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

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 · see citing works

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

Chou, T.-C., & Talalay, P. (1984) · Advances in Enzyme Regulation · doi:10.1016/0065-2571(84)90007-4 · Cited by 7,178 · see citing works

AKT/PKB signaling: navigating downstream

Manning, B. D., & Cantley, L. C. (2007) · Cell · doi:10.1016/j.cell.2007.06.009 · Cited by 6,115 · see citing works

Targeting RAS signalling pathways in cancer therapy

Downward, J. (2003) · Nature reviews. Cancer · doi:10.1038/nrc969 · Cited by 3,262 · see citing works

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 · see citing works

Targeting the phosphoinositide 3-kinase pathway in cancer

Liu, P., Cheng, H.-L. M., Roberts, T. M., & Zhao, J. J. (2009) · Nature Reviews Drug Discovery · doi:10.1038/nrd2926 · Cited by 2,722 · see citing works

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

McCubrey, J. A., Steelman, L. S., Chappell, W. H., Abrams, S. L., Wong, E. W. T., Chang, F., Lehmann, B. D., Terrian, D. M., Milella, M., Tafuri, A., et al. (2006) · Biochimica et Biophysica Acta (BBA) - Molecular Cell Research · doi:10.1016/j.bbamcr.2006.10.001 · Cited by 2,285 · see citing works

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

Engelman, J. A., Chen, L., Tan, X., Crosby, K., Guimaraes, A. R., Upadhyay, R., Maira, M., McNamara, K., Perera, S. A., Song, Y., et al. (2008) · Nature Medicine · doi:10.1038/nm.1890 · Cited by 1,330 · see citing works

BRAF mutation predicts sensitivity to MEK inhibition

Solit, D. B., Garraway, L. A., Pratilas, C. A., Sawai, A., Getz, G. A., Basso, A., Ye, Q., Lobo, J. M., She, Y., Osman, I., et al. (2005) · Nature · doi:10.1038/nature04304 · Cited by 1,329 · see citing works

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

Bamford, S., Dawson, E., Forbes, S. A., Clements, J., Pettett, R., Doǧan, A., Flanagan, A. M., Teague, J. W., Futreal, P. A., Stratton, M. R., et al. (2004) · British Journal of Cancer · doi:10.1038/sj.bjc.6601894 · Cited by 1,248 · see citing works

The RAF proteins take centre stage

Wellbrock, C., Karasarides, M., & Marais, R. (2004) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm1498 · Cited by 1,233 · see citing works

Bim: a novel member of the Bcl‐2 family that promotes apoptosis

O’Connor, L., Strasser, A., O’Reilly, L. A., Hausmann, G., Adams, J. M., Cory, S., & Huang, D. C. S. (1998) · The EMBO Journal · doi:10.1093/emboj/17.2.384 · Cited by 1,163 · see citing works

The Identification of 2-(1 H -Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2- d ]pyrimidine (GDC-0941) as a Potent, Selective, Orally Bioavailable Inhibitor of Class I PI3 Kinase for the Treatment of Cancer

Folkes, A. J., Ahmadi, K., ALDERTON, W. K., Alix, S., Baker, S. J., Box, G., Chuckowree, I., Clarke, P. A., Depledge, P., Eccles, S. A., et al. (2008) · Journal of Medicinal Chemistry · doi:10.1021/jm800295d · Cited by 756 · see citing works

The PIK3CA gene is mutated with high frequency in human breast cancers

Bachman, K. E., Argani, P., Samuels, Y., Silliman, N., Ptak, J., Szabo, S., Konishi, H., Karakas, B., Blair, B. G., Lin, C., et al. (2004) · Cancer Biology & Therapy · doi:10.4161/cbt.3.8.994 · Cited by 665 · see citing works

Oncogenic Mutations of PIK3CA in Human Cancers

Samuels, Y., & Velculescu, V. E. (2004) · Cell Cycle · doi:10.4161/cc.3.10.1164 · Cited by 539 · see citing works

Mutation of the PIK3CA oncogene in human cancers

Karakas, B., Bachman, K. E., & Park, B. H. (2006) · British Journal of Cancer · doi:10.1038/sj.bjc.6602970 · Cited by 505 · see citing works

In vivo Antitumor Activity of MEK and Phosphatidylinositol 3-Kinase Inhibitors in Basal-Like Breast Cancer Models

Hoeflich, K. P., O'Brien, C. L., Boyd, Z. S., Cavet, G., Guerrero, S., Jung, K., Januario, T., Savage, H. M., Punnoose, E. A., Truong, T., et al. (2009) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-09-0317 · Cited by 467 · see citing works

4E-BP1 Is a Key Effector of the Oncogenic Activation of the AKT and ERK Signaling Pathways that Integrates Their Function in Tumors

She, Q.-B., Halilovic, E., Ye, Q., Zhen, W., Shirasawa, S., Sasazuki, T., Solit, D. B., & Rosen, N. (2010) · Cancer Cell · doi:10.1016/j.ccr.2010.05.023 · Cited by 400 · see citing works

Basal Subtype and MAPK/ERK Kinase (MEK)-Phosphoinositide 3-Kinase Feedback Signaling Determine Susceptibility of Breast Cancer Cells to MEK Inhibition

