A targeted delivery strategy for the development of potent trypanocides

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 seque...

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Bibliographic Details
Published inChemical communications (Cambridge, England) Vol. 53; no. 62; pp. 8735 - 8738
Main Authors Gordhan, Heeren M., Milanes, Jillian E., Qiu, Yijian, Golden, Jennifer E., Christensen, Kenneth A., Morris, James C., Whitehead, Daniel C.
Format Journal Article
LanguageEnglish
Published CAMBRIDGE Royal Soc Chemistry 11.08.2017
Subjects
Chemistry
Chemistry, Multidisciplinary
Physical Sciences
Science & Technology
HEXOKINASE
TRYPANOSOMA-BRUCEI
PHASE PEPTIDE-SYNTHESIS
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Summary: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.
Bibliography:NIH RePORTER
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ISSN:1359-7345
1364-548X
DOI:10.1039/c7cc03378h