ABCG2 is one of a few human membrane transporters which display the amazing ability to transport multiple different chemicals out of cells. These multidrug pumps, which have orthologues in all organisms, are important in humans in the context of drug pharmacokinetics, especially with respect to resistance to chemotherapy. In 2016, we presented a mini-review on ABCG2 which identified many areas of exciting research progress as well as many areas of frustrating ignorance. Just 2 years on the field has advanced, particularly with respect to structural biology as the cryo-electron microscopy revolution has brought us new insights into the structure and mechanism of ABCG2. In this update, we evaluate the degree to which new data have enhanced our understanding of the structure and mechanism of ABCG2 and whether we are now in a position to translate some of these findings into inhibitor design and development.
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December 2018
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Review Article|
November 21 2018
ABCG2: does resolving its structure elucidate the mechanism?
Parth Kapoor;
Parth Kapoor
1School of Life Sciences, University of Nottingham, Queens Medical Centre, Nottingham NG7 2UH, U.K.
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Aaron J. Horsey;
Aaron J. Horsey
1School of Life Sciences, University of Nottingham, Queens Medical Centre, Nottingham NG7 2UH, U.K.
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Megan H. Cox;
Megan H. Cox
1School of Life Sciences, University of Nottingham, Queens Medical Centre, Nottingham NG7 2UH, U.K.
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Ian D. Kerr
1School of Life Sciences, University of Nottingham, Queens Medical Centre, Nottingham NG7 2UH, U.K.
Correspondence: Ian D. Kerr (Ian.kerr@nottingham.ac.uk)
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Publisher: Portland Press Ltd
Received:
July 19 2018
Revision Received:
September 27 2018
Accepted:
October 19 2018
Online ISSN: 1470-8752
Print ISSN: 0300-5127
© 2018 The Author(s). Published by Portland Press Limited on behalf of the Biochemical Society
2018
Biochem Soc Trans (2018) 46 (6): 1485–1494.
Article history
Received:
July 19 2018
Revision Received:
September 27 2018
Accepted:
October 19 2018
Citation
Parth Kapoor, Aaron J. Horsey, Megan H. Cox, Ian D. Kerr; ABCG2: does resolving its structure elucidate the mechanism?. Biochem Soc Trans 17 December 2018; 46 (6): 1485–1494. doi: https://doi.org/10.1042/BST20180145
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