Scott W. Altmann

TL;DR: It is shown that Niemann-Pick C1Like 1(NPC1L1) protein plays a critical role in the absorption of intestinal cholesterol, and resides in an ezetimibe-sensitive pathway responsible for intestinal cholesterol absorption.

TL;DR: A binding assay is developed and shown that labeled ezetimibe glucuronide binds specifically to a single site in brush border membranes and to human embryonic kidney 293 cells expressing NPC1L1, which unequivocally establish NPC1 L1 as the direct target of ezETimibe and should facilitate efforts to identify the molecular mechanism of cholesterol transport.

TL;DR: NPC1L1 is required for intestinal uptake of both cholesterol and phytosterols and plays a major role in cholesterol homeostasis and may be a useful drug target for the treatment of hypercholesterolemia and sitosterolemia.

TL;DR: The identification of OB-BP1/Siglec-6 as a Siglec family member, coupled with its restricted expression pattern, suggests that it may mediate cell-cell recognition events by interacting with sialylated glycoprotein ligands expressed on specific cell populations.

TL;DR: The binding of ezetimibe to cells expressing SR-B1 and the functional blockade of SR-b1-mediated cholesterol absorption in vitro suggest that SR- B1 plays a role in intestinal cholesterol metabolism and the inhibitory activity of eZetimibes.