Targeting the cancer kinome through polypharmacology

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

The protein kinase complement of the human genome

Manning, G., Whyte, D. B., Martinez, R., Hunter, T., & Sudarsanam, S. (2002) · Science · doi:10.1126/science.1075762 · Cited by 8,145 · see citing works

Paclitaxel–Carboplatin Alone or with Bevacizumab for Non–Small-Cell Lung Cancer

Sandler, A., Gray, R., Perry, M. C., Brahmer, J., Schiller, J. H., Dowlati, A., Lilenbaum, R., & Johnson, D. H. (2006) · New England Journal of Medicine · doi:10.1056/nejmoa061884 · Cited by 5,761 · see citing works

Sunitinib versus Interferon Alfa in Metastatic Renal-Cell Carcinoma

Motzer, R. J., Hutson, T. E., Tomczak, P., Michaelson, M. D., Bukowski, R. M., Rixe, O., Oudard, S. M., Négrier, S., Szczylik, C. A., Kim, S. T., et al. (2007) · New England Journal of Medicine · doi:10.1056/nejmoa065044 · Cited by 5,752 · see citing works

Erlotinib in Previously Treated Non–Small-Cell Lung Cancer

Shepherd, F. A., Rodrigues Pereira, J., Ciuleanu, T., Tan, E. H., Hirsh, V., Thongprasert, S., Campos, D., Maoleekoonpiroj, S., Smylie, M., Martins, R., et al. (2005) · New England Journal of Medicine · doi:10.1056/nejmoa050753 · Cited by 5,419 · see citing works

Efficacy and Safety of a Specific Inhibitor of the BCR-ABL Tyrosine Kinase in Chronic Myeloid Leukemia

Druker, B. J., Talpaz, M., Resta, D. J., Peng, B., Buchdunger, E., Ford, J., Lydon, N., Kantarjian, H. M., Capdeville, R., Ohno-Jones, S., et al. (2001) · New England Journal of Medicine · doi:10.1056/nejm200104053441401 · Cited by 5,237 · see citing works

Sorafenib in Advanced Clear-Cell Renal-Cell Carcinoma

Escudier, B. J., Eisen, T. G., Stadler, W. M., Szczylik, C. A., Oudard, S. M., Siebels, M., Négrier, S., Chevreau, C., Solska, E., Desai, A. A., et al. (2007) · New England Journal of Medicine · doi:10.1056/nejmoa060655 · Cited by 4,802 · see citing works

Network pharmacology: the next paradigm in drug discovery

Hopkins, A. L. (2008) · Nature Chemical Biology · doi:10.1038/nchembio.118 · Cited by 4,622 · see citing works

<i>MET</i> Amplification Leads to Gefitinib Resistance in Lung Cancer by Activating ERBB3 Signaling

Engelman, J. A., Zejnullahu, K., Mitsudomi, T., Song, Y., Hyland, C., Park, J. O., Lindeman, N., Gale, C.-M., Zhao, X., Christensen, J., et al. (2007) · Science · doi:10.1126/science.1141478 · Cited by 4,496 · see citing works

Systematic RNA interference reveals that oncogenic KRAS-driven cancers require TBK1

Barbie, D. A., Tamayo, P., Boehm, J. S., Kim, S. Y., Moody, S. E., Dunn, I. F., Schinzel, A. C., Sandy, P., Meylan, E., Scholl, C., et al. (2009) · Nature · doi:10.1038/nature08460 · Cited by 3,869 · see citing works

Erlotinib plus gemcitabine compared with gemcitabine alone in patients with advanced pancreatic cancer: a phase III trial of the National Cancer Institute of Canada Clinical Trials Group

Moore, M. J., Goldstein, D., Hamm, J., Figer, A., Hecht, J. R., Gallinger, S., Au, H. J., Murawa, P., Walde, D., Wolff, R. A., et al. (2007) · Journal of Clinical Oncology · doi:10.1200/jco.2006.07.9525 · Cited by 3,848 · see citing works

<i>K-ras</i> Mutations and Benefit from Cetuximab in Advanced Colorectal Cancer

Karapetis, C. S., Khambata-Ford, S., Jonker, D. J., O'Callaghan, C. J., Tu, D., Tebbutt, N. C., Simes, R. J., Chalchal, H., Shapiro, J. D., Robitaille, S., et al. (2008) · New England Journal of Medicine · doi:10.1056/nejmoa0804385 · Cited by 3,622 · see citing works

Acquired Resistance of Lung Adenocarcinomas to Gefitinib or Erlotinib Is Associated with a Second Mutation in the EGFR Kinase Domain

Pao, W., Miller, V. A., Politi, K. A., Riely, G. J., Somwar, R., Zakowski, M. F., Kris, M. G., & Varmus, H. (2005) · PLoS Medicine · doi:10.1371/journal.pmed.0020073 · Cited by 3,527 · see citing works

Five-Year Follow-up of Patients Receiving Imatinib for Chronic Myeloid Leukemia

Druker, B. J., Guilhot, F., O’Brien, S. G., Gathmann, I., Kantarjian, H. M., Gattermann, N., Deininger, M. W., Silver, R. T., Goldman, J. M., Stone, R. M., et al. (2006) · New England Journal of Medicine · doi:10.1056/nejmoa062867 · Cited by 3,474 · see citing works

Lapatinib plus Capecitabine for HER2-Positive Advanced Breast Cancer

Geyer, C. E., Forster, J. K., Lindquist, D. L., Chan, S. Y. T., Romieu, C. G., Pieńkowski, T., Jagiełło-Gruszfeld, A., Crown, J. P., Chan, A., Kaufman, B., et al. (2006) · New England Journal of Medicine · doi:10.1056/nejmoa064320 · Cited by 3,419 · see citing works

Anorexigenic and Orexigenic Hormone Modulation of Mammalian Target of Rapamycin Complex 1 Activity and the Regulation of Hypothalamic Agouti-Related Protein mRNA Expression

Watterson, K. R., Bestow, D., Gallagher, J. R., Hamilton, D. L., Ashford, F. B., Meakin, P. J., & Ashford, M. L. J. (2012) · Neurosignals · doi:10.1159/000334144 · Cited by 3,395 · see citing works

Specificity and mechanism of action of some commonly used protein kinase inhibitors.

Davies, S., Reddy, H., Caivano, M., & Cohen, P. (2000) · Biochemical Journal · doi:10.1042/bj3510095 · Cited by 3,164 · see citing works

The Consensus Coding Sequences of Human Breast and Colorectal Cancers

Sjöblom, T., Jones, S., Wood, L. D., Parsons, D. W., Lin, J., Barber, T. D., Mandelker, D. L., Leary, R. J., Ptak, J., Silliman, N., et al. (2006) · Science · doi:10.1126/science.1133427 · Cited by 3,161 · see citing works

Clinical Resistance to STI-571 Cancer Therapy Caused by BCR-ABL Gene Mutation or Amplification

Gorre, M. E., Mohammed, M., Ellwood, K., Hsu, N., Paquette, R., Rao, P. N., & Sawyers, C. L. (2001) · Science · doi:10.1126/science.1062538 · Cited by 3,104 · see citing works

Paclitaxel plus Bevacizumab versus Paclitaxel Alone for Metastatic Breast Cancer

Miller, K. D., Wang, M., Gralow, J. R., Dickler, M. N., Cobleigh, M., Perez, E. A., Shenkier, T. N., Cella, D. F., & Davidson, N. E. (2007) · New England Journal of Medicine · doi:10.1056/nejmoa072113 · Cited by 3,077 · see citing works

Efficacy of everolimus in advanced renal cell carcinoma: a double-blind, randomised, placebo-controlled phase III trial

Motzer, R. J., Escudier, B., Oudard, S., Hutson, T. E., Porta, C., Bracarda, S., Grünwald, V., Thompson, J. A., Figlin, R. A., Hollaender, N., et al. (2008) · The Lancet · doi:10.1016/s0140-6736(08)61039-9 · Cited by 3,019 · see citing works

The Genomic Landscapes of Human Breast and Colorectal Cancers

Wood, L. D., Parsons, D. W., Jones, S., Lin, J., Sjöblom, T., Leary, R. J., Shen, D., Boca, S. M., Barber, T., Ptak, J., et al. (2007) · Science · doi:10.1126/science.1145720 · Cited by 2,833 · see citing works

