首页> 外文期刊>Biochimica et Biophysica Acta. General Subjects >An efficient and cost-effective approach to kahalalide F N-terminal modifications using a nuisance algal bloom of Bryopsis pennata
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An efficient and cost-effective approach to kahalalide F N-terminal modifications using a nuisance algal bloom of Bryopsis pennata

机译:一种高效且经济有效的方法,利用Bryopsis pennata的滋生藻华来进行Kahalalide F N末端修饰

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Background: Kahalalide F (KF) and its isomer iso-kahalalide F (isoKF), both of which can be isolated from the mollusk Elysia rufescens and its diet alga Bryopsis pennata, are potent cytotoxic agents that have advanced through five clinical trials. Due to a short half-life, narrow spectrum of activity, and a modest response in patients, further efforts to modify the molecule are required to address its limitations. In addition, due to the high cost in producing KF analogues using solid phase peptide synthesis (SPPS), a degradation and reconstruction approach was employed using natural KF from a seasonal algal bloom to generate KF analogues.
机译:背景:可以从软体动物Elysia rufescens及其饮食藻类Bryopsis pennata中分离得到的Kahalalide F(KF)及其异构体iso-kahalalide F(isoKF)是有效的细胞毒性药物,已通过五项临床试验进行了研究。由于半衰期短,活性谱窄以及患者反应中等,因此需要进一步努力修饰该分子以解决其局限性。此外,由于使用固相肽合成(SPPS)生产KF类似物的成本较高,因此采用了从季节性藻华中提取天然KF的降解和重建方法来生成KF类似物。

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