The solute carrier SLC35F2 enables YM155-mediated DNA damage toxicity
Open accessAbstract
Genotoxic chemotherapy is the most common cancer treatment strategy. However, its untargeted generic DNA-damaging nature and associated systemic cytotoxicity greatly limit its therapeutic applications. Here, we used a haploid genetic screen in human cells to discover an absolute dependency of the clinically evaluated anticancer compound YM155 on solute carrier family member 35 F2 (SLC35F2), an uncharacterized member of the solute carrier protein family that is highly expressed in a variety of human cancers. YM155 generated DNA damage through intercalation, which was contingent on the expression of SLC35F2 and its drug-importing activity. SLC35F2 expression and YM155 sensitivity correlated across a panel of cancer cell lines, and targeted genome editing verified SLC35F2 as the main determinant of YM155-mediated DNA damage toxicity in vitro and in vivo. These findings suggest a new route to targeted DNA damage by exploiting tumor and patient-specific import of YM155.
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KBM7 cells are a valid model to capture the overall essentiality profile of both ligases.
“KBM7 cells, which are a frequently used tool to study mechanisms of drug resistance are thus a valid model to capture the overall essentiality profile of both ligases. 28–30.”
From Functional E3 ligase hotspots and resistance mechanisms to small-molecule degraders (2023) · cites this paper as [30]
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Subramanian, A., Tamayo, P., Mootha, V. K., Mukherjee, S., Ebert, B. L., Gillette, M. A., Paulovich, A., Pomeroy, S. L., Golub, T. R., Lander, E. S., et al. (2005) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0506580102 · Cited by 53,625 · see citing works
Ultrafast and memory-efficient alignment of short DNA sequences to the human genome.
Langmead, B., Trapnell, C., Pop, M., & Salzberg, S. L. (2009) · Genome Biology · doi:10.1186/gb-2009-10-3-r25 · Cited by 21,849 · see citing works
Multiplex Genome Engineering Using CRISPR/Cas Systems
Cong, L., Ran, F. A., Cox, D., Lin, S., Barretto, R., Habib, N., Hsu, P. D., Wu, X., Jiang, W., Marraffini, L. A., et al. (2013) · Science · doi:10.1126/science.1231143 · Cited by 15,339 · see citing works
TopHat: discovering splice junctions with RNA-Seq
Trapnell, C., Pachter, L. S., & Salzberg, S. L. (2009) · Bioinformatics · doi:10.1093/bioinformatics/btp120 · Cited by 11,477 · see citing works
RNA-Guided Human Genome Engineering via Cas9
Mali, P., Yang, L., Esvelt, K. M., Aach, J., Guell, M., DiCarlo, J. E., Norville, J. E., & Church, G. M. (2013) · Science · doi:10.1126/science.1232033 · Cited by 9,210 · see citing works
The Cancer Cell Line Encyclopedia enables predictive modelling of anticancer drug sensitivity
Barretina, J., Caponigro, G., Stransky, N., Venkatesan, K., Margolin, A. A., Kim, S., Wilson, C. J., Lehár, J., Kryukov, G. V., Sonkin, D., et al. (2012) · Nature · doi:10.1038/nature11003 · Cited by 7,950 · see citing works
DEGseq: an R package for identifying differentially expressed genes from RNA-seq data
Wang, L., Feng, Z., Wang, X., Wang, X., & Zhang, X. (2010) · Bioinformatics · doi:10.1093/bioinformatics/btp612 · Cited by 4,553 · see citing works
Trastuzumab emtansine for HER2-positive advanced breast cancer
Verma, S., Miles, D., Gianni, L., Krop, I. E., Welslau, M., Baselga, J., Pegram, M., Oh, D.-Y., Diéras, V., Guardino, E., et al. (2012) · New England Journal of Medicine · doi:10.1056/nejmoa1209124 · Cited by 3,834 · see citing works
Wang, H., Yang, H., Shivalila, C. S., Dawlaty, M. M., Cheng, A. W., Zhang, F., & Jaenisch, R. (2013) · Cell · doi:10.1016/j.cell.2013.04.025 · Cited by 3,495 · see citing works
DNA damage activates ATM through intermolecular autophosphorylation and dimer dissociation
Bakkenist, C. J., & Kastan, M. B. (2003) · Nature · doi:10.1038/nature01368 · Cited by 3,466 · see citing works
Membrane transporters in drug development
The International Transporter Consortium, Giacomini, K. M., Huang, S.-M., Tweedie, D. J., Benet, L. Z., Brouwer, K. L. R., Chu, X., Dahlin, A., Evers, R., Fischer, V., et al. (2010) · Nature Reviews Drug Discovery · doi:10.1038/nrd3028 · Cited by 3,340 · see citing works
RSeQC: quality control of RNA-seq experiments
Wang, L., Wang, S., & Li, W. (2012) · Bioinformatics · doi:10.1093/bioinformatics/bts356 · Cited by 2,813 · see citing works
Genetic Control of the Cell Division Cycle in Yeast
Hartwell, L. H., Culotti, J. G., Pringle, J. R., & Reid, B. J. (1974) · Science · doi:10.1126/science.183.4120.46 · Cited by 1,567 · see citing works
Brentuximab Vedotin (SGN-35) for Relapsed CD30-Positive Lymphomas
Younes, A., Bartlett, N. L., Leonard, J. P., Kennedy, D. A., Lynch, C. M., Sievers, E. L., & Forero, A. (2010) · New England Journal of Medicine · doi:10.1056/nejmoa1002965 · Cited by 1,365 · see citing works
OpenComet: An automated tool for comet assay image analysis
Gyori, B. M., Venkatachalam, G., Thiagarajan, P. S., Hsu, D., & Clement, M. (2014) · Redox Biology · doi:10.1016/j.redox.2013.12.020 · Cited by 721 · see citing works
Haploid Genetic Screens in Human Cells Identify Host Factors Used by Pathogens
Carette, J., Guimarães, C. P., Varadarajan, M., Park, A. S., Wuethrich, I., Godarova, A., Kotecki, M., Cochran, B., Spooner, E., Ploegh, H., et al. (2009) · Science · doi:10.1126/science.1178955 · Cited by 508 · see citing works
Self-citationCarrier-mediated cellular uptake of pharmaceutical drugs: an exception or the rule?
