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A time-resolved Förster resonance energy transfer assay to investigate drug and inhibitor binding to ABCG2 (2024)
Journal Article
Mitchell-White, J. I., Briggs, D. A., Mistry, S. J., Mbiwan, H. A., Kellam, B., Holliday, N. D., …Kerr, I. D. (2024). A time-resolved Förster resonance energy transfer assay to investigate drug and inhibitor binding to ABCG2. Archives of Biochemistry and Biophysics, 753, Article 109915. https://doi.org/10.1016/j.abb.2024.109915

The human ATP-binding cassette (ABC) transporter, ABCG2, is responsible for multidrug resistance in some tumours. Detailed knowledge of its activity is crucial for understanding drug transport and resistance in cancer, and has implications for wider... Read More about A time-resolved Förster resonance energy transfer assay to investigate drug and inhibitor binding to ABCG2.

A time-resolved Förster resonance energy transfer assay to investigate inhibitor binding to ABCG2 (2023)
Working Paper
Mitchell-White, J. I., Briggs, D. A., Mistry, S. J., Mbiwan, H. A., Kellam, B., Holliday, N. D., …Kerr, I. D. A time-resolved Förster resonance energy transfer assay to investigate inhibitor binding to ABCG2

The human ATP-binding cassette (ABC) transporter, ABCG2 is responsible for multidrug resistance in some tumours. Detailed knowledge of its activity is crucial for understanding drug transport and resistance in cancer, and has implications for wider p... Read More about A time-resolved Förster resonance energy transfer assay to investigate inhibitor binding to ABCG2.

Mechanistic insight into the role of AUXIN RESISTANCE4 in trafficking of AUXIN1 and LIKE AUX1-2 (2023)
Journal Article
Tidy, A., Abu Bakar, N., Carrier, D., Kerr, I. D., Hodgman, C., Bennett, M. J., & Swarup, R. (2024). Mechanistic insight into the role of AUXIN RESISTANCE4 in trafficking of AUXIN1 and LIKE AUX1-2. Plant Physiology, 194(1), 422-433. https://doi.org/10.1093/plphys/kiad506

AUXIN RESISTANCE4 (AXR4) regulates the trafficking of auxin influx carrier AUXIN1 (AUX1), a plasma-membrane protein that predominantly localizes to the endoplasmic reticulum (ER) in the absence of AXR4. In Arabidopsis (Arabidopsis thaliana), AUX1 is... Read More about Mechanistic insight into the role of AUXIN RESISTANCE4 in trafficking of AUXIN1 and LIKE AUX1-2.

Extracellular Vesicles Potentiate Medulloblastoma Metastasis in an EMMPRIN and MMP-2 Dependent Manner (2023)
Journal Article
Jackson, H. K., Mitoko, C., Linke, F., Macarthur, D., Kerr, I. D., & Coyle, B. (2023). Extracellular Vesicles Potentiate Medulloblastoma Metastasis in an EMMPRIN and MMP-2 Dependent Manner. Cancers, 15(9), Article 2601. https://doi.org/10.3390/cancers15092601

Extracellular vesicles (EVs) have emerged as pivotal mediators of communication in the tumour microenvironment. More specifically, nanosized extracellular vesicles termed exosomes have been shown to contribute to the establishment of a premetastatic... Read More about Extracellular Vesicles Potentiate Medulloblastoma Metastasis in an EMMPRIN and MMP-2 Dependent Manner.

Drug Resistance in Medulloblastoma Is Driven by YB-1, ABCB1 and a Seven-Gene Drug Signature (2023)
Journal Article
Taylor, L., Wade, P. K., Johnson, J. E. C., Aldighieri, M., Morlando, S., Di Leva, G., …Coyle, B. (2023). Drug Resistance in Medulloblastoma Is Driven by YB-1, ABCB1 and a Seven-Gene Drug Signature. Cancers, 15(4), Article 1086. https://doi.org/10.3390/cancers15041086

Therapy resistance represents an unmet challenge in the treatment of medulloblastoma. Accordingly, the identification of targets that mark drug-resistant cell populations, or drive the proliferation of resistant cells, may improve treatment strategie... Read More about Drug Resistance in Medulloblastoma Is Driven by YB-1, ABCB1 and a Seven-Gene Drug Signature.