Mirzoeva, O. K., Das, D., Heiser, L. M., Bhattacharya, S., Siwak, D. R., Gendelman, R., Bayani, N., Wang, N. J., Neve, R. M., Guan, Y., et al. (2009) · Cancer Research · doi:10.1158/0008-5472.can-08-3389 · Cited by 387 · see citing works

Strategies for optimizing combinations of molecularly targeted anticancer agents

Dancey, J. E., & Chen, H. X. (2006) · Nature Reviews Drug Discovery · doi:10.1038/nrd2089 · Cited by 368 · see citing works

Pharmacokinetic variability of anticancer agents

Undevia, S. D., Gomez-Abuin, G., & Ratain, M. J. (2005) · Nature reviews. Cancer · doi:10.1038/nrc1629 · Cited by 261 · see citing works

Predictive Biomarkers of Sensitivity to the Phosphatidylinositol 3′ Kinase Inhibitor GDC-0941 in Breast Cancer Preclinical Models

O'Brien, C. L., Wallin, J. J., Sampath, D., GuhaThakurta, D., Savage, H. M., Punnoose, E. A., Guan, J., Berry, L., Prior, W. W., Amler, L. C., et al. (2010) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-09-2828 · Cited by 256 · see citing works

Identifying genotype-dependent efficacy of single and combined PI3K- and MAPK-pathway inhibition in cancer

Sos, M. L., Fischer, S., Ullrich, R. T., Peifer, M., Heuckmann, J. M., Koker, M., Heynck, S., Stückrath, I., Weiss, J. M., Fischer, F., et al. (2009) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0907325106 · Cited by 255 · see citing works

Utilizing targeted cancer therapeutic agents in combination: novel approaches and urgent requirements

Kummar, S., Chen, H. X., Wright, J., Holbeck, S. L., Millin, M. D., Tomaszewski, J. E., Zweibel, J., Collins, J. M., & Doroshow, J. H. (2010) · Nature Reviews Drug Discovery · doi:10.1038/nrd3216 · Cited by 249 · see citing works

From basic research to clinical development of MEK1/2 inhibitors for cancer therapy

Frémin, C., & Meloche, S. (2010) · Journal of Hematology & Oncology · doi:10.1186/1756-8722-3-8 · Cited by 244 · see citing works

Treatment of B-RAF mutant human tumor cells with a MEK inhibitor requires Bim and is enhanced by a BH3 mimetic

Cragg, M. S., Jansen, E. S., Cook, M., Harris, C., Strasser, A., & Scott, C. L. (2008) · Journal of Clinical Investigation · doi:10.1172/jci35437 · Cited by 207 · see citing works

BRAF Signaling and Targeted Therapies in Melanoma

Dhomen, N. S., & Marais, R. (2009) · Hematology/Oncology Clinics of North America · doi:10.1016/j.hoc.2009.04.001 · Cited by 196 · see citing works

Antitumor Efficacy of the Novel RAF Inhibitor GDC-0879 Is Predicted by BRAFV600E Mutational Status and Sustained Extracellular Signal-Regulated Kinase/Mitogen-Activated Protein Kinase Pathway Suppression

Hoeflich, K. P., Herter, S., Tien, J., Wong, L. L.-Y., Berry, L., Chan, J., O'Brien, C. L., Modrusan, Z. D., Seshagiri, S., Lackner, M. R., et al. (2009) · Cancer Research · doi:10.1158/0008-5472.can-08-3563 · Cited by 175 · see citing works

Bim and Bmf in tissue homeostasis and malignant disease

Hofbauer, J. P., Labi, V., Egle, A., & Villunger, A. (2008) · Oncogene · doi:10.1038/onc.2009.42 · Cited by 149 · see citing works

Therapeutic Potential of Phosphoinositide 3-Kinase Inhibitors

Ward, S. G., Sotsios, Y., Dowden, J., Bruce, I., & Finan, P. M. (2003) · Chemistry & Biology · doi:10.1016/s1074-5521(03)00048-6 · Cited by 124 · see citing works

Pharmacokinetic-Pharmacodynamic Modeling of Tumor Growth Inhibition and Biomarker Modulation by the Novel Phosphatidylinositol 3-Kinase Inhibitor GDC-0941

Salphati, L., Wong, H., Belvin, M. P., Bradford, D., Edgar, K. A., Prior, W. W., Sampath, D., & Wallin, J. J. (2010) · Drug Metabolism and Disposition · doi:10.1124/dmd.110.032912 · Cited by 84 · see citing works

Development of Phosphoinositide-3 Kinase Pathway Inhibitors for Advanced Cancer

Cleary, J. M., & Shapiro, G. I. (2010) · Current Oncology Reports · doi:10.1007/s11912-010-0091-6 · Cited by 63 · see citing works

The role of phosphoinositide 3-kinase in human disease.

