Shai Y
Department of Membrane Research and Biophysics, Weizmann Institute of Science, Rehovot, Israel.
Toxicology. 1994 Feb 28;87(1-3):109-29. doi: 10.1016/0300-483x(94)90157-0.
The results of the various studies describing the mechanism involved in pore formation by pardaxin and some of its analogues, support a 'barrel-stave' model (Ehrenstein amd Lecar, 1977). In this model pardaxin exerts its activity via three successive steps: (i) a fast binding step (as reflected by the rapid increase of NBD fluorescence in the presence of vesicles); (ii) insertion of peptides into the lipid bilayer; and (iii) the monomers aggregate into a barrel-like formation in which a central aqueous pore surrounded by proteins is formed. This pore increases in diameter through the progressive recruitment of additional monomers. Both the fluorescence energy transfer (FET) studies and the observation of a significant difference in the increase of NBD fluorescence, depending on which terminal was labelled by the fluorophore, support a model by which aggregates are formed in an ordered parallel manner, where the C-terminus is more exposed to the aqueous phase.
各种描述豹蟾毒素及其某些类似物形成孔道机制的研究结果，支持了一种“桶板”模型（埃伦斯坦和勒卡尔，1977年）。在该模型中，豹蟾毒素通过三个连续步骤发挥其活性：（i）快速结合步骤（如在存在囊泡的情况下NBD荧光的快速增加所反映）；（ii）肽插入脂质双层；以及（iii）单体聚集成桶状结构，其中形成由蛋白质包围的中央水相孔道。通过逐步招募额外的单体，该孔道直径增大。荧光能量转移（FET）研究以及观察到的NBD荧光增加的显著差异（取决于荧光团标记的是哪个末端），支持了一种模型，即聚集体以有序平行的方式形成，其中C末端更暴露于水相。
