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学科主题: 临床医学
题名:
A new telomerase inhibitor and apoptosis-inducing agent in leukemia: Perylene derivative G-quadruplex ligand Tel03
作者: 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
发表日期: 2008-08-01
DOI: 10.1002/ddr.20248
卷: 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
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/51967
Appears in Collections:北京大学第一临床医学院_血液内科_期刊论文

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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

Recommended Citation:
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.
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