All Outputs (13)

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.

A time-resolved Förster resonance energy transfer assay to investigate inhibitor binding to ABCG2 (2023)
Working Paper

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.

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.

Rab27a co-ordinates actin-dependent transport by controlling organelle-associated motors and track assembly proteins (2020)
Journal Article

© 2020, The Author(s). Cell biologists generally consider that microtubules and actin play complementary roles in long- and short-distance transport in animal cells. On the contrary, using melanosomes of melanocytes as a model, we recently discovered... Read More about Rab27a co-ordinates actin-dependent transport by controlling organelle-associated motors and track assembly proteins.

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.

Nucleotide exchange factor Rab3GEP requires DENN and non-DENN elements for activation and targeting of Rab27a (2019)
Journal Article

Rab GTPases are compartment-specific molecular switches that regulate intracellular vesicular transport in eukaryotes. GDP/GTP exchange factors (GEFs) control Rab activation, and current models propose that localised and regulated GEF activity is imp... Read More about Nucleotide exchange factor Rab3GEP requires DENN and non-DENN elements for activation and targeting of Rab27a.

The adaptor protein melanophilin regulates dynamic myosin- Va: cargo interaction and dendrite development in melanocytes (2019)
Journal Article

Regulation of organelle transport by the cytoskeleton is fundamental for eukaryotic survival. Cytoskeleton motors are typically modular proteins with conserved motor and diverse cargo binding domains. Motor:cargo interactions are often indirect and m... Read More about The adaptor protein melanophilin regulates dynamic myosin- Va: cargo interaction and dendrite development in melanocytes.

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.

Inefficient recruitment of kinesin-1 to melanosomes precludes it from facilitating their transport (2017)
Journal Article
Robinson, C. L., Evans, R. D., Briggs, D. A., Ramalho, J. S., & Hume, A. N. (in press). Inefficient recruitment of kinesin-1 to melanosomes precludes it from facilitating their transport. Journal of Cell Science, 130(12), https://doi.org/10.1242/jcs.186064

Microtubules and F-actin, and associated motor proteins, are considered to play complementary roles in long- and short-range organelle transport. However, there is growing appreciation that myosin/F-actin networks can drive long-range transport. In m... Read More about Inefficient recruitment of kinesin-1 to melanosomes precludes it from facilitating their transport.

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.

Myosin-Va and dynamic actin oppose microtubules to drive long-range organelle transport (2014)
Journal Article

In animal cells, microtubule and actin tracks and their associated motors (dynein, kinesin, and myosin) are thought to regulate long- and short-range transport, respectively [1-8]. Consistent with this, microtubules extend from the perinuclear centro... Read More about Myosin-Va and dynamic actin oppose microtubules to drive long-range organelle transport.

Dimerization of ABCG2 analysed by bimolecular fluorescence complementation (2011)
Journal Article
Haider, A. J., Briggs, D., Self, T. J., Chilvers, H. L., Holliday, N. D., & Kerr, I. D. (2011). Dimerization of ABCG2 analysed by bimolecular fluorescence complementation. PLoS ONE, 6(10), Article e25818. https://doi.org/10.1371/journal.pone.0025818

ABCG2 is one of three human ATP binding cassette transporters that are functionally capable of exporting a diverse range of substrates from cells. The physiological consequence of ABCG2 multidrug transport activity in leukaemia, and some solid tumour... Read More about Dimerization of ABCG2 analysed by bimolecular fluorescence complementation.