A cell-permeable inhibitor of exocytosis and endosomal recycling
Endosidin 2 (ES2) is a cell-permeable benzylidene-benzohydrazide that binds to the exocyst component of the 70 kDa (EXO70) subunit of the exocyst complex (Kd = 253 μM, EXO70A1).[1] ES2 binding inhibits exocytosis and endosomal recycling in plant and mammalian cells. ES2 disrupts protein trafficking between the endosome and plasma membrane, which enhances trafficking to the vacuole for degradation. It also inhibits recycling of endocytosed transferrin to the plasma membrane in HeLa cells and can target multiple isoforms of mammalian EXO70, resulting in misregulation of exocytosis.
Endosidin 2（ES2）是一种细胞可渗透的亚苄基苯并酰肼，与胞外复合体（Kd=253μM，EXO70A1）的70kDa（EXO70）亚基的胞外成分结合。[1] ES2结合抑制植物和哺乳动物细胞中的胞吐和内体再循环。ES2破坏内体和质膜之间的蛋白质运输，从而增强向液泡的运输以进行降解。它还抑制HeLa细胞中内吞转铁蛋白向质膜的循环，并可靶向哺乳动物EXO70的多种异构体，导致胞吐作用的失调。
Reference:
1. Zhang, C., Brown, M.Q., van de Ven, W., et al. Endosidin2 targets conserved exocyst complex subunit EXO70 to inhibit exocytosis. Proc. Natl. Acad. Sci. USA 113(1), E41-E50 (2016).is.
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