BMB Reports 2018; 51(10): 520-525
LJ-1888, a selective antagonist for the A3 adenosine receptor, ameliorates the development of atherosclerosis and hypercholesterolemia in apolipoprotein E knock-out mice
Jong-Gil Park1,#, Se-Jin Jeong2,#, Jinha Yu3, Gyudong Kim3, Lak Shin Jeong3 and Goo Taeg Oh4,*
1Biotherapeutics Translational Research Center, Korea Research Institute of Bioscience & Biotechnology (KRIBB), Daejeon 34141, Korea, 2Cardiovascular Division, Department of Medicine, Washington University School of Medicine, St. Louis, MO, USA, 3College of Pharmacy, Seoul National University, Seoul 08826, 4Immune and Vascular Cell Network Research Center, National Creative Initiatives, Department of Life Sciences, Ewha Womans University, Seoul 03760, Korea
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#These authors contributed equally to this work.
Received: April 30, 2018; Revised: May 21, 2018; Accepted: May 21, 2018; Published online: October 31, 2018.
© Korean Society for Biochemistry and Molecular Biology. All rights reserved.

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Cardiovascular diseases arising from atherosclerosis are the leading causes of mortality and morbidity worldwide. Lipid-lowering agents have been developed in order to treat hypercholesterolemia, a major risk factor for atherosclerosis. However, the prevalence of cardiovascular diseases is increasing, indicating a need to identify novel therapeutic targets and develop new treatment agents. Adenosine receptors (ARs) are emerging as therapeutic targets in asthma, rheumatoid arthritis, cancer, ischemia, and inflammatory diseases. This study assessed whether LJ-1888, a selective antagonist for A3 AR, can inhibit the development of atherosclerosis in apolipoprotein E knock-out (ApoE-/-) mice who are fed a western diet. Plaque formation was significantly lower in ApoE-/- mice administered LJ-1888 than in mice not administered LJ-1888, without any associated liver damage. LJ-1888 treatment of ApoE-/- mice prevented western diet-induced hypercholesterolemia by markedly reducing low-density lipoprotein cholesterol levels and significantly increasing high-density lipoprotein cholesterol concentrations. Reduced hypercholesterolemia in ApoE-/- mice administered LJ-1888 was associated with the enhanced expression of genes involved in bile acid biosynthesis. These findings indicate that LJ-1888, a selective antagonist for A3 AR, may be a novel candidate for the treatment of atherosclerosis and hypercholesterolemia.
Keywords: Atherosclerosis, High-density lipoprotein cholesterol (HDL-chol), Hypercholesterolemia, Low-density lipoprotein cholesterol (LDL-chol), LJ-1888

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