A Randomized Trial of Bevacizumab, an Anti–Vascular Endothelial Growth Factor Antibody, for Metastatic Renal Cancer

Yang, J. C., Haworth, L. R., Sherry, R. M., Hwu, P., Schwartzentruber, D. J., Topalian, S. L., Steinberg, S. M., Chen, H. X., & Rosenberg, S. A. (2003) · New England Journal of Medicine · doi:10.1056/nejmoa021491 · Cited by 2,681 · see citing works

Trastuzumab — Mechanism of Action and Use in Clinical Practice

Hudis, C. A. (2007) · New England Journal of Medicine · doi:10.1056/nejmra043186 · Cited by 2,592 · see citing works

The selectivity of protein kinase inhibitors: a further update

Bain, J., Plater, L., Elliott, M., Shpiro, N., Hastie, C. J., McLauchlan, H., Klevernic, I. V., Arthur, J. S. C., Alessi, D. R., & Cohen, P. (2007) · Biochemical Journal · doi:10.1042/bj20070797 · Cited by 2,522 · see citing works

A quantitative analysis of kinase inhibitor selectivity

Karaman, M. W., Herrgard, S., Treiber, D. K., Gallant, P., Atteridge, C. E., Campbell, B. T., Chan, K. W., Ciceri, P., Davis, M. I., Edeen, P. T., et al. (2008) · Nature Biotechnology · doi:10.1038/nbt1358 · Cited by 2,466 · see citing works

Kinase Mutations and Imatinib Response in Patients With Metastatic Gastrointestinal Stromal Tumor

Heinrich, M. C., Corless, C. L., Demetri, G. D., Blanke, C. D., von Mehren, M., Joensuu, H., McGreevey, L. S., Chen, C.-J., den Abbeele, A. D. V., Druker, B. J., et al. (2003) · Journal of Clinical Oncology · doi:10.1200/jco.2003.04.190 · Cited by 2,297 · see citing works

EGFR Antagonists in Cancer Treatment

Ciardiello, F., & Tortora, G. (2008) · New England Journal of Medicine · doi:10.1056/nejmra0707704 · Cited by 2,063 · see citing works

Phosphatidylinositol-3-OH kinase direct target of Ras

Rodriguez-Viciana, P., Warne, P. H., Dhand, R., Vanhaesebroeck, B., Gout, I., Fry, M. J., Waterfield, M. D., & Downward, J. (1994) · Nature · doi:10.1038/370527a0 · Cited by 1,954 · see citing works

Cetuximab for the Treatment of Colorectal Cancer

Jonker, D. J., O'Callaghan, C. J., Karapetis, C. S., Zalcberg, J. R., Tu, D., Au, H.-J., Berry, S. R., Krahn, M., Price, T., Simes, R. J., et al. (2007) · New England Journal of Medicine · doi:10.1056/nejmoa071834 · Cited by 1,904 · see citing works

A small molecule–kinase interaction map for clinical kinase inhibitors

Fabian, M. A., Biggs, W., Treiber, D. K., Atteridge, C. E., Azimioara, M. D., Benedetti, M. G., Carter, T. A., Ciceri, P., Edeen, P. T., Floyd, M. B., et al. (2005) · Nature Biotechnology · doi:10.1038/nbt1068 · Cited by 1,901 · see citing works

Skepinone-L, a Novel Potent and Highly Selective Inhibitor of p38 MAP Kinase, Effectively Impairs Platelet Activation and Thrombus Formation

Borst, O., Walker, B., Münzer, P., Russo, A., Schmid, E., Faggio, C., Bigalke, B., Laufer, S., Gawaz, M., & Lang, F. J. W. (2013) · Cellular Physiology and Biochemistry · doi:10.1159/000350110 · Cited by 1,867 · see citing works

Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias

Talpaz, M., Shah, N. P., Kantarjian, H., Donato, N., Nicoll, J., Paquette, R., Cortes, J., O'Brien, S., Nicaise, C., Bleickardt, E., et al. (2006) · New England Journal of Medicine · doi:10.1056/nejmoa055229 · Cited by 1,760 · see citing works

A Tyrosine Kinase Created by Fusion of the PDGFRA and FIP1L1 Genes as a Therapeutic Target of Imatinib in Idiopathic Hypereosinophilic Syndrome

Cools, J., DeAngelo, D. J., Gotlib, J. R., Stover, E. H., Legare, R. D., Cortes, J. E., Kutok, J. L., Clark, J., Galinsky, I. A., Griffin, J. D., et al. (2003) · New England Journal of Medicine · doi:10.1056/nejmoa025217 · Cited by 1,704 · see citing works

Specificity and mechanism of action of some commonly used protein kinase inhibitors

Davies, S., Reddy, H., Caivano, M., & Cohen, P. (2000) · Biochemical Journal · doi:10.1042/0264-6021:3510095 · Cited by 1,618 · see citing works

Cetuximab in the treatment of colorectal cancer.

Goldberg, R. M., Venook, A. P., & Schilsky, R. L. (2004) · PubMed · Cited by 1,518 · see citing works

KRAS Mutations and Primary Resistance of Lung Adenocarcinomas to Gefitinib or Erlotinib

Pao, W. J., Wang, T. Y., Riely, G. J., Miller, V. A., Pan, Q., Ladanyi, M., Zakowski, M. F., Heelan, R. T., Kris, M. G., & VARMUS, H. E. (2005) · PLoS Medicine · doi:10.1371/journal.pmed.0020017 · Cited by 1,517 · see citing works

Molecular determinants of the response of glioblastomas to EGFR kinase inhibitors

Mellinghoff, I. K., Wang, M. Y., Vivanco, I., Haas-Kogan, D. A., Zhu, S., Dia, E. Q., Lu, K. V., Yoshimoto, K., Huang, J. H. Y., Chute, D. J., et al. (2005) · New England Journal of Medicine · doi:10.1056/nejmoa051918 · Cited by 1,442 · see citing works

Benefits of targeting both pericytes and endothelial cells in the tumor vasculature with kinase inhibitors

Bergers, G., Song, S., Meyer-Morse, N., Bergsland, E. K., & Hanahan, D. (2003) · Journal of Clinical Investigation · doi:10.1172/jci17929 · Cited by 1,361 · see citing works

Nilotinib in Imatinib-Resistant CML and Philadelphia Chromosome–Positive ALL

Kantarjian, H. M., Giles, F. J., Wunderle, L., Bhalla, K. N., O'Brien, S. M., Waßmann, B., Tanaka, C., Manley, P. W., Rae, P., Mietlowski, W. L., et al. (2006) · New England Journal of Medicine · doi:10.1056/nejmoa055104 · Cited by 1,334 · 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

Chemotherapy, Bevacizumab, and Cetuximab in Metastatic Colorectal Cancer

Tol, J., Koopman, M., Cats, A., Rodenburg, C. J., Creemers, G. J., Schrama, J. G., Erdkamp, F., Vos, A. H., van Groeningen, C. J., Sinnige, H. A. M., et al. (2009) · New England Journal of Medicine · doi:10.1056/nejmoa0808268 · 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 1,317 · see citing works

AP24534, a Pan-BCR-ABL Inhibitor for Chronic Myeloid Leukemia, Potently Inhibits the T315I Mutant and Overcomes Mutation-Based Resistance

O’Hare, T., Shakespeare, W. C., Zhu, X., Eide, C. A., Rivera, V. M., Wang, F., Adrian, L. T., Zhou, T., Huang, W.-S., Xu, Q., et al. (2009) · Cancer Cell · doi:10.1016/j.ccr.2009.09.028 · Cited by 1,270 · see citing works

Benefits of targeting both pericytes and endothelial cells in the tumor vasculature with kinase inhibitors

Bergers, G., Song, S., Meyer-Morse, N., et al. (2003) · Journal of Clinical Investigation · doi:10.1172/jci200317929 · Cited by 1,192 · see citing works

A Genome-wide RNAi Screen Identifies Multiple Synthetic Lethal Interactions with the Ras Oncogene

Luo, J., Emanuele, M. J., Li, D., Creighton, C. J., Schlabach, M. R., Westbrook, T. F., Wong, K.-K., & Elledge, S. J. (2009) · Cell · doi:10.1016/j.cell.2009.05.006 · Cited by 1,017 · see citing works

Escape from HER-family tyrosine kinase inhibitor therapy by the kinase-inactive HER3

Sergina, N. V., Rausch, M., Wang, D., Blair, J. A., Hann, B. C., Shokat, K. M., & Moasser, M. M. (2007) · Nature · doi:10.1038/nature05474 · Cited by 993 · see citing works

Coactivation of receptor tyrosine kinases affects the response of tumor cells to targeted therapies

Stommel, J. M., Kimmelman, A. C., Ying, H., Nabioullin, R., Ponugoti, A. H., Wiedemeyer, R., Stegh, A. H., Bradner, J. E., Ligon, K. L., Brennan, C., et al. (2007) · Science · doi:10.1126/science.1142946 · Cited by 938 · see citing works

Mutant PIK3CA promotes cell growth and invasion of human cancer cells.

