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....
Saved in:
| Main Authors: | , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Public Library of Science (PLoS)
2016-04-01
|
| Series: | PLoS Neglected Tropical Diseases |
| Online Access: | https://journals.plos.org/plosntds/article/file?id=10.1371/journal.pntd.0004659&type=printable |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| _version_ | 1849472503543496704 |
|---|---|
| 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 |
| collection | DOAJ |
| 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 |
| id | doaj-art-d3931aef593f48d39c5e473c5df191f8 |
| institution | Kabale University |
| issn | 1935-2727 1935-2735 |
| language | English |
| publishDate | 2016-04-01 |
| publisher | Public Library of Science (PLoS) |
| record_format | Article |
| series | PLoS Neglected Tropical Diseases |
| spelling | doaj-art-d3931aef593f48d39c5e473c5df191f82025-08-20T03:24:30ZengPublic Library of Science (PLoS)PLoS Neglected Tropical Diseases1935-27271935-27352016-04-01104e000465910.1371/journal.pntd.0004659High Throughput Screening Identifies Novel Lead Compounds with Activity against Larval, Juvenile and Adult Schistosoma mansoni.Nuha R MansourRoss PaveleyJ Mark F GardnerAndrew S BellTanya ParkinsonQuentin BickleAn 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.https://journals.plos.org/plosntds/article/file?id=10.1371/journal.pntd.0004659&type=printable |
| spellingShingle | 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. PLoS Neglected Tropical Diseases |
| title | 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_short | 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 |
| url | https://journals.plos.org/plosntds/article/file?id=10.1371/journal.pntd.0004659&type=printable |
| work_keys_str_mv | AT nuharmansour highthroughputscreeningidentifiesnovelleadcompoundswithactivityagainstlarvaljuvenileandadultschistosomamansoni AT rosspaveley highthroughputscreeningidentifiesnovelleadcompoundswithactivityagainstlarvaljuvenileandadultschistosomamansoni AT jmarkfgardner highthroughputscreeningidentifiesnovelleadcompoundswithactivityagainstlarvaljuvenileandadultschistosomamansoni AT andrewsbell highthroughputscreeningidentifiesnovelleadcompoundswithactivityagainstlarvaljuvenileandadultschistosomamansoni AT tanyaparkinson highthroughputscreeningidentifiesnovelleadcompoundswithactivityagainstlarvaljuvenileandadultschistosomamansoni AT quentinbickle highthroughputscreeningidentifiesnovelleadcompoundswithactivityagainstlarvaljuvenileandadultschistosomamansoni |