Synthesis, characterization, and plasma lipoprotein association of a nucleus-targeted boronated porphyrin
Synthesis, characterization, and plasma lipoprotein association of a nucleus-targeted boronated porphyrin
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DOI：
10.1021/jm049277q
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发表时间：
2005-01-27
影响因子：
7.3
通讯作者：
Kahl, SB
中科院分区：
文献类型：
--
作者：
Dozzo, P;Koo, MS;Kahl, SB
二元癌症疗法如BNCT和PDT的疗效关键取决于敏化剂的亚细胞定位位点。本工作首次报道了含硼卟啉与肽核定位序列的二元共轭物的合成及其与血浆脂蛋白的结合特性。卟啉-NLS缀合物在体外主要与低密度脂蛋白缔合。这种结合提供了一种潜在的选择性进入过表达LDL受体的恶性细胞的途径。
The efficacy of binary cancer therapies such as BNCT and PDT depends critically on the subcellular localization site of the sensitizer. This work presents the synthesis and plasma lipoprotein binding properties of the first reported binary conjugate of a boronated porphyrin with a peptide nuclear localization sequence. The porphyrin-NLS conjugate associates in vitro predominantly with low density lipoproteins. Such association provides a potentially selective entry pathway into malignant cells that overexpress the LDL receptor.