文章基本信息

标题：Identification of mosquito sterol carrier protein-2 inhibitors
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作者：Kim, Min-sik ; Wessely, Vilena ; Lan, Que 等
期刊名称：JLR Papers In Press
印刷版ISSN：0022-2275
电子版ISSN：1539-7262
出版年度：2005
卷号：46
期号：04
页码：650-657
DOI：10.1194/jlr.M400389-JLR200
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