Identifying new biomarkers of aggressive Group 3 and SHH medulloblastoma using 3D hydrogel models, single cell RNA sequencing and 3D OrbiSIMS imaging (2023)
Journal Article
Linke, F., Johnson, J. E. C., Kern, S., Bennett, C. D., Lourdusamy, A., Lea, D., …Coyle, B. (2023). Identifying new biomarkers of aggressive Group 3 and SHH medulloblastoma using 3D hydrogel models, single cell RNA sequencing and 3D OrbiSIMS imaging. Acta Neuropathologica Communications, 11(1), Article 6. https://doi.org/10.1186/s40478-022-01496-4

The most common malignant brain tumour in children, medulloblastoma (MB), is subdivided into four clinically relevant molecular subgroups, although targeted therapy options informed by understanding of different cellular features are lacking. Here, b... Read More about Identifying new biomarkers of aggressive Group 3 and SHH medulloblastoma using 3D hydrogel models, single cell RNA sequencing and 3D OrbiSIMS imaging.

Vinca alkaloid binding to P-glycoprotein occurs in a processive manner (2022)
Journal Article
Iqbal, S., Flux, C., Briggs, D. A., Deplazes, E., Long, J., Skrzypek, R., …Callaghan, R. (2022). Vinca alkaloid binding to P-glycoprotein occurs in a processive manner. BBA - Biomembranes, 1864(10), Article 184005. https://doi.org/10.1016/j.bbamem.2022.184005

A mechanistic understanding of how P-glycoprotein (Pgp) is able to bind and transport its astonishing range of substrates remains elusive. Pharmacological data demonstrated the presence of at least four distinct binding sites, but their locations hav... Read More about Vinca alkaloid binding to P-glycoprotein occurs in a processive manner.

Analysis of sequence divergence in mammalian abcgs predicts a structural network of residues that underlies functional divergence (2021)
Journal Article
Mitchell-White, J. I., Stockner, T., Holliday, N., Briddon, S. J., & Kerr, I. D. (2021). Analysis of sequence divergence in mammalian abcgs predicts a structural network of residues that underlies functional divergence. International Journal of Molecular Sciences, 22(6), 1-16. https://doi.org/10.3390/ijms22063012

© 2021 by the authors. Licensee MDPI, Basel, Switzerland. The five members of the mammalian G subfamily of ATP-binding cassette transporters differ greatly in their substrate specificity. Four members of the subfamily are important in lipid transport... Read More about Analysis of sequence divergence in mammalian abcgs predicts a structural network of residues that underlies functional divergence.

Function of the pseudo phosphotransfer proteins has diverged between rice and Arabidopsis (2021)
Journal Article
Vaughan-Hirsch, J., Tallerday, E. J., Burr, C. A., Hodgens, C., Louise Boeshore, S., Beaver, K., …Kieber, J. J. (2021). Function of the pseudo phosphotransfer proteins has diverged between rice and Arabidopsis. Plant Journal, 106(1), 159-173. https://doi.org/10.1111/tpj.15156

© 2021 The Authors. The Plant Journal published by Society for Experimental Biology and John Wiley & Sons Ltd. The phytohormone cytokinin plays a significant role in nearly all aspects of plant growth and development. Cytokinin signaling has primar... Read More about Function of the pseudo phosphotransfer proteins has diverged between rice and Arabidopsis.

Y-box binding protein-1: A neglected target in pediatric brain tumors? (2020)
Journal Article
Taylor, L., Kerr, I. D., & Coyle, B. (2021). Y-box binding protein-1: A neglected target in pediatric brain tumors?. Molecular Cancer Research, 19(3), 375-387. https://doi.org/10.1158/1541-7786.MCR-20-0655

© 2020 American Association for Cancer Research. Brain and central nervous system tumors represent the most common childhood solid tumors. Comprising 21% of all pediatric cancers, they remain the leading cause of cancer-related mortality and morbidit... Read More about Y-box binding protein-1: A neglected target in pediatric brain tumors?.