Cantley, L. C. (2006) · PubMed · Cited by 22 · see citing works

Preclinical disposition and pharmacokinetics-pharmacodynamic modeling of biomarker response and tumour growth inhibition in xenograft mouse models of G-573, a MEK inhibitor

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

Inducible BRAF Suppression Models for Melanoma Tumorigenesis

Hoeflich, K. P., Jaiswal, B. S., Davis, D. P., & Seshagiri, S. (2008) · Methods in enzymology on CD-ROM/Methods in enzymology · doi:10.1016/s0076-6879(07)00403-x · Cited by 11 · see citing works

Next Generation of Fluorine-Containing Pharmaceuticals, Compounds Currently in Phase II–III Clinical Trials of Major Pharmaceutical Companies: New Structural Trends and Therapeutic Areas

Zhou, Y., Wang, J., Gu, Z., Wang, S., Zhu, W., Aceña, J. L., Soloshonok, V. A., Izawa, K., & Liu, H. (2016) · Chemical Reviews · doi:10.1021/acs.chemrev.5b00392 · Cited by 2,824 · see citing works

Combined Vemurafenib and Cobimetinib in BRAF -Mutated Melanoma

Larkin, J., Ascierto, P. A., Dréno, B., Atkinson, V. G., Liszkay, G., Maio, M., Mandalà, M., Демидов, Л. В., Stroyakovskiy, D., Thomas, L., et al. (2014) · New England Journal of Medicine · doi:10.1056/nejmoa1408868 · Cited by 2,061 · see citing works

PI3K/AKT signaling pathway and cancer: an updated review

Martini, M., Santis, M. C. D., Braccini, L., Gulluni, F., & Hirsch, E. (2014) · Annals of Medicine · doi:10.3109/07853890.2014.912836 · Cited by 1,176 · see citing works

RAS-targeted therapies: is the undruggable drugged?

Moore, A. R., Rosenberg, S. C., McCormick, F., & Malek, S. (2020) · Nature Reviews Drug Discovery · doi:10.1038/s41573-020-0068-6 · Cited by 1,103 · see citing works

The Genetic Landscape of Clinical Resistance to RAF Inhibition in Metastatic Melanoma

Allen, E. M. V., Wagle, N., Sucker, A., Treacy, D. J., Johannessen, C. M., Goetz, E. M., Place, C. S., Taylor-Weiner, A. N., Whittaker, S. R., Kryukov, G. V., et al. (2013) · Cancer Discovery · doi:10.1158/2159-8290.cd-13-0617 · Cited by 904 · see citing works

MAP Kinase Inhibition Promotes T Cell and Anti-tumor Activity in Combination with PD-L1 Checkpoint Blockade.

Ebert, P. J. R., Cheung, J., Yang, Y., McNamara, E., Hong, R., Moskalenko, M., Gould, S. E., Maecker, H., Irving, B. A., Kim, J. M., et al. (2016) · Immunity · doi:10.1016/j.immuni.2016.01.024 · Cited by 713 · see citing works

Melanoma treatment in review

Domingues, B., Lopes, J. M., Soares, P., & Pópulo, H. (2018) · ImmunoTargets and Therapy · doi:10.2147/itt.s134842 · Cited by 701 · see citing works

A comprehensive transcriptional portrait of human cancer cell lines

Klijn, C. N., Durinck, S., Stawiski, E. W., Haverty, P. M., Jiang, Z., Liu, H., Degenhardt, J. D., Mayba, O., Gnad, F., Liu, J., et al. (2014) · Nature Biotechnology · doi:10.1038/nbt.3080 · Cited by 650 · see citing works

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 · see citing works

Drug resistance and new therapies in colorectal cancer

Jeught, K. V. D., Xu, H.-C., Li, Y.-J., Lu, X.-B., & Ji, G. (2018) · World Journal of Gastroenterology · doi:10.3748/wjg.v24.i34.3834 · Cited by 597 · see citing works

Mechanisms of resistance to EGFR tyrosine kinase inhibitors

Huang, L., & Fu, L. (2015) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2015.07.001 · Cited by 596 · see citing works

Role of oncogenic KRAS in the prognosis, diagnosis and treatment of colorectal cancer

Zhu, G., Pei, L., Xia, H., Tang, Q., & Bi, F. (2021) · Molecular Cancer · doi:10.1186/s12943-021-01441-4 · Cited by 482 · see citing works

Targeting cancer with kinase inhibitors

Gross, S. D., Rahal, R., Stransky, N., Lengauer, C., & Hoeflich, K. P. (2015) · Journal of Clinical Investigation · doi:10.1172/jci76094 · Cited by 442 · see citing works

Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

Xie, X., Yu, T., Li, X., Zhang, N., Foster, L. J., Peng, C., Huang, W., & He, G. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01589-z · Cited by 396 · 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 323 · see citing works

A Novel Tankyrase Small-Molecule Inhibitor Suppresses <i>APC</i> Mutation–Driven Colorectal Tumor Growth

Lau, T., Chan, E., Callow, M., Waaler, J., Boggs, J., Blake, R. A., Magnuson, S., Sambrone, A., Schutten, M., Firestein, R., et al. (2013) · Cancer Research · doi:10.1158/0008-5472.can-12-4562 · Cited by 316 · see citing works

Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR Cascade Inhibitors: How Mutations Can Result in Therapy Resistance and How to Overcome Resistance

McCubrey, J. A., Steelman, L. S., Chappell, W. H., Abrams, S. L., Franklin, R. A., Montalto, G., Cervello, M., Libra, M., Candido, S., Malaponte, G., et al. (2012) · Oncotarget · doi:10.18632/oncotarget.659 · Cited by 313 · 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

MEK and the inhibitors: from bench to bedside

Akinleye, A., Furqan, M., Mukhi, N., Ravella, P., & Liu, D. (2013) · Journal of Hematology &amp; Oncology · doi:10.1186/1756-8722-6-27 · Cited by 291 · see citing works

PI3K Inhibitors in Cancer: Clinical Implications and Adverse Effects

Mishra, R., Patel, H. M., Alanazi, S., Kilroy, M. K., & Garrett, J. T. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms22073464 · Cited by 292 · see citing works

Mechanism-based cancer therapy: resistance to therapy, therapy for resistance

Ramos, P. M., & Bentires‐Alj, M. (2014) · Oncogene · doi:10.1038/onc.2014.314 · Cited by 276 · see citing works

MEK in cancer and cancer therapy.

