High Throughput Screening Identifies Novel Lead Compounds with Activity against Larval, Juvenile and Adult Schistosoma mansoni.
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....
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ftdoajarticles:oai:doaj.org/article:d3931aef593f48d39c5e473c5df191f8 2023-05-15T15:04:45+02:00 High Throughput Screening Identifies Novel Lead Compounds with Activity against Larval, Juvenile and Adult Schistosoma mansoni. Nuha R Mansour Ross Paveley J Mark F Gardner Andrew S Bell Tanya Parkinson Quentin Bickle 2016-04-01T00:00:00Z https://doi.org/10.1371/journal.pntd.0004659 https://doaj.org/article/d3931aef593f48d39c5e473c5df191f8 EN eng Public Library of Science (PLoS) http://europepmc.org/articles/PMC4851381?pdf=render https://doaj.org/toc/1935-2727 https://doaj.org/toc/1935-2735 1935-2727 1935-2735 doi:10.1371/journal.pntd.0004659 https://doaj.org/article/d3931aef593f48d39c5e473c5df191f8 PLoS Neglected Tropical Diseases, Vol 10, Iss 4, p e0004659 (2016) Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270 article 2016 ftdoajarticles https://doi.org/10.1371/journal.pntd.0004659 2022-12-31T03:28:56Z 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. Article in Journal/Newspaper Arctic Directory of Open Access Journals: DOAJ Articles Arctic PLOS Neglected Tropical Diseases 10 4 e0004659 |
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Open Polar |
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Directory of Open Access Journals: DOAJ Articles |
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ftdoajarticles |
language |
English |
topic |
Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270 |
spellingShingle |
Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270 Nuha R Mansour Ross Paveley J Mark F Gardner Andrew S Bell Tanya Parkinson Quentin Bickle High Throughput Screening Identifies Novel Lead Compounds with Activity against Larval, Juvenile and Adult Schistosoma mansoni. |
topic_facet |
Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270 |
description |
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. |
format |
Article in Journal/Newspaper |
author |
Nuha R Mansour Ross Paveley J Mark F Gardner Andrew S Bell Tanya Parkinson Quentin Bickle |
author_facet |
Nuha R Mansour Ross Paveley J Mark F Gardner Andrew S Bell Tanya Parkinson Quentin Bickle |
author_sort |
Nuha R Mansour |
title |
High Throughput Screening Identifies Novel Lead Compounds with Activity against Larval, Juvenile and Adult Schistosoma mansoni. |
title_short |
High Throughput Screening Identifies Novel Lead Compounds with Activity against Larval, Juvenile and Adult Schistosoma mansoni. |
title_full |
High Throughput Screening Identifies Novel Lead Compounds with Activity against Larval, Juvenile and Adult Schistosoma mansoni. |
title_fullStr |
High Throughput Screening Identifies Novel Lead Compounds with Activity against Larval, Juvenile and Adult Schistosoma mansoni. |
title_full_unstemmed |
High Throughput Screening Identifies Novel Lead Compounds with Activity against Larval, Juvenile and Adult Schistosoma mansoni. |
title_sort |
high throughput screening identifies novel lead compounds with activity against larval, juvenile and adult schistosoma mansoni. |
publisher |
Public Library of Science (PLoS) |
publishDate |
2016 |
url |
https://doi.org/10.1371/journal.pntd.0004659 https://doaj.org/article/d3931aef593f48d39c5e473c5df191f8 |
geographic |
Arctic |
geographic_facet |
Arctic |
genre |
Arctic |
genre_facet |
Arctic |
op_source |
PLoS Neglected Tropical Diseases, Vol 10, Iss 4, p e0004659 (2016) |
op_relation |
http://europepmc.org/articles/PMC4851381?pdf=render https://doaj.org/toc/1935-2727 https://doaj.org/toc/1935-2735 1935-2727 1935-2735 doi:10.1371/journal.pntd.0004659 https://doaj.org/article/d3931aef593f48d39c5e473c5df191f8 |
op_doi |
https://doi.org/10.1371/journal.pntd.0004659 |
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PLOS Neglected Tropical Diseases |
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10 |
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4 |
container_start_page |
e0004659 |
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1766336482585346048 |