Targeting G-quadruplex with Small Molecules: An NMR View

2018 ◽  
pp. 2189-2210
Author(s):  
Irene Bessi ◽  
Julia Wirmer-Bartoschek ◽  
Jyotirmayee Dash ◽  
Harald Schwalbe
Keyword(s):  
2016 ◽  
Vol 8 (44) ◽  
pp. 29968-29976 ◽  
Author(s):  
Suyan Qiu ◽  
Fusheng Zhao ◽  
Oussama Zenasni ◽  
Jingting Li ◽  
Wei-Chuan Shih

2017 ◽  
Vol 7 (1) ◽  
Author(s):  
Paul E. Reyes-Gutiérrez ◽  
Tomáš Kapal ◽  
Blanka Klepetářová ◽  
David Šaman ◽  
Radek Pohl ◽  
...  

2010 ◽  
Vol 2010 ◽  
pp. 1-7 ◽  
Author(s):  
Bruno Pagano ◽  
Iolanda Fotticchia ◽  
Stefano De Tito ◽  
Carlo A. Mattia ◽  
Luciano Mayol ◽  
...  

Guanine-rich nucleic acid sequences can adopt G-quadruplex structures stabilized by layers of four Hoogsteen-paired guanine residues. Quadruplex-prone sequences are found in many regions of human genome and in the telomeres of all eukaryotic organisms. Since small molecules that target G-quadruplexes have been found to be effective telomerase inhibitors, the identification of new specific ligands for G-quadruplexes is emerging as a promising approach to develop new anticancer drugs. Distamycin A is known to bind to AT-rich sequences of duplex DNA, but it has recently been shown to interact also with G-quadruplexes. Here, isothermal titration calorimetry (ITC) and NMR techniques have been employed to characterize the interaction between a dicationic derivative of distamycin A (compound1) and the [d(TGGGGT)]4quadruplex. Additionally, to compare the binding behaviour of netropsin and compound1to the same target, a calometric study of the interaction between netropsin and [d(TGGGGT)]4has been performed. Experiments show that netropsin and compound1are able to bind to [d(TGGGGT)]4with good affinity and comparable thermodynamic profiles. In both cases the interactions are entropically driven processes with a small favourable enthalpic contribution. Interestingly, the structural modifications of compound1decrease the affinity of the ligand toward the duplex, enhancing the selectivity.


2021 ◽  
Vol 14 (7) ◽  
pp. 671
Author(s):  
Jéssica Lopes-Nunes ◽  
Paula Oliveira ◽  
Carla Cruz

G-quadruplexes (G4s) are a class of nucleic acids (DNA and RNA) with single-stranded G-rich sequences. Owing to the selectivity of some G4s, they are emerging as targeting agents to overtake side effects of several potential anticancer drugs, and delivery systems of small molecules to malignant cells, through their high affinity or complementarity to specific targets. Moreover, different systems are being used to improve their potential, such as gold nano-particles or liposomes. Thus, the present review provides relevant data about the different studies with G4s as drug delivery systems and the challenges that must be overcome in the future research.


2019 ◽  
Vol 116 (3) ◽  
pp. 39a
Author(s):  
Parastoo Maleki ◽  
Hamza Balci

2019 ◽  
Vol 23 (11n12) ◽  
pp. 1195-1215 ◽  
Author(s):  
Ariana Yett ◽  
Linda Yingqi Lin ◽  
Dana Beseiso ◽  
Joanne Miao ◽  
Liliya A. Yatsunyk

[Formula: see text]-methyl mesoporphyrin IX (NMM) is a water-soluble, non-symmetric porphyrin with excellent optical properties and unparalleled selectivity for G-quadruplex (GQ) DNA. G-quadruplexes are non-canonical DNA structures formed by guanine-rich sequences. They are implicated in genomic stability, longevity, and cancer. The ability of NMM to selectively recognize GQ structures makes it a valuable scaffold for designing novel GQ binders. In this review, we survey the literature describing the GQ-binding properties of NMM as well as its wide utility in chemistry and biology. We start with the discovery of the GQ-binding properties of NMM and the development of NMM-binding aptamers. We then discuss the optical properties of NMM, focusing on the light-switch effect — high fluorescence of NMM induced upon its binding to GQ DNA. Additionally, we examine the affinity and selectivity of NMM for GQs, as well as its ability to stabilize GQ structures and favor parallel GQ conformations. Furthermore, a portion of the review is dedicated to the applications of NMM-GQ complexes as biosensors for heavy metals, small molecules ([Formula: see text] ATP and pesticides), DNA, and proteins. Finally and importantly, we discuss the utility of NMM as a probe to investigate the roles of GQs in biological processes.


2017 ◽  
pp. 1-22 ◽  
Author(s):  
Irene Bessi ◽  
Julia Wirmer-Bartoschek ◽  
Jyotirmayee Dash ◽  
Harald Schwalbe
Keyword(s):  

2018 ◽  
Vol 1154 ◽  
pp. 1-7 ◽  
Author(s):  
Shuo-Bin Chen ◽  
Guo-Cai Liu ◽  
Lian-Quan Gu ◽  
Zhi-Shu Huang ◽  
Jia-Heng Tan

Sign in / Sign up

Export Citation Format

Share Document