390/biomedicines13082020 · Cited by 31

Role of the E3 ubiquitin ligase RNF157 as a novel downstream effector linking PI3K and MAPK signaling pathways to the cell cycle

Dogan, T., Gnad, F., Chan, J., Phu, L., Young, A. E., Chen, J., Doll, S., Stokes, M. P., Belvin, M. P., Friedman, L. S., et al. (2017) · Journal of Biological Chemistry · doi:10.1074/jbc.m117.792754 · Cited by 25

Targeting RAS in neuroblastoma: Is it possible?

Lin, L., Miao, L., Lin, H., Cheng, J., Li, M., Zhuo, Z., & He, J. (2021) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2021.108054 · Cited by 24

Design, synthesis and pharmacological evaluation of 2-arylurea-1,3,5-triazine derivative (XIN-9): A novel potent dual PI3K/mTOR inhibitor for cancer therapy

Sun, X., Zhang, B., Luo, L., Yang, Y., He, B., Zhang, Q., Wang, L., Xu, S., Zheng, P., & Zhu, W. (2022) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2022.106157 · Cited by 23

MAPK Pathway Inhibition Enhances the Efficacy of an Anti-Endothelin B Receptor Drug Conjugate by Inducing Target Expression in Melanoma

Asundi, J., Lacap, J. A., Clark, S., Nannini, M., Roth, L. A., & Polakis, P. G. (2014) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-13-0446 · Cited by 26

A Bifunctional MAPK/PI3K Antagonist for Inhibition of Tumor Growth and Metastasis

Galbán, S., Apfelbaum, A. A., Espinoza, C. E., Heist, K., Haley, H. R., Bedi, K., Ljungman, M. E., Galbán, C. J., Luker, G. D., Dort, M. V., et al. (2017) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-17-0207 · Cited by 22

Preclinical evaluation and reverse phase protein Array-based profiling of PI3K and MEK inhibitors in endometrial carcinoma in vitro

Aslan, O., Cremona, M., Morgan, C., Cheung, L. W. T., Mills, G. B., & Hennessy, B. T. (2018) · BMC Cancer · doi:10.1186/s12885-018-4035-0 · Cited by 23

Prognostic and predictive molecular biomarkers in colorectal cancer

Zhang, J., Zhu, H., Liu, W., Miao, J., Mao, Y., & Li, Q. (2025) · Frontiers in Oncology · doi:10.3389/fonc.2025.1532924 · Cited by 24

DRAP: a toolbox for drug response analysis and visualization tailored for preclinical drug testing on patient-derived xenograft models

Li, Q., Dai, W., Liu, J., Li, Y., & Li, Y. (2019) · Journal of Translational Medicine · doi:10.1186/s12967-019-1785-7 · Cited by 23

Blocking Y-Box Binding Protein-1 through Simultaneous Targeting of PI3K and MAPK in Triple Negative Breast Cancers

Tiwari, A., Iida, M., Kosnopfel, C., Abbariki, M., Menegakis, A., Fehrenbacher, B., Maier, J., Schaller, M., Brucker, S. Y., Wheeler, D. L., et al. (2020) · Cancers · doi:10.3390/cancers12102795 · Cited by 22

Allosteric modulators of MEK1: drug design and discovery

Shang, J., Lu, S., Jiang, Y., & Zhang, J. (2016) · Chemical Biology & Drug Design · doi:10.1111/cbdd.12780 · Cited by 23

Cyclical Treatment of Colorectal Tumor Spheroids Induces Resistance to MEK Inhibitors

Thakuri, P. S., Luker, G. D., & Tavana, H. (2018) · Translational Oncology · doi:10.1016/j.tranon.2018.11.009 · Cited by 22

Binimetinib, pemetrexed and cisplatin, followed by maintenance of binimetinib and pemetrexed in patients with advanced non-small cell lung cancer (NSCLC) and KRAS mutations. The phase 1B SAKK 19/16 trial

Froesch, P., Mark, M. T., Rothschild, S. I., Li, Q., Godar, G., Rusterholz, C., Leibundgut, E. O., Schmid, S., Colombo, I., Metaxas, Y., et al. (2021) · Lung Cancer · doi:10.1016/j.lungcan.2021.04.002 · Cited by 20

Role of the ERK1/2 pathway in tumor chemoresistance and tumor therapy.

