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Scavenger receptor class B, type I (SR-BI) inhibitors act as molecular tools to probe for the function of SR-BI in greater detail. Additionally, because of the known role of SR-BI in the transfer of cholesterol between cells and high-density lipoproteins (HDL), SR-BI inhibitors can be used to increase plasma HDL-cholesterol (HDL-C) concentration, which epidemiologic studies have shown is inversely related to atherosclerosis severity. SR-BI inhibitors could also potentially block cellular entry of HCV and malaria parasites that use SR-BI as co-receptors, thus, acting as potential therapy against HCV infection and malaria.