Samuels, Y., Diaz, L. A., Schmidt-Kittler, O., Cummins, J. M., DeLong, L., Cheong, I., Rago, C., Huso, D. L., Lengauer, C., Kinzler, K. W., et al. (2005) · Cancer Cell · doi:10.1016/j.ccr.2005.05.014 · Cited by 915 · see citing works

Ligand-Independent HER2/HER3/PI3K Complex Is Disrupted by Trastuzumab and Is Effectively Inhibited by the PI3K Inhibitor GDC-0941

Junttila, T. T., Akita, R. W., Parsons, K. L., Fields, C. T., Phillips, G. D. L., Friedman, L. S., Sampath, D., & Sliwkowski, M. X. (2009) · Cancer Cell · doi:10.1016/j.ccr.2009.03.020 · Cited by 829 · see citing works

Features of Selective Kinase Inhibitors

Knight, Z. A., & Shokat, K. M. (2005) · Chemistry & Biology · doi:10.1016/j.chembiol.2005.04.011 · Cited by 663 · see citing works

Differential effects of oncogenic K-Ras and N-Ras on proliferation, differentiation and tumor progression in the colon

Haigis, K. M., Kendall, K. R., Wang, Y., Cheung, A., Haigis, M. C., Glickman, J. N., Niwa-Kawakita, M., Sweet-Cordero, A., Sebolt-Leopold, J., Shannon, K. M., et al. (2008) · Nature Genetics · doi:10.1038/ng.115 · Cited by 610 · see citing works

Mutations in a signalling pathway

Parsons, D. W., Wang, T., Samuels, Y., Bardelli, A., Cummins, J. M., Wood, L. D., Silliman, N., Ptak, J., Szabo, S., Willson, J. K. V., et al. (2005) · Nature · doi:10.1038/436792a · Cited by 599 · see citing works

Binding of Ras to Phosphoinositide 3-Kinase p110α Is Required for Ras- Driven Tumorigenesis in Mice

Gupta, S., Ramjaun, A. R., Haiko, P., Wang, Y., Warne, P. H., Nicke, B., Nye, E. L., Stamp, G., Alitalo, K. K., & Downward, J. (2007) · Cell · doi:10.1016/j.cell.2007.03.051 · Cited by 589 · see citing works

A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma

Fan, Q.-W., Knight, Z. A., Goldenberg, D., Yu, W., Mostov, K. E., Stokoe, D., Shokat, K. M., & Weiss, W. A. (2006) · Cancer Cell · doi:10.1016/j.ccr.2006.03.029 · Cited by 584 · see citing works

Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases

Carter, T. A., Wodicka, L. M., Shah, N. P., Velasco, A. M., Fabian, M. A., Treiber, D. K., Milanov, Z. V., Atteridge, C. E., Biggs, W., Edeen, P. T., et al. (2005) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0504952102 · Cited by 550 · see citing works

Results of a Phase III, Randomized, Placebo-Controlled Study of Sorafenib in Combination With Carboplatin and Paclitaxel As Second-Line Treatment in Patients With Unresectable Stage III or Stage IV Melanoma

Hauschild, A., Agarwala, S. S., Trefzer, U., Hogg, D., Robert, C., Hersey, P., Eggermont, A. M. M., Grabbe, S., Gonzalez, R. C., Gille, J., et al. (2009) · Journal of Clinical Oncology · doi:10.1200/jco.2007.15.7636 · Cited by 548 · see citing works

Epidermal growth factor receptor (HER1) tyrosine kinase inhibitor ZD1839 (Iressa) inhibits HER2/neu (erbB2)-overexpressing breast cancer cells in vitro and in vivo.

Moulder, S. L., Yakes, F. M., Muthuswamy, S. K., Bianco, R., Simpson, J. F., & Arteaga, C. L. (2001) · PubMed · Cited by 548 · see citing works

Synthetic Lethal Interaction between Oncogenic KRAS Dependency and STK33 Suppression in Human Cancer Cells

Scholl, C., Fröhling, S., Dunn, I. F., Schinzel, A. C., Barbie, D. A., Kim, S. Y., Silver, S. J., Tamayo, P., Wadlow, R. C., Ramaswamy, S., et al. (2009) · Cell · doi:10.1016/j.cell.2009.03.017 · Cited by 539 · see citing works

Requirement for NF-κB signalling in a mouse model of lung adenocarcinoma

Meylan, E., Dooley, A. L., Feldser, D. M., Shen, L., Turk, E., Ouyang, C., & Jacks, T. (2009) · Nature · doi:10.1038/nature08462 · Cited by 514 · see citing works

Phosphatidylinositol 3-kinase hyperactivation results in lapatinib resistance that is reversed by the mTOR/phosphatidylinositol 3-kinase inhibitor NVP-BEZ235

Eichhorn, P. J. A., Gili, M., Scaltriti, M., Serra, V., Guzman, M., Nijkamp, W., Beijersbergen, R. L., Valero, V., Seoane, J., Bernards, R., et al. (2008) · Cancer Research · doi:10.1158/0008-5472.can-08-1740 · Cited by 499 · see citing works

Can we rationally design promiscuous drugs?

HOPKINS, A., MASON, J., & OVERINGTON, J. (2006) · Current Opinion in Structural Biology · doi:10.1016/j.sbi.2006.01.013 · Cited by 469 · see citing works

PI3K Pathway Activation Mediates Resistance to MEK Inhibitors in KRAS Mutant Cancers

Wee, S., Jagani, Z., Xiang, K. X., Loo, A., Dorsch, M., Yao, Y.-M., Sellers, W. R., Lengauer, C., & Stegmeier, F. (2009) · Cancer Research · doi:10.1158/0008-5472.can-08-4765 · Cited by 455 · see citing works

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases

Apsel, B., Blair, J. A., González, B., Nazif, T. M., Feldman, M. E., Aizenstein, B., Hoffman, R., Williams, R. L., Shokat, K. M., & Knight, Z. A. (2008) · Nature Chemical Biology · doi:10.1038/nchembio.117 · Cited by 452 · see citing works

Discovery of a novel Raf kinase inhibitor.

Lyons, J. F., Wilhelm, S. M., Hibner, B., & Bollag, G. E. (2001) · Endocrine Related Cancer · doi:10.1677/erc.0.0080219 · Cited by 415 · see citing works

Sequential ABL kinase inhibitor therapy selects for compound drug-resistant BCR-ABL mutations with altered oncogenic potency

Shah, N. P., Skaggs, B. J., Branford, S., Hughes, T. P., Nicoll, J. M., PAQUETTE, R. L., & Sawyers, C. L. (2007) · Journal of Clinical Investigation · doi:10.1172/jci30890 · Cited by 409 · see citing works

MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation

Giles, F. J., Cortes, J. E., Jones, D. M., Bergstrom, D. A., Kantarjian, H. M., & Freedman, S. J. (2006) · Blood · doi:10.1182/blood-2006-05-025049 · Cited by 361 · see citing works

A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases

Fedorov, O., Marsden, B. D., Pogačić, V., Rellos, P., Müller, S., Bullock, A. N., Schwaller, J., Sundström, M., & Knapp, S. (2007) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0708800104 · Cited by 361 · see citing works

Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling

McDermott, U., Sharma, S. V., Dowell, L., Greninger, P., Montagut, C. O., Lamb, J. A., Archibald, H., Raudales, R., Tam, A., Lee, D. W., et al. (2007) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0707498104 · Cited by 352 · see citing works

