Synthesis and Evaluation of a Rationally Designed Click-Based Library for G-Quadruplex Selective DNA Photocleavage

Molecules

Dominic McBrayer¹  Sean M. Kerwin¹ 

[1] Department of Chemistry and Biochemistry, The University of Texas, Austin, TX 78712, USA; E-Mail:

关键词: DNA;    photocleavage;    alkyne-azide click reaction;    PAGE;   

DOI  :  10.3390/molecules200916446

来源: mdpi

【 摘 要 】

DNA containing repeating G-rich sequences can adopt higher-order structures known as G-quadruplexes (G4). These structures are believed to form within telomeres and the promoter regions of some genes, particularly in a number of proto-oncogenes, where they may play a role in regulating transcription. Alternatively, G4 DNA may act as a barrier to replication. To investigate these potential biological roles, probes that combine highly selective G4 DNA targeting with photocleavage activity can allow temporal detection of G4 DNA, providing opportunities to obtain novel insights about the biological roles of G4 DNA. We have designed, synthesized, and screened a small library of potential selective G-quadruplex DNA photocleavage agents incorporating the G-quadruplex targeting moiety of 360A with known photocleavage groups linked via “click” chemistry.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.