کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1370418 | 981819 | 2011 | 5 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Utilizing G-quadruplex formation to target 8-oxoguanine in telomeric sequences Utilizing G-quadruplex formation to target 8-oxoguanine in telomeric sequences](/preview/png/1370418.png)
Utilizing G-quadruplex specific ligands that can induce/bind G-quadruplex DNA in human telomeric regions has recently become an attractive means for cancer chemotherapy because the formation of G-quadruplex structures inhibits the activity of telomerase, a reverse transcriptase mainly expressed in cancer cells. In the present work, we synthesized a type of bifunctional molecules that selectively bind to telomeric DNA via G-quadruplex formation and subsequently react with proximate OxodG in the presence of one-electron oxidant. Such molecules could be useful for telomerase inhibition. Perylene derivatives (7 and 9) containing 1,3-diamino moieties were prepared for demonstration. The binding of 7 with G-quadruplex DNA was determined using UV thermal denaturation and the corresponding binding constant was derived from UV titration. The interactions of 7 with G-quadruplex DNA containing OxodG were characterized using circular dichroism. Gel electrophoresis revealed that 7 can form more adducts with OxodG in G-quadruplex regions than that in duplex DNA.
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Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 21, 1 November 2011, Pages 6357–6361