科学家发现代谢大多数药物分子的结构

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根据一项新研究的结果,科学家们发现了一种负责代谢超过一半药物的分子的结构。这些发现发表在《科学》杂志的在线版上,将帮助制药商更好地了解药物是如何被分解和处理的,并应有助于预防药物之间危险的交叉反应。

这种关键分子,被称为PXR,控制着一种名为细胞色素P450-3A(缩写为CYP3A)的蛋白质,该蛋白质负责分解药物。它通过与化合物结合来实现这一点,从而标记它们以便降解。但与大多数生物相互作用(其中一个分子或受体与单一化学物质结合)不同,北卡罗来纳大学化学家马修·R·雷丁博指出,PXR是“高度混杂的”,它与从抗癌药物紫杉醇到堕胎药RU-486等多种化合物结合。如果有人服用不止一种药物,这可能会导致问题。雷丁博说:“想象一下,你正在服用口服避孕药,同时也在服用草药圣约翰草。众所周知,圣约翰草的一种成分金丝桃素与PXR结合并激活CYP3A4,然后CYP3A4会分解肝脏中的许多化合物,包括避孕药。” 他补充说,PXR介导的其他负面相互作用可能导致免疫抑制剂环孢菌素和抗HIV药物茚地那韦的分解。这项新研究为这种介导分子提供了可喜的见解。雷丁博评论说:“使用PXR的晶体结构,我们也许能够预测这些影响并预防此类药物-药物相互作用。”

Kate Wong is an award-winning science writer and senior editor at 大众科学 focused on evolution, ecology, anthropology, archaeology, paleontology and animal behavior. She is fascinated by human origins, which she has covered for more than 25 years. Recently she has become obsessed with birds. Her reporting has taken her to caves in France and Croatia that Neandertals once called home, to the shores of Kenya's Lake Turkana in search of the oldest stone tools in the world, to Madagascar on an expedition to unearth ancient mammals and dinosaurs, to the icy waters of Antarctica, where humpback whales feast on krill, and on a "Big Day" race around the state of Connecticut to find as many bird species as possible in 24 hours. Kate is co-author, with Donald Johanson, of Lucy's Legacy: The Quest for Human Origins. She holds a bachelor of science degree in biological anthropology and zoology from the University of Michigan. Follow Wong on X (formerly Twitter) @katewong

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