Dobson, P. D., & Kell, D. B. (2008) · Nature Reviews Drug Discovery · doi:10.1038/nrd2438 · Cited by 475 · see citing works
Giaccone, G., Zatloukal, P., Roubec, J., Floor, K., Musil, J., Kůta, M., van Klaveren, R. J., Chaudhary, S., Gunther, A., & Shamsili, S. (2009) · Journal of Clinical Oncology · doi:10.1200/jco.2008.21.1862 · Cited by 247 · see citing works
Phase I and Pharmacokinetic Study of YM155, a Small-Molecule Inhibitor of Survivin
Tolcher, A. W., Mita, A. C., Lewis, L. D., Garrett, C. R., Till, E., DAUD, A. I., Patnaik, A., Papadopoulos, K. P., Takimoto, C. H. M., Bartels, P., et al. (2008) · Journal of Clinical Oncology · doi:10.1200/jco.2008.17.2064 · Cited by 239 · see citing works
MCT1-mediated transport of a toxic molecule is an effective strategy for targeting glycolytic tumors
Birsoy, K., Wang, T., Possemato, R., Yilmaz, Ö. H., Koch, C. E., Chen, W. W., Hutchins, A., Gültekin, Y., Peterson, T. R., Carette, J. E., et al. (2012) · Nature Genetics · doi:10.1038/ng.2471 · Cited by 226 · see citing works
Self-citationMolecular physiology and pathology of the nucleotide sugar transporter family (SLC35)
Ishida, N., & Kawakita, M. (2004) · Pflügers Archiv - European Journal of Physiology · doi:10.1007/s00424-003-1093-0 · Cited by 185 · see citing works
Kell, D. B., Dobson, P. D., & Oliver, S. G. (2011) · Drug Discovery Today · doi:10.1016/j.drudis.2011.05.010 · Cited by 184 · see citing works
ATR signaling can drive cells into senescence in the absence of DNA breaks
Toledo, L. I., Murga, M., Gutierrez-Martinez, P., Soria, R., & Fernandez-Capetillo, O. (2008) · Genes & Development · doi:10.1101/gad.452308 · Cited by 183 · see citing works
Roles of the nucleotide sugar transporters (SLC35 family) in health and disease
Song, Z. (2013) · Molecular Aspects of Medicine · doi:10.1016/j.mam.2012.12.004 · Cited by 142 · see citing works
Inhibition of DNA and RNA polymerase reactions by chloroquine.
