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首页> 外文期刊>Life sciences >Inhibitory effects of uridine diphosphate on UDP-glucuronosyltransferase.
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Inhibitory effects of uridine diphosphate on UDP-glucuronosyltransferase.

机译：尿苷二磷酸对UDP-葡萄糖醛酸转移酶的抑制作用。

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摘要

Inhibitory effects of uridine diphosphate on the enzymatic activity of UDP-glucuronosyltransferase (UGT) were investigated. Pyrimidine nucleotides such as UDP, UTP and cytidine diphosphate reduced the activity of rat purified UGT (phenol UGT) to about 10%, 48% and 46% of the control, respectively, at the same concentration as a donor substrate, UDP-glucuronic acid. Purine nucleotides, uridine monophosphate, glucuronic acid and some UDP-sugars were only slightly inhibitory toward the transferase. Similar effects were observed in the expressed UGT (UGT1A6; corresponding to phenol UGT) in yeast cells and rat liver microsomal membrane-binding UGT, indicating that uracil and diphosphate residues are essential for the UDP inhibition. Interestingly, 2'-deoxy UDP was found to be a less effective inhibitor (about 50% inhibition) than UDP on the purified, the expressed (UGT1A6 and UGT2B1) and microsomal membrane-binding UGTs. These results indicate that not only uracil and diphosphate residues but also 2'-hydroxyl residue of UDP ribose participates in the interactions between UDP and UDP-glucuronosyltransferase.
机译：研究了尿苷二磷酸对UDP-葡萄糖醛酸糖基转移酶（UGT）酶活性的抑制作用。嘧啶核苷酸，例如UDP，UTP和胞苷二磷酸酯，在与供体底物UDP-葡萄糖醛酸相同的浓度下，将大鼠纯化的UGT（酚UGT）的活性分别降低至对照的约10％，48％和46％ 。嘌呤核苷酸，尿苷一磷酸，葡萄糖醛酸和一些UDP糖对转移酶的抑制作用很小。在酵母细胞和大鼠肝微粒体膜结合UGT中表达的UGT（UGT1A6;对应于酚UGT）中观察到了相似的效果，表明尿嘧啶和二磷酸酯残基对于UDP抑制至关重要。有趣的是，在纯化的，表达的（UGT1A6和UGT2B1）和微粒体膜结合型UGT上，发现2'-脱氧UDP比UDP效果更差（约50％抑制）。这些结果表明，不仅UDP残基的尿嘧啶和二磷酸残基而且2'-羟基残基也参与UDP和UDP-葡糖醛酸糖基转移酶之间的相互作用。

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