Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 14, Pages 3903-3908Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.03.106
Keywords
G-quadruplex DNA; Perylene derivatives; Polyamines; Telomerase inhibitors; FRET; TRAP assay; CD spectroscopy; UV/vis absorption; Competition experiments
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Funding
- PRIN
- Fondazione Cenci- Bolognetti
- Istituto Pasteur (Rome)
- Cancer Research UK (London)
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The human telomeric G-quadruplex structure is a promising target for the design of cancer drugs. The selectivity of G-quadruplex ligands with respect to duplex genomic DNA is of especial importance. The high selectivity of polyamine conjugated perylene derivatives appears to be regulated by side-chain charge density, as indicated by data from a FRET melting assay and induced CD spectroscopy. (C) 2009 Elsevier Ltd. All rights reserved.
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