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Inside Back Cover: Molecular Recognition of Parallel DNA Quadruplex d(TTAGGGT) 4 by Mitoxantrone: Binding with 1:2 Stoichiometry Leading to Thermal Stabilization and Telomerase Inhibition (ChemBioChem 7/2016)
Author(s) -
Tripathi Sweta,
Pradeep Tarikere Palakshan,
Barthwal Ritu
Publication year - 2016
Publication title -
chembiochem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.201600128
Subject(s) - mitoxantrone , dna , chemistry , base pair , telomerase , stereochemistry , chromophore , telomere , small molecule , anthraquinone , g quadruplex , biophysics , combinatorial chemistry , biochemistry , biology , photochemistry , genetics , organic chemistry , chemotherapy , gene
The inside back cover picture shows the structure of two molecules of mitoxantrone (an anthraquinone‐based semisynthetic compound used as chemotherapeutic agent) bound externally at two different sites of the DNA G‐quadruplex d(TTAGGGT) 4 containing the human telomere repeat sequence TTAGGG. The binding by partial insertion of the mitoxantrone chromophore between base pairs and interaction of its side chains at the grooves of DNA thermally stabilize the G‐quadruplex by 13–20 K, thus resulting in subsequent telomerase inhibition (IC 50 =2 µ m ). This specific molecular recognition between a ligand and DNA serves as a platform for rational drug design. More information can be found in the communication by R. Barthwal et al. on page 554 in Issue 7, 2016 (DOI: 10.1002/cbic.201500588).