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合成具有吲哚醌结构的靶向 c(RGDyK)的 SN38 前药用于还原型药物释放。

The synthesis of a c(RGDyK) targeted SN38 prodrug with an indolequinone structure for bioreductive drug release.

机构信息

Michigan Nanotechnology Institute for Medicine and Biological Sciences, University of Michigan, Ann Arbor, Michigan 48109, USA.

出版信息

Org Lett. 2010 Apr 2;12(7):1384-7. doi: 10.1021/ol1002626.

DOI:10.1021/ol1002626
PMID:20192275
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2851157/
Abstract

Preparation of a novel c(RGDyK) targeted SN38 prodrug incorporating an indolequinone structure for bioreductively triggered drug release is described. This design yields a prodrug that targets surface molecules on tumor cells (alpha(v)beta(3) integrins) and releases drug under bioreductive conditions. There are three moieties in the prodrug design, namely a therapeutic drug SN38, an indolequinone structure serving as a drug releasing trigger, and an alpha(v)beta(3) integrin targeting peptide c(RGDyK). Preliminary studies showed that SN38 is released in the presence of a bioreductive enzyme (DT-diaphorase).

摘要

描述了一种新型靶向 c(RGDyK)的 SN38 前药的制备，该前药包含吲哚醌结构，用于生物还原触发的药物释放。这种设计产生了一种前药，它靶向肿瘤细胞表面分子（α(v)β(3)整合素），并在生物还原条件下释放药物。前药设计中有三个部分，即治疗药物 SN38、作为药物释放触发的吲哚醌结构和靶向α(v)β(3)整合素的肽 c(RGDyK)。初步研究表明，在生物还原酶 (DT-二氢嘧啶酶) 的存在下释放 SN38。

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本文引用的文献

[1]
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Biochem Pharmacol. 2002-5-1

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