Liu, Q.-H., Shi, M.-L., Sun, C., Bai, J., & Zheng, J.-N. (2015) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2014.11.076 · Cited by 17

Research Advances in Chaperone-Mediated Autophagy (CMA) and CMA-Based Protein Degraders

Pan, Z., Huang, X., Liu, M., Jiang, X. L., & He, G. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c02681 · Cited by 21

Biomarker results from a phase II study of MEK1/2 inhibitor binimetinib (MEK162) in patients with advanced NRAS- or BRAF-mutated melanoma

van Herpen, C. V., Agarwala, S., Hauschild, A., Berking, C., Beck, J. T., Schadendorf, D., Jansen, R., Queirolo, P., Ascierto, P., Blank, C. U., et al. (2019) · OncoTarget · doi:10.18632/oncotarget.26753 · Cited by 17

Induction of MEK/ERK activity by AZD8055 confers acquired resistance in neuroblastoma

Xu, D., Toyoda, H., Qi, L., Morimoto, M., Hanaki, R., Iwamoto, S., Komada, Y., & Hirayama, M. (2018) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2018.03.143 · Cited by 20

Mechanism of bioactive polysaccharide from Lachnum sp. acts synergistically with 5‐fluorouracil against human hepatocellular carcinoma

Zong, S., Li, J., Yang, L., Huang, Q., Hou, G., Ye, Z., & Ye, M. (2019) · Journal of Cellular Physiology · doi:10.1002/jcp.28202 · Cited by 20

Transcriptional Subtypes Resolve Tumor Heterogeneity and Identify Vulnerabilities to MEK Inhibition in Lung Adenocarcinoma

Daemen, A., Cooper, J. E., Myrta, S., Wongchenko, M. J., Lin, E., Long, J. E., Foreman, O., Modrusan, Z. D., Tremayne, J. R., de la Cruz, C. C., et al. (2020) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-20-1835 · Cited by 20

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

Simultaneous targeting PI3K and PERK pathways promotes cell death and improves the clinical prognosis in esophageal squamous carcinoma

Wang, S., Wang, X., Zheng, K., Liu, K., Wang, S., & Xie, C. (2017) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2017.08.156 · Cited by 19

Combination therapy of melanoma using kinase inhibitors

Heppt, M. V., Tietze, J. K., Graf, S. A., & Berking, C. (2015) · Current Opinion in Oncology · doi:10.1097/cco.0000000000000160 · Cited by 20

Phosphoinositide 3-kinase α inhibitors: a patent review

Denny, W. A. (2013) · Expert Opinion on Therapeutic Patents · doi:10.1517/13543776.2013.779673 · Cited by 19

Cobimetinib Alone and Plus Venetoclax With/Without Atezolizumab in Patients With Relapsed/Refractory Multiple Myeloma

Schjesvold, F. H., Paiva, B., Ribrag, V., Rodríguez‐Otero, P., Miguel, J. F. S., Robak, P. J., Hansson, M., Onishi, M., Hamidi, H., Malhi, V., et al. (2022) · Clinical Lymphoma Myeloma & Leukemia · doi:10.1016/j.clml.2022.10.006 · Cited by 18

Advancements in dual-target inhibitors of PI3K for tumor therapy: Clinical progress, development strategies, prospects

Hu, J., Fu, S., Zhan, Z., & Zhang, J. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.116109 · Cited by 19

Combinatorial drug screening and molecular profiling reveal diverse mechanisms of intrinsic and adaptive resistance to BRAF inhibition in V600E BRAF mutant melanomas

Roller, D. G., Capaldo, B. J., Bekiranov, S., Mackey, A. J., Conaway, M. R., Petricoin, E. F., Gioeli, D. G., & Weber, M. J. (2015) · Oncotarget · doi:10.18632/oncotarget.6548 · Cited by 18

