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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 ; Locher, Kaspar P.



Abstract

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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