Potential of 4 '-(p-Toluenesulfonylamide)-4-hydroxychalcone to Inhibit the Human Cytochrome P450 2J2 Isoform

Title
Potential of 4 '-(p-Toluenesulfonylamide)-4-hydroxychalcone to Inhibit the Human Cytochrome P450 2J2 Isoform
Author(s)
강원구이보람[이보람]손종철[손종철]박기훈[박기훈]송경식[송경식]류광현[류광현]
Keywords
HUMAN LIVER-MICROSOMES; IN-VITRO; CYP2J2; METABOLISM; TERFENADINE; ASTEMIZOLE; PROMOTES; ENZYMES; CANCER; HYDROXYEBASTINE
Issue Date
201402
Publisher
KOREAN SOC APPLIED BIOLOGICAL CHEMISTRY
Citation
JOURNAL OF THE KOREAN SOCIETY FOR APPLIED BIOLOGICAL CHEMISTRY, v.57, no.1, pp.31 - 34
Abstract
Human CYP2J2 isoform, the only member of the human CYP2J subfamily, is also over-expressed in human liver carcinoma tissues and hepatocarcinoma cells, and promotes tumor growth and proliferation. 4'-(p-Toluenesulfonylamide)-4-hydroxychalcone (TSAHC) is a synthetic sulfonylamino chalcone compound, which has anti-cancer effect. Inhibitory potential of a promising anti-cancer agent TSAHC against CYP2J2 activity was evaluated using human liver microsomes. TSAHC inhibited CYP2J2-mediated astemizole O-demethylation activity with K-i value of 2.03+/-0.40 mu M in a competitive mode, suggesting that TSAHC is a potential candidate for further evaluation for its CYP2J2 targeting anti-cancer activities. Studies are presently underway to estimate TSAHC as potential therapeutic agent for cancer.
URI
http://hdl.handle.net/YU.REPOSITORY/33127http://dx.doi.org/10.1007/s13765-013-4307-y
ISSN
1738-2203
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약학대학 > 약학부 > Articles
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