Cohen, S. N., & Yielding, K. L. (1965) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.54.2.521 · Cited by 118 · see citing works
Reiling, J. H., Clish, C. B., Carette, J. E., Varadarajan, M., Brummelkamp, T. R., & Sabatini, D. M. (2011) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1018098108 · Cited by 104 · see citing works
Self-citationThe “survivin suppressants” NSC 80467 and YM155 induce a DNA damage response
Glaros, T., Stockwin, L. H., Mullendore, M. E., Smith, B., Morrison, B. L., & Newton, D. L. (2012) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-012-1868-0 · Cited by 94 · see citing works
Lanthaler, K., Bilsland, E., Dobson, P. D., Moss, H. J., Pir, P., Kell, D. B., & Oliver, S. G. (2011) · BMC Biology · doi:10.1186/1741-7007-9-70 · Cited by 82 · see citing works
Interleukin Enhancer-binding Factor 3/NF110 Is a Target of YM155, a Suppressant of Survivin
Nakamura, N., Yamauchi, T., Hiramoto, M., Yuri, M., Naito, M., Takeuchi, M., Yamanaka, K., Kita, A., Nakahara, T., Kinoyama, I., et al. (2012) · Molecular & Cellular Proteomics · doi:10.1074/mcp.m111.013243 · Cited by 66 · see citing works
Cordes, N., & Beinke, C. (2004) · Cancer Biology & Therapy · doi:10.4161/cbt.3.1.570 · Cited by 58 · see citing works
Minematsu, T., Iwai, M., Umehara, K., Usui, T., & Kamimura, H. (2009) · Drug Metabolism and Disposition · doi:10.1124/dmd.109.028142 · Cited by 57 · see citing works
Biological characterization of MLN944: A potent DNA binding agent
Sappal, D. S., McClendon, A. K., Fleming, J., Thoroddsen, V., Connolly, K., Reimer, C., Blackman, R. K., Bulawa, C., Osheroff, N., Charlton, P., et al. (2004) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.47.3.1 · Cited by 52 · see citing works
Minematsu, T., Iwai, M., Sugimoto, K., Shirai, N., Nakahara, T., Usui, T., & Kamimura, H. (2008) · Drug Metabolism and Disposition · doi:10.1124/dmd.108.025254 · Cited by 27 · see citing works
Sarangi, A., Bupp, K., & Roth, M. J. (2007) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0704182104 · Cited by 24 · see citing works
Global gene disruption in human cells to assign genes to phenotypes
Carette, J. E., Guimarães, C. P., Wüthrich, I., Blomen, V. A., Varadarajan, M., Sun, C., Bell, G. W., Yuan, B., Muellner, M. K., Nijman, S. M. B., et al. (2011) · PubMed Central · doi:10.1038/nbt.1857
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Human Haploid Cell Genetics Reveals Roles for Lipid Metabolism Genes in Nonapoptotic Cell Death
Dixon, S. J., Winter, G. E., Musavi, L. S., Lee, E. D., Snijder, B., Rebsamen, M., Superti-Furga, G., & Stockwell, B. R. (2015) · ACS Chemical Biology · doi:10.1021/acschembio.5b00245 · Cited by 1,043 · see citing works
Self-citationCorrelating chemical sensitivity and basal gene expression reveals mechanism of action
Rees, M. G., Seashore-Ludlow, B. A., Cheah, J. H., Adams, D., Price, E. V., Gill, S., Javaid, S., Coletti, M. E., Jones, V., Bodycombe, N. E., et al. (2015) · Nature Chemical Biology · doi:10.1038/nchembio.1986 · Cited by 874 · see citing works
A Call for Systematic Research on Solute Carriers
César‐Razquin, A., Snijder, B., Frappier‐Brinton, T., Isserlin, R., Gyimesi, G., Bai, X., Reithmeier, R. A., Hepworth, D., Hediger, M. A., Edwards, A. M., et al. (2015) · Cell · doi:10.1016/j.cell.2015.07.022 · Cited by 581 · see citing works
Self-citationCurrin, A., Swainston, N., Day, P. J., & Kell, D. B. (2014) · Chemical Society Reviews · doi:10.1039/c4cs00351a · Cited by 383 · see citing works
A Pharmacogenomic Landscape in Human Liver Cancers
Qiu, Z., Li, H., Zhang, Z., Zhu, Z., He, S., Wang, X., Wang, P., Qin, J., Zhuang, L., Wang, W., et al. (2019) · Cancer Cell · doi:10.1016/j.ccell.2019.07.001 · Cited by 202 · see citing works
Membrane transporter engineering in industrial biotechnology and whole cell biocatalysis
Kell, D. B., Swainston, N., Pir, P., & Oliver, S. G. (2015) · Trends in biotechnology · doi:10.1016/j.tibtech.2015.02.001 · Cited by 195 · see citing works
Kell, D. B., & Oliver, S. G. (2014) · Frontiers in Pharmacology · doi:10.3389/fphar.2014.00231 · Cited by 155 · see citing works