A Missense Mutation in KIT Kinase Domain 1 Correlates with Imatinib Resistance in Gastrointestinal Stromal Tumors

Chen, L. L., Trent, J. C., Wu, E. F., Fuller, G. N., Ramdas, L., Zhang, W., Raymond, A. K., Prieto, V. G., Oyedeji, C. O., Hunt, K. K., et al. (2004) · Cancer Research · doi:10.1158/0008-5472.can-04-0085 · Cited by 339 · see citing works

A new mutation in the KIT ATP pocket causes acquired resistance to imatinib in a gastrointestinal stromal tumor patient

Tamborini, E., Bonadiman, L., Greco, A., Albertini, V., Negri, T., Gronchi, A., Bertulli, R., Colecchia, M., Casali, P. G., Pierotti, M. A., et al. (2004) · Gastroenterology · doi:10.1053/j.gastro.2004.02.021 · Cited by 323 · see citing works

Randomized Phase II Study of Erlotinib Combined With Bevacizumab Compared With Bevacizumab Alone in Metastatic Renal Cell Cancer

Bukowski, R. M., Kabbinavar, F. F., Figlin, R. A., Flaherty, K. T., Srinivas, S., Vaishampayan, U. N., Drabkin, H. A., Dutcher, J. P., Ryba, S., Xia, Q., et al. (2007) · Journal of Clinical Oncology · doi:10.1200/jco.2007.11.5154 · Cited by 314 · see citing works

Treatment of hypereosinophilic syndrome with imatinib mesilate

Gleich, G. J., Leiferman, K. M., Pardanani, A. D., Tefferi, A., & Butterfield, J. H. (2002) · The Lancet · doi:10.1016/s0140-6736(02)08505-7 · Cited by 303 · see citing works

Renewing the conspiracy theory debate: does Raf function alone to mediate Ras oncogenesis?

Repasky, G. A., Chenette, E. J., & Der, C. J. (2004) · Trends in Cell Biology · doi:10.1016/j.tcb.2004.09.014 · Cited by 299 · see citing works

Cooperative inhibitory effect of ZD1839 (Iressa) in combination with trastuzumab (Herceptin) on human breast cancer cell growth

Normanno, N., Campiglio, M., Luca, A. D., Somenzi, G., Maiello, M. R., Ciardiello, F., Gianni, L., Salomon, D. S., & Ménard, S. (2002) · Annals of Oncology · doi:10.1093/annonc/mdf020 · Cited by 273 · see citing works

Chemical Genetics: Where Genetics and Pharmacology Meet

Knight, Z. A., & Shokat, K. M. (2007) · Cell · doi:10.1016/j.cell.2007.01.021 · Cited by 244 · see citing works

Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo

Luo, Y., Shoemaker, A. R., Liu, X., Woods, K. W., Thomas, S. A., de Jong, R., Han, E. K.-H., Li, T., Stoll, V. S., Powlas, J. A., et al. (2005) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-05-0005 · Cited by 233 · see citing works

Transient Potent BCR-ABL Inhibition Is Sufficient to Commit Chronic Myeloid Leukemia Cells Irreversibly to Apoptosis

Shah, N. P., Kasap, C., Weier, C. A., Balbas, M., Nicoll, J. M., Bleickardt, E. W., Nicaise, C., & Sawyers, C. L. (2008) · Cancer Cell · doi:10.1016/j.ccr.2008.11.001 · Cited by 231 · see citing works

Use of isogenic human cancer cells for high-throughput screening and drug discovery

Torrance, C. J., Agrawal, V., Vogelstein, B., & Kinzler, K. W. (2001) · Nature Biotechnology · doi:10.1038/nbt1001-940 · Cited by 228 · see citing works

A Dual Phosphoinositide-3-Kinase α/mTOR Inhibitor Cooperates with Blockade of Epidermal Growth Factor Receptor in PTEN -Mutant Glioma

Fan, Q.-W., Cheng, C. K., Nicolaides, T. P., Hackett, C. S., Knight, Z. A., Shokat, K. M., & Weiss, W. A. (2007) · Cancer Research · doi:10.1158/0008-5472.can-07-2154 · Cited by 193 · see citing works

Target Identification in Chemical Genetics

Burdine, L. J., & Kodadek, T. J. (2004) · Chemistry & Biology · doi:10.1016/j.chembiol.2004.05.001 · Cited by 191 · see citing works

Simultaneous targeting of Aurora kinases and Bcr-Abl kinase by the small molecule inhibitor PHA-739358 is effective against imatinib-resistant BCR-ABL mutations including T315I

Gontarewicz, A., Balabanov, S., Keller, G., Colombo, R., Graziano, A., Pesenti, E. A., Benten, D., Bokemeyer, C., Fiedler, W., Moll, J. K., et al. (2008) · Blood · doi:10.1182/blood-2007-09-113175 · Cited by 166 · see citing works

Assessment of Chemical Coverage of Kinome Space and Its Implications for Kinase Drug Discovery

Bamborough, P., Drewry, D. H., Harper, G., Smith, G. K., & Schneider, K. (2008) · Journal of Medicinal Chemistry · doi:10.1021/jm8011036 · Cited by 162 · see citing works

Synergistic Antitumor Effects of Combined Epidermal Growth Factor Receptor and Vascular Endothelial Growth Factor Receptor-2 Targeted Therapy

Tonra, J. R., Deevi, D. S., Corcoran, E., Li, H., Wang, S., Carrick, F. E., & Hicklin, D. J. (2006) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-05-1682 · Cited by 148 · see citing works

Disorders in cell circuitry associated with multistage carcinogenesis: exploitable targets for cancer prevention and therapy.

Weinstein, I. B., Begemann, M., Zhou, P., Han, E. K.-H., Sgambato, A., Doki, Y., Arber, N., Ciaparrone, M., & Yamamoto, H. (1997) · PubMed · Cited by 125 · see citing works

Augmentation of apoptosis and tumor regression by flavopiridol in the presence of CPT-11 in Hct116 colon cancer monolayers and xenografts.

Motwani, M., Jung, C. P., Sirotnak, F. M., She, Y., Shah, M. A., Gönen, M., & Schwartz, G. K. (2001) · PubMed · Cited by 117 · see citing works

Kinase-targeted libraries: The design and synthesis of novel, potent, and selective kinase inhibitors

Akritopoulou‐Zanze, I., & Hajduk, P. J. (2009) · Drug Discovery Today · doi:10.1016/j.drudis.2008.12.002 · Cited by 116 · see citing works

Results of phase I pharmacokinetic and pharmacodynamic studies of the Raf kinase inhibitor BAY 43-9006 in patients with solid tumors

Strumberg, D., Voliotis, D., Moeller, J.-G., Hilger, R. A., Richly, H., Kredtke, S., Beling, C., Scheulen, M. E., & Seeber, S. (2002) · International Journal of Clinical Pharmacology and Therapeutics · doi:10.5414/cpp40580 · Cited by 104 · see citing works

A Phase I Clinical Trial of the Sequential Combination of Irinotecan Followed by Flavopiridol

Shah, M. A., Kortmansky, J. S., Motwani, M., Drobnjak, M., Gönen, M., Yi, S., Weyerbacher, A. R., Cordon‐Cardo, C., Lefkowitz, R. A., Brenner, B., et al. (2005) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-04-2651 · Cited by 101 · see citing works

Kinase requirements in human cells: I. Comparing kinase requirements across various cell types

Grueneberg, D. A., Degot, S., Pearlberg, J., Li, W., Davies, J. E., Baldwin, A. E., Endege, W. O., Doench, J. G., Sawyer, J., Hu, Y., et al. (2008) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0808019105 · Cited by 88 · see citing works

Treatment of HER-2/ neu Overexpressing Breast Cancer Xenograft Models with Trastuzumab (Herceptin) and Gefitinib (ZD1839): Drug Combination Effects on Tumor Growth, HER-2/ neu and Epidermal Growth Factor Receptor Expression, and Viable Hypoxic Cell Fraction

Warburton, C., Dragowska, W. H., Gelmon, K. A., Chia, S., Yan, H., Masin, D., Denyssevych, T., Wallis, A. E., & Bally, M. B. (2004) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-03-0244 · Cited by 83 · see citing works

SGX393 inhibits the CML mutant Bcr-Abl T315I and preempts in vitro resistance when combined with nilotinib or dasatinib

