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.
Keywords: DNA Tetraplex, Antitumour Telomerase, nucleic acid biotargets, malignant transformation, covalent fixation processes, chemotherapeutic target, Guanine rich, telomerase activity, isothermal titration calorimetry, stacked G tetrads, mesoporphyrin NMM dye
Mini-Reviews in Medicinal Chemistry
Title: DNA Tetraplex-Binding Drugs Structure-Selective Targeting is Critical for Antitumour Telomerase Inhibition
Volume: 1 Issue: 1
Author(s): Philip J. Perry and Terence C. Jenkins
Affiliation:
Keywords: DNA Tetraplex, Antitumour Telomerase, nucleic acid biotargets, malignant transformation, covalent fixation processes, chemotherapeutic target, Guanine rich, telomerase activity, isothermal titration calorimetry, stacked G tetrads, mesoporphyrin NMM dye
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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Cite this article as:
Perry J. Philip and Jenkins C. Terence, DNA Tetraplex-Binding Drugs Structure-Selective Targeting is Critical for Antitumour Telomerase Inhibition, Mini-Reviews in Medicinal Chemistry 2001; 1 (1) . https://dx.doi.org/10.2174/1389557013407304
DOI https://dx.doi.org/10.2174/1389557013407304 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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