出版社：American Society for Biochemistry and Molecular Biology
摘要：A mosquito sterol carrier protein-2, AeSCP-2, has been shownto aid in the uptake of cholesterol in mosquito cells. The discoveryof chemical inhibitors of AeSCP-2 is reported here. AeSCP-2inhibitors (SCPIs) belong to several chemotypes of hydrophobiccompounds. Those inhibitors competed with cholesterol for AeSCP-2,binding with relatively high binding affinities. In culturedinsect cells, SCPIs reduced cholesterol uptake by as much as30% at 1–5 µM concentrations. SCPIs were potentlarvicides to the yellow fever mosquito, Aedes aegypti, andto 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 functionalsimilarity in two different insect species.Supplementary key words cholesterol • insecticide • high throughput screening
Abbreviations: GST, glutathione S-transferase; HDLp, high density lipophorin; RBA, relative binding affinity; SCP, sterol carrier protein; SCP-2, sterol carrier protein-2; SCP-x, sterol carrier protein-x; SCPI, sterol carrier protein-2 inhibitor
