Min K L, Steghens J P, Henry R, Doutheau A, Collombel C
Laboratoire de Biochimie C, Hôpital Edouard Herriot, Lyon, France.
Biochim Biophys Acta. 1997 Jun 5;1357(1):49-56. doi: 10.1016/s0167-4889(97)00013-x.
New phosphorylated guanidines have been synthesized and examined as potential inhibitors for creatine kinase. These compounds show a significant increase of inhibitory activity in comparison with the corresponding guanidines. Unlike the guanidines, they are competitive inhibitors because of the phosphoryl group. N-Phospho-N'-2-(2,6-dichlorophenyl)ethylguanidine is a potent inhibitor (K(i) = 2.0 mM and 1.2 mM respectively for muscle and brain-type creatine kinase). Although these phosphorylated analogs of creatine phosphate have a very poor substrate activity in the reverse reaction, the phosphoryl group is important for binding to the enzyme.
新型磷酸化胍已被合成并作为肌酸激酶的潜在抑制剂进行了研究。与相应的胍相比，这些化合物的抑制活性显著增加。与胍不同，由于磷酰基的存在，它们是竞争性抑制剂。N-磷酸-N'-2-(2,6-二氯苯基)乙基胍是一种强效抑制剂（对肌肉型和脑型肌酸激酶的K(i)分别为2.0 mM和1.2 mM）。尽管这些磷酸肌酸的磷酸化类似物在逆反应中的底物活性非常低，但磷酰基对于与酶的结合很重要。