Neuzillet, C., Tijeras-Raballand, A., de Mestier, L., Cros, J., Faivre, S., & Raymond, E. (2014) · Pharmacology and Therapeutics · doi:10.1016/j.pharmthera.2013.10.001 · Cited by 266 · see citing works

Challenges for the Clinical Development of PI3K Inhibitors: Strategies to Improve Their Impact in Solid Tumors

Hanker, A. B., Kaklamani, V., & Arteaga, C. L. (2019) · Cancer Discovery · doi:10.1158/2159-8290.cd-18-1175 · Cited by 256 · see citing works

Targeted therapy in cancer

Tsimberidou, A. M. (2015) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-015-2861-1 · Cited by 255 · see citing works

PI3K regulates MEK/ERK signaling in breast cancer via the Rac-GEF, P-Rex1

Ebi, H., Costa, C., Faber, A. C., Nishtala, M. V., Kotani, H., Juric, D., Pelle, P. D., Song, Y., Yano, S., Mino-Kenudson, M. A., et al. (2013) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1314124110 · Cited by 209 · see citing works

Time-resolved protein activation by proximal decaging in living systems

Wang, J., Liu, Y., Liu, Y., Zheng, S., Wang, X., Zhao, J., Yang, F., Zhang, G., Wang, C., & Chen, P. R. (2019) · Nature · doi:10.1038/s41586-019-1188-1 · Cited by 202 · see citing works

Strategies for co-targeting the PI3K/AKT/mTOR pathway in NSCLC

Heavey, S., O'Byrne, K. J., & Gately, K. A. (2013) · Cancer Treatment Reviews · doi:10.1016/j.ctrv.2013.08.006 · Cited by 177 · see citing works

Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973)

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

Complementary activity of tyrosine kinase inhibitors against secondary kit mutations in imatinib-resistant gastrointestinal stromal tumours

Serrano, C., Mariño‐Enríquez, A., Tao, D. L., Ketzer, J., Eilers, G., Zhu, M. J., Yu, C., Mannan, A. M., Rubin, B. P., Demetri, G. D., et al. (2019) · British Journal of Cancer · doi:10.1038/s41416-019-0389-6 · Cited by 168 · see citing works

Synthetic Approaches to the New Drugs Approved During 2015.

Flick, A. C., Ding, H. X., Leverett, C., Kyne, R. E., Liu, K., Fink, S. J., & O'Donnell, C. J. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b00010 · Cited by 113 · see citing works

Small Molecule Kinase Inhibitors for the Treatment of Brain Cancer

Heffron, T. P. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b00618 · Cited by 141 · see citing works

BRAF and MEK Inhibitors: Use and Resistance in BRAF-Mutated Cancers

Sanchez, J., Wang, T., & Cohen, M. S. (2018) · Drugs · doi:10.1007/s40265-018-0884-8 · Cited by 141 · see citing works

PI3K inhibition reduces mammary tumor growth and facilitates antitumor immunity and anti-PD1 responses

Sai, J., Owens, P., Novitskiy, S. V., Hawkins, O. E., Vilgelm, A. E., Yang, J., Sobolik, T., Lavender, N., Johnson, A. C., McClain, C., et al. (2017) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-16-2142 · Cited by 138 · see citing works

Reversal of Lactate and PD-1–mediated Macrophage Immunosuppression Controls Growth of PTEN/p53-deficient Prostate Cancer

Chaudagar, K. K., Hieromnimon, H. M., Khurana, R., Labadie, B. W., Hirz, T., Mei, S., Hasan, R., Shafran, J. S., Kelley, A., Apostolov, E., et al. (2023) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-22-3350 · Cited by 137 · see citing works

Current State and Future Challenges for PI3K Inhibitors in Cancer Therapy

Sirico, M., D’Angelo, A., Gianni, C., Casadei, C., Merloni, F., & De Giorgi, U. (2023) · Cancers · doi:10.3390/cancers15030703 · Cited by 121 · see citing works

Targeting Mutant KRAS for Anticancer Therapeutics: A Review of Novel Small Molecule Modulators

Wang, Y., Kaiser, C. E., Frett, B., & Li, H. (2013) · Journal of Medicinal Chemistry · doi:10.1021/jm3017706 · Cited by 121 · see citing works

Allosteric MEK1/2 inhibitors including cobimetanib and trametinib in the treatment of cutaneous melanomas.

