- Title
- Screening for small molecule modulators of Trypanosoma brucei Hsp70 chaperone activity based upon alcyonarian coral-derived natural products
- Creator
- Andreassend, Sarah K, Bentley, Stephen, Blatch, Gregory L, Boshoff, Aileen, Keyzers, Robert A
- Subject
- To be catalogued
- Date
- 2020
- Type
- text
- Type
- article
- Identifier
- http://hdl.handle.net/10962/426045
- Identifier
- vital:72309
- Identifier
- xlink:href="https://doi.org/10.3390/md18020081"
- Description
- 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.
- Format
- computer, online resource, application/pdf, 1 online resource (38 pages), pdf
- Publisher
- MDPI
- Language
- English
- Relation
- Marine Drugs, Andreassend, S.K., Bentley, S.J., Blatch, G.L., Boshoff, A. and Keyzers, R.A. (2020) Screening for small molecule modulators of Trypanosoma brucei Hsp70 chaperone activity based upon alcyonarian coral-derived natural products. Marine Drugs. 18 (2):81, Marine Drugs volume 18 number 2 p. 81 2020 1660-3397
- Rights
- Publisher
- Rights
- Use of this resource is governed by the terms and conditions of the MDPI Open Access Statement (https://www.int-res.com/journals/terms-of-use/)
- Rights
- Open Access
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- Visitors: 243
- Downloads: 10
Collections
RU DST/NRF SARChI for Biotechnology Innovation and Engagement
Boshoff, Aileen (Assoc Prof)
Blatch, Gregory Lloyd (Prof)
SDG 09. Industry, Innovation and Infrastructure
RU Department of Biochemistry, Microbiology and Bioinformatics
SDG 03. Good Health and Well-Being
SDG 14. Life Below Water
| Thumbnail | File | Description | Size | Format | |||
|---|---|---|---|---|---|---|---|
| View Details Download | SOURCE1 | Screening for small molecule modulators of Trypanosoma brucei Hsp70 chaperone.pdf | 5 MB | Adobe Acrobat PDF | View Details Download |