Structures of the multidrug exporter AcrB reveal a proximal multisite drug-binding pocket

Ryosuke Nakashima, Keisuke Sakurai, Seiji Yamasaki, Kunihiko Nishino and Akihito Yamaguchi ()
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Ryosuke Nakashima: Institute of Scientific and Industrial Research, Osaka University, Ibaraki, Osaka567-0047, Japan
Keisuke Sakurai: Institute of Scientific and Industrial Research, Osaka University, Ibaraki, Osaka567-0047, Japan
Seiji Yamasaki: Graduate School of Pharmaceutical Sciences, Osaka University, Suita, Osaka 565-0871, Japan
Kunihiko Nishino: Laboratory of Microbiology and Infectious Diseases, Institute of Scientific and Industrial Research, Osaka University, Ibaraki, Osaka567-0047, Japan
Akihito Yamaguchi: Institute of Scientific and Industrial Research, Osaka University, Ibaraki, Osaka567-0047, Japan

Nature, 2011, vol. 480, issue 7378, 565-569

Abstract: Crystallographic studies show that high-molecular-mass drugs bind to the bacterial multidrug transporter AcrB at a previously unseen ‘proximal’ binding pocket before peristaltic transfer to the known ‘distal’ pocket, whereas low-molecular-mass drugs bind directly to the distal pocket.

Date: 2011
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DOI: 10.1038/nature10641

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