All Outputs (25)

A time-resolved Förster resonance energy transfer assay to investigate drug and inhibitor binding to ABCG2 (2024)
Journal Article

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.

Mechanistic insight into the role of AUXIN RESISTANCE4 in trafficking of AUXIN1 and LIKE AUX1-2 (2023)
Journal Article

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

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

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

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

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

© 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

© 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

© 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

© 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

© 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

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

© 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.

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.

Overcoming ABCG2-mediated drug resistance with imidazo-[1,2-b]-pyridazine-based Pim1 kinase inhibitors (2015)
Journal Article

Purpose Multidrug efflux pumps such as ABCG2 confer drug resistance to a number of cancer types, leading to poor prognosis and outcome. To date, the strategy of directly inhibiting multidrug efflux pumps in order to overcome drug resistance in can... Read More about Overcoming ABCG2-mediated drug resistance with imidazo-[1,2-b]-pyridazine-based Pim1 kinase inhibitors.

Identification of residues in ABCG2 affecting protein trafficking and drug transport, using co-evolutionary analysis of ABCG sequences (2015)
Journal Article

ABCG2 is an ABC (ATP-binding cassette) transporter with a physiological role in urate transport in the kidney and is also implicated in multi-drug efflux from a number of organs in the body. The trafficking of the protein and the mechanism by which i... Read More about Identification of residues in ABCG2 affecting protein trafficking and drug transport, using co-evolutionary analysis of ABCG sequences.