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Small Molecule “Silmitasertib” Repurposed as Inhibitor of Transforming Growth Factor Beta 1 for the Development of Therapeutics for Oral Submucous Fibrosis
Oral submucous fibrosis (OSMF) is considered a premalignant condition characterized by aggressive fibrosis of the submucosal tissues of the oral cavity reflecting its malignant transformation potential. Activation of transforming growth factor beta (TGF-β) signaling has been reported to lead increas...
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Hindawi
2021
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8035005/ https://www.ncbi.nlm.nih.gov/pubmed/33869629 http://dx.doi.org/10.1155/2021/6631848 |
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author | Boreak, Nezar |
author_facet | Boreak, Nezar |
author_sort | Boreak, Nezar |
collection | PubMed |
description | Oral submucous fibrosis (OSMF) is considered a premalignant condition characterized by aggressive fibrosis of the submucosal tissues of the oral cavity reflecting its malignant transformation potential. Activation of transforming growth factor beta (TGF-β) signaling has been reported to lead increased collagen production and fibrosis. Recently, significant upregulation of TGF-β1 has been reported in OSMF as compared to normal tissues. Therefore, inhibition of the TGF-β1 may pave for the development of therapeutics of OSMF. Based on the structure-assisted drug designing, we found “silmitasertib” as potent inhibitor of TGF-β1. We suggest that this molecule can be validated and implemented for the treatment of OSMF. |
format | Online Article Text |
id | pubmed-8035005 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | Hindawi |
record_format | MEDLINE/PubMed |
spelling | pubmed-80350052021-04-16 Small Molecule “Silmitasertib” Repurposed as Inhibitor of Transforming Growth Factor Beta 1 for the Development of Therapeutics for Oral Submucous Fibrosis Boreak, Nezar Biomed Res Int Research Article Oral submucous fibrosis (OSMF) is considered a premalignant condition characterized by aggressive fibrosis of the submucosal tissues of the oral cavity reflecting its malignant transformation potential. Activation of transforming growth factor beta (TGF-β) signaling has been reported to lead increased collagen production and fibrosis. Recently, significant upregulation of TGF-β1 has been reported in OSMF as compared to normal tissues. Therefore, inhibition of the TGF-β1 may pave for the development of therapeutics of OSMF. Based on the structure-assisted drug designing, we found “silmitasertib” as potent inhibitor of TGF-β1. We suggest that this molecule can be validated and implemented for the treatment of OSMF. Hindawi 2021-04-01 /pmc/articles/PMC8035005/ /pubmed/33869629 http://dx.doi.org/10.1155/2021/6631848 Text en Copyright © 2021 Nezar Boreak. https://creativecommons.org/licenses/by/4.0/This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Research Article Boreak, Nezar Small Molecule “Silmitasertib” Repurposed as Inhibitor of Transforming Growth Factor Beta 1 for the Development of Therapeutics for Oral Submucous Fibrosis |
title | Small Molecule “Silmitasertib” Repurposed as Inhibitor of Transforming Growth Factor Beta 1 for the Development of Therapeutics for Oral Submucous Fibrosis |
title_full | Small Molecule “Silmitasertib” Repurposed as Inhibitor of Transforming Growth Factor Beta 1 for the Development of Therapeutics for Oral Submucous Fibrosis |
title_fullStr | Small Molecule “Silmitasertib” Repurposed as Inhibitor of Transforming Growth Factor Beta 1 for the Development of Therapeutics for Oral Submucous Fibrosis |
title_full_unstemmed | Small Molecule “Silmitasertib” Repurposed as Inhibitor of Transforming Growth Factor Beta 1 for the Development of Therapeutics for Oral Submucous Fibrosis |
title_short | Small Molecule “Silmitasertib” Repurposed as Inhibitor of Transforming Growth Factor Beta 1 for the Development of Therapeutics for Oral Submucous Fibrosis |
title_sort | small molecule “silmitasertib” repurposed as inhibitor of transforming growth factor beta 1 for the development of therapeutics for oral submucous fibrosis |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8035005/ https://www.ncbi.nlm.nih.gov/pubmed/33869629 http://dx.doi.org/10.1155/2021/6631848 |
work_keys_str_mv | AT boreaknezar smallmoleculesilmitasertibrepurposedasinhibitoroftransforminggrowthfactorbeta1forthedevelopmentoftherapeuticsfororalsubmucousfibrosis |