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Structural basis of small-molecule inhibition of human multidrug transporter ABCG2

Jackson, Scott M., Manolaridis, Ioannis, Kowal, Julia, Zechner, Melanie, Taylor, Nicholas M. I., Bause, Manuel, Bauer, Stefanie, Bartholomaeus, Ruben, Bernhardt, Günther , König, Burkhard , Buschauer, Armin , Stahlberg, Henning, Altmann, Karl-Heinz and Locher, Kaspar P. (2018) Structural basis of small-molecule inhibition of human multidrug transporter ABCG2. Nature Structural & Molecular Biology 25 (4), pp. 333-340.

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Other URL: http://doi.org/10.1038/s41594-018-0049-1


ABCG2 is an ATP-binding cassette (ABC) transporter that protects tissues against xenobiotics, affects the pharmacokinetics of drugs and contributes to multidrug resistance. Although many inhibitors and modulators of ABCG2 have been developed, understanding their structure–activity relationship requires high-resolution structural insight. Here, we present cryo-EM structures of human ABCG2 bound to ...


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Item type:Article
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König
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Dewey Decimal Classification:500 Science > 570 Life sciences
500 Science > 540 Chemistry & allied sciences
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Item ID:37979
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