Hamblett, K. J., Jacob, A. P., Gurgel, J. L., Tometsko, M. E., Rock, B. M., Patel, S. K., Milburn, R. R., Siu, S., Ragan, S. P., Rock, D. A., et al. (2015) · Cancer Research · doi:10.1158/0008-5472.can-15-1610 · Cited by 144 · see citing works
A widespread role for SLC transmembrane transporters in resistance to cytotoxic drugs
Girardi, E., César‐Razquin, A., Lindinger, S., Παπακώστας, Κ., Konecka, J., Hemmerich, J., Kickinger, S., Kartnig, F., Gürtl, B., Klavins, K., et al. (2020) · Nature Chemical Biology · doi:10.1038/s41589-020-0483-3 · Cited by 133 · see citing works
Self-citationFunctional E3 ligase hotspots and resistance mechanisms to small-molecule degraders
Hanzl, A., Casement, R., Imrichova, H., Hughes, S. J., Barone, E., Testa, A., Bauer, S., Wright, J., Brand, M., Ciulli, A., et al. (2023) · Nature Chemical Biology · doi:10.1038/s41589-022-01177-2 · Cited by 133 · see citing works
Self-citationThe metabolome 18 years on: a concept comes of age
Kell, D. B., & Oliver, S. G. (2016) · Metabolomics · doi:10.1007/s11306-016-1108-4 · Cited by 127 · see citing works
Epistasis-driven identification of SLC25A51 as a regulator of human mitochondrial NAD import
Girardi, E., Agrimi, G., Goldmann, U., Fiume, G., Lindinger, S., Sedlyarov, V., Srndic, I., Gürtl, B., Agerer, B., Kartnig, F., et al. (2020) · Nature Communications · doi:10.1038/s41467-020-19871-x · Cited by 123 · see citing works
Self-citationThe Druggability of Solute Carriers
Wang, W., Gallo, L. H., Jadhav, A. M., Hawkins, R., & Parker, C. G. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b01237 · Cited by 109 · see citing works
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Bunnage, M. E., Gilbert, A. M., Jones, L. H., & Hett, E. C. (2015) · Nature Chemical Biology · doi:10.1038/nchembio.1813 · Cited by 100 · see citing works
O’Hagan, S., Muelas, M. W., Day, P. J., Lundberg, E. K., & Kell, D. B. (2018) · Cell Systems · doi:10.1016/j.cels.2018.01.003 · Cited by 95 · see citing works
Liu, S., Ono, R. J., Yang, C. H., Gao, S., Tan, J. Y. M., Hedrick, J. L., & Yang, Y. Y. (2018) · ACS Applied Materials & Interfaces · doi:10.1021/acsami.8b01954 · Cited by 92 · see citing works
Compromising the 19S proteasome complex protects cells from reduced flux through the proteasome
Tsvetkov, P., Mendillo, M. L., Zhao, J., Carette, J. E., Merrill, P. H., Cikes, D., Varadarajan, M., van Diemen, F. R., Penninger, J. M., Goldberg, A. L., et al. (2015) · eLife · doi:10.7554/elife.08467 · Cited by 83 · see citing works
Self-citationFunctional genomics to uncover drug mechanism of action
Nijman, S. M. B. (2015) · Nature Chemical Biology · doi:10.1038/nchembio.1963 · Cited by 73 · see citing works
An Overview of Cell-Based Assay Platforms for the Solute Carrier Family of Transporters
Dvorak, V., Wiedmer, T., Inglés‐Prieto, Á., Altermatt, P., Batoulis, H., Bärenz, F., Bender, E., Digles, D., Dürrenberger, F., Heitman, L. H., et al. (2021) · Frontiers in Pharmacology · doi:10.3389/fphar.2021.722889 · Cited by 69 · see citing works
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O’Hagan, S., & Kell, D. B. (2015) · PeerJ · doi:10.7717/peerj.1405 · Cited by 63 · see citing works
Bioactive Compound Collections: From Design to Target Identification
Laraia, L., Robke, L., & Waldmann, H. (2018) · Chem · doi:10.1016/j.chempr.2018.01.012 · Cited by 61 · see citing works
Protein‐facilitated transport of hydrophobic molecules across the yeast plasma membrane
Claus, S., Jezierska, S., & Bogaert, I. V. (2019) · FEBS Letters · doi:10.1002/1873-3468.13469 · Cited by 58 · see citing works
Chidley, C., Trauger, S. A., Birsoy, K., & O’Shea, E. K. (2016) · eLife · doi:10.7554/elife.14601 · Cited by 57 · see citing works
Kell, D. B. (2014) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2014.10.005 · Cited by 54 · see citing works
Cocucci, E., Kim, J., Bai, Y., & Pabla, N. (2016) · Clinical Pharmacology & Therapeutics · doi:10.1002/cpt.545 · Cited by 54 · see citing works
Schlessinger, A., Welch, M. A., van Vlijmen, H., Korzekwa, K., Swaan, P. W., & Matsson, P. (2018) · Clinical Pharmacology & Therapeutics · doi:10.1002/cpt.1174 · Cited by 53 · see citing works
In silico drug repositioning: from large-scale transcriptome data to therapeutics
Kwon, O., Kim, W., Cha, H., & Lee, H. (2019) · Archives of Pharmacal Research · doi:10.1007/s12272-019-01176-3 · Cited by 52 · see citing works
