L-Penicillamine is a mechanism-based inhibitor of serine palmitoyltransferase by forming a pyridoxal-5′-phosphate-thiazolidine adduct
L-Penicillamine is a mechanism-based inhibitor of serine palmitoyltransferase by forming a pyridoxal-5′-phosphate-thiazolidine adduct
复制标题
DOI：
10.1039/c2md20020a
复制
发表时间：
2012-08-01
期刊：
影响因子：
--
通讯作者：
Campopiano, Dominic J.
中科院分区：
文献类型：
--
作者：
Lowther, Jonathan;Beattie, Ashley E.;Campopiano, Dominic J.
丝氨酸棕榈酰转移酶 (SPT) 催化鞘脂从头生物合成的第一个关键步骤。来自少动鞘氨醇单胞菌的细菌 SPT 同源物是一种同型二聚体酶，含有与每个亚基结合的必需吡哆醛-5'-磷酸 (PLP) 辅因子。 SPT 抑制剂是有用的鞘脂生物合成阻断剂。在这里，我们使用紫外可见光谱、酶动力学和质谱来研究青霉胺 (Pen) 对 SPT 的抑制作用，青霉胺是一种具有一系列有用医学应用的药物。
Serine palmitoyltransferase (SPT) catalyses the first committed step of de novo sphingolipid biosynthesis. The bacterial SPT homologue from Sphingomonas paucimobilis is a homodimeric enzyme that contains an essential pyridoxal-5'-phosphate (PLP) cofactor bound to each subunit. Inhibitors of SPT are useful blockers of sphingolipid biosynthesis. Here we use UV-vis spectroscopy, enzyme kinetics and mass spectrometry to investigate inhibition of SPT by penicillamine (Pen), a drug with a range of useful medicinal applications.