Structural Basis of DNA Quadruplex Recognition by an Acridine Drug
- 1 May 2008
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of the American Chemical Society
- Vol. 130 (21) , 6722-6724
- https://doi.org/10.1021/ja8016973
Abstract
The crystal structure of a complex between the bimolecular human telomeric quadruplex d(TAGGGTTAGGGT)2 and the experimental anticancer drug BRACO-19, has been determined, to 2.5 Å resolution. The binding site for the BRACO-19 molecule is at the interface of two parallel-folded quadruplexes, sandwiched between a G-tetrad surface and a TATA tetrad, and held in the site by networks of water molecules. The structure rationalizes the existing structure−activity data and provides a starting-point for the structure-based design of quadruplex-binding ligandsKeywords
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