pyridostatin

Pyridostatin (PDS) is a synthetic small molecule that functions as a potent and highly selective stabilizer of G-quadruplex (G4) DNA and RNA structures. It binds with high affinity (Kd of 490 nM) to G4 structures, which are secondary nucleic acid conformations found in guanine-rich regions such as telomeres and the promoter sequences of various proto-oncogenes, including c-kit, K-ras, Bcl-2, and Src. By stabilizing these structures, pyridostatin induces replication- and transcription-dependent DNA damage, leading to the activation of the DNA damage response, cell cycle arrest, and growth inhibition in cancer cells. Preclinical research has highlighted its potential anti-tumor activity, particularly in BRCA1/2-deficient tumors and those resistant to PARP inhibitors, by exploiting synthetic lethality. Currently, pyridostatin is primarily utilized as a chemical biology research tool and is not approved for clinical use.

Other names

4-(2-aminoethoxy)-N2,N6-bis[4-(2-aminoethoxy)-2-quinolinyl]-2,6-pyridinedicarboxamide