'Irreversible' slow-onset inhibition of orotate phosphoribosyltransferase by an amidrazone phosphate transition-state mimic.
'Irreversible' slow-onset inhibition of orotate phosphoribosyltransferase by an amidrazone phosphate transition-state mimic.
复制标题
磷酸氨基腙过渡态模拟物对乳清酸磷酸核糖基转移酶的“不可逆”缓慢起效抑制。
DOI：
10.1016/j.bmcl.2006.08.109
复制
发表时间：
2006
影响因子：
2.7
通讯作者：
McClard,RonaldW
中科院分区：
文献类型：
--
作者：
Witte,JohnF;Bray,KathrynE;Thornburg,ChelseaK;McClard,RonaldW
一个假定的过渡态中间体的模拟物已被合成，并发现是一个非常缓慢的酵母乳清酸磷酸核糖基转移酶的抑制剂。抑制机制可能涉及酶的速率决定异构化，使其成为接受抑制剂的形式，然后保持紧密结合。
A mimic of the putative transition-state intermediate has been synthesized and found to be a very slow-onset inhibitor of yeast orotate phosphoribosyltransferase. The mechanism of inhibition may involve a rate-determining isomerization of the enzyme to a form receptive to the inhibitor, which then remains tightly bound.