Nucleic Acids in Medicinal Chemistry

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (26 July 2023) | Viewed by 1954

Special Issue Editors


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Department of Pharmacy, School of Medicine and Surgery, Università degli Studi di Napoli Federico II, 80131 Naples, Italy
Interests: noncanonical nucleic acids; structural biology
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Department of Pharmacy, University of Naples Federico II, Via D. Montesano 49, 80131 Naples, Italy
Interests: chemometrics; cell metabolomics

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Department of Pharmacy, University of Naples Federico II, 80131 Naples, Italy
Interests: noncanonical nucleic acids; cellular and molecular biology; medicinal chemistry
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Guest Editor
Molecular Cell Biology of Autophagy laboratory, the Francis Crick Institute, London NW1 1AT, UK
Interests: cellular and molecular biology; noncanonical nucleic acids; autophagy; membrane trafficking

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Guest Editor
Department of Pharmacy, University of Naples Federico II, Via D. Montesano 49, 80131 Naples, Italy
Interests: chemistry of nucleic acids; nucleic acids therapeutics; nucleic acid-targeting drugs
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

 For several decades, nucleic acids (NAs) have been of interest to the research communities of chemists and biochemists for their crucial role in storing genetic information, as well as in regulating a myriad of biological functions. Notably, NAs have become an attractive focus for medicinal chemists to develop novel therapeutical approaches using DNA and RNA as drug targets for their investigations. Interestingly, in the recent years, NAs turned out to be extremely versatile biomolecules revealing unique and unexpected biological functions and applications. Ranging from their use as therapeutic agents, as in the case of aptamers, to the covalent conjugation of functional ligands and the explosion as building blocks for constructing nanostructures, NAs have evolved from being just “genetic” material to represent “generic” material for several applications.The main purpose of this Special Issue is to encourage the submission and publication of rigorous research using state-of-the-art techniques as well as novel findings and recent advances in the field of nucleic acids. The related topics include DNA and RNA; gene therapy; artificial nucleic acids (morpholino, LNA, PNA, GNA, SNA, TNA, and HNA); antisense oligonucleotides; RNA interference; DNA-based nanomaterials for drug delivery; aptamers; theranostics; nucleic acid-based biosensors; fluorescent nucleic acids; oligonucleotide conjugates; noncanonical DNA structures (G-quadruplex, i-motif, Holliday junction, and triplex); nucleic acid-targeting drugs; nucleoside and nucleotide analogs and modifications. The collection of manuscripts will be published as a Special Issue of Pharmaceuticals. The range of topics in this Special Issue accurately reflects the vigor of current investigations in the “hot” area of nucleic acids and underlines the expanding opportunities for medicinal chemistry in this central discipline. Prof. Antonio RandazzoProf. Jussara AmatoDr. Stefano De TitoDr. Nunzia IaccarinoDr. Anna Di Porzio

Prof. Dr. Antonio Randazzo
Dr. Nunzia Iaccarino
Dr. Anna Di Porzio
Dr. Stefano De Tito
Prof. Dr. Jussara Amato
Guest Editors

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. Pharmaceuticals is an international peer-reviewed open access monthly 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 2900 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

  • DNA
  • RNA
  • Artificial nucleic acids (morpholino, LNA, PNA, GNA, SNA, TNA, HNA)
  • Antisense
  • RNA interference
  • DNA-based nanomaterials for drug delivery
  • Aptamers
  • Theranostics
  • Nucleic acid-based biosensors
  • Fluorescent nucleic acids
  • Oligonucleotide conjugates
  • Noncanonical DNA structures (G-quadruplex, i-motif, Holliday junction, triplex)
  • Nucleic acid-targeting drugs
  • Nucleoside and nucleotide analogs and modifications
  • Gene therapy

Published Papers (1 paper)

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Research

13 pages, 18443 KiB  
Article
Binding-Induced Diversity of a Human Telomeric G-Quadruplex Stability Phase Space
by Domen Oblak, San Hadži, Črtomir Podlipnik and Jurij Lah
Pharmaceuticals 2022, 15(9), 1150; https://doi.org/10.3390/ph15091150 - 15 Sep 2022
Cited by 1 | Viewed by 1431
Abstract
The structural polymorphism of G-quadruplex nucleic acids is an important factor in their recognition by proteins and small-molecule ligands. However, it is not clear why the binding of several ligands alters G-quadruplex topology. We addressed this question by following the (un)folding and binding [...] Read more.
The structural polymorphism of G-quadruplex nucleic acids is an important factor in their recognition by proteins and small-molecule ligands. However, it is not clear why the binding of several ligands alters G-quadruplex topology. We addressed this question by following the (un)folding and binding of the human telomeric fragment 5′-(GGGTTA)3GGGT-3′ (22GT) by calorimetry (DSC, ITC) and spectroscopy (CD). A thermodynamic analysis of the obtained data led to a detailed description of the topological phase space of stability (phase diagram) of 22GT and shows how it changes in the presence of a specific bisquinolinium ligand (360A). Various 1:1 and 2:1 ligand–quadruplex complexes were observed. With increasing temperature, the 1:1 complexes transformed into 2:1 complexes, which is attributed to the preferential binding of the ligand to the folding intermediates. Overall, the dissection of the thermodynamic parameters in combination with molecular modelling clarified the driving forces of the topological quadruplex transformations in a wide range of ligand concentrations and temperatures. Full article
(This article belongs to the Special Issue Nucleic Acids in Medicinal Chemistry)
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