O’Hare, T., Eide, C. A., Tyner, J. W., Corbin, A. S., Wong, M. J., Buchanan, S. G., Holme, K. R., Jessen, K. A., Tang, C. M., Lewis, H. A., et al. (2008) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0800587105 · Cited by 80 · see citing works

A Phase I-II Study of Combined Blockade of the ErbB Receptor Network with Trastuzumab and Gefitinib in Patients with HER2 (ErbB2)-Overexpressing Metastatic Breast Cancer

Arteaga, C. L., O’Neill, A., Moulder, S. L., Pins, M., Sparano, J. A., Sledge, G. W., & Davidson, N. E. (2008) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-08-0482 · Cited by 79 · see citing works

Challenges and Opportunities in Defining the Essential Cancer Kinome

Manning, B. D. (2009) · Science Signaling · doi:10.1126/scisignal.263pe15 · Cited by 59 · see citing works

Mixing cocktails

Sawyers, C. L. (2007) · Nature · doi:10.1038/449993a · Cited by 59 · see citing works

RNAi-based screening of the human kinome identifies Akt-cooperating kinases: a new approach to designing efficacious multitargeted kinase inhibitors

Morgan-Lappe, S. E., Woods, K. W., Li, Q., Anderson, M. G., Schurdak, M. E., Luo, Y., Giranda, V. L., Fesik, S. W., & Leverson, J. D. (2005) · Oncogene · doi:10.1038/sj.onc.1209169 · Cited by 53 · see citing works

Kinase requirements in human cells: II. Genetic interaction screens identify kinase requirements following HPV16 E7 expression in cancer cells

Baldwin, A. E., Li, W., Grace, M. R., Pearlberg, J., Harlow, E., Münger, K., & Grueneberg, D. A. (2008) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0806195105 · Cited by 46 · see citing works

For Investigational Targeted Drugs, Combination Trials Pose Challenges

Goldman, B. (2003) · JNCI Journal of the National Cancer Institute · doi:10.1093/jnci/95.23.1744 · Cited by 15 · see citing works

Is the gefitinib plus trastuzumab combination feasible in breast cancer patients?

Normanno, N., Campiglio, M., Perrone, F., Luca, A. D., & Ménard, S. (2005) · Annals of Oncology · doi:10.1093/annonc/mdi325 · Cited by 11 · see citing works

History and Accomplishments of the Inter-Company Collaboration for Aids Drug Development

Barry, D. W., & Distlerath, L. M. (2000) · Drug Information Journal · doi:10.1177/009286150003400310 · Cited by 3 · see citing works

Optimising strategies for clinical development of combinations of targeted agents

Chen, H. (2007) · European Journal of Cancer Supplements · doi:10.1016/j.ejcsup.2007.09.030 · Cited by 1 · see citing works

Comprehensive analysis of kinase inhibitor selectivity

Davis, M. I., Hunt, J. P., Herrgard, S., Ciceri, P., Wodicka, L. M., Pallares, G., Hocker, M., Treiber, D. K., & Zarrinkar, P. P. (2011) · Nature Biotechnology · doi:10.1038/nbt.1990 · Cited by 2,409 · see citing works

The ErbB/HER family of protein-tyrosine kinases and cancer

Roskoski, R. J. (2013) · Pharmacological Research · doi:10.1016/j.phrs.2013.11.002 · Cited by 1,365 · see citing works

Kinase-targeted cancer therapies: progress, challenges and future directions

Bhullar, K. S., Orrego-Lagarón, N., McGowan, E. M., Parmar, I., Jha, A., Hubbard, B. P., & Rupasinghe, H. P. V. (2018) · Molecular Cancer · doi:10.1186/s12943-018-0804-2 · Cited by 1,260 · see citing works

Target identification and mechanism of action in chemical biology and drug discovery

Schenone, M., Dančík, V., Wagner, B. K., & Clemons, P. A. (2013) · Nature Chemical Biology · doi:10.1038/nchembio.1199 · Cited by 1,107 · see citing works

Polypharmacology: Challenges and Opportunities in Drug Discovery: Miniperspective

Anighoro, A., Bajorath, J., & Rastelli, G. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm5006463 · Cited by 1,131 · see citing works

Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity

Anastassiadis, T., Deacon, S. W., Devarajan, K., Ma, H., & Peterson, J. R. (2011) · Nature Biotechnology · doi:10.1038/nbt.2017 · Cited by 919 · see citing works

Automated design of ligands to polypharmacological profiles

Besnard, J., Ruda, G. F., Setola, V., Abecassis, K., Rodriguiz, R. M., Huang, X.-P., Norval, S., Sassano, M. F., Shin, A. I., Webster, L. A., et al. (2012) · Nature · doi:10.1038/nature11691 · Cited by 832 · see citing works

Thermal proteome profiling for unbiased identification of direct and indirect drug targets using multiplexed quantitative mass spectrometry

Franken, H., Mathieson, T., Childs, D., Sweetman, G. M. A., Werner, T., Tögel, I., Doce, C., Gade, S., Bantscheff, M., Drewes, G., et al. (2015) · Nature Protocols · doi:10.1038/nprot.2015.101 · Cited by 638 · see citing works

Making Sense of Large-Scale Kinase Inhibitor Bioactivity Data Sets: A Comparative and Integrative Analysis

Tang, J. P., Szwajda, A., Shakyawar, S. K., Xu, T., Hintsanen, P., Wennerberg, K., & Aittokallio, T. A. (2014) · Journal of Chemical Information and Modeling · doi:10.1021/ci400709d · Cited by 664 · see citing works

Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine

Gelbert, L. M., Cai, S., Lin, X., Sanchez-Martinez, C., del Prado, M., Lallena, M. J., Torres, R., Ajamie, R. T., Wishart, G. N., Flack, R. S., et al. (2014) · Investigational New Drugs · doi:10.1007/s10637-014-0120-7 · Cited by 577 · see citing works

Multiplexed mass cytometry profiling of cellular states perturbed by small-molecule regulators

Bodenmiller, B., Zunder, E. R., Finck, R., Chen, T. J., Savig, E. S., Bruggner, R. V., Simonds, E. F., Bendall, S. C., Sachs, K., Krutzik, P. O., et al. (2012) · Nature Biotechnology · doi:10.1038/nbt.2317 · Cited by 546 · see citing works

SynergyFinder: a web application for analyzing drug combination dose–response matrix data

Ianevski, A., He, L., Aittokallio, T. A., & Tang, J. P. (2017) · Bioinformatics · doi:10.1093/bioinformatics/btx162 · Cited by 535 · see citing works

Polypharmacology by Design: A Medicinal Chemist’s Perspective on Multitargeting Compounds

Proschak, E., Stark, H., & Merk, D. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00760 · Cited by 498 · see citing works

Polypharmacology – Foe or Friend?

Peters, J. (2013) · Journal of Medicinal Chemistry · doi:10.1021/jm400856t · Cited by 477 · see citing works

Drug combination therapy increases successful drug repositioning

Sun, W., Sanderson, P. E. J., & Zheng, W. (2016) · Drug Discovery Today · doi:10.1016/j.drudis.2016.05.015 · Cited by 438 · see citing works

Drugging the undruggables: exploring the ubiquitin system for drug development

Huang, X., & Dixit, V. M. (2016) · Cell Research · doi:10.1038/cr.2016.31 · Cited by 427 · see citing works

Advances in sarcoma genomics and new therapeutic targets

Taylor, B. S., Barretina, J. G., Maki, R. G., Antonescu, C. R., Singer, S., & Ladanyi, M. (2011) · Nature reviews. Cancer · doi:10.1038/nrc3087 · Cited by 428 · see citing works

FAS and NF-κB signalling modulate dependence of lung cancers on mutant EGFR

Bivona, T. G., Hieronymus, H., Parker, J., Chang, K., Taron, M., Rosell, R., Moonsamy, P., Dahlman, K., Miller, V. A., Costa, C., et al. (2011) · Nature · doi:10.1038/nature09870 · Cited by 396 · see citing works

The Evolution of Protein Kinase Inhibitors from Antagonists to Agonists of Cellular Signaling

Dar, A. C., & Shokat, K. M. (2011) · Annual Review of Biochemistry · doi:10.1146/annurev-biochem-090308-173656 · Cited by 388 · see citing works

