Publications
Selected publications
- Biomarkers of NRF2 signalling: Current status and future challenges. (Journal article - 2024)
- Advances and challenges in therapeutic targeting of NRF2 (Journal article - 2023)
- Pharmacological Activation of Nrf2 Enhances Functional Liver Regeneration (Journal article - 2021)
- Managing the challenge of drug-induced liver injury: a roadmap for the development and deployment of preclinical predictive models (Journal article - 2020)
- Characterisation of the NRF2 transcriptional network and its response to chemical insult in primary human hepatocytes: implications for prediction of drug-induced liver injury (Journal article - 2019)
2024
Limitations of acetaminophen as a reference hepatotoxin for the evaluation of in vitro liver models
Livoti, L. A., Sison-Young, R., Reddyhoff, D., Fisher, C. P., Gardner, I., Diaz-Nieto, R., . . . Copple, I. M. (n.d.). Limitations of acetaminophen as a reference hepatotoxin for the evaluation of in vitro liver models. Toxicological Sciences. doi:10.1093/toxsci/kfae133
Biomarkers of NRF2 signalling: Current status and future challenges.
Morgenstern, C., Lastres-Becker, I., Demirdöğen, B. C., Costa, V. M., Daiber, A., Foresti, R., . . . Copple, I. M. (2024). Biomarkers of NRF2 signalling: Current status and future challenges.. Redox biology, 72, 103134. doi:10.1016/j.redox.2024.103134
2023
A systems approach reveals species differences in hepatic stress response capacity
Russomanno, G., Sison-Young, R., Livoti, L. A., Coghlan, H., Jenkins, R. E., Kunnen, S. J., . . . Copple, I. M. (2023). A systems approach reveals species differences in hepatic stress response capacity. TOXICOLOGICAL SCIENCES. doi:10.1093/toxsci/kfad085
Modulating the expression of tumor suppressor genes using activating oligonucleotide technologies as a therapeutic approach in cancer
Gregory, G. L., & Copple, I. M. (2023). Modulating the expression of tumor suppressor genes using activating oligonucleotide technologies as a therapeutic approach in cancer. MOLECULAR THERAPY-NUCLEIC ACIDS, 31, 211-223. doi:10.1016/j.omtn.2022.12.016
Advances and challenges in therapeutic targeting of NRF2
Dinkova-Kostova, A. T., & Copple, I. M. (2023). Advances and challenges in therapeutic targeting of NRF2. TRENDS IN PHARMACOLOGICAL SCIENCES, 44(3), 137-149. doi:10.1016/j.tips.2022.12.003
2022
Interruption of bile acid uptake by hepatocytes after acetaminophen overdose ameliorates hepatotoxicity
Ghallab, A., Hassan, R., Hofmann, U., Friebel, A., Hobloss, Z., Brackhagen, L., . . . Hengstler, J. G. (2022). Interruption of bile acid uptake by hepatocytes after acetaminophen overdose ameliorates hepatotoxicity. JOURNAL OF HEPATOLOGY, 77(1), 71-83. doi:10.1016/j.jhep.2022.01.020
2021
Pharmacological Activation of Nrf2 Enhances Functional Liver Regeneration
Chan, B. K. Y., Elmasry, M., Forootan, S. S., Russomanno, G., Bunday, T. M., Zhang, F., . . . Copple, I. M. (2021). Pharmacological Activation of Nrf2 Enhances Functional Liver Regeneration. HEPATOLOGY, 74(2), 973-986. doi:10.1002/hep.31859
Gene signatures reduce the stress of preclinical drug hepatotoxicity screening.
