The development of novel molecular therapeutic agents targeting ion transporters for the treatment of hormone refractory prostate cancer

开发针对离子转运蛋白的新型分子治疗剂，用于治疗激素难治性前列腺癌

• 批准号: 22659290
• 负责人: MIKI Tsuneharu
• 金额: $ 2.14万
• 依托单位: Kyoto Prefectural University of Medicine
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Challenging Exploratory Research
• 财政年份: 2010
• 资助国家: 日本
• 起止时间: 2010 至 2011
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-22659290/
• 关键词: 前立腺癌; 細胞増殖; クロライドイオン; KCC; N-ethylmaleimide

We showed that activation of K^+/Cl^-cotransporter(KCC) led the intracellular Cl^-concentration of androgen-independent prostate cancer cells and decreased proliferation of the cells. We produced various derivatives of N-ethylmaleimide(NEM), KCC activator, and investigated the effect of them on proliferation of androgen-independent prostate cancer cells. The specific derivative for the cells induced the antitumor effect in mouse model of prostate cancer.

我们发现，K^+/Cl^-协同转运蛋白（KCC）的激活导致雄激素非依赖性前列腺癌细胞内Cl^-浓度升高，并降低细胞增殖。我们生产了KCC激活剂N-乙基马来酰亚胺（NEM）的各种衍生物，并研究了它们对雄激素非依赖性前列腺癌细胞增殖的影响。细胞特异性衍生物在小鼠前列腺癌模型中诱导抗肿瘤作用。