3D hydrogels reveal medulloblastoma subgroup differences and identify extracellular matrix subtypes that predict patient outcome (2020)
Journal Article
Linke, F., Aldighieri, M., Lourdusamy, A., Grabowska, A. M., Stolnik, S., Kerr, I. D., …Coyle, B. (2021). 3D hydrogels reveal medulloblastoma subgroup differences and identify extracellular matrix subtypes that predict patient outcome. Journal of Pathology, 253(3), 326-338. https://doi.org/10.1002/path.5591

© 2020 The Authors. The Journal of Pathology published by John Wiley & Sons, Ltd. on behalf of The Pathological Society of Great Britain and Ireland. Medulloblastoma (MB) is the most common malignant brain tumour in children and is subdivided into... Read More about 3D hydrogels reveal medulloblastoma subgroup differences and identify extracellular matrix subtypes that predict patient outcome.

Application of fluorescence correlation spectroscopy to study substrate binding in styrene maleic acid lipid copolymer encapsulated ABCG2 (2020)
Journal Article
Horsey, A. J., Briggs, D. A., Holliday, N. D., Briddon, S. J., & Kerr, I. D. (2020). Application of fluorescence correlation spectroscopy to study substrate binding in styrene maleic acid lipid copolymer encapsulated ABCG2. BBA - Biomembranes, 1862(6), https://doi.org/10.1016/j.bbamem.2020.183218

© 2020 The Authors ABCG2 is one of a trio of human ATP binding cassette transporters that have the ability to bind and transport a diverse array of chemical substrates out of cells. This so-called “multidrug” transport has numerous physiological cons... Read More about Application of fluorescence correlation spectroscopy to study substrate binding in styrene maleic acid lipid copolymer encapsulated ABCG2.

Disruption of the Unique ABCG-Family NBD:NBD Interface Impacts Both Drug Transport and ATP Hydrolysis (2020)
Journal Article
Kapoor, P., Briggs, D. A., Cox, M. H., & Kerr, I. D. (2020). Disruption of the Unique ABCG-Family NBD:NBD Interface Impacts Both Drug Transport and ATP Hydrolysis. International Journal of Molecular Sciences, 21(3), https://doi.org/10.3390/ijms21030759

ABCG2 is one of a triumvirate of human multidrug ATP binding cassette (ABC) transporters that are implicated in defense of cells and tissues against cytotoxic chemicals, but which can confer chemotherapy resistance states in oncology. Understanding t... Read More about Disruption of the Unique ABCG-Family NBD:NBD Interface Impacts Both Drug Transport and ATP Hydrolysis.

A role for ABCB1 in prognosis, invasion and drug resistance in ependymoma (2019)
Journal Article
Sabnis, D. H., Storer, L. C. D., Liu, J., Jackson, H. K., Kilday, J. P., Grundy, R. G., …Coyle, B. (2019). A role for ABCB1 in prognosis, invasion and drug resistance in ependymoma. Scientific Reports, 9(1), 1-9. https://doi.org/10.1038/s41598-019-46700-z

© 2019, The Author(s). Three of the hallmarks of poor prognosis in paediatric ependymoma are drug resistance, local invasion and recurrence. We hypothesised that these hallmarks were due to the presence of a sub-population of cancer stem cells expres... Read More about A role for ABCB1 in prognosis, invasion and drug resistance in ependymoma.

Cellular patterning of Arabidopsis roots under low phosphate conditions (2018)
Journal Article
Janes, G., von Wangenheim, D., Cowling, S., Kerr, I. D., Band, L. R., French, A. P., & Bishopp, A. (2018). Cellular patterning of Arabidopsis roots under low phosphate conditions. Frontiers in Plant Science, 9, Article 735. https://doi.org/10.3389/fpls.2018.00735

Phosphorus is a crucial macronutrient for plants playing a critical role in many cellular signaling and energy cycling processes. In light of this, phosphorus acquisition efficiency is an important target trait for crop improvement, but it also provi... Read More about Cellular patterning of Arabidopsis roots under low phosphate conditions.

