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Potential of 4 '-(p-Toluenesulfonylamide)-4-hydroxychalcone to Inhibit the Human Cytochrome P450 2J2 Isoform
- Issue Date
- Feb-2014
- Publisher
- KOREAN SOC APPLIED BIOLOGICAL CHEMISTRY
- Keywords
- CYP2J2; cytotoxicity; drug interactions; human liver microsomes; TSAHC
- Citation
- JOURNAL OF THE KOREAN SOCIETY FOR APPLIED BIOLOGICAL CHEMISTRY, v.57, no.1, pp 31 - 34
- Pages
- 4
- Indexed
- SCIE
SCOPUS
KCI
- Journal Title
- JOURNAL OF THE KOREAN SOCIETY FOR APPLIED BIOLOGICAL CHEMISTRY
- Volume
- 57
- Number
- 1
- Start Page
- 31
- End Page
- 34
- ISSN
- 1738-2203
2234-344X
- 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.
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