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Ligand Selectivity in the Recognition of Protoberberine Alkaloids by Hybrid-2 Human Telomeric G-Quadruplex: Binding Free Energy Calculation, Fluorescence Binding, and NMR Experiments
Open AccessFeature PaperReview

Molecular Recognition of the Hybrid-Type G-Quadruplexes in Human Telomeres

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Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, 575 W Stadium Ave, West Lafayette, IN 47907, USA
2
Purdue Center for Cancer Research, 201 S University St, West Lafayette, IN 47906, USA
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Purdue Institute for Drug Discovery, 720 Clinic Dr, West Lafayette, IN 47907, USA
*
Author to whom correspondence should be addressed.
Academic Editor: Ramon Eritja
Molecules 2019, 24(8), 1578; https://doi.org/10.3390/molecules24081578
Received: 23 March 2019 / Revised: 17 April 2019 / Accepted: 19 April 2019 / Published: 22 April 2019
(This article belongs to the Special Issue G-Quadruplex Ligands and Cancer)
G-quadruplex (G4) DNA secondary structures formed in human telomeres have been shown to inhibit cancer-specific telomerase and alternative lengthening of telomere (ALT) pathways. Thus, human telomeric G-quadruplexes are considered attractive targets for anticancer drugs. Human telomeric G-quadruplexes are structurally polymorphic and predominantly form two hybrid-type G-quadruplexes, namely hybrid-1 and hybrid-2, under physiologically relevant solution conditions. To date, only a handful solution structures are available for drug complexes of human telomeric G-quadruplexes. In this review, we will describe two recent solution structural studies from our labs. We use NMR spectroscopy to elucidate the solution structure of a 1:1 complex between a small molecule epiberberine and the hybrid-2 telomeric G-quadruplex, and the structures of 1:1 and 4:2 complexes between a small molecule Pt-tripod and the hybrid-1 telomeric G-quadruplex. Structural information of small molecule complexes can provide important information for understanding small molecule recognition of human telomeric G-quadruplexes and for structure-based rational drug design targeting human telomeric G-quadruplexes. View Full-Text
Keywords: human telomeres; G-quadruplex; G4; anticancer drug; solution structure; molecular recognition; rational drug design; hybrid-2; hybrid-1; epi-berberine; platinum-tripod human telomeres; G-quadruplex; G4; anticancer drug; solution structure; molecular recognition; rational drug design; hybrid-2; hybrid-1; epi-berberine; platinum-tripod
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Wu, G.; Chen, L.; Liu, W.; Yang, D. Molecular Recognition of the Hybrid-Type G-Quadruplexes in Human Telomeres. Molecules 2019, 24, 1578.

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