A Novel Combination Treatment Targeting BCL-XL and MCL1 for KRAS/BRAF -mutated and BCL2L1 -amplified Colorectal Cancers

Cho, S., Han, J. Y., Na, D., Kang, W., Lee, A., Kim, J., Lee, J. L., Min, S., Kang, J., Chae, J., et al. (2017) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-16-0735 · Cited by 18

Prospects for MEK inhibitors for treating cancer

Martín-Liberal, J., Lagares‐Tena, L., & Larkin, J. (2014) · Expert Opinion on Drug Safety · doi:10.1517/14740338.2014.892578 · Cited by 18

Radiotherapy with BRAF Inhibitor Therapy for Melanoma: Progress and Possibilities

Zahnreich, S., Mayer, A., Loquai, C., Grabbe, S., & Schmidberger, H. (2015) · Future Oncology · doi:10.2217/fon.15.297 · Cited by 17

Therapeutic Targeting of Cancer Stem Cells Prevents Resistance of Colorectal Cancer Cells to MEK Inhibition

Lamichhane, A., Thakuri, P. S., Singh, S. K., Nejad, P. R., Heiss, J., Luker, G. D., & Tavana, H. (2022) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.1c00257 · Cited by 17

Immunoaffinity Enrichment Coupled to Quantitative Mass Spectrometry Reveals Ubiquitin-Mediated Signaling Events

Yu, K., Phu, L., Varfolomeev, E. E., Bustos, D. J., Vucic, D., & Kirkpatrick, D. S. (2015) · Journal of Molecular Biology · doi:10.1016/j.jmb.2015.03.018 · Cited by 17

Customizing the Therapeutic Response of Signaling Networks to Promote Antitumor Responses by Drug Combinations

Goltsov, A., Langdon, S. P., Goltsov, G., Harrison, D. J., & Bown, J. (2014) · Frontiers in Oncology · doi:10.3389/fonc.2014.00013 · Cited by 16

Bilateral blockade of MEK- and PI3K-mediated pathways downstream of mutant KRAS as a treatment approach for peritoneal mucinous malignancies

Kuracha, M. R., Thomas, P., Loggie, B. W., & Govindarajan, V. (2017) · PLoS ONE · doi:10.1371/journal.pone.0179510 · Cited by 16

Intermittent Versus Continuous Dosing of MAPK Inhibitors in the Treatment of BRAF-Mutated Melanoma

de Moura, C. R., Vercellino, L., Jouenne, F., Baroudjian, B., Sadoux, A., Louveau, B., Delyon, J., Serror, K., Goldwirt, L., Merlet, P., et al. (2019) · Translational Oncology · doi:10.1016/j.tranon.2019.10.003 · Cited by 16

Cobimetinib (GDC-0973, XL518)

Andrlová, H., Zeiser, R., & Meiß, F. (2018) · Recent results in cancer research/Recent Results in Cancer Research · doi:10.1007/978-3-319-91442-8_12 · Cited by 16

Vemurafenib Plus Cobimetinib in the Treatment of Mutated Metastatic Melanoma: The CoBRIM Trial

Grimaldi, A. M., Simeone, E., & Ascierto, P. A. (2015) · Melanoma Management · doi:10.2217/mmt.15.22 · Cited by 15

Discovery of 2-(aminopyrimidin-5-yl)-4-(morpholin-4-yl)-6- Substituted Triazine as PI3K and BRAF Dual Inhibitor

Wang, H., Shen, Y. H., Zhang, H., Hei, Y., Zhao, H., Xin, M., Lu, S., & Zhang, S. (2018) · Future Medicinal Chemistry · doi:10.4155/fmc-2018-0145 · Cited by 15

Bcl-xl and Mcl-1 are the major determinants of the apoptotic response to dual PI3K and MEK blockage

Jokinen, E., & Koivunen, J. P. (2015) · International Journal of Oncology · doi:10.3892/ijo.2015.3071 · Cited by 16

