氯丙嗪与小鼠脑微管蛋白相互作用的圆二色性研究

A circular dichroism study of the interaction of chlorpromazine with mouse brain tubulin.

作者信息

Rao A G, Hare D L, Cann J R

出版信息

Biochemistry. 1978 Oct 31;17(22):4735-9. doi: 10.1021/bi00615a020.

Abstract

A circular dichroism study with subsidiary ultracentrifuge measurements on the interaction of chlorpromazine with mouse brain tubulin establishes the previous inference from binding studies that the drug induces a change in the structure of the protein. Binding of the first mole of chlorpromazine causes an alteration in secondary structure, which is reversible with respect to drug concentration, without detected change in tertiary structure or significant change in the state of association of the protein. The conformationally altered tubulin binds additional chlorpromazine molecules without further change in secondary structure.

摘要

一项关于氯丙嗪与小鼠脑微管蛋白相互作用的圆二色性研究，并辅以超速离心测量，证实了之前结合研究得出的推断，即该药物会诱导蛋白质结构发生变化。第一摩尔氯丙嗪的结合会导致二级结构改变，这种改变相对于药物浓度是可逆的，三级结构未检测到变化，蛋白质的缔合状态也无显著变化。构象改变的微管蛋白会结合额外的氯丙嗪分子，而二级结构不再进一步变化。