Identification of mosquito sterol carrier protein-2 inhibitors
Autor(es): Kim, MS; Wessely, V; Lan, Q
Resumo: 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 mu M concentrations. SCPIs were potent larvicides to the yellow fever mosquito, Aedes aegypti, and to the tobacco hornworm, Manduca sexta, with 50% lethal doses (LD(50)s) of 5-21 mu M and 0.013-15 ng/mg diet, respectively. The results indicate that sterol carrier protein-2 has functional similarity in two different insect species.
Palavras-Chave: Cholesterol; Insecticide; High Throughput Screening
Imprenta: Journal of Lipid Research, v. 46, n. 4, p. 650-657, 2005
Identificador do objeto digital: 10.1194/jlr.M400389-JLR200
Descritores: Aedes aegypti - Cell ; Aedes aegypti - Proteins ; Aedes aegypti - Larvicide
Data de publicação: 2005
