Neidle, S; (2016) Quadruplex Nucleic Acids as Novel Therapeutic Targets. Journal of Medicinal Chemistry , 59 (13) pp. 5987-6011. 10.1021/acs.jmedchem.5b01835.

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Abstract

Quadruplex-forming sequences are widely prevalent in human and other genomes, including bacterial ones. These sequences are over-represented in eukaryotic telomeres, promoters and 5' untranslated regions. They can form quadruplex structures, which may be transient in many situations in normal cells since they can be effectively resolved by helicase action. Mutated helicases in cancer cells are unable to unwind quadruplexes, which are impediments to transcription, translation or replication, depending on their location within a particular gene. Small molecules that can stabilise quadruplex structures augment these effects and produce cell and proliferation growth inhibition. This article surveys the chemical biology of quadruplexes and critically examines the major classes of quadruplex-binding small molecules that have been developed to date, and the various approaches to discovering selective agents. The challenges of requiring (and achieving) small-molecule targeted selectivity for a particular quadruplex are discussed in relation to the potential of these small molecules as potentially clinically-useful therapeutic agents.

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