Transcriptomic analysis of MCF7 breast cancer cells treated with MGBs reveals a profound inhibition of estrogen receptor genes.

Autor: Alniss HY; College of Pharmacy, Department of Medicinal Chemistry, University of Sharjah, Sharjah 27272, United Arab Emirates; Research Institute for Medical and Health Sciences, University of Sharjah, Sharjah 27272, United Arab Emirates. Electronic address: halniss@sharjah.ac.ae., Saber-Ayad MM; Research Institute for Medical and Health Sciences, University of Sharjah, Sharjah 27272, United Arab Emirates; College of Medicine, University of Sharjah, Sharjah 27272, United Arab Emirates., Ramadan WS; Research Institute for Medical and Health Sciences, University of Sharjah, Sharjah 27272, United Arab Emirates., Manasa Bhamidimarri P; Research Institute for Medical and Health Sciences, University of Sharjah, Sharjah 27272, United Arab Emirates., Msallam YA; College of Pharmacy, Department of Medicinal Chemistry, University of Sharjah, Sharjah 27272, United Arab Emirates; Research Institute for Medical and Health Sciences, University of Sharjah, Sharjah 27272, United Arab Emirates., Al-Jubeh HM; Research Institute for Medical and Health Sciences, University of Sharjah, Sharjah 27272, United Arab Emirates., Ravi A; Research Institute for Medical and Health Sciences, University of Sharjah, Sharjah 27272, United Arab Emirates., Menon V; Research Institute for Medical and Health Sciences, University of Sharjah, Sharjah 27272, United Arab Emirates., Hamoudi R; Research Institute for Medical and Health Sciences, University of Sharjah, Sharjah 27272, United Arab Emirates; College of Medicine, University of Sharjah, Sharjah 27272, United Arab Emirates; Center of Excellence for Precision Medicine, University of Sharjah, Sharjah 27272, United Arab Emirates; BIMAI-Lab, Biomedically Informed Artificial Intelligence Laboratory, University of Sharjah, Sharjah 27272, United Arab Emirates; Division of Surgery and Interventional Science, Faculty of Medicine, University College London, London, United Kingdom., El-Awady R; College of Pharmacy, Department of Medicinal Chemistry, University of Sharjah, Sharjah 27272, United Arab Emirates; Research Institute for Medical and Health Sciences, University of Sharjah, Sharjah 27272, United Arab Emirates.
Jazyk: angličtina
Zdroj: Bioorganic chemistry [Bioorg Chem] 2024 Oct; Vol. 151, pp. 107680. Date of Electronic Publication: 2024 Jul 27.
DOI: 10.1016/j.bioorg.2024.107680
Abstrakt: Breast cancer poses a significant health risk worldwide. However, the effectiveness of current chemotherapy is limited due to increasing drug resistance and side effects, making it crucial to develop new compounds with novel mechanism of action that can surpass these limitations. As a consequence of their reversible and targeted mechanism, DNA minor groove binders (MGBs) are considered as a relatively safer and more effective alternative. In this study, transcriptomic analysis was conducted to reveal the dysregulated genes and signaling pathways in MCF7 cancer cells following treatment with novel MGB ligands to gain insights into the mechanism of action of MGBs at the molecular level. The transcriptomic results were validated using real-time PCR. The findings of this study indicate that the investigated MGBs primarily inhibit the genes associated with the estrogen receptor. Remarkably, ligand 5 showed downregulation of 34 out of the 35 genes regulated by estrogen receptor, highlighting its potential as a promising candidate for breast cancer therapy.
Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2024 Elsevier Inc. All rights reserved.)
Databáze: MEDLINE
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