Heo Jae Ho, Seo Han Na, Choe Yun Jeong, Kim Sujin, Oh Chun Rim, Kim Young Deuk, Rhim Hyewhon, Choo Dong Joon, Kim Jungahn, Lee Jae Yeol
Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University, 1 Hoegi-Dong, Dongdaemun-Gu, Seoul 130-701, Republic of Korea.
Bioorg Med Chem Lett. 2008 Jul 15;18(14):3899-901. doi: 10.1016/j.bmcl.2008.06.034. Epub 2008 Jun 14.
In order to further clarify the role of T-type Ca(2+) channels in cell proliferation, we have measured the growth inhibition of human cancer cells by using our potent T-type Ca(2+) channel blockers. As a result, KYS05090, a most potent T-type Ca(2+) channel blocker, was found to be as potent as doxorubicin against some human cancer cells without acute toxicity. Therefore, this letter provides the biological results that T-type calcium channel is important in regulating the important cellular phenotype transition leading to cell proliferation, and thus novel T-type Ca(2+) channel blocker presents new prospects for cancer treatment.
为了进一步阐明T型钙通道在细胞增殖中的作用，我们使用强效的T型钙通道阻滞剂测量了其对人癌细胞的生长抑制作用。结果发现，最有效的T型钙通道阻滞剂KYS05090在某些人癌细胞上与阿霉素的效力相当，且无急性毒性。因此，本信函提供了生物学结果，表明T型钙通道在调节导致细胞增殖的重要细胞表型转变中起重要作用，因此新型T型钙通道阻滞剂为癌症治疗带来了新的前景。