Roskoski, R. (2017) · Pharmacological Research · doi:10.1016/j.phrs.2016.12.009 · Cited by 113 · see citing works

Dual Inhibition of MEK and PI3K Pathway in KRAS and BRAF Mutated Colorectal Cancers

Temraz, S., Mukherji, D., & Shamseddine, A. (2015) · International Journal of Molecular Sciences · doi:10.3390/ijms160922976 · Cited by 117 · see citing works

MEK and PI3K inhibition in solid tumors: rationale and evidence to date

Jokinen, E., & Koivunen, J. P. (2015) · Therapeutic Advances in Medical Oncology · doi:10.1177/1758834015571111 · Cited by 116 · see citing works

Immunomodulatory Properties of PI3K/AKT/mTOR and MAPK/MEK/ERK Inhibition Augment Response to Immune Checkpoint Blockade in Melanoma and Triple-Negative Breast Cancer

Zhang, Z., Richmond, A. J., & Yan, C. W. (2022) · International Journal of Molecular Sciences · doi:10.3390/ijms23137353 · Cited by 105 · see citing works

Navigating the Therapeutic Complexity of PI3K Pathway Inhibition in Melanoma

Kwong, L. N., & Davies, M. A. (2013) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-13-0142 · Cited by 103 · see citing works

MEK1 Is Required for PTEN Membrane Recruitment, AKT Regulation, and the Maintenance of Peripheral Tolerance

Zmajkovicova, K., Jesenberger, V., Catalanotti, F., Baumgärtner, C., Reyes, G. X., & Baccarini, M. (2013) · Molecular Cell · doi:10.1016/j.molcel.2013.01.037 · Cited by 99 · 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

Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi‐targeted kinase inhibitors in pimasertib‐resistant human lung and colorectal cancer cells

Martinelli, E., Troiani, T., D'Aiuto, E., Morgillo, F., Vitagliano, D., Capasso, A., Costantino, S., Ciuffreda, L. P., Merolla, F., Vecchione, L., et al. (2013) · International Journal of Cancer · doi:10.1002/ijc.28236 · Cited by 92 · see citing works

Combined MEK and ERK inhibition overcomes therapy-mediated pathway reactivation in RAS mutant tumors

Merchant, M. A., Moffat, J. G., Schaefer, G., Chan, J., Wang, X., Orr, C., Cheng, J. H., Hunsaker, T., Shao, L., Wang, S. J., et al. (2017) · PLoS ONE · doi:10.1371/journal.pone.0185862 · Cited by 92 · see citing works

PI3K-AKT-mTOR pathway alterations in advanced NSCLC patients after progression on EGFR-TKI and clinical response to EGFR-TKI plus everolimus combination therapy

Fang, W., Huang, Y., Gu, W., Gan, J., Wang, W., Zhang, S., Wang, K., Zhan, J., Yang, Y., Huang, Y., et al. (2020) · Translational Lung Cancer Research · doi:10.21037/tlcr-20-141 · Cited by 93 · see citing works

Immunotherapy Combined or Sequenced With Targeted Therapy in the Treatment of Solid Tumors: Current Perspectives

Atkins, M. B., & Larkin, J. (2016) · JNCI Journal of the National Cancer Institute · doi:10.1093/jnci/djv414 · Cited by 91 · see citing works

Phase Ib study of the MEK inhibitor cobimetinib (GDC-0973) in combination with the PI3K inhibitor pictilisib (GDC-0941) in patients with advanced solid tumors

Shapiro, G. I., LoRusso, P., Kwak, E., Pandya, S., Rudin, C. M., Kurkjian, C., Cleary, J. M., Pilat, M. J., Jones, S., de Crespigny, A., et al. (2020) · Investigational New Drugs · doi:10.1007/s10637-019-00776-6 · Cited by 90 · see citing works

A first-in-human phase I study to evaluate the MEK1/2 inhibitor, cobimetinib, administered daily in patients with advanced solid tumors

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

Phase Ib Study of Combination Therapy with MEK Inhibitor Binimetinib and Phosphatidylinositol 3‐Kinase Inhibitor Buparlisib in Patients with Advanced Solid Tumors with RAS/RAF Alterations

Bardia, A., Gounder, M., Rodón, J., Janku, F., Lolkema, M., Stephenson, J., Bédard, P., Schuler, M., Sessa, C., LoRusso, P., et al. (2019) · The Oncologist · doi:10.1634/theoncologist.2019-0297 · Cited by 79 · see citing works

Targeted therapies in development for non-small cell lung cancer

Dy, G. K., & Reungwetwattana, T. (2013) · Journal of Carcinogenesis · doi:10.4103/1477-3163.123972 · Cited by 80 · see citing works

Cracking the context-specific PI3K signaling code

Madsen, R. R., & Vanhaesebroeck, B. (2020) · Science Signaling · doi:10.1126/scisignal.aay2940 · Cited by 82 · see citing works

A phase Ib dose-escalation study of the MEK inhibitor trametinib in combination with the PI3K/mTOR inhibitor GSK2126458 in patients with advanced solid tumors

Grilley-Olson, J. E., Bedard, P. L., Fasolo, A., Cornfeld, M., Cartee, L., Razak, A. R. A., Stayner, L.-A., Wu, Y., Greenwood, R., Singh, R., et al. (2016) · Investigational New Drugs · doi:10.1007/s10637-016-0377-0 · Cited by 81 · see citing works

Bridging the Gap between Preclinical and Clinical Studies Using Pharmacokinetic–Pharmacodynamic Modeling: An Analysis of GDC-0973, a MEK Inhibitor

Wong, H., Vernillet, L., Peterson, A., Ware, J. A., Lee, L., Martini, J., Yu, P., Li, C., Rosario, G. D., Choo, E. F., et al. (2012) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-12-0445 · Cited by 80 · see citing works

