Eponemycin analogues: syntheses and use as probes of angiogenesis.
Eponemycin analogues: syntheses and use as probes of angiogenesis.
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DOI：
10.1016/s0968-0896(98)00089-3
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发表时间：
1998-08
影响因子：
3.5
通讯作者：
N. Sin;L. Meng;H. Auth;C. Crews
中科院分区：
文献类型：
--
作者：
N. Sin;L. Meng;H. Auth;C. Crews
合成了天然产物eponemycin的环氧-β-氨基酮衍生物，以研究这种抗血管生成化合物的分子作用方式。生物素化二氢埃坡霉素类似物的合成和使用证明，二氢埃坡霉素在人内皮细胞中与至少两种细胞内蛋白质形成共价加合物。用5当量过量的二氢埃坡尼霉素预处理细胞阻止了生物素-二氢埃坡尼霉素结合，表明天然产物与靶蛋白之间存在特异性相互作用。这种生物素-二氢埃坡霉素衍生物将被证明在埃坡霉素受体的纯化和鉴定中是有用的。
Derivatives of the epoxy-β-aminoketone containing natural product eponemycin have been prepared in order to study the molecular mode of action of this anti-angiogenic compound. Synthesis and use of a biotinylated dihydroeponemycin analogue demonstrated that dihydroeponemycin forms a covalent adduct with at least two intracellular proteins in human endothelial cells. Pretreatment of cells with a five equivalent excess of dihydroeponemycin precluded biotin-dihydroeponemycin binding indicating a specific interaction between natural product and the target proteins. This biotin-dihydroeponemycin derivative will prove useful in the purification and identification of eponemycin receptors.