IBP-I-K-3, a novel Kv10.1 channel inhibitor for hepatoma therapy
编号:55 访问权限:仅限参会人 更新:2021-08-03 19:14:03 浏览:714次 张贴报告

报告开始:2021年08月07日 14:40(Asia/Shanghai)

报告时间:20min

所在会场:[S2] Poster session [Po] Poster session

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摘要
Abstract: Liver cancer remains difficult to treat, owing to a paucity of drugs that target therapy. Targeting Kv10.1 channel may represent a strategy for the treatment of liver cancer. Therefore, the screening of Kv10.1 channel inhibitors with specificity and safety is very essential. Here, we identified that IBP-I-K-3, a natural compound, is a novel Kv10.1 channel inhibitor and it can suppress Kv10.1 current in a dose-dependent manner. The IC50 value of IBP-I-K-3 to Kv10.1 whole-cell current is 49.7 ± 0.9 nM. Further, IBP-I-K-3 concentration-dependently inhibited the proliferation and migration of HepG2, Huh-7 or Lo2-Kv10.1 cells, and the inhibition effect for HepG2 can be abolished by knockdown of the endogenous Kv10.1 with shRNA. In addition, we injected IBP-I-K-3 on xenograft mouse model which exhibited highly effective anti-tumor activity without adverse effects. In summary, IBP-I-K-3 can be used as a lead compound for anti-hepatocellular carcinoma drugs targeting Kv10.1.
 
关键词
Liver cancer, Kv10.1; inhibitor; IBP-I-K-3; therapeutic.
报告人
mabiao
河北工业大学生物物理研究所

稿件作者
mabiao 河北工业大学生物物理研究所
安海龙 河北工业大学
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重要日期
  • 会议日期

    08月06日

    2021

    08月09日

    2021

  • 08月09日 2021

    注册截止日期

主办单位
中国神经科学学会离子通道与受体分会
承办单位
河北工业大学
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