Oxazole-Based Peptide Macrocycles: A New Class of G-Quadruplex Binding Ligands
نویسندگان
چکیده
منابع مشابه
A new method for the study of G-quadruplex ligands.
A new method for the study of G-quadruplex ligands was developed, in which the interaction of G-quadruplexes with ligands can be judged by the naked eye, eliminating the need for any expensive machines.
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Ligands Pravin S. Shirude,† Elizabeth R. Gillies,‡ Sylvain Ladame,† Frédéric Godde,‡ Kazuo Shin-ya,§ Ivan Huc,*,‡ and Shankar Balasubramanian*,† UniVersity Chemical Laboratory, UniVersity of Cambridge, Lensfield Road, Cambridge CB2 1EW, U.K., Institut Européen de Chimie et Biologie, UniVersité Bordeaux 1-CNRS UMR 5248, 2 rue Robert Escarpit, 33607 Pessac, France, and Chemical Biology Team, Biol...
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We report here on the discovery and preliminary evaluation of a novel non-macrocyclic low molecular weight quadruplex-stabilizing chemotype. The lead compounds, based on a furan core, show high G-quadruplex stabilisation and selectivity as well as potent in vitro anti-proliferative activity.
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We report a novel class of biaryl polyamides highly selective for G-quadruplex DNA, and with significant cytotoxicity in several cancer cell lines; they form planar U-shaped structures that match the surface area dimensions of a terminal G-quartet in quadruplex structures rather than the grooves of duplex DNA.
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The G-rich overhang of human telomere tends to form a G-quadruplex structure, and G-quadruplex formation can effectively inhibit telomerase activity in most cancer cells. Therefore, it is important to identify the formation and properties of the G-quadruplex, with the particular aim of selecting G-quadruplex-binding ligands that could potentially lead to the development of anticancer therapeuti...
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ژورنال
عنوان ژورنال: Journal of the American Chemical Society
سال: 2006
ISSN: 0002-7863,1520-5126
DOI: 10.1021/ja064713e