• Biochem. Biophys. Res. Commun. · Jul 2013

    Thio-Cl-IB-MECA, a novel A₃ adenosine receptor agonist, suppresses angiogenesis by regulating PI3K/AKT/mTOR and ERK signaling in endothelial cells.

    • Gi Dae Kim, Jedo Oh, Lak Shin Jeong, and Sang Kook Lee.
    • College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea.
    • Biochem. Biophys. Res. Commun. 2013 Jul 19; 437 (1): 79-86.

    AbstractAlthough A₃AR agonists exhibit a variety of biological activities including anticancer effects, their possible anti-angiogenic effects have not yet been investigated. In the present study, we assayed the anti-angiogenic activity of thio-Cl-IB-MECA, a novel A₃AR agonist, in cultured HUVECs and mES/EB-derived endothelial cells. Thio-Cl-IB-MECA inhibited migration and tube formation by endothelial cells and dramatically decreased ex vivo microvessel sprouting in cultured mouse aortic rings. The anti-angiogenic activity of thio-Cl-IB-MECA was associated with suppression of the expression of the endothelial biomarker PECAM via regulation of PI3K/AKT/mTOR and ERK signaling in mES/EB-derived endothelial cells.Copyright © 2013 Elsevier Inc. All rights reserved.

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