DNA Tetraplex-Binding Drugs Structure-Selective Targeting is Critical for Antitumour Telomerase Inhibition

Authors: Perry P.J.; Jenkins T.C.

Source: Mini Reviews in Medicinal Chemistry, Volume 1, Number 1, May 2001 , pp. 31-41(10)

Publisher: Bentham Science Publishers

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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

Language: English

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1389557013407304

Publication date: 2001-05-01

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The aim of Mini-Reviews in Medicinal Chemistry is to publish short reviews on the important recent developments in medicinal chemistry and allied disciplines.

The scope of Mini-Reviews in Medicinal Chemistry will cover all areas of medicinal chemistry including developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies.

Mini-Reviews in Medicinal Chemistry is an essential journal for every medicinal and pharmaceutical chemist who wishes to be kept informed and up-to-date with the latest and most important developments.