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The first crystal structure of a drug (daunomycin) bound to a parallel-stranded intermolecular telomeric G4 quadruplex (d(TGGGGT)4) has been determined to high resolution. A planar assemblage of three daunomycin molecules stacks onto the 5' end of the G4 column, with the daunosamine substituents occupying three of the four quadruplex grooves. The surface area of the terminal G-quartet in this parallel DNA quadruplex, presently occupied by three daunomycins, is sufficiently large that it could easily accommodate other potential telomerase inhibitors such as substituted porphyrins or telomestatin.
Structure of the first parallel DNA quadruplex-drug complex.,Clark GR, Pytel PD, Squire CJ, Neidle S J Am Chem Soc. 2003 Apr 9;125(14):4066-7. PMID:12670225[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
↑ Clark GR, Pytel PD, Squire CJ, Neidle S. Structure of the first parallel DNA quadruplex-drug complex. J Am Chem Soc. 2003 Apr 9;125(14):4066-7. PMID:12670225 doi:10.1021/ja0297988
