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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / pharmacology*
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Calcium Channel Blockers / chemical synthesis*
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Calcium Channel Blockers / pharmacology*
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Calcium Channels, T-Type / chemistry*
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Calcium Channels, T-Type / metabolism
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Cell Line, Tumor
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Cell Proliferation
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Chemistry, Pharmaceutical / methods
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Doxorubicin / pharmacology
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Drug Design
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Drug Screening Assays, Antitumor*
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Humans
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Inhibitory Concentration 50
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Mice
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Models, Chemical
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Quinazolines / chemical synthesis
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Quinazolines / pharmacology*
Substances
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Antineoplastic Agents
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Calcium Channel Blockers
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Calcium Channels, T-Type
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KYS05080
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Quinazolines
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Doxorubicin