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Open AccessFeature PaperArticle

Screening for Small Molecule Modulators of Trypanosoma brucei Hsp70 Chaperone Activity Based upon Alcyonarian Coral-Derived Natural Products

1
School of Chemical and Physical Sciences, Victoria University of Wellington, Wellington 6012, New Zealand
2
Centre for Biodiscovery, Victoria University of Wellington, Wellington 6012, New Zealand
3
Biotechnology Innovation Centre, Rhodes University, Grahamstown 6140, South Africa
4
Biomedical Biotechnology Research Unit, Department of Biochemistry and Microbiology, Grahamstown 6140, South Africa
5
Office of the PVC Research, The University of Notre Dame Australia, Fremantle, Western Australia 6959, Australia
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Mar. Drugs 2020, 18(2), 81; https://doi.org/10.3390/md18020081
Received: 13 December 2019 / Revised: 14 January 2020 / Accepted: 16 January 2020 / Published: 27 January 2020
(This article belongs to the Special Issue Chemical Modification of Marine Natural Products)
The Trypanosoma brucei Hsp70/J-protein machinery plays an essential role in survival, differentiation, and pathogenesis of the protozoan parasite, and is an emerging target against African Trypanosomiasis. This study evaluated a set of small molecules, inspired by the malonganenones and nuttingins, as modulators of the chaperone activity of the cytosolic heat inducible T. brucei Hsp70 and constitutive TbHsp70.4 proteins. The compounds were assessed for cytotoxicity on both the bloodstream form of T. b. brucei parasites and a mammalian cell line. The compounds were then investigated for their modulatory effect on the aggregation suppression and ATPase activities of the TbHsp70 proteins. A structure–activity relationship for the malonganenone-class of alkaloids is proposed based upon these results. View Full-Text
Keywords: anti-parasitic; heat shock protein; malonganenone; SAR; African Trypanosomiasis anti-parasitic; heat shock protein; malonganenone; SAR; African Trypanosomiasis
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MDPI and ACS Style

Andreassend, S.K.; Bentley, S.J.; Blatch, G.L.; Boshoff, A.; Keyzers, R.A. Screening for Small Molecule Modulators of Trypanosoma brucei Hsp70 Chaperone Activity Based upon Alcyonarian Coral-Derived Natural Products. Mar. Drugs 2020, 18, 81.

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