Anticancer drug resistance: An update and perspective

Nussinov, R., Tsai, C., & Jang, H. (2021) · Drug Resistance Updates · doi:10.1016/j.drup.2021.100796 · Cited by 395 · see citing works

Network‐based Approaches in Pharmacology

Boezio, B., Audouze, K., Ducrot, P., & Taboureau, O. (2017) · Molecular Informatics · doi:10.1002/minf.201700048 · Cited by 364 · see citing works

Redox Signaling by Reactive Electrophiles and Oxidants

Parvez, S., Long, M. J. C., Poganik, J. R., & Aye, Y. (2018) · Chemical Reviews · doi:10.1021/acs.chemrev.7b00698 · Cited by 357 · see citing works

Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development

Donovan, K. A., Ferguson, F. M., Bushman, J. W., Eleuteri, N. A., Bhunia, D., Ryu, S., Tan, L., Shi, K., Yue, H., Liu, X., et al. (2020) · Cell · doi:10.1016/j.cell.2020.10.038 · Cited by 359 · see citing works

Targeting Cyclin-Dependent Kinases in Human Cancers: From Small Molecules to Peptide Inhibitors

Peyressatre, M., Prével, C., Pellerano, M., & Morris, M. C. (2015) · Cancers · doi:10.3390/cancers7010179 · Cited by 345 · see citing works

Drug resistance in metastatic castration-resistant prostate cancer

Šeruga, B., Ocaña, A., & Tannock, I. F. (2010) · Nature Reviews Clinical Oncology · doi:10.1038/nrclinonc.2010.136 · Cited by 337 · see citing works

Dual or multi-targeting inhibitors: The next generation anticancer agents

Raghavendra, N. M., Pingili, D., Kadasi, S., Mettu, A., & Prasad, S. V. U. M. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2017.10.021 · Cited by 333 · see citing works

SCF ubiquitin ligase-targeted therapies

Skaar, J. R., Pagan, J. K., & Pagano, M. (2014) · Nature Reviews Drug Discovery · doi:10.1038/nrd4432 · Cited by 336 · see citing works

Chemical genetic discovery of targets and anti-targets for cancer polypharmacology

Dar, A. C., Das, T. K., Shokat, K. M., & Cagan, R. L. (2012) · Nature · doi:10.1038/nature11127 · Cited by 334 · see citing works

Activation pathway of Src kinase reveals intermediate states as targets for drug design

Shukla, D., Meng, Y., Roux, B., & Pande, V. S. (2014) · Nature Communications · doi:10.1038/ncomms4397 · Cited by 333 · see citing works

Melanoma plasticity and phenotypic diversity: therapeutic barriers and opportunitiesPreprint

Rambow, F., Marine, J., & Goding, C. R. (2019) · Genes & Development · doi:10.1101/gad.329771.119 · Cited by 316 · see citing works

Review of therapeutic drug monitoring of anticancer drugs part two – Targeted therapies

Widmer, N., Bardin, C., Chatelut, É., Paci, A., Beijnen, J. H., Levêque, D., Veal, G. J., & Astier, A. (2014) · European Journal of Cancer · doi:10.1016/j.ejca.2014.04.015 · Cited by 299 · see citing works

The Mitochondrial Chaperone TRAP1 Promotes Neoplastic Growth by Inhibiting Succinate Dehydrogenase

Sciacovelli, M., Guzzo, G., Morello, V., Frezza, C., Zheng, L., Nannini, N., Calabrese, F., Laudiero, G., Esposito, F., Landriscina, M., et al. (2013) · Cell Metabolism · doi:10.1016/j.cmet.2013.04.019 · Cited by 269 · see citing works

Active-learning strategies in computer-assisted drug discovery

Reker, D., & Schneider, G. (2014) · Drug Discovery Today · doi:10.1016/j.drudis.2014.12.004 · Cited by 262 · see citing works

In situ selectivity profiling and crystal structure of SML-8-73-1, an active site inhibitor of oncogenic K-Ras G12C

Hunter, J. C., Gurbani, D., Ficarro, S. B., Carrasco, M. A., Lim, S. M., Choi, H. G., Xie, T., Marto, J. A., Chen, Z., Gray, N. S., et al. (2014) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1404639111 · Cited by 242 · see citing works

Botanical Drugs, Synergy, and Network Pharmacology: Forth and Back to Intelligent Mixtures

Gertsch, J. (2011) · Planta Medica · doi:10.1055/s-0030-1270904 · Cited by 251 · see citing works

Anticancer kinase inhibitors impair intracellular viral trafficking and exert broad-spectrum antiviral effects

Bekerman, E., Neveu, G., Shulla, A., Brannan, J. M., Pu, S., Wang, S., Xiao, F., Barouch‐Bentov, R., Bakken, R. R., Mateo, R., et al. (2017) · Journal of Clinical Investigation · doi:10.1172/jci89857 · Cited by 231 · see citing works

Targeting tumour-supportive cellular machineries in anticancer drug development

Dobbelstein, M., & Moll, U. M. (2014) · Nature Reviews Drug Discovery · doi:10.1038/nrd4201 · Cited by 229 · see citing works

Dual Inhibitors of Human DNA Topoisomerase II and Other Cancer-Related Targets

Skok, Ž., Zidar, N., Kikelj, D., & Ilaš, J. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00726 · Cited by 226 · see citing works

Autophagy in the physiological endometrium and cancer

Devis, L., Eritja, N., Davis, M. L., Matías‐Guiu, X., & Llobet‐Navàs, D. (2020) · Autophagy · doi:10.1080/15548627.2020.1752548 · Cited by 226 · see citing works

A Dual PI3K/HDAC Inhibitor Induces Immunogenic Ferroptosis to Potentiate Cancer Immune Checkpoint Therapy

Fan, F., Liu, P., Bao, R., Chen, J., Zhou, M., Mo, Z., Ma, Y., Liu, H., Zhou, Y., Cai, X., et al. (2021) · Cancer Research · doi:10.1158/0008-5472.can-21-1547 · Cited by 213 · see citing works

Medicinal chemistry strategies for discovering antivirals effective against drug-resistant viruses

Ma, Y., Frutos-Beltrán, E., Kang, D., Pannecouque, C. C., Clercq, E. D., Menéndez‐Arias, L., Liu, X., & Zhan, P. (2021) · Chemical Society Reviews · doi:10.1039/d0cs01084g · Cited by 208 · see citing works

Chromosomal instability and aneuploidy in cancer: from yeast to man

Pfau, S. J., & Amon, A. (2012) · EMBO Reports · doi:10.1038/embor.2012.65 · Cited by 201 · see citing works

Progress with covalent small-molecule kinase inhibitors

Zhao, Z., & Bourne, P. E. (2018) · Drug Discovery Today · doi:10.1016/j.drudis.2018.01.035 · Cited by 200 · see citing works

Novel Computational Approaches to Polypharmacology as a Means to Define Responses to Individual Drugs

Xie, L., Xie, L., Kinnings, S., & Bourne, P. E. (2011) · The Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev-pharmtox-010611-134630 · Cited by 198 · see citing works

Strategies for the Selective Regulation of Kinases with Allosteric Modulators: Exploiting Exclusive Structural Features

Fang, Z., Grütter, C., & Rauh, D. (2013) · ACS Chemical Biology · doi:10.1021/cb300663j · Cited by 197 · see citing works

Inhibition of KRAS -Driven Tumorigenicity by Interruption of an Autocrine Cytokine Circuit

Zhu, Z., Aref, A. R., Cohoon, T. J., Barbie, T. U., Imamura, Y., Yang, S., Moody, S. E., Shen, R. R., Schinzel, A. C., Thai, T. C., et al. (2014) · Cancer Discovery · doi:10.1158/2159-8290.cd-13-0646 · Cited by 193 · see citing works

Modern Phenotypic Drug Discovery Is a Viable, Neoclassic Pharma Strategy

Lee, J. A., Uhlik, M. T., Moxham, C. M., Tomandl, D., & Sall, D. J. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm201649s · Cited by 190 · see citing works

Mechanisms of drug resistance in kinases

Barouch‐Bentov, R., & Sauer, K. (2011) · Expert Opinion on Investigational Drugs · doi:10.1517/13543784.2011.546344 · Cited by 187 · see citing works

Computational Multitarget Drug Design

Zhang, W., Pei, J., & Lai, L. (2017) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.6b00491 · Cited by 186 · see citing works

