A Cisplatin Derivative Tetra-Pt(bpy) as an Oncotherapeutic Agent for Targeting ALT Cancer.

Background: In approximately 15% of human cancers, telomere length is maintained independently of telomerase by the homologous recombination (HR)-mediated alternative lengthening of telomeres (ALT) pathway. Whether the ALT pathway can be exploited for therapeutic treatment remains unknown. The purpo...

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Publicado en:JNCI: Journal of the National Cancer Institute Vol. 109; no. 10; pp. 1 - 12
Autores principales: Xiao-hui Zheng, Xin Nie, Yiming Fang, Zepeng Zhang, Yingnan Xiao, Zongwan Mao, Haiying Liu, Jian Ren, Feng Wang, Lixin Xia, Junjiu Huang, Yong Zhao, Zheng, Xiao-Hui, Nie, Xin, Fang, Yiming, Zhang, Zepeng, Xiao, Yingnan, Mao, Zongwan, Liu, Haiying, Ren, Jian
Formato: pictorial research tables/charts Journal Article
Publicado: Oxford University Press / USA Oct2017
Acceso en línea:Ver este registro en EBSCOhost
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      dt: Oct2017
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      pub: Oxford University Press / USA
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        atl: A Cisplatin Derivative Tetra-Pt(bpy) as an Oncotherapeutic Agent for Targeting ALT Cancer.
      aug:
        au:
          Xiao-hui Zheng
          Xin Nie
          Yiming Fang
          Zepeng Zhang
          Yingnan Xiao
          Zongwan Mao
          Haiying Liu
          Jian Ren
          Feng Wang
          Lixin Xia
          Junjiu Huang
          Yong Zhao
          Zheng, Xiao-Hui
          Nie, Xin
          Fang, Yiming
          Zhang, Zepeng
          Xiao, Yingnan
          Mao, Zongwan
          Liu, Haiying
          Ren, Jian
        affil: Key Laboratory of Gene Engineering of the Ministry of Education, School of Life Sciences, Sun Yat-sen University, Guangzhou, P. R. China
      sug:
        subj:
          Neoplasms
          Cell Division Drug Effects
          Cisplatin Analogs and Derivatives
          Drug Therapy Methods
          Antineoplastic Agents Pharmacodynamics
          Telomere Drug Effects
          Mice
          Antineoplastic Agents Therapeutic Use
          Cell Line, Tumor
          Female
          Cisplatin Pharmacodynamics
          Neoplasms Pathology
          Animals
          Neoplasms Drug Therapy
          Human
          Animal Studies
          Molecular Structure
          Female
      ab: Background: In approximately 15% of human cancers, telomere length is maintained independently of telomerase by the homologous recombination (HR)-mediated alternative lengthening of telomeres (ALT) pathway. Whether the ALT pathway can be exploited for therapeutic treatment remains unknown. The purpose of this study is to develop oncotherapeutic agent to target ALT cancers.Methods: Surface plasmon resonance assay, antibody to G-quadruplex, and fluorescence in situ hybridization (FISH) were used to discover Tetra-Pt(bpy), a cisplatin derivative that specifically targets telomeric G-quadruplex. We used immunofluorescence, FISH, C-circle assay, and chromosome orientation FISH to evaluate the inhibitory effect of Tetra-Pt(bpy) on ALT activity in human ALT cancers. The shortening of telomere length induced by Tetra-Pt(bpy) was determined by telomere restriction fragment or Q-FISH. Cell destination after Tetra-Pt(bpy) treatment was determined by β-gal staining or apoptosis assay. Nude mice (n = 4 per group) were injected with U2OS cells to evaluate the effects of Tetra-Pt(bpy) on tumor growth. All statistical tests were two-sided.Results: Tetra-Pt(bpy) inhibits the strand invasion/annealing step of telomeric homologous recombination by selectively converting telomeric ssDNA to a G-quadruplex. ALT-cells treated with Tetra-Pt(bpy) show fewer ALT-associated promyelocytic leukemia bodies (untreated: mean±SD = 5.9±0.2 vs treated: mean±SD = 3.1±0.1, P < .001), fewer extrachromosomal C-circles (untreated: mean±SD = 100.5±1.6 vs treated: mean±SD = 18.0±1.7, P < .001), and reduced telomere sister chromatin exchanges (untreated: mean±SD = 25.2%±1.5% vs treated: mean±SD = 13.1%±1.9%, P < .001). Consequently, critically short telomeres accumulate after multiple population doublings (untreated: mean±SD = 18.9%±1.7% vs treated: mean±SD = 57.4%±2.2%, P < .001), resulting in cell death by apoptosis or senescence. In vivo, Tetra-Pt(bpy) severely inhibits the growth of ALT-cell xenograft tumors in mice (untreated: mean±SD = 57.1±3.7 mm 3 vs treated: mean±SD = 19.0±3.2 mm 3 , P < .001). Importantly, Tetra-Pt(bpy) exhibits no adverse effects on proliferation, gene expression, or telomere metabolism in normal cells.Conclusions: These results reveal the potential of Tetra-Pt(bpy) as a novel oncotherapeutic agent for targeting ALT cancer cells.
      pubtype: Academic Journal
      doctype:
        pictorial
        research
        tables/charts
        Journal Article
      ougenre: Article
    language: English
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