Bcl-2/Bcl-xL Inhibition Increases the Efficacy of MEK Inhibition Alone and in Combination with PI3 Kinase Inhibition in Lung and Pancreatic Tumor Models

Tan, N., Wong, M., Nannini, M., Hong, R., Lee, L. B., Price, S., Williams, K. R., Savy, P., Yue, P., Sampath, D., et al. (2013) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-12-0949 · Cited by 79 · see citing works

Comparative analysis of MAPK and PI3K/AKT pathway activation and inhibition in human and canine melanoma

Fowles, J. S., Denton, C. L., & Gustafson, D. L. (2013) · Veterinary and Comparative Oncology · doi:10.1111/vco.12044 · Cited by 78 · see citing works

Pharmacological Induction of RAS-GTP Confers RAF Inhibitor Sensitivity in KRAS Mutant Tumors

Yen, I., Shanahan, F., Merchant, M. A., Orr, C., Hunsaker, T., Durk, M. R., La, H., Zhang, X., Martin, S. E., Lin, E., et al. (2018) · Cancer Cell · doi:10.1016/j.ccell.2018.09.002 · Cited by 78 · see citing works

Synthetic lethal interaction between PI3K/Akt/mTOR and Ras/MEK/ERK pathway inhibition in rhabdomyosarcoma

Guenther, M. K., Graab, U., & Fulda, S. (2013) · Cancer Letters · doi:10.1016/j.canlet.2013.05.010 · Cited by 77 · see citing works

Emerging insights into resistance to BRAF inhibitors in melanoma

Bucheit, A. D., & Davies, M. A. (2013) · Biochemical Pharmacology · doi:10.1016/j.bcp.2013.11.013 · Cited by 75 · see citing works

MEK inhibitors under development for treatment of non-small-cell lung cancer

Kim, C. G., & Giaccone, G. (2017) · Expert Opinion on Investigational Drugs · doi:10.1080/13543784.2018.1415324 · Cited by 73 · see citing works

Phase I Dose-Escalation Study of the Safety, Pharmacokinetics, and Pharmacodynamics of the MEK Inhibitor RO4987655 (CH4987655) in Patients with Advanced Solid Tumors

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

Phase I Expansion and Pharmacodynamic Study of the Oral MEK Inhibitor RO4987655 (CH4987655) in Selected Patients with Advanced Cancer with <i>RAS–RAF</i> Mutations

Zimmer, L., Barlesi, F., Martinez-Garcia, M., Dieras, V., Schellens, J. H. M., Spano, J.-P., Middleton, M. R., Calvo, E., Paz-Ares, L., Larkin, J., et al. (2014) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-14-0341 · Cited by 71 · see citing works

Exploiting polypharmacology for improving therapeutic outcome of kinase inhibitors (KIs): An update of recent medicinal chemistry efforts

Ma, X., Lv, X., & Zhang, J. (2017) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2017.11.049 · Cited by 70 · see citing works

K-RAS Mutant Pancreatic Tumors Show Higher Sensitivity to MEK than to PI3K Inhibition In Vivo

Hofmann, I., Weiss, A., Elain, G., Schwaederle, M. C., Sterker, D., Romanet, V., Schmelzle, T., Lai, A., Brachmann, S. M., Bentires‐Alj, M., et al. (2012) · PLoS ONE · doi:10.1371/journal.pone.0044146 · Cited by 69 · see citing works

Targeting BRAF in an Inducible Murine Model of Melanoma

Hooijkaas, A. I., Gadiot, J., van der Valk, M., Mooi, W. J., & Blank, C. U. (2012) · American Journal Of Pathology · doi:10.1016/j.ajpath.2012.06.002 · Cited by 65 · see citing works

Suppression of Tumor Cell Lactate-generating Signaling Pathways Eradicates Murine PTEN/p53-deficient Aggressive-variant Prostate Cancer via Macrophage Phagocytosis

Chaudagar, K. K., Hieromnimon, H. M., Kelley, A., Labadie, B. W., Shafran, J. S., Rameshbabu, S., Drovetsky, C., Bynoe, K. M., Solanki, A., Markiewicz, E. J., et al. (2023) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-23-1441 · Cited by 66 · see citing works

Kras mutant genetically engineered mouse models of human cancers are genomically heterogeneous

Chung, W., Daemen, A., Cheng, J. H., Long, J. E., Cooper, J. E., Wang, B.-E., Tran, C., Singh, M., Gnad, F., Modrusan, Z. D., et al. (2017) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1708391114 · Cited by 61 · see citing works

Quantitative Size-Based Analysis of Tumor Spheroids and Responses to Therapeutics

Thakuri, P. S., Gupta, M., Plaster, M., & Tavana, H. (2019) · Assay and Drug Development Technologies · doi:10.1089/adt.2018.895 · Cited by 62 · see citing works

FDG-PET is a good biomarker of both early response and acquired resistance in BRAFV600 mutant melanomas treated with vemurafenib and the MEK inhibitor GDC-0973

Baudy, A. R., Dogan, T., Flores-Mercado, J. E., Hoeflich, K. P., Su, F., van Bruggen, N., & Williams, S. (2012) · EJNMMI Research · doi:10.1186/2191-219x-2-22 · Cited by 61 · see citing works

Modeling Targeted Inhibition of MEK and PI3 Kinase in Human Pancreatic Cancer

Junttila, M. R., Devasthali, V., Cheng, J. H., Castillo, J., Metcalfe, C., Clermont, A. C., Otter, D. D., Chan, E., Bou-Reslan, H., Cao, T. C., et al. (2014) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-14-0030 · Cited by 62 · see citing works

