肌醇霉素对CDP - 二脂酰甘油：肌醇转移酶的抑制作用
Inhibition of CDP-DG: inositol transferase by inostamycin.
作者信息
Imoto M, Taniguchi Y, Umezawa K
机构信息
Department of Applied Chemistry, Faculty of Science and Technology, Keio University, Kanagawa.
出版信息
J Biochem. 1992 Aug;112(2):299-302. doi: 10.1093/oxfordjournals.jbchem.a123894.
Inostamycin, a novel microbial secondary metabolite, inhibited [3H]inositol and 32P1 incorporation into phosphatidylinositol (PtdIns) induced by epidermal growth factor (EGF) in cultured A431 cells, the IC50 being 0.5 micrograms/ml, without inhibiting macromolecular synthesis. The drug inhibited cellular inositol phosphate formation only when it was added at the same time as labeled inositol. It was found to inhibit in vitro CDP-DG:inositol transferase activity of the A431 cell membrane, the IC50 being about 0.02 micrograms/ml. It did not inhibit tyrosine kinase, PtdIns phospholipase C, or PtdIns kinase. Therefore, inhibition of PtdIns turnover by inostamycin must be due to the inhibition of CDP-DG:inositol transferase. Thus, inostamycin is a novel inhibitor of CDP-DG:inositol transferase.
肌醇霉素是一种新型微生物次级代谢产物，它能抑制表皮生长因子（EGF）诱导培养的A431细胞中[3H]肌醇和32P1掺入磷脂酰肌醇（PtdIns），IC50为0.5微克/毫升，且不抑制大分子合成。该药物仅在与标记肌醇同时添加时才抑制细胞肌醇磷酸的形成。研究发现它能抑制A431细胞膜的体外CDP-DG：肌醇转移酶活性，IC50约为0.02微克/毫升。它不抑制酪氨酸激酶、PtdIns磷脂酶C或PtdIns激酶。因此，肌醇霉素对PtdIns周转的抑制作用必定是由于其对CDP-DG：肌醇转移酶的抑制。所以，肌醇霉素是一种新型的CDP-DG：肌醇转移酶抑制剂。
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