1236926-61-6Relevant articles and documents
Pyridostatin analogues promote telomere dysfunction and long-term growth inhibition in human cancer cells
Müller, Sebastian,Sanders, Deborah A.,Di Antonio, Marco,Matsis, Stephanos,Riou, Jean-Fran?ois,Rodriguez, Rapha?l,Balasubramanian, Shankar
supporting information; experimental part, p. 6537 - 6546 (2012/09/08)
The synthesis, biophysical and biological evaluation of a series of G-quadruplex interacting small molecules based on a N,N′-bis(quinolinyl) pyridine-2,6-dicarboxamide scaffold is described. The synthetic analogues were evaluated for their ability to stabilize telomeric G-quadruplex DNA, some of which showed very high stabilization potential associated with high selectivity over double-stranded DNA. The compounds exhibited growth arrest of cancer cells with detectable selectivity over normal cells. Long-time growth arrest was accompanied by senescence, where telomeric dysfunction is a predominant mechanism together with the accumulation of restricted DNA damage sites in the genome. Our data emphasize the potential of a senescence-mediated anticancer therapy through the use of G-quadruplex targeting small molecules based on the molecular framework of pyridostatin.
Small molecule-mediated inhibition of translation by targeting a native RNA G-quadruplex
Bugaut, Anthony,Rodriguez, Raphael,Kumari, Sunita,Hsu, Shang-Te Danny,Balasubramanian, Shankar
supporting information; experimental part, p. 2771 - 2776 (2010/08/21)
Herein, we show that a naturally occurring RNA G-quadruplex element within the 5′ UTR of the human NRAS proto-oncogene is a target for a small molecule that inhibits translation in vitro. The present study provides a first demonstration that natural 5′ UTR mRNA G-quadruplexes have potential as molecular targets for small molecules that modulate translation.
