A targeted delivery strategy for the development of potent trypanocides.
A targeted delivery strategy for the development of potent trypanocides.
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开发强效锥虫杀剂的靶向递送策略。
DOI：
10.1039/c7cc03378h
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发表时间：
2017
期刊：
影响因子：
--
通讯作者：
Whitehead,DanielC
中科院分区：
文献类型：
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作者：
Gordhan,HeerenM;Milanes,JillianE;Qiu,Yijian;Golden,JenniferE;Christensen,KennethA;Morris,JamesC;Whitehead,DanielC
研究了一种新的药物递送策略，用于开发针对布氏锥虫（非洲昏睡病的病原体）的有效抗寄生虫化合物。因此，有效的体外己糖激酶抑制剂通过附加三肽过氧化物酶体靶向序列而具有细胞毒性，所述三肽过氧化物酶体靶向序列促进将分子货物递送至寄生虫中的适当细胞器。
A new drug delivery strategy was investigated for the development of potent anti-parasitic compounds against Trypanosoma brucei, the causative agent of African sleeping sickness. Thus, potent in vitro hexokinase inhibitors were rendered cytotoxic by appending a tripeptide peroxosomal targeting sequence that facilitated delivery of the molecular cargo to the appropriate organelle in the parasite.