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首页> 外文期刊>Acta Pharmacologica Sinica >Application of secondary structure prediction in antisense drug design targeting protein kinase C-αmRNA and ASAR analysis
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Application of secondary structure prediction in antisense drug design targeting protein kinase C-αmRNA and ASAR analysis

机译:二级结构预测在针对蛋白激酶C-αmRNA和ASAR分析的反义药物设计中的应用

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摘要

Three S-ODN:( 5-AGCCCA- GCCGCTTGGCTGGG-3', 5'-AGGAGTGCAGCTGC- GTCAAG-3', 5'-TCAGAGGG-ACTGATGACTTT-3') Had lower IC_50[(48±7),(50±4),(64±2.7) nmol. L~-1, respectively]than that of ISIS3521[(81±25) nmol.L~-1]. Computer aided design was Helpful to obtain S-ODN with better in vitro effect than Current positive drug. The degree of instability of sec- ondary structural elements and △G°_37 were important factors for drug activity. Other important factors need- ed for further investigation.
机译:三个S-ODN :( 5-AGCCCA- GCCGCTTGGCTGGG-3',5'-AGGAGTGCAGCTGC- GTCAAG-3',5'-TCAGAGGG-ACTGATGACTTT-3')IC_50较低((48±7),(50±4) ,(64±2.7)nmol。分别比ISIS3521的L〜-1] [(81±25)nmol.L〜-1]。计算机辅助设计有助于获得比目前的阳性药物具有更好的体外作用的S-ODN。二级结构元素的不稳定性和△G°_37是影响药物活性的重要因素。需要进一步调查的其他重要因素。

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