Pyridostatin hydrochloride is a G-quadruplexe stabilizer, with a Kd of 490 nM. Kd: 490 nM (G-quadruplexe)[1]
Pyridostatin hydrochloride is a G-quadruplexe stabilizer, with a Kd of 490 nM[1]. Pyridostatin (PDS) shows neurotoxic activity against primary cortical neurons at 0.01-5 μM, causes DNA double-strand breaks (DSBs) at 1 μM, downregulates BRCA1 in neurons at 1, 2 or 5 μM[2]. Pyridostatin interacts with G-quadruplex motifs in SRC and alters mRNA levels of damaged genes[3].
[1]. Koirala D, et al. A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands. Nat Chem. 2011 Aug 28;3(10):782-7. [2]. Moruno-Manchon JF, et al. The G-quadruplex DNA stabilizing drug pyridostatin promotes DNA damage and downregulates transcription of Brca1 in neurons. Aging (Albany NY). 2017 Sep 12;9(9):1957-1970. [3]. Rodriguez R, et al. Small-molecule-induced DNA damage identifies alternative DNA structures in human genes. Nat Chem Biol. 2012 Feb 5;8(3):301-10.