几种抗疟药和吩噻嗪化合物对网格蛋白包被结构形成的影响。

Effects of several antimalarials and phenothiazine compounds on the formation of coat structure from clathrin.

作者信息

Van Jaarsveld P P, Lippoldt R E, Nandi P K, Edelhoch H

出版信息

Biochem Pharmacol. 1982 Mar 1;31(5):793-8. doi: 10.1016/0006-2952(82)90465-8.

Abstract

We have evaluated the effects of two phenothiazine and several antimalarial drugs on the rates of polymerization of 8S clathrin molecules to 300S coat structures. Most of the drugs investigated have been shown in other studies to inhibit receptor-mediated endocytosis through the coated pit regions of plasma membranes. The two types of drugs were found to accelerate the polymerization rate without having much effect on the size distribution of the polymer species. The activities of the drugs appear to depend on the dibasic moiety and a large, hydrophobic aromatic ring in their structures.

摘要

我们评估了两种吩噻嗪类药物和几种抗疟药物对8S网格蛋白分子聚合成300S包被结构的速率的影响。在其他研究中，大多数所研究的药物已被证明可通过质膜的包被小窝区域抑制受体介导的内吞作用。发现这两类药物可加速聚合速率，而对聚合物种类的大小分布影响不大。这些药物的活性似乎取决于其结构中的二元部分和一个大的疏水性芳香环。