T-type Ca2+ channel blockers suppress the growth of human cancer cells.

Abstract

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.

• Authors: Jae Ho Heo, Han Na Seo, Yun Jeong Choe, Sujin Kim, Chun Rim Oh, Young Deuk Kim, Hyewhon Rhim, Dong Joon Choo, Jungahn Kim, Jae Yeol Lee
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 18 Issue 14 Pg. 3899-901 (Jul 15 2008) ISSN: 1464-3405 [Electronic] England
• PMID: 18585035 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Calcium Channel Blockers
• Calcium Channels, T-Type
• KYS05080
• Quinazolines
• Doxorubicin

Topics

• Animals
• Antineoplastic Agents (chemistry, pharmacology)
• Calcium Channel Blockers (chemical synthesis, pharmacology)
• Calcium Channels, T-Type (chemistry, metabolism)
• Cell Line, Tumor
• Cell Proliferation
• Chemistry, Pharmaceutical (methods)
• Doxorubicin (pharmacology)
• Drug Design
• Drug Screening Assays, Antitumor
• Humans
• Inhibitory Concentration 50
• Mice
• Models, Chemical
• Quinazolines (chemical synthesis, pharmacology)