Quadruplex Bindingclicks Into Place

摘要

Small molecules selectively targeting four-stranded DNA could lead to anticancer drugs without the toxic side-effects, say scientists in the UK.rnQuadruplex DNA is a four-strand form of the biomolecule and is associated with cancer cell replication. Stephen Neidle and William Drewe at the University of London designed a series of diphenyl urea-based structures that bind strongly to quadruplex DNA but have low affinity for duplex DNA - the two strand double helix. This selectivity means the molecules aren't toxic to healthy cells, and could specifically knock out cancer cell growth, says Neidle.rnGuanine-rich DNA quadruplexes (G4s) can be found in many telomeres, end sections of chromosomes which in healthy tissue gradually degrade until the cell can no longer divide. But in cancer cells, telomeres are continually maintained by telomerase - an enzyme switched off in most healthy adult tissue - effectivelyrnmaking cancer cells immortal. Neidle and Drewe's molecules are designed to disrupt telomerase from binding to the quadruplex.