Copple, I. M., Park, B. K., & Goldring, C. E. (2021). Gene signatures reduce the stress of preclinical drug hepatotoxicity screening.. Hepatology (Baltimore, Md.). doi:10.1002/hep.31736
2020
Managing the challenge of drug-induced liver injury: a roadmap for the development and deployment of preclinical predictive models
Weaver, R. J., Blomme, E. A., Chadwick, A. E., Copple, I. M., Gerets, H. H. J., Goldring, C. E., . . . Park, B. K. (2020). Managing the challenge of drug-induced liver injury: a roadmap for the development and deployment of preclinical predictive models. NATURE REVIEWS DRUG DISCOVERY, 19(2), 131-148. doi:10.1038/s41573-019-0048-x
2019
SFX-01 reduces residual disability after experimental autoimmune encephalomyelitis
Galea, I., Copple, I. M., Howat, D. W., & Franklin, S. (2019). SFX-01 reduces residual disability after experimental autoimmune encephalomyelitis. MULTIPLE SCLEROSIS AND RELATED DISORDERS, 30, 257-261. doi:10.1016/j.msard.2019.02.027
Attenuation of doxorubicin-induced cardiotoxicity in a human in vitro cardiac model by the induction of the NRF-2 pathway
Tomlinison, L., Lu, Z. Q., Bentley, R., Colley, H., Murdoch, C., Webb, S., . . . Sharma, P. (n.d.). Attenuation of doxorubicin-induced cardiotoxicity in a human in vitro cardiac model by the induction of the NRF-2 pathway. Biomedicine and Pharmacotherapy. doi:10.1016/j.biopha.2019.108637
Characterisation of the NRF2 transcriptional network and its response to chemical insult in primary human hepatocytes: implications for prediction of drug-induced liver injury
Copple, I. M., den Hollander, W., Callegaro, G., Mutter, F. E., Maggs, J. L., Schofield, A. L., . . . Park, B. K. (2019). Characterisation of the NRF2 transcriptional network and its response to chemical insult in primary human hepatocytes: implications for prediction of drug-induced liver injury. Archives of Toxicology, 93, 385-399. doi:10.1007/s00204-018-2354-1
Correction: The Nrf2 inhibitor brusatol is a potent antitumour agent in an orthotopic mouse model of colorectal cancer.
Evans, J. P., Winiarski, B. K., Sutton, P. A., Jones, R. P., Ressel, L., Duckworth, C. A., . . . Kitteringham, N. R. (2019). Correction: The Nrf2 inhibitor brusatol is a potent antitumour agent in an orthotopic mouse model of colorectal cancer.. Oncotarget, 10(6), 685. doi:10.18632/oncotarget.26625
2018
The Nrf2 inhibitor brusatol is a potent antitumour agent in an orthotopic mouse model of colorectal cancer
Evans, J. P., Winiarski, B. K., Sutton, P. A., Jones, R. P., Ressel, L., Duckworth, C. A., . . . Kitteringham, N. R. (2018). The Nrf2 inhibitor brusatol is a potent antitumour agent in an orthotopic mouse model of colorectal cancer. Oncotarget, 9(43), 27104-27116. doi:10.18632/oncotarget.25497
NRF2 regulates the glutamine transporter Slc38a3 (SNAT3) in kidney in response to metabolic acidosis
Lister, A., Bourgeois, S., Silva, P. H. I., Rubio-Aliaga, I., Marbet, P., Walsh, J., . . . Odermatt, A. (2018). NRF2 regulates the glutamine transporter Slc38a3 (SNAT3) in kidney in response to metabolic acidosis. SCIENTIFIC REPORTS, 8. doi:10.1038/s41598-018-24000-2
2017
Real-time in vivo imaging reveals localised Nrf2 stress responses associated with direct and metabolism-dependent drug toxicity
Forootan, S. S., Mutter, F. E., Kipar, A., Iwawaki, T., Francis, B., Goldring, C. E., . . . Copple, I. M. (2017). Real-time in vivo imaging reveals localised Nrf2 stress responses associated with direct and metabolism-dependent drug toxicity. SCIENTIFIC REPORTS, 7, 11 pages. doi:10.1038/s41598-017-16491-2
Characterisation of drug-specific signalling between primary human hepatocytes and immune cells.
