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Open-source discovery of chemical leads for next-generation chemoprotective antimalarials.

Abstract:

To discover leads for next-generation chemoprotective antimalarial drugs, we tested more than 500,000 compounds for their ability to inhibit liver-stage development of luciferase-expressing Plasmodium spp. parasites (681 compounds showed a half-maximal inhibitory concentration of less than 1 micromolar). Cluster analysis identified potent and previously unreported scaffold families as well as other series previously associated with chemoprophylaxis. Further testing through multiple phenotypic...

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Publication status:
Published
Peer review status:
Peer reviewed
Version:
Publisher's version

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Publisher copy:
10.1126/science.aat9446

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Role:
Author
ORCID:
0000-0003-2862-0407
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Role:
Author
ORCID:
0000-0003-2436-7037
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Role:
Author
ORCID:
0000-0003-0272-4443
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Role:
Author
ORCID:
0000-0001-9059-1200
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Bill and Melinda Gates Foundation More from this funder
Medicines for Malaria Venture More from this funder
Wellcome Trust More from this funder
Publisher:
American Association for the Advancement of Science Publisher's website
Journal:
Science Journal website
Volume:
362
Issue:
6419
Pages:
eaat9446
Publication date:
2018-12-07
Acceptance date:
2018-10-18
DOI:
EISSN:
1095-9203
ISSN:
0036-8075
Pubs id:
pubs:951531
URN:
uri:d9357649-0500-41bb-af26-c8aa7cbfd2eb
UUID:
uuid:d9357649-0500-41bb-af26-c8aa7cbfd2eb
Local pid:
pubs:951531
Language:
English
Keywords:

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