Micheli Emanuela, Lombardo Caterina Maria, D'Ambrosio Danilo, Franceschin Marco, Neidle Stephen, Savino Maria
Dipartimento di Chimica, Sapienza Università di Roma, Roma, Italy.
Bioorg Med Chem Lett. 2009 Jul 15;19(14):3903-8. doi: 10.1016/j.bmcl.2009.03.106. Epub 2009 Mar 26.
The human telomeric G-quadruplex structure is a promising target for the design of cancer drugs. The selectivity of G-quadruplex ligands with respect to duplex genomic DNA is of especial importance. The high selectivity of polyamine conjugated perylene derivatives appears to be regulated by side-chain charge density, as indicated by data from a FRET melting assay and induced CD spectroscopy.
人类端粒G-四链体结构是癌症药物设计的一个有前景的靶点。G-四链体配体相对于双链基因组DNA的选择性尤为重要。如荧光共振能量转移熔解实验和诱导圆二色光谱的数据所示，多胺共轭苝衍生物的高选择性似乎受侧链电荷密度的调控。