Ogese, M. O., Faulkner, L., Jenkins, R. E., French, N. S., Copple, I. M., Antoine, D. J., . . . Naisbitt, D. J. (2017). Characterization of Drug-Specific Signaling Between Primary Human Hepatocytes and Immune Cells. TOXICOLOGICAL SCIENCES, 158(1), 76-89. doi:10.1093/toxsci/kfx069
Circulating levels of miR-122 increase post-mortem, particularly following lethal dosing with pentobarbital sodium: implications for pre-clinical liver injury studies
Clarke, J. I., Forootan, S. S., Lea, J. D., Howell, L. S., Rodriguez, J. M., Kipar, A., . . . Antoine, D. J. (2017). Circulating levels of miR-122 increase post-mortem, particularly following lethal dosing with pentobarbital sodium: implications for pre-clinical liver injury studies. TOXICOLOGY RESEARCH, 6(4), 406-411. doi:10.1039/c6tx00442c
Optimising the use of medicines to reduce acute kidney injury in children and babies
Oni, L., Hawcutt, D. B., Turner, M. A., Beresford, M. W., McWilliam, S., Barton, C., . . . Antoine, D. J. (2017). Optimising the use of medicines to reduce acute kidney injury in children and babies. Pharmacology and Therapeutics, 174, 55-62. doi:10.1016/j.pharmthera.2017.02.018
A tetraoxane-based antimalarial drug candidate that overcomes PfK13-C580Y dependent artemisinin resistance
O'Neill, P. M., Amewu, R. K., Charman, S. A., Sabbani, S., Gnädig, N. F., Straimer, J., . . . Ward, S. A. (2017). A tetraoxane-based antimalarial drug candidate that overcomes PfK13-C580Y dependent artemisinin resistance. Nature Communications, 8. doi:10.1038/ncomms15159
NRF2 as an Emerging Therapeutic Target
Copple, I. M., Dinkova-Kostova, A. T., Kensler, T. W., Liby, K. T., & Wigley, W. C. (2017). NRF2 as an Emerging Therapeutic Target. OXIDATIVE MEDICINE AND CELLULAR LONGEVITY, 2017. doi:10.1155/2017/8165458
2016
Design and Synthesis of Irreversible Analogues of Bardoxolone Methyl for the Identification of Pharmacologically Relevant Targets and Interaction Sites
Wong, M. H. L., Bryan, H. K., Copple, I. M., Jenkins, R. E., Chiu, P. H., Bibby, J., . . . Park, B. K. (2016). Design and Synthesis of Irreversible Analogues of Bardoxolone Methyl for the Identification of Pharmacologically Relevant Targets and Interaction Sites. JOURNAL OF MEDICINAL CHEMISTRY, 59(6), 2396-2409. doi:10.1021/acs.jmedchem.5b01292
Roles of Nrf2 in drug and chemical toxicity
Clarke, J. L., Murray, J. B., Park, B. K., & Copple, I. M. (2016). Roles of Nrf2 in drug and chemical toxicity. Current Opinion in Toxicology, 1, 104-110. doi:10.1016/j.cotox.2016.10.004
2015
Integrated transcriptomic and proteomic analyses uncover regulatory roles of Nrf2 in the kidney
Shelton, L. M., Lister, A., Walsh, J., Jenkins, R. E., Wong, M. H. L., Rowe, C., . . . Copple, I. M. (2015). Integrated transcriptomic and proteomic analyses uncover regulatory roles of Nrf2 in the kidney. KIDNEY INTERNATIONAL, 88(06), 1261-1273. doi:10.1038/ki.2015.286
Value of monitoring Nrf2 activity for the detection of chemical and oxidative stress
Mutter, F. E., Park, B. K., & Copple, I. M. (2015). Value of monitoring Nrf2 activity for the detection of chemical and oxidative stress. BIOCHEMICAL SOCIETY TRANSACTIONS, 43, 657-662. doi:10.1042/BST20150044
Brusatol provokes a rapid and transient inhibition of Nrf2 signaling and sensitizes mammalian cells to chemical toxicity—implications for therapeutic targeting of Nrf2
Olayanju, A., Copple, I. M., Bryan, H. K., Edge, G. T., Sison, R. L., Wong, M. W., . . . Park, B. K. (2015). Brusatol provokes a rapid and transient inhibition of Nrf2 signaling and sensitizes mammalian cells to chemical toxicity—implications for therapeutic targeting of Nrf2. Free Radical Biology and Medicine, 78, 202-212. doi:10.1016/j.freeradbiomed.2014.11.003
2014
Identification and quantification of the basal and inducible Nrf2-dependent proteomes in mouse liver: Biochemical, pharmacological and toxicological implications
