叶酸靶向单分散 PEG 喜树碱缀合物的合成与活性。
Synthesis and activity of a folate targeted monodisperse PEG camptothecin conjugate.
机构信息
Division of Science, Governors State University, 1 University Parkway, University Park, IL 60484, USA.
出版信息
Bioorg Med Chem Lett. 2013 Nov 1;23(21):5810-3. doi: 10.1016/j.bmcl.2013.08.113. Epub 2013 Sep 7.
PMID:24064501
Abstract
A folate targeted camptothecin small molecule drug conjugate (SMDC) was synthesized using a monodisperse PEG spacer linked to folate via a releasable disulfide carbonate linker. Cell cytotoxicity in human KB cells exhibited an IC50 of 6nM. Importantly, activity of the prodrug was blocked by excess folate, demonstrating receptor-mediated celluar uptake of the PEG conjugate.
摘要
一种叶酸靶向喜树碱小分子药物偶联物（SMDC）是通过可释放的二硫碳酸酯连接子将单分散的 PEG 间隔臂连接到叶酸上来合成的。在人 KB 细胞中的细胞毒性实验表明，其 IC50 为 6nM。重要的是，前药的活性被过量的叶酸所阻断，这表明 PEG 偶联物是通过受体介导的细胞摄取。
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