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A new telomerase inhibitor and apoptosis-inducing agent in leukemia: Perylene derivative G-quadruplex ligand Tel03
Chu, Bin1; Yuan, Gu2; Zhou, Jiang2; Ou, Yuan1; Zhu, Ping1
关键词G-quadruplex Telomerase Mass Spectrometry Apoptosis Leukemia
刊名DRUG DEVELOPMENT RESEARCH
2008-08-01
DOI10.1002/ddr.20248
69期:5页:235-241
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal ; Pharmacology & Pharmacy
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]IONIZATION MASS-SPECTROMETRY ; DOUBLE-STRANDED OLIGODEOXYNUCLEOTIDES ; DNA TETRAPLEX FORMATION ; C-KIT ONCOGENE ; PROMOTER REGION ; NONCOVALENT COMPLEXES ; INTERACTIVE AGENTS ; SMALL-MOLECULE ; NUCLEIC-ACIDS ; IN-VITRO
英文摘要

Tel03 (N,N′-Bis-(2-(dimethylamino)ethyl)-3,4,9,10-perylentetra-carboxylic acid diimide), a perylene derivative, was synthesized and its interaction with different forms of human telomeric DNA examined. The effect of Tel03 on leukemia cells in short-term Cultures was also used to explore its molecular actions. Electrospray ionization mass spectrometry (ESI-MS) analysis indicated that Tel03 specifically recognizes telomeric quadruplex, not duplex DNA. After the treatment with Tel03 (0.1-10 mu M) for 48h, telomerase activity in K562 leukemia cell extracts was inhibited in a dose-dependent manner as assessed with a telomere repeat amplification protocol (TRAP) assay. MTT assay results showed that Tel03 (0.1-10 mu M) inhibited the proliferation of K562 cells after treatment for 72 h. In addition, apoptosis was observed. Using real-time quantitative PCR and Western Not analysis, the expression of c-myc and bcl-2 was markedly down-regulated at both the mRNA and protein levels. However, no changes were observed in the expression of bax. We conclude that G-quadruplex ligand, Tel03, is a novel telomerase inhibitor and apoptosis-inducing agent in leukemia cells acting via down-regulation of bcl-2 and c-myc. Tel03 has the potential to be developed as an antileukemia drug.

语种英语
WOS记录号WOS:000259889700001
引用统计
被引频次:7[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/51967
专题北京大学第一临床医学院_血液内科
作者单位1.Peking Univ, Hosp 1, Dept Hematol, Beijing 100034, Peoples R China
2.Peking Univ, Coll Chem & Mol Engn, Dept Biol Chem, Beijing 100034, Peoples R China
推荐引用方式
GB/T 7714
Chu, Bin,Yuan, Gu,Zhou, Jiang,et al. A new telomerase inhibitor and apoptosis-inducing agent in leukemia: Perylene derivative G-quadruplex ligand Tel03[J]. DRUG DEVELOPMENT RESEARCH,2008,69(5):235-241.
APA Chu, Bin,Yuan, Gu,Zhou, Jiang,Ou, Yuan,&Zhu, Ping.(2008).A new telomerase inhibitor and apoptosis-inducing agent in leukemia: Perylene derivative G-quadruplex ligand Tel03.DRUG DEVELOPMENT RESEARCH,69(5),235-241.
MLA Chu, Bin,et al."A new telomerase inhibitor and apoptosis-inducing agent in leukemia: Perylene derivative G-quadruplex ligand Tel03".DRUG DEVELOPMENT RESEARCH 69.5(2008):235-241.
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