Ezetimib influences the expression of raft-associated antigens in human monocytes.
Aminopeptidase N (CD13) was recently identified as a molecular target of the cholesterol absorption inhibitor Ezetimib. Regarding that CD13 is expressed in lipid rafts of monocytic cells, we have investigated whether Ezetimib influences raft function in these cells. Expression of raft-associated antigens (CD11b, CD13, CD14, CD16, CD36, and CD64) was followed by flow cytometry and/or immunoblot in human monocyte-derived macrophages in response to in vitro administration of Ezetimib. Cellular redistribution of CD13 was assessed by confocal imaging. Ezetimib significantly decreased the surface expression of CD13, CD16, CD64, and CD36; furthermore, it induced a shift of CD13 from plasma membrane to intracellular vesicles, and thus it quite likely modulated monocytic raft-assembly.
Institute for Clinical Chemistry and Laboratory Medicine, University of Regensburg, Regensburg, Germany.
Evelyn
E
Orsó
Tobias
T
Werner
Zsuzsanna
Z
Wolf
Sascha
S
Bandulik
Werner
W
Kramer
Gerd
G
Schmitz
D000924:Anticholesteremic Agents / Q000494:pharmacology; D015703:Antigens, CD / Q000032:analysis / Q000378:metabolism; D000954:Antigens, Surface / Q000032:analysis* / Q000378:metabolism; D001384:Azetidines / Q000494:pharmacology*; D039481:CD11b Antigen / Q000032:analysis / Q000378:metabolism; D018826:CD13 Antigens / Q000032:analysis / Q000378:metabolism; D018955:CD36 Antigens / Q000032:analysis / Q000378:metabolism; D002454:Cell Differentiation / Q000187:drug effects; D002462:Cell Membrane / Q000737:chemistry / Q000187:drug effects / Q000378:metabolism; D000069438:Ezetimibe; D005434:Flow Cytometry; D058851:GPI-Linked Proteins; D006801:Humans; D018950:Lipopolysaccharide Receptors / Q000032:analysis / Q000378:metabolism; D016173:Macrophage Colony-Stimulating Factor / Q000494:pharmacology; D008264:Macrophages / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D021962:Membrane Microdomains / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism; D008856:Microscopy, Fluorescence; D009000:Monocytes / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D021381:Protein Transport / Q000187:drug effects; D017452:Receptors, IgG / Q000032:analysis / Q000378:metabolism
D000924:Anticholesteremic Agents; D015703:Antigens, CD; D000954:Antigens, Surface; D001384:Azetidines; D039481:CD11b Antigen; D018955:CD36 Antigens; C428200:FCGR3B protein, human; D058851:GPI-Linked Proteins; D018950:Lipopolysaccharide Receptors; D017452:Receptors, IgG; D016173:Macrophage Colony-Stimulating Factor; D018826:CD13 Antigens; D000069438:Ezetimibe