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

Konopleva, M. Y., Dail, M., Daver, N. G., Garcia, J. S., Jonas, B. A., Yee, K. W. L., Kelly, K. R., Vey, N., Assouline, S. E., Roboz, G. J., et al. (2024) · Clinical Lymphoma Myeloma & Leukemia · doi:10.1016/j.clml.2024.01.007 · Cited by 14

Drugs That Inhibit Signaling Pathways for Tumor Cell Growth and Proliferation

Avendaño, C., & Menéndez, J. C. (2015) · Elsevier eBooks · doi:10.1016/b978-0-444-62649-3.00010-7 · Cited by 14

New RAF kinase inhibitors in cancer therapy

Martín-Liberal, J., & Larkin, J. (2014) · Expert Opinion on Pharmacotherapy · doi:10.1517/14656566.2014.911286 · Cited by 14

MEK Inhibition Induces Canonical WNT Signaling through YAP in KRAS Mutated HCT-15 Cells, and a Cancer Preventive FOXO3/FOXM1 Ratio in Combination with TNKS Inhibition

Solberg, N. T., Melheim, M., Strand, M. F., Olsen, P. A., & Krauss, S. J. K. (2019) · Cancers · doi:10.3390/cancers11020164 · Cited by 14

Emerging Therapies in the Treatment of Advanced Melanoma

Massand, S., & Neves, R. I. (2021) · Clinics in Plastic Surgery · doi:10.1016/j.cps.2021.06.008 · Cited by 13

The Enhanced In Vivo Activity of the Combination of a MEK and a PI3K Inhibitor Correlates with [18F]-FLT PET in Human Colorectal Cancer Xenograft Tumour-Bearing Mice

Haagensen, E. J., Thomas, H. D., Wilson, I., Harnor, S. J., Payne, S. L., Rennison, T., Smith, K. M., Maxwell, R. J., & Newell, D. R. (2013) · PLoS ONE · doi:10.1371/journal.pone.0081763 · Cited by 13

Structure-Guided Design and Initial Studies of a Bifunctional MEK/PI3K Inhibitor (ST-168)

Dort, M. E. V., Galbán, S., Nino, C. A., Hong, H., Apfelbaum, A. A., Luker, G. D., Thurber, G. M., Atangcho, L., Besirli, C. G., & Ross, B. D. (2017) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.7b00111 · Cited by 13

Potential benefit of treatment with MEK inhibitors and chemotherapy in BRAF-mutated KRAS wild-type pancreatic ductal adenocarcinoma patients: a case reportPreprint

Ardalan, B., Azqueta, J. I., England, J. S., & Eatz, T. A. (2021) · Molecular Case Studies · doi:10.1101/mcs.a006108 · Cited by 13

Synergistic Inhibition of Kinase Pathways Overcomes Resistance of Colorectal Cancer Spheroids to Cyclic Targeted Therapies

Thakuri, P. S., Gupta, M., Joshi, R., Singh, S. K., & Tavana, H. (2019) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.9b00042 · Cited by 12

Pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione derivatives as RAF-MEK-ERK pathway signaling pathway blockers: Synthesis, cytotoxic activity, mechanistic investigation and structure-activity relationships

Xie, Q., Shen, Y., Meng, Y., Liang, J., Xu, J., Liang, S., Liu, X., Wang, Y., & Hu, C. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114579 · Cited by 11

Fibroblast growth factor receptor 1 inhibition suppresses pancreatic cancer chemoresistance and chemotherapy-driven aggressiveness

Lin, Q., Serratore, A., Niu, J., Shen, S., Chaudhuri, T. R., Ma, W. W., Qu, J., Kandel, E., & Straubinger, R. M. (2024) · Drug Resistance Updates · doi:10.1016/j.drup.2024.101064 · Cited by 12

Approach in Improving Potency and Selectivity of Kinase Inhibitors: Allosteric Kinase Inhibitors

Wei, S., Zhao, T., Wang, J., & Zhai, X. (2020) · Mini-Reviews in Medicinal Chemistry · doi:10.2174/1389557521666201222144355 · Cited by 12

Combinatorial Therapies to Overcome BRAF/MEK Inhibitors Resistance in Melanoma Cells: An in vitro Study