Structural basis for the delivery of activated sialic acid into Golgi for sialyation
Nji, E., Gulati, A., Qureshi, A. A., Coincon, M., & Drew, D. (2019) · Nature Structural & Molecular Biology · doi:10.1038/s41594-019-0225-y · Cited by 50 · see citing works
Yuan, P., Mao, X., Chong, K. C., Fu, J., Pan, S., Wu, S., Yu, C., & Yao, S. Q. (2017) · Small · doi:10.1002/smll.201700569 · Cited by 49 · see citing works
A combinatorial screen of the CLOUD uncovers a synergy targeting the androgen receptor
Licciardello, M. P., Ringler, A., Markt, P., Klepsch, F., Lardeau, C.-H., Sdelci, S., Schirghuber, E., Müller, A. C., Caldera, M., Wagner, A., et al. (2017) · Nature Chemical Biology · doi:10.1038/nchembio.2382 · Cited by 48 · see citing works
Self-citationRepair of UV-Induced DNA Damage Independent of Nucleotide Excision Repair Is Masked by MUTYH
Mazouzi, A., Battistini, F., Moser, S. C., da Silva, J. F., Wiedner, M., Owusu, M., Lardeau, C.-H., Ringler, A., Weil, B., Neesen, J., et al. (2017) · Molecular Cell · doi:10.1016/j.molcel.2017.10.021 · Cited by 47 · see citing works
Self-citationYM155 potently triggers cell death in breast cancer cells through an autophagy-NF-kB network
Véquaud, É., Séveno, C., Loussouarn, D., Engelhart, L., Campone, M., Juin, P. P., & Barillé‐Nion, S. (2015) · Oncotarget · doi:10.18632/oncotarget.3638 · Cited by 46 · see citing works
Voges, Y., Michaelis, M., Rothweiler, F., Schaller, T., Schneider, C., Politt, K., Mernberger, M., Nist, A., Stiewe, T., Wass, M. N., et al. (2016) · Cell Death and Disease · doi:10.1038/cddis.2016.257 · Cited by 46 · see citing works
Recent Advances in Nanomedicine and Survivin Targeting in Brain Cancers
Mazur, J., Roy, K., & Kanwar, J. R. (2017) · Nanomedicine · doi:10.2217/nnm-2017-0286 · Cited by 46 · see citing works
Zhao, N., Mao, Y., Han, G., Ju, Q., Zhou, L., Liu, F., Yang, X., & Zhao, X. (2015) · Oncotarget · doi:10.18632/oncotarget.4315 · Cited by 45 · see citing works
Kalxdorf, M., Gade, S., Eberl, H. C., & Bantscheff, M. (2017) · Molecular & Cellular Proteomics · doi:10.1074/mcp.m116.063859 · Cited by 45 · see citing works
Harnessing Solute Carrier Transporters for Precision Oncology
Nyquist, M. D., Prasad, B., & Mostaghel, E. A. (2017) · Molecules · doi:10.3390/molecules22040539 · Cited by 44 · see citing works
Kiyohara, Y., Yoshino, K., Kubota, S., Okuyama, H., Endo, H., Ueda, Y., Kimura, T., Kimura, T., Kamiura, S., & Inoue, M. (2016) · Cancer Science · doi:10.1111/cas.12898 · Cited by 44 · see citing works
Arrayed mutant haploid embryonic stem cell libraries facilitate phenotype-driven genetic screens
Liu, G., Wang, X. L., Liu, Y., Zhang, M., Cai, T., Shen, Z., Jia, Y., & Huang, Y. (2017) · Nucleic Acids Research · doi:10.1093/nar/gkx857 · Cited by 44 · see citing works
Gateway to the Golgi: molecular mechanisms of nucleotide sugar transporters
Parker, J. L., & Newstead, S. L. (2019) · Current Opinion in Structural Biology · doi:10.1016/j.sbi.2019.03.019 · Cited by 42 · see citing works
Quantifying the impact of transporters on cellular drug permeability
Matsson, P., Fenu, L. A., Lundquist, P., Wiśniewski, J. R., Kansy, M., & Artursson, P. (2015) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2015.02.009 · Cited by 41 · see citing works
Shen, H. M., McHale, C. M., Smith, M. T., & Zhang, L. (2015) · Mutation Research/Reviews in Mutation Research · doi:10.1016/j.mrrev.2015.01.002 · Cited by 40 · see citing works
Technical approaches to induce selective cell death of pluripotent stem cells
Jeong, H.-C., Cho, S.-J., Lee, M.-O., & Cha, H.-J. (2017) · Cellular and Molecular Life Sciences · doi:10.1007/s00018-017-2486-0 · Cited by 33 · see citing works
Jindal, S., Yang, L., Day, P. J., & Kell, D. B. (2019) · BMC Microbiology · doi:10.1186/s12866-019-1561-0 · Cited by 40 · see citing works
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Dickens, D., Rädisch, S., Chiduza, G. N., Giannoudis, A., Cross, M. J., Malik, H., Schaeffeler, E., Sison-Young, R. L. C., Wilkinson, E. L., Goldring, C. E., et al. (2018) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.8b00547 · Cited by 39 · see citing works
