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Published on: January 7, 2017
DNA tetraplex-binding drugs: structure-selective targeting is critical for antitumour telomerase inhibition
1Yorkshire Cancer Research Laboratory of Drug Design, University of Bradford, West Yorkshire BD7 1DP, UK.
Abstract:
Four-stranded tetraplex ("G-quadruplex") DNA represents a new paradigm for the design of DNA-interactive antitumour drugs, as the formed DNA-drug complexes have been suggested to interfere with critical telomerase function. The unique structural features presented by tetraplex over duplex DNA have stimulated the design of small ligand molecules able to selectively promote the formation and/or stabilisation of such higher-order DNA structures. Current developments in tetraplex-targeted telomerase inhibitors, and importantly their DNA structural selectivity, are explored.
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