Synthesis and activity of a folate peptide camptothecin prodrug
Synthesis and activity of a folate peptide camptothecin prodrug
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叶酸肽喜树碱原药的合成与活性
DOI：
10.1016/j.bmcl.2006.07.076
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发表时间：
2006-10-15
影响因子：
2.7
通讯作者：
Low, Philip S.
中科院分区：
文献类型：
--
作者：
Henne, Walter A.;Doorneweerd, Derek D.;Low, Philip S.
使用通过可释放的二硫键碳酸酯接头与叶酸连接的亲水性肽间隔基合成了一种靶向叶酸受体的喜树碱前药。发现该缀合物对叶酸受体表达细胞具有高亲和力，并抑制人KB细胞中的细胞增殖，IC50为10 nM。前药的活性被过量的叶酸完全阻断，表明受体介导的摄取。(c)2006爱思唯尔有限公司保留所有权利。
A folate receptor targeted camptothecin prodrug was synthesized using a hydrophilic peptide spacer linked to folate via a releasable disulfide carbonate linker. The conjugate was found to possess high affinity for folate receptor-expressing cells and inhibited cell proliferation in human KB cells with an IC50 of 10 nM. Activity of the prodrug was completely blocked by excess folic acid, demonstrating receptor-mediated uptake. (c) 2006 Elsevier Ltd. All rights reserved.