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He, J., Jin, Y., Zhou, M., Li, X., Chen, W., Wang, Y., Gu, S., Cao, Y., Chu, C., Liu, X., et al. (2017) · Cancer Science · doi:10.1111/cas.13478 · Cited by 38 · see citing works
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Kell, D. B. (2016) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2015.44 · Cited by 37 · see citing works
Ho, S. S., Sim, M. Y., Yee, W.-L. S., Yang, T., Yuen, S. P. J., & Go, M. (2015) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2015.09.026 · Cited by 35 · see citing works
Dai, C.-H., Shu, Y., Chen, P., Wu, J., Zhu, L.-H., Yuan, R., Long, W., Zhu, Y., & Li, J. (2018) · Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease · doi:10.1016/j.bbadis.2018.10.015 · Cited by 34 · see citing works
Radic-Sarikas, B., Halász, M., Huber, K., Winter, G. E., Tsafou, K. P., Papamarkou, T., Brunak, S., Kölch, W., & Superti‐Furga, G. (2017) · Scientific Reports · doi:10.1038/s41598-017-03129-6 · Cited by 33 · see citing works
Self-citationThe human organic cation transporter OCT1 and its role as a target for drug responses
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Chandrasekaran, A. P., Kaushal, K., Park, C., Kim, K.-S., & Ramakrishna, S. (2021) · Theranostics · doi:10.7150/thno.63806 · Cited by 33 · see citing works
Reactive Oxygen Species Synergize To Potently and Selectively Induce Cancer Cell Death
Lee, H. Y., Parkinson, E. I., Granchi, C., Paterni, I., Panigrahy, D., Seth, P., Minutolo, F., & Hergenrother, P. J. (2017) · ACS Chemical Biology · doi:10.1021/acschembio.7b00015 · Cited by 32 · see citing works
Fitting Transporter Activities to Cellular Drug Concentrations and Fluxes: Why the Bumblebee Can Fly
Mendes, P., Oliver, S. G., & Kell, D. B. (2015) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2015.07.006 · Cited by 30 · see citing works
The efflux pump ABCC1/MRP1 constitutively restricts PROTAC sensitivity in cancer cells
Wolf, G., Craigon, C., Teoh, S. T., Essletzbichler, P., Onstein, S., Cassidy, D. M., Uijttewaal, E. C. H., Dvorak, V., Cao, Y., Bensimon, A., et al. (2025) · Cell chemical biology · doi:10.1016/j.chembiol.2024.11.009 · Cited by 31 · see citing works
Self-citationO’Hagan, S., & Kell, D. B. (2016) · Frontiers in Pharmacology · doi:10.3389/fphar.2016.00266 · Cited by 29 · see citing works
The Pathognomonic FOXL2 C134W Mutation Alters DNA-Binding Specificity
Carles, A., Trigo‐Gonzalez, G., Cao, Q., Cheng, S., Moksa, M., Bilenky, M., Huntsman, D. D., Morin, G. B., & Hirst, M. (2020) · Cancer Research · doi:10.1158/0008-5472.can-20-0104 · Cited by 30 · see citing works
Causes and Significance of Increased Compound Potency in Cellular or Physiological Contexts
Schwaid, A. G., & Cornella‐Taracido, I. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b00762 · Cited by 29 · see citing works
Wani, T. H., Surendran, S., Jana, A., Chakrabarty, A., & Chowdhury, G. (2018) · Chemical Research in Toxicology · doi:10.1021/acs.chemrestox.8b00094 · Cited by 29 · see citing works
Che, B., Du, Y., Yuan, R., Xiao, H., Zhang, W., Shao, J., Lu, H., Yu, Y., Xiang, M., Hao, L., et al. (2023) · Oncogene · doi:10.1038/s41388-023-02843-y · Cited by 29 · see citing works
O’Hagan, S., & Kell, D. B. (2017) · Journal of Cheminformatics · doi:10.1186/s13321-017-0198-y · Cited by 26 · see citing works
Kim, K.-T., Park, J.-C., Jang, H., Lee, H., Park, S., Kim, J., Kwon, O., Go, Y.-H., Jin, Y., Kim, W., et al. (2020) · Biomaterials · doi:10.1016/j.biomaterials.2020.120295 · Cited by 26 · see citing works
Evaluating Cellular Drug Uptake with Fluorescent Sensor Proteins
Scarabelli, S., Tan, K., Griss, R., Hovius, R., D’Alessandro, P. L., Vorherr, T. E., & Johnsson, K. (2017) · ACS Sensors · doi:10.1021/acssensors.7b00331 · Cited by 28 · see citing works
YM155 inhibits topoisomerase function
Hong, M., Ren, M., Silva, J., Paul, A., Wilson, W. D., Schroeder, C., Weinberger, P., Janik, J. E., & Hao, Z. (2016) · Anti-Cancer Drugs · doi:10.1097/cad.0000000000000441 · Cited by 26 · see citing works
Grixti, J. M., O’Hagan, S., Day, P. J., & Kell, D. B. (2017) · Frontiers in Pharmacology · doi:10.3389/fphar.2017.00155 · Cited by 27 · see citing works
The mystery of the human proton-organic cation antiporter: One transport protein or many?