Clinical responses to ERK inhibition in BRAF V600E-mutant colorectal cancer predicted using a computational model

Kirouac, D. C., Schaefer, G., Chan, J., Merchant, M., Orr, C., Huang, S.-M. A., Moffat, J., Liu, L., Gadkar, K., & Ramanujan, S. (2017) · npj Systems Biology and Applications · doi:10.1038/s41540-017-0016-1 · Cited by 60 · see citing works

Genome-based cancer therapeutics: targets, kinase drug resistance and future strategies for precision oncology

Workman, P., Al‐Lazikani, B., & Clarke, P. A. (2013) · Current Opinion in Pharmacology · doi:10.1016/j.coph.2013.06.004 · Cited by 58 · see citing works

Melanoma therapeutics: a literature review

Dhanyamraju, P. K., & Patel, T. (2022) · Journal of Biomedical Research · doi:10.7555/jbr.36.20210163 · Cited by 61 · see citing works

Phase I dose-escalation trial of the oral AKT inhibitor uprosertib in combination with the oral MEK1/MEK2 inhibitor trametinib in patients with solid tumors

Tolcher, A. W., Kurzrock, R., Valero, V., Gonzalez, R. C., Heist, R. S., Tan, A. R., Means-Powell, J. A., Werner, T. L., Becerra, C. R., Wang, C., et al. (2020) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-020-04038-8 · Cited by 59 · see citing works

Inhibition of PI3K/AKT/mTOR Pathway Enhances Temozolomide-Induced Cytotoxicity in Pituitary Adenoma Cell Lines in Vitro and Xenografted Pituitary Adenoma in Female Nude Mice

Dai, C., Zhang, B., Liu, X., Ma, S., Yang, Y., Yao, Y., Feng, M., Bao, X., Li, G., Wang, J., et al. (2013) · Endocrinology · doi:10.1210/en.2012-1908 · Cited by 58 · see citing works

Treatment of NRAS -mutated advanced or metastatic melanoma: rationale, current trials and evidence to date

Boespflug, A. M., Caramel, J., Dalle, S., & Thomas, L. (2017) · Therapeutic Advances in Medical Oncology · doi:10.1177/1758834017708160 · Cited by 57 · see citing works

Phosphoproteomic characterization of DNA damage response in melanoma cells following MEK/PI3K dual inhibition

Kirkpatrick, D. S., Bustos, D. J., Dogan, T., Chan, J., Phu, L., Young, A. E., Friedman, L. S., Belvin, M. P., Song, Q., Bakalarski, C. E., et al. (2013) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1309473110 · Cited by 54 · see citing works

PI3 kinase inhibitors in the clinic: an update.

Kurtz, J., & Ray-Coquard, I. L. (2012) · PubMed · Cited by 55 · see citing works

KRAS: A Druggable Target in Colon Cancer Patients

Negri, F., Bottarelli, L., de’Angelis, G. L., & Gnetti, L. (2022) · International Journal of Molecular Sciences · doi:10.3390/ijms23084120 · Cited by 55 · see citing works

Challenging chemoresistant metastatic colorectal cancer: therapeutic strategies from the clinic and from the laboratory

Bianchi, A. S., Loupakis, F., Argilés, G., & Prager, G. W. (2016) · Annals of Oncology · doi:10.1093/annonc/mdw191 · Cited by 54 · see citing works

Systemic BRAF/MEK Inhibitors as a Potential Treatment Option in Metastatic Conjunctival Melanoma

Mor, J. M., & Heindl, L. M. (2016) · Ocular Oncology and Pathology · doi:10.1159/000452473 · Cited by 53 · see citing works

PAK1 mediates pancreatic cancer cell migration and resistance to MET inhibition

Zhou, W., Jubb, A. M., Lyle, K. S., Xiao, Q., Ong, C. C., Desai, R. M., Fu, L. L., Gnad, F., Song, Q., Haverty, P. M., et al. (2014) · The Journal of Pathology · doi:10.1002/path.4412 · Cited by 53 · see citing works

Discovery of Bifunctional Oncogenic Target Inhibitors against Allosteric Mitogen-Activated Protein Kinase (MEK1) and Phosphatidylinositol 3-Kinase (PI3K)

Dort, M. E. V., Hong, H., Wang, H., Nino, C. A., Lombardi, R. L., Blanks, A., Galbán, S., & Ross, B. D. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b01655 · Cited by 51 · see citing works

Combined MEK and BCL-2/XL Inhibition Is Effective in High-Grade Serous Ovarian Cancer Patient–Derived Xenograft Models and BIM Levels Are Predictive of Responsiveness

Iavarone, C., Zervantonakis, I. K., Selfors, L. M., Palakurthi, S. S., Liu, J. F., Drapkin, R., Matulonis, U. A., Hallberg, D. L., Velculescu, V. E., Leverson, J. D., et al. (2019) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-18-0413 · Cited by 51 · see citing works

Onco-immunomodulatory properties of pharmacological interference with RAS-RAF-MEK-ERK pathway hyperactivation

Avery, T. Y., Köhler, N., Zeiser, R., Brummer, T., & Ruess, D. A. (2022) · Frontiers in Oncology · doi:10.3389/fonc.2022.931774 · Cited by 51 · see citing works

