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Inhibition of cell proliferation through cell cycle arrest and apoptosis by thio-Cl-IB-MECA, a novel A3 adenosine receptor agonist, in human lung cancer cells

Title
Inhibition of cell proliferation through cell cycle arrest and apoptosis by thio-Cl-IB-MECA, a novel A3 adenosine receptor agonist, in human lung cancer cells
Authors
Kim S.-J.Min H.-Y.Chung H.-J.Park E.-J.Hong J.-Y.Kang Y.-J.Shin D.-H.Jeong L.S.Lee S.K.
Ewha Authors
정낙신이상국
Issue Date
2008
Journal Title
Cancer Letters
ISSN
0304-3835JCR Link
Citation
vol. 264, no. 2, pp. 309 - 315
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
Human A3 adenosine receptor (A3AR) agonists showed the anti-tumor activity in various in vitro and in vivo studies. The present study investigates the anti-proliferative effect of a novel adenosine analog 2-chloro-N6-(3-iodobenzyl)-4′-thioadenosine-5′-N-methyluronamide (thio-Cl-IB-MECA) in A549 human lung cancer cells. Thio-Cl-IB-MECA induced arrest of cell cycle progression in G0/G1 phase at lower concentrations (up to 20 μM) and apoptotic cell death at a higher concentration (80 μM), which were manifested by down-regulation of cyclin D1, c-myc, and CDK4, activation of caspase-3 and -9, and cleavage of poly(ADP-ribose) polymerase (PARP). The activation of Akt-mediated signaling was also inhibited by treatment with thio-Cl-IB-MECA. These data might suggest the potential therapeutic value of an adenosine analog in the treatment of human lung cancer. © 2008 Elsevier Ireland Ltd. All rights reserved.
DOI
10.1016/j.canlet.2008.01.037
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약학대학 > 약학과 > Journal papers
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