论文部分内容阅读
霍乱毒素(CT)中的A亚基(CTA)具有ADP-核糖基转移酶(ART)活性,能使肠管上皮细胞GTP结合蛋白质(Gsα)的精氨酸残基ADP核糖基化而引起剧烈的水样腹泻。目的:筛选对CTA的ADP-ART活性有抑制作用的物质并阐明其作用机制。方法:以氨基酸精氨酸的衍生物——胍基丁胺为基质,在[腺嘌呤-~(14)C]NAD存在的条件下,通过测定形成的[~(14)C]ADP核糖基化胍
The A subunit (CTA) in cholera toxin (CT) has ADP-ribosyltransferase (ART) activity and can cause severe ADP ribosylation of the arginine residue of GTP-binding protein (Gsα) in intestinal epithelial cells. Watery diarrhea. OBJECTIVE: To screen substances that inhibit the activity of ADP-ART in CTA and elucidate the mechanism of action. METHODS: The [14C]ADP ribosyl group formed was determined by using the adenine amino acid arginine derivative agmatine as the substrate in the presence of [Adenine-14C]NAD. Chemical