Small structural alterations greatly influence the membrane affinity of lipophilic ligands: Membrane interactions of bafilomycinA1 and its desmethyl derivative bearing 19F-labeling.
Small structural alterations greatly influence the membrane affinity of lipophilic ligands: Membrane interactions of bafilomycinA1 and its desmethyl derivative bearing 19F-labeling.
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微小的结构改变极大地影响亲脂性配体的膜亲和力：巴弗洛霉素A1及其带有19F标记的去甲基衍生物的膜相互作用。
DOI：
10.1016/j.bmc.2019.03.017
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发表时间：
2019
期刊：
影响因子：
--
通讯作者：
Tatsuru Hayashi, Hiroshi Tsuchikawa, Yuichi Umegawa, Michio Murata.
中科院分区：
文献类型：
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作者：
Tatsuru Hayashi, Hiroshi Tsuchikawa, Yuichi Umegawa, Michio Murata.
双层膜环境下的分子行为是研究有机分子与细胞膜相互作用时如何发挥其生物活性的重要课题之一。然而，与配体-受体相互作用的结构生物学策略相比，这种性质的化学方法并不成功。本文从化学角度研究了亲脂性ATP酶抑制剂巴弗洛霉素A1及其衍生物在脂质环境中的分子行为。我们的研究结果揭示了具有不同抑制效力的配体之间的膜亲和力和动力学的显着差异，表明配体-膜相互作用对其生物活性的具体贡献。
Molecular behavior under bilayer membrane environments is one of the important research topics concerning how organic molecules exert their biological activities when interacting with cellular membranes. However, chemistry-based approaches to this property have not been successful when compared with the structural biological strategy on ligand-receptor interactions. Here, we investigated the molecular behavior of the lipophilic ATPase inhibitor bafilomycin A1and its derivatives under a lipid environment from a chemical point of view. Our results revealed significant differences in membrane affinity and dynamics among ligands having different inhibitory potencies, suggesting the specific contribution of ligand-membrane interactions to their biological activity.