How Chemoproteomics Can Enable Drug Discovery and Development

Moellering, R. E., & Cravatt, B. F. (2012) · Chemistry &amp; Biology · doi:10.1016/j.chembiol.2012.01.001 · Cited by 182 · see citing works

Phosphoproteomics in cancer

Gowda, H., & Pandey, A. (2010) · Molecular Oncology · doi:10.1016/j.molonc.2010.09.004 · Cited by 177 · see citing works

Discovery and development of natural product oridonin-inspired anticancer agents

Ding, Y., Ding, C., Ye, N., Liu, Z., Wold, E. A., Chen, H., Wild, C., Shen, Q., & Zhou, J. (2016) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2016.06.015 · Cited by 178 · see citing works

Network Pharmacology Strategies Toward Multi-Target Anticancer Therapies: From Computational Models to Experimental Design Principles

Tang, J. P., & Aittokallio, T. A. (2014) · Current Pharmaceutical Design · doi:10.2174/13816128113199990470 · Cited by 184 · see citing works

Taking aim at Mer and Axl receptor tyrosine kinases as novel therapeutic targets in solid tumors

Linger, R. M. A., Keating, A. K., Earp, H. S., & Graham, D. K. (2010) · Expert Opinion on Therapeutic Targets · doi:10.1517/14728222.2010.515980 · Cited by 167 · see citing works

Drug Discovery Using Chemical Systems Biology: Weak Inhibition of Multiple Kinases May Contribute to the Anti-Cancer Effect of Nelfinavir

Xie, L., Evangelidis, T., Xie, L., & Bourne, P. E. (2011) · PLoS Computational Biology · doi:10.1371/journal.pcbi.1002037 · Cited by 163 · see citing works

Structure-based systems biology for analyzing off-target binding

Xie, L., Xie, L., & Bourne, P. E. (2011) · Current Opinion in Structural Biology · doi:10.1016/j.sbi.2011.01.004 · Cited by 152 · see citing works

Induction of Antagonistic Soluble Decoy Receptor Tyrosine Kinases by Intronic PolyA Activation

Vorlová, S., Rocco, G., LeFave, C. V., Jodelka, F. M., Hess, K. C., Hastings, M. L., Henke, E., & Cartegni, L. (2011) · Molecular Cell · doi:10.1016/j.molcel.2011.08.009 · Cited by 142 · see citing works

CRISPR/Cas9 mutagenesis invalidates a putative cancer dependency targeted in on-going clinical trials

Lin, A., Giuliano, C. J., Sayles, N. M., & Sheltzer, J. M. (2017) · eLife · doi:10.7554/elife.24179 · Cited by 144 · see citing works

Compound promiscuity: what can we learn from current data?

Hu, Y., & Bajorath, J. (2013) · Drug Discovery Today · doi:10.1016/j.drudis.2013.03.002 · Cited by 142 · see citing works

The Landscape of Atypical and Eukaryotic Protein Kinases

Kanev, G. K., de Graaf, C., de Esch, I. J. P., Leurs, R., Würdinger, T., Westerman, B. A., & Kooistra, A. J. (2019) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2019.09.002 · Cited by 143 · see citing works

Mitosis Is a Source of Potential Markers for Screening and Survival and Therapeutic Targets in Cervical Cancer

Espinosa-García, A. M., Alfaro, A., Román-Basaure, E., Guardado-Estrada, M., Lara, I. P., Serralde, C., Medina, I., Juárez, E., Bermúdez, M., Márquez, E., et al. (2013) · PLoS ONE · doi:10.1371/journal.pone.0055975 · Cited by 140 · see citing works

Combined Targeting of JAK2 and Bcl-2/Bcl-xL to Cure Mutant JAK2-Driven Malignancies and Overcome Acquired Resistance to JAK2 Inhibitors

Waibel, M., Solomon, V. S., Knight, D. A., Ralli, R., Kim, S., Banks, K.-M., Vidacs, E., Virely, C., Sia, K. C. S., Bracken, L. S., et al. (2013) · Cell Reports · doi:10.1016/j.celrep.2013.10.038 · Cited by 138 · see citing works

Towards novel paradigms for cancer therapy

Pavet, V., Portal, M. M., Moulin, J.-F., Herbrecht, R., & Gronemeyer, H. (2010) · Oncogene · doi:10.1038/onc.2010.460 · Cited by 132 · see citing works

Neoclassic Drug Discovery: The Case for Lead Generation Using Phenotypic and Functional Approaches

Lee, J. A., & Berg, E. L. (2013) · SLAS DISCOVERY · doi:10.1177/1087057113506118 · Cited by 125 · see citing works

A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery

Gao, Y., Davies, S. P., Augustin, M. A., Woodward, A. M., Patel, U. A., Kovelman, R., & Harvey, K. J. (2013) · Biochemical Journal · doi:10.1042/bj20121418 · Cited by 126 · see citing works

Computational-experimental approach to drug-target interaction mapping: A case study on kinase inhibitors

Cichońska, A., Ravikumar, B., Parri, E., Timonen, S., Pahikkala, T., Airola, A., Wennerberg, K., Rousu, J., & Aittokallio, T. A. (2017) · PLoS Computational Biology · doi:10.1371/journal.pcbi.1005678 · Cited by 122 · see citing works

Epigenetic polypharmacology: A new frontier for epi‐drug discovery

Tomaselli, D., Lucidi, A., Rotili, D., & Mai, A. (2019) · Medicinal Research Reviews · doi:10.1002/med.21600 · Cited by 126 · see citing works

Sunitinib depletes myeloid-derived suppressor cells and synergizes with a cancer vaccine to enhance antigen-specific immune responses and tumor eradication

Draghiciu, O., Nijman, H. W., Hoogeboom, B. N., Meijerhof, T., & Daemen, T. (2015) · OncoImmunology · doi:10.4161/2162402x.2014.989764 · Cited by 123 · see citing works

Targeting apoptosis pathways in cancer stem cells

Signore, M., Ricci‐Vitiani, L., & Maria, R. D. (2011) · Cancer Letters · doi:10.1016/j.canlet.2011.01.013 · Cited by 123 · see citing works

The Small Molecules AZD0530 and Dasatinib Inhibit Dengue Virus RNA Replication via Fyn Kinase

de Wispelaere, M., LaCroix, A. J., & Yang, P. L. (2013) · Journal of Virology · doi:10.1128/jvi.00632-13 · Cited by 122 · see citing works

Anthelmintic Drug Discovery: Into the Future

Geary, T. G., Sakanari, J. A., & Caffrey, C. R. (2015) · Journal of Parasitology · doi:10.1645/14-703.1 · Cited by 122 · 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

Discovery of benzimidazole derivatives as novel multi-target EGFR, VEGFR-2 and PDGFR kinase inhibitors

Li, Y., Tan, C., Gao, C., Zhang, C., Luan, X., Chen, X., Liu, H., Chen, Y., & Jiang, Y. (2011) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2011.06.022 · Cited by 120 · see citing works

Dual Drug Conjugated Nanoparticle for Simultaneous Targeting of Mitochondria and Nucleus in Cancer Cells

Mallick, A., More, P. A., Ghosh, S., Chippalkatti, R., Chopade, B. A., Lahiri, M., & Basu, S. (2015) · ACS Applied Materials & Interfaces · doi:10.1021/am5090226 · Cited by 119 · see citing works

The role of fragment-based and computational methods in polypharmacology

Bottegoni, G., Favia, A. D., Recanatini, M., & Cavalli, A. (2011) · Drug Discovery Today · doi:10.1016/j.drudis.2011.08.002 · Cited by 116 · see citing works

Quercetin inhibits a large panel of kinases implicated in cancer cell biology

Kiss (2010) · International Journal of Oncology · doi:10.3892/ijo.2010.890 · Cited by 116 · see citing works

Design, synthesis and biological evaluation of novel benzimidazole amidines as potent multi-target inhibitors for the treatment of non-small cell lung cancer

Bistrović, A., Krstulović, L., Harej, A., Grbčić, P., Sedić, M., Koštrun, S., Pavelić, S. K., Bajić, M., & Raić‐Malić, S. (2017) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2017.10.061 · Cited by 115 · see citing works

Challenges and Opportunities in the Development of Protein Phosphatase-Directed Therapeutics

