Bile Acid Tethered Docetaxel-Based Nanomicelles Mitigate Tumor Progression through Epigenetic Changes.
作者： Arnab Mukhopadhyay , Sagar Sengupta , Ujjaini Dasgupta , Avinash Bajaj , Vedagopuram Sreekanth
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摘要: In this study, we describe the engineering of sub-100 nm nanomicelles (DTX-PC NMs) derived from phosphocholine derivative docetaxel (DTX)-conjugated lithocholic acid (DTX-PC) and poly(ethylene glycol)-tethered acid. Administration DTX-PC NMs decelerate tumor progression increase mice survivability compared to Taxotere (DTX-TS), FDA-approved formulation DTX. Unlike DTX-TS, do not cause any systemic toxicity slow decay rate plasma DTX concentration in rodents non-rodent species including non-human primates. We further demonstrate that target demethylation CpG islands Sparcl1 (a suppressor gene) by suppressing DNA methyltransferase activity, expression leads regression. Therefore, unique system has potential improve quality life cancer patients, can be translated as a next-generation chemotherapeutic.
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