Role of P-Glycoprotein on the Brain Penetration and Brain Pharmacodynamic Activity of the MEK Inhibitor Cobimetinib

Choo, E. F., Ly, J., Chan, J., Shahidi-Latham, S. K., Messick, K., Plise, E. G., Quiason, C. M., & Yang, L. (2014) · Molecular Pharmaceutics · doi:10.1021/mp500435s · Cited by 50 · see citing works

Dual inhibition of allosteric mitogen-activated protein kinase (MEK) and phosphatidylinositol 3-kinase (PI3K) oncogenic targets with a bifunctional inhibitor

Dort, M. E. V., Galbán, S., Wang, H., Sebolt, J. S., Whitehead, C. E., Hong, H., Rehemtulla, A., & Ross, B. D. (2015) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2015.02.053 · Cited by 49 · see citing works

Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349

Pei, Z., Blackwood, E. R., Liu, L., Malek, S., Belvin, M. P., Koehler, M. F. T., Ortwine, D. F., Chen, H., Cohen, F., Kenny, J. R., et al. (2012) · ACS Medicinal Chemistry Letters · doi:10.1021/ml3003132 · Cited by 48 · see citing works

CRAF dimerization with ARAF regulates KRAS-driven tumor growth

Venkatanarayan, A., Liang, J., Yen, I., Shanahan, F., Haley, B., Phu, L., Verschueren, E., Hinkle, T. B., Kan, D., Segal, E., et al. (2022) · Cell Reports · doi:10.1016/j.celrep.2022.110351 · Cited by 45 · see citing works

MEK inhibition suppresses B regulatory cells and augments anti-tumor immunity

Yarchoan, M. M., Mohan, A. A., Dennison, L., Vithayathil, T., Ruggieri, A. N., Lesinski, G. B., Armstrong, T. D., Azad, N. S., & Jaffee, E. M. (2019) · PLoS ONE · doi:10.1371/journal.pone.0224600 · Cited by 45 · see citing works

Potent and Selective Mitogen-Activated Protein Kinase Kinase 1/2 (MEK1/2) Heterobifunctional Small-molecule Degraders

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

The Biology and Clinical Development of MEK Inhibitors for Cancer

Luke, J., Ott, P., & Shapiro, G. (2014) · Drugs · doi:10.1007/s40265-014-0315-4 · Cited by 38 · see citing works

Synergistic Effects of Concurrent Blockade of PI3K and MEK Pathways in Pancreatic Cancer Preclinical Models

Zhong, H., Sanchez, C. G., Dirk, S., Plambeck-Suess, S., Gibbs, J., Hawkins, W. G., DeNardo, D. G., Gao, F., Pufahl, R. A., Lockhart, A. C., et al. (2013) · PLoS ONE · doi:10.1371/journal.pone.0077243 · Cited by 43 · see citing works

Trametinib in the treatment of melanoma

Thota, R., Johnson, D. B., & Sosman, J. (2015) · Expert Opinion on Biological Therapy · doi:10.1517/14712598.2015.1026323 · Cited by 30 · see citing works

MEK inhibitors and their potential in the treatment of advanced melanoma: the advantages of combination therapy

Maverakis, E. M., Tran, K. A., Cheng, M., Mitra, A., Ogawa, H., Shi, V. Y., Olney, L. P., & Kloxin, A. M. (2015) · Drug Design Development and Therapy · doi:10.2147/dddt.s93545 · Cited by 40 · see citing works

How far we have come targeting BRAF-mutant non-small cell lung cancer (NSCLC)

Tabbò, F., Pisano, C., Mazières, J., Mezquita, L., Nadal, E., Planchard, D., Pradines, A., Santamarı́a, D., Swalduz, A., Ambrogio, C., et al. (2021) · Cancer Treatment Reviews · doi:10.1016/j.ctrv.2021.102335 · Cited by 41 · see citing works

Alternative dosing of dual PI3K and MEK inhibition in cancer therapy

Jokinen, E., Laurila, N., & Koivunen, J. P. (2012) · BMC Cancer · doi:10.1186/1471-2407-12-612 · Cited by 40 · see citing works

Dissecting mechanisms of resistance to targeted drug combination therapy in human colorectal cancer

Clarke, P. A., Roe, T., Swabey, K., Hobbs, S., McAndrew, C., Tomlin, K., Westwood, I. M., Burke, R., van Montfort, R., & Workman, P. (2019) · Oncogene · doi:10.1038/s41388-019-0780-z · Cited by 42 · see citing works

Direct binding of MEK1 and MEK2 to AKT induces Foxo1 phosphorylation, cellular migration and metastasis

Procaccia, S., Ordan, M., Cohen, I., Bendetz-Nezer, S., & Seger, R. (2017) · Scientific Reports · doi:10.1038/srep43078 · Cited by 39 · see citing works

Quantitative Proteomics Reveals Fundamental Regulatory Differences in Oncogenic HRAS and Isocitrate Dehydrogenase (IDH1) Driven Astrocytoma

Doll, S., Urisman, A., Osés-Prieto, J. A., Arnott, D. P., & Burlingame, A. L. (2016) · Molecular & Cellular Proteomics · doi:10.1074/mcp.m116.063883 · Cited by 37 · see citing works

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 · see citing works

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 · see citing works

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 · see citing works

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 · see citing works

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