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G-Quadruplexes and i-Motif DNA

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Chemical Biology".

Deadline for manuscript submissions: closed (1 March 2022) | Viewed by 2803

Special Issue Editor


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Guest Editor
Université Grenoble Alpes, CNRS, Département de Chimie Moléculaire, UMR 5250, Grenoble, CEDEX 9, France
Interests: chemical biology; nucleic acids conjugates; G-quadruplex; I-motif; SPR; chemical ligation; click-chemistry

Special Issue Information

Dear Colleagues,

Beyond canonical double helical-based structures, such as B-DNA, A-DNA, and Z-DNA, recent decades have seen accumulating evidence of the existence and biological relevance of four-stranded nucleic acid structures, including G-quadruplexes (G4) and i-motifs. In the context of chemical biology, several studies have been devoted to the development of chemical and/or biophysical tools to understand the biological role of these high-ordered nucleic acid structures. Structural investigations have been achieved using NMR, RX, CD, and mass spectrometry analysis, which have, in particular, emphasized the high polymorphism associated with those tetrameric nucleic acid structures. The design of ligands that can selectively interact with G4 or i-motif nucleic acid structures has attracted substantial interest not only to realize chemical probes for G4 or i-motif structures but also to develop molecules with therapeutic properties. Concerning the design of ligands, several assays (in vitro, in cell, and in vivo) have been elaborated to select and study the most efficient ligands.

This Special Issue will cover the design of G4 or i-motifs ligands and their applications for a better understanding of the biological role of tetrameric nucleic acid structures, as well as for therapeutic uses. It also includes the development of chemical or biophysical tools to study these tetrameric structures, from in vitro to in vivo.

Prof. Eric Defrancq
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • G-quadruplex
  • i-motif
  • chemical biology
  • synthesis
  • modeling
  • biophysics
  • probes

Published Papers (1 paper)

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Research

15 pages, 1824 KiB  
Article
Targeted Downregulation of MYC through G-quadruplex Stabilization by DNAi
by Alexandra Maria Psaras, Katarina T. Chang, Taisen Hao and Tracy A. Brooks
Molecules 2021, 26(18), 5542; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26185542 - 13 Sep 2021
Cited by 3 | Viewed by 2392
Abstract
Modulating the expression or function of the enigmatic MYC protein has demonstrated efficacy in an array of cancer types and a marked potential therapeutic index and safety profile. Despite its high therapeutic value, specific and selective inhibitors or downregulating therapeutics have proven difficult [...] Read more.
Modulating the expression or function of the enigmatic MYC protein has demonstrated efficacy in an array of cancer types and a marked potential therapeutic index and safety profile. Despite its high therapeutic value, specific and selective inhibitors or downregulating therapeutics have proven difficult to develop. In the current study, we expanded our work on a MYC promoter G-quadruplex (G4) stabilizing DNA clamp to develop an oligonucleotide interfering DNA (DNAi) therapeutic. We explored six DNAi for G4-stabilization through EMSA, DMS footprinting, and thermal stability studies, focusing on the DNAi 5T as the lead therapeutic. 5T, but not its scramble control 5Tscr, was then shown to enter the nucleus, modulate cell viability, and decrease MYC expression through G4-stabilization. DNAi 5T is thus described to be our lead DNAi, targeting MYC regulation through stabilization of the higher-order DNA G4 structure in the proximal promoter, and it is poised for further preclinical development as an anticancer therapeutic. Full article
(This article belongs to the Special Issue G-Quadruplexes and i-Motif DNA)
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