Pópulo, H., Domingues, B., Sampaio, C., Lopes, J. M., & Soares, P. (2021) · Journal of Experimental Pharmacology · doi:10.2147/jep.s297831 · Cited by 11

Dissection of Kinase Isoforms through Orthogonal and Chemical Inducible Signaling Cascades

Zheng, S., Fan, X., Wang, J., Zhao, J.-Y., & Chen, P. R. (2017) · ChemBioChem · doi:10.1002/cbic.201700255 · Cited by 11

MEK1/2 as a Therapeutic Target in Sickle Cell Disease

Zennadi, R. (2019) · International Journal of Blood Research and Disorders · doi:10.23937/2469-5696/1410038 · Cited by 10

Therapeutic potential of trametinib to inhibit the mutagenesis by inactivating the protein kinase pathway in non-small cell lung cancer

Jeanson, A., Boyer, A., Greillier, L., Tomasini, P., & Barlési, F. (2018) · Expert Review of Anticancer Therapy · doi:10.1080/14737140.2019.1554440 · Cited by 9

Drug Combinatorial Therapies for the Treatment of KRAS Mutated Lung Cancers

He, H., Xu, C., Cheng, Z., Qian, X., & Zheng, L. (2019) · Current Topics in Medicinal Chemistry · doi:10.2174/1568026619666190902150555 · Cited by 10

Modeling Adaptive Resistance of KRAS Mutant Colorectal Cancer to MAPK Pathway Inhibitors with a Three-Dimensional Tumor Model

Thakuri, P. S., Lamichhane, A., Singh, S. K., Gupta, M., Luker, G. D., & Tavana, H. (2020) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.0c00115 · Cited by 11

A Perspective Study on the RTK, PI3K, B‐Raf, CDK and the Multi‐Protein Targeting in Medicinal Chemistry

Mohamed, A. R., & Kerdawy, A. M. E. (2022) · Chemistry & Biodiversity · doi:10.1002/cbdv.202200328 · Cited by 9

Enhanced anti-tumour activity of the combination of the novel MEK inhibitor WX-554 and the novel PI3K inhibitor WX-037

Haagensen, E. J., Thomas, H. D., Schmalix, W. A., Payne, A. C., Kevorkian, L., Allen, R. A., Bevan, P., Maxwell, R. J., & Newell, D. R. (2016) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-016-3186-4 · Cited by 9

High-throughput ex vivo drug testing identifies potential drugs and drug combinations for NRAS-positive malignant melanoma

Kohtamäki, L. M., Arjama, M., Mäkelä, S., Ianevski, P., Välimäki, K. E., Juteau, S., Ilmonen, S., Ungureanu, D., Kallioniemi, O., Murumägi, A., et al. (2021) · Translational Oncology · doi:10.1016/j.tranon.2021.101290 · Cited by 8

Activity and Selectivity of Novel Chemical Metallic Complexes with Potential Anticancer Effects on Melanoma Cells

Ciardulli, M. C., Mariconda, A., Sirignano, M., Lamparelli, E. P., Longo, R., Scala, P., D’Auria, R., Santoro, A., Guadagno, L., Porta, G. D., et al. (2023) · Molecules · doi:10.3390/molecules28124851 · Cited by 8

Establishment of a BRAF V595E ‐mutant canine prostate cancer cell line and the antitumor effects of MEK inhibitors against canine prostate cancer

Kobayashi, M., Onozawa, M., Watanabe, S., Nagashima, T., Tamura, K., Kubo, Y., Ikeda, A., Ochiai, K., Michishita, M., Bonkobara, M., et al. (2023) · Veterinary and Comparative Oncology · doi:10.1111/vco.12879 · Cited by 9

Inhibiting BRAF/EGFR/MEK suppresses cancer stemness and drug resistance of primary colorectal cancer cells

Lamichhane, A., Luker, G. D., Agarwal, S., & Tavana, H. (2023) · Oncotarget · doi:10.18632/oncotarget.28517 · Cited by 7

Intermittent MEK Inhibition with GITR Costimulation Rescues T-cell Function for Increased Efficacy with CTLA-4 Blockade in Solid Tumor Models