Walsh, J., Jenkins, R. E., Wong, M., Olayanju, A., Powell, H., Copple, I., . . . Park, B. K. (2014). Identification and quantification of the basal and inducible Nrf2-dependent proteomes in mouse liver: Biochemical, pharmacological and toxicological implications. JOURNAL OF PROTEOMICS, 108, 171-187. doi:10.1016/j.jprot.2014.05.007
Chemical Tuning Enhances Both Potency Toward Nrf2 and In Vitro Therapeutic Index of Triterpenoids
Copple, I., Shelton, L. M., Walsh, J., Kratschmar, D. V., Lister, A., Odermatt, A., . . . Park, K. (2014). Chemical Tuning Enhances Both Potency Toward Nrf2 and In Vitro Therapeutic Index of Triterpenoids. Toxicological Sciences, 140(2), 462-469. doi:10.1093/toxsci/kfu080
Chemical Tuning Enhances Both Potency Toward Nrf2 and In Vitro Therapeutic Index of Triterpenoids
Copple, I. M., Shelton, L. M., Walsh, J., Kratschmar, D. V., Lister, A., Odermatt, A., . . . Park, B. K. (2014). Chemical Tuning Enhances Both Potency Toward Nrf2 and In Vitro Therapeutic Index of Triterpenoids. Toxicological Sciences, 140(2), 462-469. doi:10.1093/toxsci/kfu080
2013
The S349T mutation of <i>SQSTM1</i> links Keap1/Nrf2 signalling to Paget's disease of bone
Wright, T., Rea, S. L., Goode, A., Bennett, A. J., Ratajczak, T., Long, J. E., . . . Layfield, R. (2013). The S349T mutation of <i>SQSTM1</i> links Keap1/Nrf2 signalling to Paget's disease of bone. BONE, 52(2), 699-706. doi:10.1016/j.bone.2012.10.023
Role of Nrf2 in protection against acute kidney injury
Shelton, L. M., Park, B. K., & Copple, I. M. (2013). Role of Nrf2 in protection against acute kidney injury. KIDNEY INTERNATIONAL, 84(6), 1090-1095. doi:10.1038/ki.2013.248
2012
Examination of the Cytotoxic and Embryotoxic Potential and Underlying Mechanisms of Next-Generation Synthetic Trioxolane and Tetraoxane Antimalarials
Copple, I. M., Mercer, A. E., Firman, J., Donegan, G., Herpers, B., Wong, M. H. L., . . . Park, B. K. (2012). Examination of the Cytotoxic and Embryotoxic Potential and Underlying Mechanisms of Next-Generation Synthetic Trioxolane and Tetraoxane Antimalarials. MOLECULAR MEDICINE, 18(7), 1045-1055. doi:10.2119/molmed.2012.00154
The Keap1-Nrf2 Cell Defense Pathway - A Promising Therapeutic Target?
Copple, I. M. (2012). The Keap1-Nrf2 Cell Defense Pathway - A Promising Therapeutic Target?. CURRENT CONCEPTS IN DRUG METABOLISM AND TOXICOLOGY, 63, 43-79. doi:10.1016/B978-0-12-398339-8.00002-1
2011
Nrf2 is overexpressed in pancreatic cancer: implications for cell proliferation and therapy
Lister, A., Nedjadi, T., Kitteringham, N. R., Campbell, F., Costello, E., Lloyd, B., . . . Park, B. K. (2011). Nrf2 is overexpressed in pancreatic cancer: implications for cell proliferation and therapy. MOLECULAR CANCER, 10. doi:10.1186/1476-4598-10-37
The Role of Heme and the Mitochondrion in the Chemical and Molecular Mechanisms of Mammalian Cell Death Induced by the Artemisinin Antimalarials
Mercer, A. E., Copple, I. M., Maggs, J. L., O'Neill, P. M., & Park, B. K. (2011). The Role of Heme and the Mitochondrion in the Chemical and Molecular Mechanisms of Mammalian Cell Death Induced by the Artemisinin Antimalarials. JOURNAL OF BIOLOGICAL CHEMISTRY, 286(2), 987-996. doi:10.1074/jbc.M110.144188
2010
Physical and Functional Interaction of Sequestosome 1 with Keap1 Regulates the Keap1-Nrf2 Cell Defense Pathway
Copple, I. M., Lister, A., Obeng, A. D., Kitteringham, N. R., Jenkins, R. E., Layfield, R., . . . Park, B. K. (2010). Physical and Functional Interaction of Sequestosome 1 with Keap1 Regulates the Keap1-Nrf2 Cell Defense Pathway. JOURNAL OF BIOLOGICAL CHEMISTRY, 285(22), 16782-16788. doi:10.1074/jbc.M109.096545
The keap1-nrf2 cellular defense pathway: mechanisms of regulation and role in protection against drug-induced toxicity.
