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A potent estrogen receptor and microtubule specific purine-benzothiazole-based fluorescent molecular probe induces apoptotic death of breast cancer cells

Breast cancer is the most common malignancy in women and is a heterogeneous disease at molecular level. Early detection and specificity are the key prerequisite for the treatment of this deadly cancer. To address these issues attention on the breast cancer specific receptor protein(s) is the most re...

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Autores principales: Barman, Surajit, Ghosh, Subhajit, Roy, Rajsekhar, Gupta, Varsha, Ghosh, Satyajit, Ghosh, Surajit
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9232585/
https://www.ncbi.nlm.nih.gov/pubmed/35750870
http://dx.doi.org/10.1038/s41598-022-12933-8
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author Barman, Surajit
Ghosh, Subhajit
Roy, Rajsekhar
Gupta, Varsha
Ghosh, Satyajit
Ghosh, Surajit
author_facet Barman, Surajit
Ghosh, Subhajit
Roy, Rajsekhar
Gupta, Varsha
Ghosh, Satyajit
Ghosh, Surajit
author_sort Barman, Surajit
collection PubMed
description Breast cancer is the most common malignancy in women and is a heterogeneous disease at molecular level. Early detection and specificity are the key prerequisite for the treatment of this deadly cancer. To address these issues attention on the breast cancer specific receptor protein(s) is the most realistic option. Herein estrogen (E) and progesterone (Pg) receptors(R) were considered to design fluorescent molecular probes with possible therapeutic option. We adopted QSAR technique to design a library of benzothiazole-purine hybrid molecules. Molecular docking offers us three screened molecules as most potential. Among these molecules one abbreviated as “CPIB” showed blue fluorescence and detected ER positive cancer cells at 1 nM concentration. At elevated concentration, CPIB induces apoptotic deaths of same cancer cells through targeting intracellular microtubules without affecting normal cells or ER negative cells. CPIB is one of its kind with two-in-one potential of “Detection and Destroy” ability targeting ER positive breast cancer cells.
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spelling pubmed-92325852022-06-26 A potent estrogen receptor and microtubule specific purine-benzothiazole-based fluorescent molecular probe induces apoptotic death of breast cancer cells Barman, Surajit Ghosh, Subhajit Roy, Rajsekhar Gupta, Varsha Ghosh, Satyajit Ghosh, Surajit Sci Rep Article Breast cancer is the most common malignancy in women and is a heterogeneous disease at molecular level. Early detection and specificity are the key prerequisite for the treatment of this deadly cancer. To address these issues attention on the breast cancer specific receptor protein(s) is the most realistic option. Herein estrogen (E) and progesterone (Pg) receptors(R) were considered to design fluorescent molecular probes with possible therapeutic option. We adopted QSAR technique to design a library of benzothiazole-purine hybrid molecules. Molecular docking offers us three screened molecules as most potential. Among these molecules one abbreviated as “CPIB” showed blue fluorescence and detected ER positive cancer cells at 1 nM concentration. At elevated concentration, CPIB induces apoptotic deaths of same cancer cells through targeting intracellular microtubules without affecting normal cells or ER negative cells. CPIB is one of its kind with two-in-one potential of “Detection and Destroy” ability targeting ER positive breast cancer cells. Nature Publishing Group UK 2022-06-24 /pmc/articles/PMC9232585/ /pubmed/35750870 http://dx.doi.org/10.1038/s41598-022-12933-8 Text en © The Author(s) 2022 https://creativecommons.org/licenses/by/4.0/Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) .
spellingShingle Article
Barman, Surajit
Ghosh, Subhajit
Roy, Rajsekhar
Gupta, Varsha
Ghosh, Satyajit
Ghosh, Surajit
A potent estrogen receptor and microtubule specific purine-benzothiazole-based fluorescent molecular probe induces apoptotic death of breast cancer cells
title A potent estrogen receptor and microtubule specific purine-benzothiazole-based fluorescent molecular probe induces apoptotic death of breast cancer cells
title_full A potent estrogen receptor and microtubule specific purine-benzothiazole-based fluorescent molecular probe induces apoptotic death of breast cancer cells
title_fullStr A potent estrogen receptor and microtubule specific purine-benzothiazole-based fluorescent molecular probe induces apoptotic death of breast cancer cells
title_full_unstemmed A potent estrogen receptor and microtubule specific purine-benzothiazole-based fluorescent molecular probe induces apoptotic death of breast cancer cells
title_short A potent estrogen receptor and microtubule specific purine-benzothiazole-based fluorescent molecular probe induces apoptotic death of breast cancer cells
title_sort potent estrogen receptor and microtubule specific purine-benzothiazole-based fluorescent molecular probe induces apoptotic death of breast cancer cells
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9232585/
https://www.ncbi.nlm.nih.gov/pubmed/35750870
http://dx.doi.org/10.1038/s41598-022-12933-8
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