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A targeted delivery strategy for the development of potent trypanocides.


ABSTRACT: 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.

SUBMITTER: Gordhan HM 

PROVIDER: S-EPMC5576345 | biostudies-literature | 2017 Aug

REPOSITORIES: biostudies-literature

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A targeted delivery strategy for the development of potent trypanocides.

Gordhan Heeren M HM   Milanes Jillian E JE   Qiu Yijian Y   Golden Jennifer E JE   Christensen Kenneth A KA   Morris James C JC   Whitehead Daniel C DC  

Chemical communications (Cambridge, England) 20170720 62


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. ...[more]

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