Rodríguez-Liñares B, Walker T, Watson S
Department of Pharmacology, Oxford, U.K.
Biochem Pharmacol. 1991 Mar 1;41(5):835-8. doi: 10.1016/0006-2952(91)90089-n.
We have investigated the action of a novel inhibitor of DG-kinase, R59949. This agent was found to produce partial inhibition of formation of phosphatidic acid in human platelets challenged with thrombin, DC8 or OAG. However, this effect was not associated with enhanced phosphorylation of a 47 kDa protein, a known substrate for protein kinase C. We therefore believe that this compound does not represent a major advance on its earlier prototype, R59022.
我们研究了新型二酰甘油激酶抑制剂R59949的作用。发现该药物对用凝血酶、DC8或1-油酰基-2-乙酰基-sn-甘油(OAG)刺激的人血小板中磷脂酸的形成产生部分抑制作用。然而,这种作用与蛋白激酶C的已知底物——一种47 kDa蛋白的磷酸化增强无关。因此,我们认为该化合物在其早期原型R59022的基础上并没有取得重大进展。