Abstract
Glioblastoma multiforme (GBM) is account for 70% of all primary malignancies of the central nervous system. The median survival of human patients after treatment is around 15 months. There are several biological targets which have been reported that can be pursued using ligands with varied structures to treat this disease. In our group, we have developed several ligands that target a wide range of proteins involved in anticancer effects, such as histone deacetylase (HDACs), G protein-coupled estrogen receptor 1 (GPER), estrogen receptor-beta (ERβ) and NADPH oxidase (NOX), that were screened on bidimensional (2D) and tridimensional (3D) GBM stem cells like (GSC). Our results show that some HDAC inhibitors show antiproliferative properties at 21–32 µM. These results suggest that in this 3D culture, HDACs could be the most relevant targets that are modulated to induce the antiproliferative effects that require in the future further experimental studies.
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Acknowledgments
Y.S.L. thanks to CONACYT for PhD scholarship.
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We gratefully acknowledge to CONACYT (Grants: CB-254600, 284243, 286653, APN-782 and SEP-CONACYT-ANUIES-ECOS Francia: 296636), to Instituto Politécnico Nacional (Grant: Proyectos Insignia IPN-2015) and to COFAA-SIP/IPN.
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YSL wrote the manuscript and synthetized HDACi; EM performed cell culture; JBGV synthetized compounds and wrote the manuscript; JFV synthetized analysis compounds; MCRH synthetized compounds, wrote paper; OZL synthetized and analyzed compound; DML synthetized compounds, JAGV synthetized and analyzed HDACi; DC performed biological assays; BN designed project and wrote the manuscript; JBC designed project and wrote the manuscript.
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Sixto-López, Y., Marhuenda, E., García-Vazquez, J.B. et al. Targeting Several Biologically Reported Targets of Glioblastoma Multiforme by Assaying 2D and 3D Cultured Cells. Cell Mol Neurobiol 42, 1909–1920 (2022). https://doi.org/10.1007/s10571-021-01072-9
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DOI: https://doi.org/10.1007/s10571-021-01072-9