| Literature DB >> 20192275 |
Baohua Huang1, Ankur Desai, Shengzhuang Tang, Thommey P Thomas, James R Baker.
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).Entities:
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Year: 2010 PMID: 20192275 PMCID: PMC2851157 DOI: 10.1021/ol1002626
Source DB: PubMed Journal: Org Lett ISSN: 1523-7052 Impact factor: 6.005