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TOFA研究進(jìn)展

發(fā)布日期：2017-10-27   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/TOFA.htmlTOFA/a產(chǎn)品描述：TOFA (RMI14514;MDL14514) is an allosteric inhibitor of ac
<a href="https://www.medchemexpress.com/TOFA.html">TOFA</a>產(chǎn)品描述：TOFA (RMI14514;MDL14514) is an allosteric inhibitor of acetyl-CoA carboxylase-α (<b>ACCA </b>).

<i><b>In Vitro:</b></i> TOFA (5-tetradecyloxy-2-furoic acid) is cytotoxic to lung cancer cells NCI-H460 and colon carcinoma cells HCT-8 and HCT-15, with an IC<sub>50</sub> at approximately 5.0, 5.0, and 4.5 μg/mL, respectively. TOFA at 1.0–20.0 μg/mL effectively blocks fatty acid synthesis and induces cell death in a dose-dependent manner<sup>[1]</sup>. TOFA is found to be cytotoxic to COC1 and COC1/DDP cells with IC<sub>50</sub> values of ~26.1 and 11.6 µg/mL, respectively. TOFA inhibits the proliferation of the cancer cells examined in a time  and dose dependent manner, arrests the cells in the G0/G1 cell cycle phase and induces apoptosis<sup>[2]</sup>. Acetyl-CoA-carboxylase-α (ACCA) is a key enzyme in the regulation of fatty acids synthesis. Inhibition of ACCA by TOFA decreases fatty acid synthesis and induces caspase activation and cell death in most PCa cell lines<sup>[3]</sup>.

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