Screening Potential Antitumor Agents from Natural Plant Extracts by G-Quadruplex Recognition and NMR Methods

摘要

A currently unique G-quadruplex motif has emerged as a biologically crucial structure that is implicated in several physiologically important regulatory processes, with special emphasis on carcinogenesis. Small molecules that can facilitate the formation of or stabilize the G-quadruplex structures have the potential for the arrest of cancer-cell growth through disruption of telomere maintenance or alteration of oncogene expression levels, and may be potentially valuable as antitumor drugs. A good case in point is the compound quarfloxin (CX-3543), which targets the parallel/mixed class of quadruplexes that are overexpressed in the ribosomal RNA (rRNA) gene during rRNA biogenesis in cancer cells and is currently in clinical trials as an antitumor agent. There is thus a considerable interest in discovering G-quadruplex ligands that could ultimately be used against cancer cells.