Munter, S. D., Köhn, M., & Bollen, M. (2012) · ACS Chemical Biology · doi:10.1021/cb300597g · Cited by 114 · see citing works

Blueprint for cancer research: Critical gaps and opportunities

Elmore, L. W., Greer, S. F., Daniels, E. C., Saxe, C. C., Melner, M. H., Krawiec, G. M., Cance, W. G., & Phelps, W. C. (2020) · CA A Cancer Journal for Clinicians · doi:10.3322/caac.21652 · Cited by 121 · see citing works

Pyrimidine and fused pyrimidine derivatives as promising protein kinase inhibitors for cancer treatment

Abdellatif, K. R. A., & Bakr, R. B. (2020) · Medicinal Chemistry Research · doi:10.1007/s00044-020-02656-8 · Cited by 111 · see citing works

Quantitative network mapping of the human kinome interactome reveals new clues for rational kinase inhibitor discovery and individualized cancer therapy

Cheng, F., Jia, P., Wang, Q., & Zhao, Z. (2014) · Oncotarget · doi:10.18632/oncotarget.1984 · Cited by 105 · see citing works

Deciphering UV‐induced DNA Damage Responses to Prevent and Treat Skin Cancer

Lee, J. W., Ratnakumar, K., Hung, K., Rokunohe, D., & Kawasumi, M. (2020) · Photochemistry and Photobiology · doi:10.1111/php.13245 · Cited by 112 · see citing works

New Electrophiles and Strategies for Mechanism-Based and Targeted Covalent Inhibitor Design

Ray, S., & Murkin, A. S. (2019) · Biochemistry · doi:10.1021/acs.biochem.9b00293 · Cited by 108 · see citing works

Design and synthesis of novel 4-benzothiazole amino quinazolines Dasatinib derivatives as potential anti-tumor agents

Cai, J., Sun, M., Wu, X., Chen, J., Wang, P., Zong, X., & Ji, M. (2013) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2013.03.013 · Cited by 105 · see citing works

Polypharmacology in Drug Discovery: A Review from Systems Pharmacology Perspective

Zhang, W., Bai, Y., Wang, Y., & Xiao, W. (2016) · Current Pharmaceutical Design · doi:10.2174/1381612822666160224142812 · Cited by 105 · see citing works

ChemProt: a disease chemical biology database

Taboureau, O., Nielsen, S. K., Audouze, K., Weinhold, N., Edsgärd, D., Roque, F. S., Kouskoumvekaki, I. A., Bora, A., Curpan, R. F., Jensen, T. S., et al. (2010) · Nucleic Acids Research · doi:10.1093/nar/gkq906 · Cited by 105 · see citing works

INKA, an integrative data analysis pipeline for phosphoproteomic inference of active kinases

Beekhof, R., van Alphen, C., Henneman, A. A., Knol, J. C., Pham, T. V., Rolfs, F., Labots, M., Henneberry, E., Le Large, T. Y., de Haas, R. R., et al. (2019) · Molecular Systems Biology · doi:10.15252/msb.20188250 · Cited by 97 · see citing works

Comparison of the Cancer Gene Targeting and Biochemical Selectivities of All Targeted Kinase Inhibitors Approved for Clinical Use

Uitdehaag, J. C. M., de Roos, J. A. D. M., van Doornmalen, A. M., Prinsen, M. B. W., de Man, J., Tanizawa, Y., Kawase, Y., Yoshino, K., Buijsman, R. C., & Zaman, G. J. R. (2014) · PLoS ONE · doi:10.1371/journal.pone.0092146 · Cited by 105 · see citing works

Polypharmacology: The Rise of Multitarget Drugs over Combination Therapies

Rosini, M. (2014) · Future Medicinal Chemistry · doi:10.4155/fmc.14.25 · Cited by 103 · see citing works

Prediction of Chemical-Protein Interactions Network with Weighted Network-Based Inference Method

Cheng, F., Zhou, Y., Li, W., Liu, G., & Tang, Y. (2012) · PLoS ONE · doi:10.1371/journal.pone.0041064 · Cited by 100 · see citing works

Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases

Zhang, K., Lai, F., Lin, S., Ji, M., Zhang, J., Zhang, Y., Jin, J., Fu, R., Wu, D., Tian, H., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00390 · Cited by 99 · see citing works

Polypharmacology-based ceritinib repurposing using integrated functional proteomics

Kuenzi, B. M., Rix, L. L. R., Stewart, P. A., Fang, B., Kinose, F., Bryant, A. T., Boyle, T. A., Koomen, J. M., Haura, E. B., & Rix, U. (2017) · Nature Chemical Biology · doi:10.1038/nchembio.2489 · Cited by 98 · see citing works

Systems-pharmacology dissection of a drug synergy in imatinib-resistant CML

Winter, G. E., Rix, U., Carlson, S. M., Gleixner, K. V., Grebien, F., Gridling, M., Müller, A. C., Breitwieser, F. P., Bilban, M., Colinge, J., et al. (2012) · Nature Chemical Biology · doi:10.1038/nchembio.1085 · Cited by 97 · see citing works

Predicting resistance of clinical Abl mutations to targeted kinase inhibitors using alchemical free-energy calculations

Hauser, K., Negron, C., Albanese, S. K., Ray, S. S., Steinbrecher, T. B., Abel, R., Chodera, J. D., & Wang, L. (2018) · Communications Biology · doi:10.1038/s42003-018-0075-x · Cited by 91 · see citing works

Breakthroughs in modern cancer therapy and elusive cardiotoxicity: Critical research‐practice gaps, challenges, and insights

Zheng, P., Li, J., & Kros, J. M. (2017) · Medicinal Research Reviews · doi:10.1002/med.21463 · Cited by 97 · see citing works

De novo generation of multi-target compounds using deep generative chemistry

Munson, B. P., Chen, M., Bogosian, A., Kreisberg, J. F., Licon, K., Abagyan, R. A., Kuenzi, B. M., & Ideker, T. E. (2024) · Nature Communications · doi:10.1038/s41467-024-47120-y · Cited by 95 · see citing works

Repurposing of Kinase Inhibitors as Broad-Spectrum Antiviral Drugs

Schor, S., & Einav, S. (2017) · DNA and Cell Biology · doi:10.1089/dna.2017.4033 · Cited by 94 · see citing works

Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation

Li, X., Li, Z. S., Wu, X., Xiong, Z., Yang, T., Fu, Z., Liu, X., Tan, X., Zhong, F., Wan, X., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00855 · Cited by 93 · see citing works

Repurposing sertraline sensitizes non–small cell lung cancer cells to erlotinib by inducing autophagy

Jiang, X., Lü, W., Shen, X., Wang, Q., Lv, J., Liu, M., Cheng, F., Zhao, Z., & Pang, X. (2018) · JCI Insight · doi:10.1172/jci.insight.98921 · Cited by 90 · see citing works

Turning liabilities into opportunities: Off-target based drug repurposing in cancer

Palve, V. C., Liao, Y., Rix, L. L. R., & Rix, U. (2020) · Seminars in Cancer Biology · doi:10.1016/j.semcancer.2020.02.003 · Cited by 92 · see citing works

Recent Advances in the Development of Multi-Kinase Inhibitors

Krug, M., & Hilgeroth, A. (2008) · Mini-Reviews in Medicinal Chemistry · doi:10.2174/138955708786369591 · Cited by 95 · 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

Targeted Therapies in Cancer: To Be or Not to Be, Selective

Montoya, S., Soong, D., Nguyen, N. T., Affer, M., Munamarty, S. P., & Taylor, J. (2021) · Biomedicines · doi:10.3390/biomedicines9111591 · Cited by 49 · see citing works

Kinase Inhibitors in Multitargeted Cancer Therapy

Gentile, C., Martorana, A., Lauria, A., & Bonsignore, R. (2017) · Current Medicinal Chemistry · doi:10.2174/0929867324666170112112734 · Cited by 46 · see citing works

Combining kinase inhibitors for optimally co‐targeting cancer and drug escape by exploitation of drug target promiscuities

Chen, S., Yang, S. Y., Zeng, X. L., Zhu, F., Tan, Y. C., Jiang, Y., & Chen, Y. (2020) · Drug Development Research · doi:10.1002/ddr.21738 · Cited by 1 · see citing works