Sachkova, A., Jensen, O., Dücker, C., Ansari, S., & Brockmöller, J. (2022) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2022.108283 · Cited by 25 · see citing works
Mochizuki, T., Mizuno, T., Kurosawa, T., Yamaguchi, T., Higuchi, K., Tega, Y., Nozaki, Y., Kawabata, K., Deguchi, Y., & Kusuhara, H. (2020) · Drug Metabolism and Disposition · doi:10.1124/dmd.120.000115 · Cited by 25 · see citing works
Neophytou, C. M., Mesaritis, A., Gregoriou, G., & Constantinou, A. I. (2019) · Scientific Reports · doi:10.1038/s41598-019-50884-9 · Cited by 24 · see citing works
Guo, K. X., Huang, P., Xu, N., Xu, P., Kaku, H., Zheng, S., Xu, A., Matsuura, E., Liu, C., & Kumon, H. (2015) · Oncotarget · doi:10.18632/oncotarget.4121 · Cited by 23 · see citing works
In silico Prioritization of Transporter–Drug Relationships From Drug Sensitivity Screens
César‐Razquin, A., Girardi, E., Yang, M., Brehme, M., Sáez-Rodríguez, J., & Superti‐Furga, G. (2018) · Frontiers in Pharmacology · doi:10.3389/fphar.2018.01011 · Cited by 23 · see citing works
Self-citationCui, Q., Huang, C., Liu, J., & Zhang, J. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c01130 · Cited by 23 · see citing works
Xia, H., Chen, J., Shi, M., Deivasigamani, A., Ooi, L. L., & Hui, K. M. (2015) · Oncotarget · doi:10.18632/oncotarget.3337 · Cited by 23 · see citing works
Hyperthermia induces apoptosis by targeting Survivin in esophageal cancer
Qin, S., Xu, C., Li, S., Wang, X., Sun, X., Wang, P., Zhang, B., & Ren, H. (2015) · Oncology Reports · doi:10.3892/or.2015.4252 · Cited by 23 · see citing works
Hunting Viral Receptors Using Haploid Cells
Pillay, S., & Carette, J. E. (2015) · Annual Review of Virology · doi:10.1146/annurev-virology-100114-055119 · Cited by 23 · see citing works
Exploiting AR-Regulated Drug Transport to Induce Sensitivity to the Survivin Inhibitor YM155
Nyquist, M. D., Corella, A. N., Burns, J., Coleman, I. M., Gao, S., Tharakan, R., Riggan, L., Cai, C., Corey, E., Nelson, P. S., et al. (2017) · Molecular Cancer Research · doi:10.1158/1541-7786.mcr-16-0315 · Cited by 23 · see citing works
Kotolloshi, R., Hölzer, M., Gajda, M. R., Grimm, M., & Steinbach, D. (2021) · Cells · doi:10.3390/cells10010080 · Cited by 22 · see citing works
Kell, D. B. (2015) · Perspectives in Science · doi:10.1016/j.pisc.2015.06.004 · Cited by 21 · see citing works
Systematic identification of biomarker-driven drug combinations to overcome resistance
Rees, M. G., Brenan, L., DoCarmo, M., Duggan, P., Bajrami, B., Arciprete, M., Boghossian, A. S., Vaimberg, E. W., Ferrara, S. J., Lewis, T. A., et al. (2022) · Nature Chemical Biology · doi:10.1038/s41589-022-00996-7 · Cited by 21 · see citing works
Metabolic mapping of the human solute carrier superfamily
Wiedmer, T., Teoh, S. T., Christodoulaki, E., Wolf, G., Tian, C., Sedlyarov, V., Jarret, A. P., Leippe, P., Frommelt, F., Inglés‐Prieto, Á., et al. (2025) · Molecular Systems Biology · doi:10.1038/s44320-025-00106-4 · Cited by 21 · see citing works
Self-citationThe solute carrier superfamily interactome
Frommelt, F., Ladurner, R., Goldmann, U., Wolf, G., Inglés‐Prieto, Á., Liñeiro, E., Gelová, Z., Hopp, A.-K., Christodoulaki, E., Teoh, S. T., et al. (2025) · Molecular Systems Biology · doi:10.1038/s44320-025-00109-1 · Cited by 20 · see citing works
Self-citationLi, W. L., Lee, M.-R., & Cho, M.-Y. (2016) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2016.02.009 · Cited by 20 · see citing works
Recent advances in understanding hepatic drug transport
Stieger, B., & Hagenbuch, B. (2016) · F1000Research · doi:10.12688/f1000research.9466.1 · Cited by 19 · see citing works
Ahenkorah, S., Coertzen, D., Tong, J. X., Fridianto, K. T., Wittlin, S., Birkholtz, L., Tan, K. S. W., Lam, Y., Go, M., & Haynes, R. K. (2019) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.9b00457 · Cited by 19 · see citing works
Membrane Transporters Involved in the Antimicrobial Activities of Pyrithione in Escherichia coli
Salcedo-Sora, J. E., Robison, A. T. R., Zaengle-Barone, J. M., Franz, K. J., & Kell, D. B. (2021) · Molecules · doi:10.3390/molecules26195826 · Cited by 17 · see citing works
