Caterino, Marco published the artcileSelective binding of a bioactive porphyrin-based photosensitizer to the G-quadruplex from the KRAS oncogene promoter, Computed Properties of 111-87-5, the main research area is cervical cancer KRAS porphyrin G quadruplex photosensitizer photodynamic therapy; Biophysics; Chlorins; G-quadruplex; Ligands; Photodynamic activity; Singlet oxygen generation.
The G-quadruplex-forming sequence within the KRAS proto-oncogene P1 promoter is a promising target for anticancer therapy. Porphyrin derivatives are among the most rewarding G-quadruplex binders. They can also behave as photosensitizers. Three water-soluble, pos. charged porphyrin-like compounds were synthesized and tested for their interaction with the KRAS G-quadruplex by CD, fluorescence, and mol. docking calculations For a comparison of ligands binding affinity and selectivity, TMPyP4 was taken as a reference One out of the three tested compounds proved biol. activity and selectivity for G-quadruplex over duplex DNA. It also showed to discriminate between different G-quadruplex topologies, with a preference for the parallel over antiparallel conformation. Mol. docking studies suggested a preferential binding to the 3′-end of the KRAS G-quadruplex driven through π-π stacking interactions. Biol. assays also revealed a good photodynamic-induced cytotoxicity on HeLa cells. The reported results show that these porphyrin-like compounds could actually give the basis for the development of G-quadruplex ligands with effective photodynamic-induced cytotoxicity on cancer cells. The possibility of obtaining photosensitizers with improved physico-chem. features and able to selectively target G-quadruplexes is a very interesting perspective to develop new therapeutic agents.
International Journal of Biological Macromolecules published new progress about Antitumor agents. 111-87-5 belongs to class alcohols-buliding-blocks, name is n-Octanol, and the molecular formula is C8H18O, Computed Properties of 111-87-5.
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