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G-Quadruplexes in c-MYC Promoter as Targets for Cancer Therapy

Cancer is a societal burden demanding innovative approaches. A major problem with the conventional chemotherapeutic agents is their strong toxicity and other side effects due to their poor selectivity. Uncontrolled proliferation of cancer cells is due to mutations, deletions, or amplifications in ge...

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Autores principales: Bahls, Bárbara, Aljnadi, Israa M., Emídio, Rita, Mendes, Eduarda, Paulo, Alexandra
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10046398/
https://www.ncbi.nlm.nih.gov/pubmed/36979947
http://dx.doi.org/10.3390/biomedicines11030969
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author Bahls, Bárbara
Aljnadi, Israa M.
Emídio, Rita
Mendes, Eduarda
Paulo, Alexandra
author_facet Bahls, Bárbara
Aljnadi, Israa M.
Emídio, Rita
Mendes, Eduarda
Paulo, Alexandra
author_sort Bahls, Bárbara
collection PubMed
description Cancer is a societal burden demanding innovative approaches. A major problem with the conventional chemotherapeutic agents is their strong toxicity and other side effects due to their poor selectivity. Uncontrolled proliferation of cancer cells is due to mutations, deletions, or amplifications in genes (oncogenes) encoding for proteins that regulate cell growth and division, such as transcription factors, for example, c-MYC. The direct targeting of the c-MYC protein has been attempted but so far unsuccessfully, as it lacks a definite binding site for the modulators. Meanwhile, another approach has been explored since the discovery that G-quadruplex secondary DNA structures formed in the guanine-rich sequences of the c-MYC promoter region can downregulate the transcription of this oncogene. Here, we will overview the major achievements made in the last decades towards the discovery of a new class of anticancer drugs targeting G-quadruplexes in the c-MYC promoter of cancer cells.
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spelling pubmed-100463982023-03-29 G-Quadruplexes in c-MYC Promoter as Targets for Cancer Therapy Bahls, Bárbara Aljnadi, Israa M. Emídio, Rita Mendes, Eduarda Paulo, Alexandra Biomedicines Review Cancer is a societal burden demanding innovative approaches. A major problem with the conventional chemotherapeutic agents is their strong toxicity and other side effects due to their poor selectivity. Uncontrolled proliferation of cancer cells is due to mutations, deletions, or amplifications in genes (oncogenes) encoding for proteins that regulate cell growth and division, such as transcription factors, for example, c-MYC. The direct targeting of the c-MYC protein has been attempted but so far unsuccessfully, as it lacks a definite binding site for the modulators. Meanwhile, another approach has been explored since the discovery that G-quadruplex secondary DNA structures formed in the guanine-rich sequences of the c-MYC promoter region can downregulate the transcription of this oncogene. Here, we will overview the major achievements made in the last decades towards the discovery of a new class of anticancer drugs targeting G-quadruplexes in the c-MYC promoter of cancer cells. MDPI 2023-03-21 /pmc/articles/PMC10046398/ /pubmed/36979947 http://dx.doi.org/10.3390/biomedicines11030969 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Bahls, Bárbara
Aljnadi, Israa M.
Emídio, Rita
Mendes, Eduarda
Paulo, Alexandra
G-Quadruplexes in c-MYC Promoter as Targets for Cancer Therapy
title G-Quadruplexes in c-MYC Promoter as Targets for Cancer Therapy
title_full G-Quadruplexes in c-MYC Promoter as Targets for Cancer Therapy
title_fullStr G-Quadruplexes in c-MYC Promoter as Targets for Cancer Therapy
title_full_unstemmed G-Quadruplexes in c-MYC Promoter as Targets for Cancer Therapy
title_short G-Quadruplexes in c-MYC Promoter as Targets for Cancer Therapy
title_sort g-quadruplexes in c-myc promoter as targets for cancer therapy
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10046398/
https://www.ncbi.nlm.nih.gov/pubmed/36979947
http://dx.doi.org/10.3390/biomedicines11030969
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