Dong, L., Choi, H., Budhu, S., Schulze, I., Verma, S., Mangarin, L. M. B., Navarro, V. E., Mehanna, N., Khan, J. F., Venkatesh, D., et al. (2024) · Cancer Immunology Research · doi:10.1158/2326-6066.cir-23-0729 · Cited by 7

Translating Genomic Profiling to Gastrointestinal Cancer Treatment

Harada, K., Kaya, D. M., Shimodaira, Y., Song, S., Baba, H., & Ajani, J. A. (2017) · Future Oncology · doi:10.2217/fon-2016-0422 · Cited by 7

An overview of recent advancements in small molecules suppression of oncogenic signaling of K-RAS: an updated review

Sabt, A., Tawfik, H. O., Khaleel, E. F., Badi, R. M., Ibrahim, H. A. A., Elkaeed, E. B., & Eldehna, W. M. (2024) · Molecular Diversity · doi:10.1007/s11030-023-10777-6 · Cited by 8

PI3 Kinase in Cancer: From Biology to Clinic

Workman, P., & Clarke, P. (2012) · American Society of Clinical Oncology Educational Book · doi:10.14694/edbook_am.2012.32.89 · Cited by 7

In vitro long-term treatment with MAPK inhibitors induces melanoma cells with resistance plasticity to inhibitors while retaining sensitivity to CD8 T cells

Rowdo, F. P. M., Barón, A., von Euw, E. M., & Mordoh, J. (2017) · Oncology Reports · doi:10.3892/or.2017.5363 · Cited by 7

Targeted therapy sensitivity and resistance in solid malignancies

Jokinen, E. (2014) · Cited by 6

The antiviral effects of a MEK1/2 inhibitor promote tumor regression in a preclinical model of human papillomavirus infection-induced tumorigenesis

Luna, A. J., Young, J. M., Sterk, R. T., Bondu, V., Schultz, F. A., Kusewitt, D. F., Kang, H., & Ozbun, M. A. (2023) · Antiviral Research · doi:10.1016/j.antiviral.2023.105667 · Cited by 6

Towards Targeting Endothelial Rap1B to Overcome Vascular Immunosuppression in Cancer

Nakhchi, B. G., Kosuru, R., & Chrzanowska‐Wodnicka, M. (2024) · International Journal of Molecular Sciences · doi:10.3390/ijms25189853 · Cited by 7

Abstract A250: Preclinical combination efficacy and identification of biomarkers of MEK and PI3K inhibitors in phase I

Hoeflich, K. P., Merchant, M. A., Otter, D. D., Chan, J., Chan, E. W., Orr, C., Friedman, L. S., Chan, I. T., Prescott, J., Berry, L., et al. (2009) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.targ-09-a250 · Cited by 1

PK-PD modeling of combination efficacy effect from administration of the MEK inhibitor GDC-0973 and PI3K inhibitor GDC-0941 in A2058 xenografts

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

Abstract 873: Combined targeting of Akt and MEK with the Akt inhibitor GDC-0068 and MEK inhibitor GDC-0973 demonstrates synergistic anti-tumor effects

Nannini, M., Hong, R., Lee, B. B., Arrazate, A., Kassees, R., Lin, J., Degtyarev, M. Y., Sampath, D., & Lin, K. (2012) · Cancer Research · doi:10.1158/1538-7445.am2012-873 · Cited by 2

The synergistic interaction of MEK and PI3K inhibitors is modulated by mTOR inhibition

Haagensen, E. J., Kyle, S., Beale, G., Maxwell, R. J., & Newell, D. R. (2012) · British Journal of Cancer · doi:10.1038/bjc.2012.70 · Cited by 80

Synergistic effects of multi-level targeting of the MAPK and PI3-kinase pathways in breast cancer cells.

Mirzoeva, O. K., Gendelman, R., Knight, Z. A., Neve, R. M., Feiler, H. S., Han, J., Kuo, W., Bayani, N., Siwak, D. R., Mills, G. B., et al. (2007) · Molecular Cancer Therapeutics