Identification of mosquito sterol carrier protein-2 inhibitors
A mosquito sterol carrier protein-2, AeSCP-2, has been shown to aid in the uptake of cholesterol in mosquito cells. The discovery of chemical inhibitors of AeSCP-2 is reported here. AeSCP-2 inhibitors (SCPIs) belong to several chemotypes of hydrophobic compounds. Those inhibitors competed with chole...
| Main Authors: | , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Elsevier
2005-04-01
|
| Series: | Journal of Lipid Research |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S0022227520339997 |
| _version_ | 1818598987049992192 |
|---|---|
| author | Min-sik Kim Vilena Wessely Que Lan |
| author_facet | Min-sik Kim Vilena Wessely Que Lan |
| author_sort | Min-sik Kim |
| collection | DOAJ |
| description | A mosquito sterol carrier protein-2, AeSCP-2, has been shown to aid in the uptake of cholesterol in mosquito cells. The discovery of chemical inhibitors of AeSCP-2 is reported here. AeSCP-2 inhibitors (SCPIs) belong to several chemotypes of hydrophobic compounds. Those inhibitors competed with cholesterol for AeSCP-2, binding with relatively high binding affinities. In cultured insect cells, SCPIs reduced cholesterol uptake by as much as 30% at 1–5 μM concentrations. SCPIs were potent larvicides to the yellow fever mosquito, Aedes aegypti, and to the tobacco hornworm, Manduca sexta, with 50% lethal doses (LD50s) of 5–21 μM and 0.013–15 ng/mg diet, respectively.The results indicate that sterol carrier protein-2 has functional similarity in two different insect species. |
| first_indexed | 2024-12-16T12:12:25Z |
| format | Article |
| id | doaj.art-ecc54e6a9c6a4e2ea7c91b96e7aa07ee |
| institution | Directory Open Access Journal |
| issn | 0022-2275 |
| language | English |
| last_indexed | 2024-12-16T12:12:25Z |
| publishDate | 2005-04-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Journal of Lipid Research |
| spelling | doaj.art-ecc54e6a9c6a4e2ea7c91b96e7aa07ee2022-12-21T22:32:09ZengElsevierJournal of Lipid Research0022-22752005-04-01464650657Identification of mosquito sterol carrier protein-2 inhibitorsMin-sik Kim0Vilena Wessely1Que Lan2Department of Entomology, University of Wisconsin–Madison, Madison, WisconsinDepartment of Entomology, University of Wisconsin–Madison, Madison, WisconsinDepartment of Entomology, University of Wisconsin–Madison, Madison, WisconsinA mosquito sterol carrier protein-2, AeSCP-2, has been shown to aid in the uptake of cholesterol in mosquito cells. The discovery of chemical inhibitors of AeSCP-2 is reported here. AeSCP-2 inhibitors (SCPIs) belong to several chemotypes of hydrophobic compounds. Those inhibitors competed with cholesterol for AeSCP-2, binding with relatively high binding affinities. In cultured insect cells, SCPIs reduced cholesterol uptake by as much as 30% at 1–5 μM concentrations. SCPIs were potent larvicides to the yellow fever mosquito, Aedes aegypti, and to the tobacco hornworm, Manduca sexta, with 50% lethal doses (LD50s) of 5–21 μM and 0.013–15 ng/mg diet, respectively.The results indicate that sterol carrier protein-2 has functional similarity in two different insect species.http://www.sciencedirect.com/science/article/pii/S0022227520339997cholesterolinsecticidehigh throughput screening |
| spellingShingle | Min-sik Kim Vilena Wessely Que Lan Identification of mosquito sterol carrier protein-2 inhibitors Journal of Lipid Research cholesterol insecticide high throughput screening |
| title | Identification of mosquito sterol carrier protein-2 inhibitors |
| title_full | Identification of mosquito sterol carrier protein-2 inhibitors |
| title_fullStr | Identification of mosquito sterol carrier protein-2 inhibitors |
| title_full_unstemmed | Identification of mosquito sterol carrier protein-2 inhibitors |
| title_short | Identification of mosquito sterol carrier protein-2 inhibitors |
| title_sort | identification of mosquito sterol carrier protein 2 inhibitors |
| topic | cholesterol insecticide high throughput screening |
| url | http://www.sciencedirect.com/science/article/pii/S0022227520339997 |
| work_keys_str_mv | AT minsikkim identificationofmosquitosterolcarrierprotein2inhibitors AT vilenawessely identificationofmosquitosterolcarrierprotein2inhibitors AT quelan identificationofmosquitosterolcarrierprotein2inhibitors |