Telomerase inhibition, telomere shortening, and decreased cell proliferation by cell permeable 2′-O-methoxyethyl oligonucleotides

被引:19
作者
Chen, Z
Monia, BP
Corey, DR [1 ]
机构
[1] SW Texas State Univ, Ctr Med, Dept Pharmacol, Dallas, TX 75390 USA
[2] SW Texas State Univ, Ctr Med, Dept Biochem, Dallas, TX 75390 USA
[3] ISIS Pharmaceut, Carlsbad, CA 92008 USA
关键词
D O I
10.1021/jm025563v
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
Telomerase is an attractive target for chemotherapy. Testing this hypothesis will require potent inhibitors with favorable pharmacokinetic properties. We report that 2'-methoxyethyl oligonucleotides complementary to the telomerase RNA component diffuse across cell membranes without the need for cationic carrier lipid, inhibit telomerase, and cause telomeres to shorten. The ability of antitelomerase oligomers to enter cells without the need to add lipid will simplify preclinical studies and may suggest advantages for clinical use.
引用
收藏
页码:5423 / 5425
页数:3
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