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Biomolecules
Special Issues
From G-Quadruplex Stabilization to Anticancer Therapy
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From G-Quadruplex Stabilization to Anticancer Therapy

A special issue of Biomolecules (ISSN 2218-273X). This special issue belongs to the section "Synthetic Biology and Bioengineering".

Deadline for manuscript submissions: closed (15 October 2022) | Viewed by 3364

Special Issue Editors

Dr. Catarina I. V. Ramos

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Guest Editor
QOPNA & LAQV-REQUIMTE, Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal
Interests: drug development; water-soluble tetrapyrrolic macrocycles for biomedical applications; cationic and anionic derivatives; spectrophotometric methodologies; mass spectrometry; high-order DNA structures; G-quadruplex–porphyrinoid interactions; targeting telomeres and telomerase; telomerase inhibition; oncogenes; cancer cell proliferation control; photodynamic therapy in cancer
Special Issues, Collections and Topics in MDPI journals
Dr. Carla Cruz

E-Mail Website
Guest Editor
CICS-UBI—Centro de Investigação em Ciências da Saúde, Universidade da Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, Portugal
Interests: DNA and RNA G-quadruplexes; G-quadruplexes aptamers; G-quadruplex ligands; biomolecular interactions; biophysical techniques; drug design and development; cancer; drug delivery systems
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Maria G. P. M. S. Neves

E-Mail Website1 Website2
Guest Editor
Department of Chemistry and LAQV-REQUIMTE , University of Aveiro, 3810-193 Aveiro, Portugal
Interests: organic synthesis; tetrapyrrolic macrocycles; photodynamic therapy; sensing; G-quadruplex ligands
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The formation of G-quadruplex DNA at the end of telomeres has been reported to inhibit telomerase activity, since the enzyme will not be able to bypass the folded form of its DNA substrate. Furthermore, the formation of G-quadruplexes in the promoter regions of several human genes and oncogenes supports their regulatory potential toward cancer cell growth.

The stabilization of DNA G-quadruplexes by ligands promotes the indirect inactivation of telomerase in cancer cells and leads to downregulation of the expression of genes in oncogene promoters, thus being considered a potential and valuable anticancer therapy. The development of G-quadruplexes stabilizing ligands could open new avenues in antitumor drug design that envisages selective anticancer therapies based on G-quadruplexes.

The identification of key structural characteristics that can potentiate ligand specificity and affinity for G-quadruplexes could provide significant inputs for the design of drugs that effectively control cancer cell proliferation.

The aim of this Special Issue, “From G-Quadruplex Stabilization to anticancer Therapy”, is to provide the opportunity to share recent advances on G-quadruplex-based drug design and development of new antitumor drugs and therapies. We invite original research papers and comprehensive reviews covering any aspect related to the abovementioned topics.

Dr. Catarina I. V. Ramos
Dr. Carla Cruz
Prof. Dr. M. Graça P. M. S. Neves
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. Biomolecules 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 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 stabilization
  • drug design
  • telomerase inhibition
  • oncogenes
  • anticancer therapy

Published Papers (1 paper)

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Review

28 pages, 5126 KiB  
Review
The Interactions of H2TMPyP, Analogues and Its Metal Complexes with DNA G-Quadruplexes—An Overview
by Catarina I. V. Ramos, Ana R. Monteiro, Nuno M. M. Moura, Maria Amparo F. Faustino, Tito Trindade and Maria Graça P. M. S. Neves
Biomolecules 2021, 11(10), 1404; https://0-doi-org.brum.beds.ac.uk/10.3390/biom11101404 - 25 Sep 2021
Cited by 7 | Viewed by 2612
Abstract
The evidence that telomerase is overexpressed in almost 90% of human cancers justifies the proposal of this enzyme as a potential target for anticancer drug design. The inhibition of telomerase by quadruplex stabilizing ligands is being considered a useful approach in anticancer drug [...] Read more.
The evidence that telomerase is overexpressed in almost 90% of human cancers justifies the proposal of this enzyme as a potential target for anticancer drug design. The inhibition of telomerase by quadruplex stabilizing ligands is being considered a useful approach in anticancer drug design proposals. Several aromatic ligands, including porphyrins, were exploited for telomerase inhibition by adduct formation with G-Quadruplex (GQ). 5,10,15,20-Tetrakis(N-methyl-4-pyridinium)porphyrin (H2TMPyP) is one of the most studied porphyrins in this field, and although reported as presenting high affinity to GQ, its poor selectivity for GQ over duplex structures is recognized. To increase the desired selectivity, porphyrin modifications either at the peripheral positions or at the inner core through the coordination with different metals have been handled. Herein, studies involving the interactions of TMPyP and analogs with different DNA sequences able to form GQ and duplex structures using different experimental conditions and approaches are reviewed. Some considerations concerning the structural diversity and recognition modes of G-quadruplexes will be presented first to facilitate the comprehension of the studies reviewed. Additionally, considering the diversity of experimental conditions reported, we decided to complement this review with a screening where the behavior of H2TMPyP and of some of the reviewed metal complexes were evaluated under the same experimental conditions and using the same DNA sequences. In this comparison under unified conditions, we also evaluated, for the first time, the behavior of the AgII complex of H2TMPyP. In general, all derivatives showed good affinity for GQ DNA structures with binding constants in the range of 106–107 M−1 and ligand-GQ stoichiometric ratios of 3:1 and 4:1. A promising pattern of selectivity was also identified for the new AgII derivative. Full article
(This article belongs to the Special Issue From G-Quadruplex Stabilization to Anticancer Therapy)
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