Copple, I. M., Goldring, C. E., Kitteringham, N. R., & Park, B. K. (2010). The keap1-nrf2 cellular defense pathway: mechanisms of regulation and role in protection against drug-induced toxicity.. Handbook of experimental pharmacology, (196), 233-266. doi:10.1007/978-3-642-00663-0_9
2009
Extract of <i>Ginkgo biloba</i> induces glutathione-S-transferase subunit-P1 <i>in vitro</i>
Liu, X. -P., Goldring, C. E. P., Wang, H. -Y., Copple, I. M., Kitteringham, N. R., & Park, B. K. (2009). Extract of <i>Ginkgo biloba</i> induces glutathione-S-transferase subunit-P1 <i>in vitro</i>. PHYTOMEDICINE, 16(5), 451-455. doi:10.1016/j.phymed.2008.11.001
2008
The hepatotoxic metabolite of acetaminophen directly activates the Keap1-Nrf2 cell defense system
Copple, I. M., Goldring, C. E., Jenkins, R. E., Chia, A. J. L., Randle, L. E., Hayes, J. D., . . . Park, B. K. (2008). The hepatotoxic metabolite of acetaminophen directly activates the Keap1-Nrf2 cell defense system. HEPATOLOGY, 48(4), 1292-1301. doi:10.1002/hep.22472
The Nrf2-Keapl defence pathway: Role in protection against drug-induced toxicity
Copple, I. M., Goldring, C. E., Kitteringham, N. R., & Park, B. K. (2008). The Nrf2-Keapl defence pathway: Role in protection against drug-induced toxicity. TOXICOLOGY, 246(1), 24-33. doi:10.1016/j.tox.2007.10.029
Extract of <i>Ginkgo biloba</i> induces glutamate cysteine ligase catalytic subunit (GCLC)
Liu, X. -P., Goldring, C. E. P., Wang, H. -Y., Copple, I. M., Kitteringharn, N. R., Park, B. K., & Wei, W. (2008). Extract of <i>Ginkgo biloba</i> induces glutamate cysteine ligase catalytic subunit (GCLC). PHYTOTHERAPY RESEARCH, 22(3), 367-371. doi:10.1002/ptr.2328
2007
Extract of <i>Ginkgo biloba</i> induces phase 2 genes through Keap1-Nrf2-ARE signaling pathway
Liu, X. -P., Goldring, C. E. P., Copple, I. M., Wang, H. -Y., Wei, W., Kitteringham, N. R., & Park, B. K. (2007). Extract of <i>Ginkgo biloba</i> induces phase 2 genes through Keap1-Nrf2-ARE signaling pathway. LIFE SCIENCES, 80(17), 1586-1591. doi:10.1016/j.lfs.2007.01.034
2006
Plasticity in cell defence: access to and reactivity of critical protein residues and DNA response elements
Goldring, C., Kitteringham, N., Jenkins, R., Copple, I., Jeannin, J. F., & Park, B. K. (2006). Plasticity in cell defence: access to and reactivity of critical protein residues and DNA response elements. JOURNAL OF EXPERIMENTAL BIOLOGY, 209(12), 2337-2343. doi:10.1242/jeb.02209