磷酰胆碱
磷脂酰胆碱
酶
黄药
磷脂酶A2
磷脂酶C
磷脂酶
生物化学
酶抑制剂
立体化学
作用机理
生物
化学
磷脂
体外
膜
有机化学
出处
期刊:PubMed
日期:1996-01-01
卷期号:22 (6): 287-94
被引量:108
摘要
The effect of the antiviral, antitumoural xanthate D609 on the activity of phospholipase A2, C (PC- and Pi-specific) and D was investigated. D609 is the first model substance of a new concept of antiviral therapy that interferes with cellular regulation mechanisms, rather than with virus coded enzymes. Exclusively phosphatidylcholine (PC) specific phospholipase C (PC-PLC) was found to be inhibited in a dose-dependent manner. Enzyme activity was determined either as the rate of acid release from PC or as the rate of phosphorylcholine production form 3H labelled PC. Lineweaver-Burk plots revealed D609 as a competitive inhibitor of PC-PLC with a Ki of 6.4 microM. In addition, D609 competitively inhibited PC-PLC mediated cleavage of P-nitrophenylphosphorylcholine (p-NPP), a pseudo-substrate of PC-PLC with a Ki of 8.8 microM. These data suggest that D609 competes with the phosphorylcholine residue of PC for binding to PC-PLC.
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