[HTML][HTML] The steroidal analog GW707 activates the SREBP pathway through disruption of intracellular cholesterol trafficking
J Zhang, N Dudley-Rucker, JR Crowley… - Journal of lipid …, 2004 - ASBMB
Recently, a new class of lipid-lowering agents has been described that upregulate LDL
receptor (LDLr) activity. These agents are proposed to activate sterol-regulated gene
expression through binding to the sterol regulatory element binding protein (SREBP)
cleavage-activating protein (SCAP). Here, we show that the steroidal LDLr upregulator,
GW707, induces accumulation of lysosomal free cholesterol and inhibits LDL-stimulated
cholesterol esterification, similar to that observed in U18666A-treated cells and in Niemann …
receptor (LDLr) activity. These agents are proposed to activate sterol-regulated gene
expression through binding to the sterol regulatory element binding protein (SREBP)
cleavage-activating protein (SCAP). Here, we show that the steroidal LDLr upregulator,
GW707, induces accumulation of lysosomal free cholesterol and inhibits LDL-stimulated
cholesterol esterification, similar to that observed in U18666A-treated cells and in Niemann …