High throughput screening identifies novel lead compounds with activity against larval, juvenile and adult Schistosoma mansoni
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Author(s)
Type
Journal Article
Abstract
An estimated 600 million people are affected by the helminth disease schistosomiasis caused by parasites of the genus Schistosoma. There is currently only one drug recommended for treating schistosomiasis, praziquantel (PZQ), which is effective against adult worms but not against the juvenile stage. In an attempt to identify improved drugs for treating the disease, we have carried out high throughput screening of a number of small molecule libraries with the aim of identifying lead compounds with balanced activity against all life stages of Schistosoma. A total of almost 300,000 compounds were screened using a high throughput assay based on motility of worm larvae and image analysis of assay plates. Hits were screened against juvenile and adult worms to identify broadly active compounds and against a mammalian cell line to assess cytotoxicity. A number of compounds were identified as promising leads for further chemical optimization.
Date Issued
2016-04
Date Acceptance
2016-04-01
Citation
PLoS Neglected Tropical Diseases, 2016, 10 (4)
ISSN
1935-2727
Publisher
Public Library of Science (PLoS)
Journal / Book Title
PLoS Neglected Tropical Diseases
Volume
10
Issue
4
Copyright Statement
© 2016 Mansour et al. This is an open
access article distributed under the terms of the
Creative Commons Attribution License, which permits
unrestricted use, distribution, and reproduction in any
medium, provided the original author and source are
credited.
access article distributed under the terms of the
Creative Commons Attribution License, which permits
unrestricted use, distribution, and reproduction in any
medium, provided the original author and source are
credited.
License URL
Identifier
https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000375376700073&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=a2bf6146997ec60c407a63945d4e92bb
Subjects
ASSAY
DRUG DISCOVERY
HIT
Infectious Diseases
INHIBITORS
LIBRARY
Life Sciences & Biomedicine
Parasitology
PRAZIQUANTEL
Science & Technology
STRATEGIES
Tropical Medicine
Publication Status
Published
Article Number
e0004659
Date Publish Online
2016-04-29