Witte John F, Bray Kathryn E, Thornburg Chelsea K, McClard Ronald W
Arthur F. Scott Laboratory of Chemistry, Reed College, Portland, OR 97202-8199, USA.
Bioorg Med Chem Lett. 2006 Dec 1;16(23):6112-5. doi: 10.1016/j.bmcl.2006.08.109. Epub 2006 Sep 18.
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.
一种假定的过渡态中间体的模拟物已被合成出来，并且发现它是酵母乳清酸磷酸核糖基转移酶的一种起效非常缓慢的抑制剂。抑制机制可能涉及酶向一种易于接受抑制剂的形式进行的限速异构化，然后抑制剂会紧密结合在这种形式上。
