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Synthesis and Biological Evaluation of Potential Oncoimmunomodulator Agents
dc.contributor.author | Gil-Edo, Raquel | |
dc.contributor.author | ESPEJO, SARA | |
dc.contributor.author | Falomir, Eva | |
dc.contributor.author | Carda, Miguel | |
dc.date.accessioned | 2024-03-26T13:10:37Z | |
dc.date.available | 2024-03-26T13:10:37Z | |
dc.date.issued | 2023-01-30 | |
dc.identifier.citation | International Journal of Molecular Sciences. 2023; 24(3) | ca_CA |
dc.identifier.issn | 1422-0067 | |
dc.identifier.uri | http://hdl.handle.net/10234/206323 | |
dc.description.abstract | Fourteen triazole-scaffold derivatives were synthetized and biologically evaluated as potential oncoimmunomodultator agents by targeting both PD-L1 and c-Myc. First, the antiproliferative activity of these molecules on the monocultures of several tumor cell lines (HT-29, A-549, and MCF-7) and on the non-tumor cell line HEK-293 was studied. Then, the effects on the mentioned biological targets were also evaluated. Finally, the effect on cancer cell viability when the molecules were co-cultured with immune cells (Jurkat T cells or THP-1) was also determined. Compounds bearing a bromoophenyl group were selected because of their excellent results, and their effect on IL-6 secretion was also studied. In conclusion, we found compounds that are capable of downregulating c-Myc, as well as influencing and altering the distribution of PD-L1 in tumor cells; the compounds are thus capable of influencing the behavior of defensive cells towards cancer cells. p-Bromophenyltriazol 3 is the most active of these as a PD-L1 and c-Myc downregulator and as a potential immunomodulator agent. Moreover, it exhibits an interesting action on inflammation-related cytokine IL-6. | ca_CA |
dc.format.extent | 20 p. | ca_CA |
dc.format.mimetype | application/pdf | ca_CA |
dc.language.iso | eng | ca_CA |
dc.publisher | MDPI | ca_CA |
dc.relation.isPartOf | International Journal of Molecular Sciences. 2023; 24(3) | ca_CA |
dc.rights | © 2023 by the authors. | ca_CA |
dc.rights.uri | http://creativecommons.org/licenses/by/4.0/ | ca_CA |
dc.subject | PD-L1 | ca_CA |
dc.subject | c-Myc | ca_CA |
dc.subject | IL-6 | ca_CA |
dc.subject | multitarget inhibitors | ca_CA |
dc.subject | immunomodulation | ca_CA |
dc.subject | angiogenesis | ca_CA |
dc.subject | small molecules | ca_CA |
dc.subject | co-cultures | ca_CA |
dc.subject | flow cytometry | ca_CA |
dc.title | Synthesis and Biological Evaluation of Potential Oncoimmunomodulator Agents | ca_CA |
dc.type | info:eu-repo/semantics/article | ca_CA |
dc.identifier.doi | 10.3390/ijms24032614 | |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | ca_CA |
dc.relation.publisherVersion | https://www.mdpi.com/1422-0067/24/3/2614 | ca_CA |
dc.type.version | info:eu-repo/semantics/publishedVersion | ca_CA |
project.funder.name | Asociación Española Contra el Cancer | ca_CA |
project.funder.name | Universitat Jaume I for the Juan Murga Clausell | ca_CA |
project.funder.name | Ministerio de Economía y Competitividad | ca_CA |
project.funder.name | Universitat Jaume I | ca_CA |
oaire.awardNumber | PRDCA18002CARD | ca_CA |
oaire.awardNumber | UJI-2020-709 | ca_CA |
oaire.awardNumber | RTI2018-097345-B-I00 | ca_CA |
oaire.awardNumber | UJI-B2018-38, UJI-B2019-43 | ca_CA |
dc.subject.ods | 3. Salud y bienestar | ca_CA |
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