Residues contributing to drug transport by ABCG2 are localised to multiple drug-binding pockets (2018)
Journal Article
Cox, M. H., Kapoor, P., Briggs, D. A., & Kerr, I. D. (2018). Residues contributing to drug transport by ABCG2 are localised to multiple drug-binding pockets. Biochemical Journal, 475(9), https://doi.org/10.1042/BCJ20170923

Multidrug binding and transport by the ATP binding cassette transporter ABCG2 is a factor in the clinical resistance to chemotherapy in leukaemia, and a contributory factor to the pharmacokinetic profiles of many other prescribed drugs. Despite its i... Read More about Residues contributing to drug transport by ABCG2 are localised to multiple drug-binding pockets.

Location of contact residues in pharmacologically distinct drug binding sites on P-glycoprotein (2016)
Journal Article
Mittra, R., Pavy, M., Subramanian, N., George, A. M., O'Mara, M. L., Kerr, I. D., & Callaghan, R. (2017). Location of contact residues in pharmacologically distinct drug binding sites on P-glycoprotein. Biochemical Pharmacology, 123, 19-28. https://doi.org/10.1016/j.bcp.2016.10.002

© 2016 Elsevier Inc. The multidrug resistance P-glycoprotein (P-gp) is characterised by the ability to bind and/or transport an astonishing array of drugs. This poly-specificity is imparted by at least four pharmacologically distinct binding sites wi... Read More about Location of contact residues in pharmacologically distinct drug binding sites on P-glycoprotein.

The multidrug transporter ABCG2: still more questions than answers (2016)
Journal Article
Horsey, A. J., Cox, M. H., Sarwat, S., & Kerr, I. D. (2016). The multidrug transporter ABCG2: still more questions than answers. Biochemical Society Transactions, 44(3), 824-830. https://doi.org/10.1042/BST20160014

ABCG2 is one of at least three human ATP binding cassette (ABC) transporters which can facilitate the export from cells of a wide range of chemically unrelated drug molecules. This capacity for multidrug transport is not only a confounding factor in... Read More about The multidrug transporter ABCG2: still more questions than answers.

Long-term exposure to irinotecan reduces cell migration in glioma cells. (2016)
Journal Article
Al-Ghafari, A. B., Punjaruk, W., Storer, L., Carrier, D., Hussein, D., Coyle, B., & Kerr, I. D. (2016). Long-term exposure to irinotecan reduces cell migration in glioma cells. Journal of Neuro-Oncology, 127(3), 455-462. https://doi.org/10.1007/s11060-016-2058-4

In spite of considerable research into the therapies for glioblastoma multiforme this tumour type remains very difficult to treat. As well as having a tendency to be inherently resistant to chemotherapy, glioblastoma multiforme also displays local in... Read More about Long-term exposure to irinotecan reduces cell migration in glioma cells..

Plasma membrane dynamics and tetrameric organisation of ABCG2 transporters in mammalian cells revealed by single particle imaging techniques (2015)
Journal Article
Wong, K., Briddon, S. J., Holliday, N. D., & Kerr, I. D. (2016). Plasma membrane dynamics and tetrameric organisation of ABCG2 transporters in mammalian cells revealed by single particle imaging techniques. Biochimica et Biophysica Acta (BBA) - Molecular Cell Research, 1863(1), 19-29. https://doi.org/10.1016/j.bbamcr.2015.10.002

ABCG2 is one of three human ATP binding cassette (ABC) transporters involved in the export from cells of a chemically and structurally diverse range of compounds. This multidrug efflux capability, together with a broad tissue distribution in the body... Read More about Plasma membrane dynamics and tetrameric organisation of ABCG2 transporters in mammalian cells revealed by single particle imaging techniques.