Lone, I. M., Nabi, A., Dar, N. J., Hussain, A., Nazam, N., Hamid, A., & Ahmad, W. (2016) · Chemosphere · doi:10.1016/j.chemosphere.2016.08.131 · Cited by 19 · see citing works
West, T. J., Bi, J., Martínez‐Peña, F., Curtis, E. J., Gazaniga, N. R., Mischel, P. S., & Lairson, L. L. (2023) · Journal of the American Chemical Society · doi:10.1021/jacs.2c11715 · Cited by 16 · see citing works
Selection of Effective Therapies Using Three-Dimensional in vitro Modeling of Chondrosarcoma
Palubeckaitė, I., Venneker, S., Bruijn, I. H. B., van den Akker, B. E., Krol, A. D. G., Gelderblom, H. A. J., & Bovée, J. V. M. G. (2020) · Frontiers in Molecular Biosciences · doi:10.3389/fmolb.2020.566291 · Cited by 16 · see citing works
Kell, D. B. (2021) · Advances in microbial physiology/Advances in Microbial Physiology · doi:10.1016/bs.ampbs.2021.01.001 · Cited by 16 · see citing works
Go, Y., Lim, C., Jeong, H.-C., Kwon, O.-S., Chung, S., Lee, H., Kim, W., Suh, Y., Son, W.-S., Lee, M.-O., et al. (2019) · Frontiers in Chemistry · doi:10.3389/fchem.2019.00298 · Cited by 13 · see citing works
Wani, T. H., Chowdhury, G., & Chakrabarty, A. (2021) · RSC Medicinal Chemistry · doi:10.1039/d0md00383b · Cited by 15 · see citing works
Application of CRISPR-Cas9 System to Study Biological Barriers to Drug Delivery
He, J., Biswas, R., Bugde, P., Li, J., Liu, D., & Li, Y. (2022) · Pharmaceutics · doi:10.3390/pharmaceutics14050894 · Cited by 15 · see citing works
Chiou, J., Lee, Y., Huang, C., Wang, L., Shi, Y., & Chang, L. (2021) · Biochemical Pharmacology · doi:10.1016/j.bcp.2021.114544 · Cited by 15 · see citing works
Hao, Y., Langford, T. F., Moon, S. J., Eller, K. A., & Sikes, H. D. (2021) · Cell chemical biology · doi:10.1016/j.chembiol.2021.09.003 · Cited by 15 · see citing works
High doses of alcohol during pregnancy cause DNA damages in osteoblasts of newborns rats
Carvalho, I. C. S., Dutra, T. P., de Andrade, D. P., Balducci, I., Soares, C. P., & da Rocha, R. F. (2015) · Birth Defects Research Part A Clinical and Molecular Teratology · doi:10.1002/bdra.23468 · Cited by 14 · see citing works
Kangaspeska, S., Hultsch, S., Jaiswal, A., Edgren, H., Mpindi, J.-P., Eldfors, S., Brück, O. E., Aittokallio, T. A., & Kallioniemi, O. (2016) · BMC Cancer · doi:10.1186/s12885-016-2452-5 · Cited by 14 · see citing works
Biotoxins Mediated DNA Damage and Role of Phytochemicals in DNA Protection
Singh, N., & Sharma, B. (2018) · Biochemistry & Molecular Biology Journal · doi:10.21767/2471-8084.100054 · Cited by 14 · see citing works
- Authors
- Winter, G. E., Radic, B., Mayor-Ruiz, C., Blomen, V. A., Trefzer, C., Kandasamy, R. K., Huber, K. V. M., Gridling, M., Chen, D., Klampfl, T., Kralovics, R., Kubicek, S., Fernandez-Capetillo, O., Brummelkamp, T. R., & Superti-Furga, G.
- Affiliations
- Austrian Academy of Sciences (AT)
- The Netherlands Cancer Institute (NL)
- ORCID
- Venue
- Nature Chemical Biology
- Published
- 2014-07-27
- Volume
- 10
- Issue
- 9
- Pages
- 768-773
- ISSN
- 1552-4450 (ISSN-L)
- 1552-4469
- PMC
- PMC4913867
- OpenAlex
- W2057000572
- Cited by
- 175
- References
- 35
- Citations by year
- 2026: 5 · 2025: 9 · 2024: 5 · 2023: 12 · 2022: 8 · 2021: 12 · 2020: 18 · 2019: 17 · 2018: 12 · 2017: 24 · 2016: 19 · 2015: 29 · 2014: 3
- FWCI
- 12.05
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Nature Chemical Biology (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- FreiDok plus (Universitätsbibliothek Freiburg) (submittedVersion)
- Topics
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Cancer therapeutics and mechanisms
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Toxicology › Bioactive Compounds and Antitumor Agents
- Keywords
- YM155, drug importation, solute carrier proteins, genotoxic chemotherapy, anticancer drug sensitivity, DNA intercalation, cancer cell lines
- MeSH terms
- Animals, Cell Division, Cell Survival, Cloning, Molecular, DNA Damage, Haploidy, Humans, Imidazoles, Immunohistochemistry, Intercalating Agents, Naphthoquinones, RNA, Neoplasm, Genome, Human, Mice, SCID, Apoptosis, Comet Assay, Membrane Transport Proteins, Cell Line, Tumor, Mice
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