The folding of the single-stranded 3' end of the human telomere into G-quadruplex arrangements inhibits the overhang from hybridizing with the RNA template of telomerase and halts telomere maintenance in cancer cells. The ability to thermally stabilize human telomeric DNA as a four-stranded G-quadruplex structure by developing selective small molecule compounds is a therapeutic path to regulating telomerase activity and thereby selectively inhibit cancer cell growth. The development of compounds with the necessary selectivity and affinity to target parallel-stranded G-quadruplex structures has proved particularly challenging to date, relying heavily upon limited structural data. Here you can see an example of structure-based approach to the design of quadruplex-binding ligands to enhance affinity and selectivity for human telomeric DNA. This is the crystal structure of this telomeric DNA in complex with a naphtalene-diimide ligand (PDB code: 3T5E)
#molecularart ... #immolecular ... #telomere ... #DNA ... #drug ... #binding ... Rendered with @proteinimaging and finished with @corelphotopaint
#molecularart ... #immolecular ... #telomere ... #DNA ... #drug ... #binding ... Rendered with @proteinimaging and finished with @corelphotopaint
