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G907 是 ABC transporter, MsbA 的选择性小分子拮抗剂。 G907 抑制两栖动物中纯化的大肠杆菌 MsbA (IC50=18 nM)。G907 通过楔入结构上保守的跨膜袋,使 MsbA 陷入向内的脂多糖结合构象中。G907 具有杀菌活性。
G907 is a selective small-molecule antagonist of ATP-binding cassette (ABC) transporter, MsbA. It inhibits purified E. coli MsbA in amphipols with an IC50 of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket. Bactericidal activity[1].
[1]. Ho H, et al. Structural basis for dual-mode inhibition of the ABC transporter MsbA. Nature. 2018 May;557(7704):196-201.
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