Taxifolin and Lucidin as Potential E6 Protein Inhibitors

Detalhes bibliográficos
Autor(a) principal: Gomes, Diana
Data de Publicação: 2022
Outros Autores: Yaduvanshi, Shivani, Silvestre, Samuel, Duarte, Ana Paula, Santos, Adriana O., Soares, Christiane P., Kumar, Veerendra, Passarinha, Luís, Sousa, Ângela
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10362/143976
Resumo: This work was supported by the Foundation for Science and Technology (FCT), through funds from the State Budget, and by the European Regional Development Fund through the “Pro-grama Operacional Regional do Centro (Centro 2020)—Sistema de Apoio à Investigação Científica e Tecnológica—Programas Integrados de IC&DT” (Project Centro-01-0145-FEDER-000019—C4—Centro de Competências em Cloud Computing). project LA/P/0140/2020 of the Associate Laboratory Institute for Health and Bioeconomy—i4HB. D. Gomes also acknowledges the doctoral fellowship from FCT (ref: 2020.06792.BD). This work was also supported by the Ramalingaswami Fellowship (BT/RLF/Re-entry/64/2017), Department of Biotechnology, Govt. of India (V.K.). Publisher Copyright: © 2022 by the authors. Licensee MDPI, Basel, Switzerland.
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spelling Taxifolin and Lucidin as Potential E6 Protein Inhibitorsp53 Function Re-Establishment and Apoptosis Induction in Cervical Cancer Cellscervical cancerE6 protein inhibitorshuman papillomavirusin silico toolslucidinmolecular dockingp53taxifolinOncologyCancer ResearchSDG 3 - Good Health and Well-beingThis work was supported by the Foundation for Science and Technology (FCT), through funds from the State Budget, and by the European Regional Development Fund through the “Pro-grama Operacional Regional do Centro (Centro 2020)—Sistema de Apoio à Investigação Científica e Tecnológica—Programas Integrados de IC&DT” (Project Centro-01-0145-FEDER-000019—C4—Centro de Competências em Cloud Computing). project LA/P/0140/2020 of the Associate Laboratory Institute for Health and Bioeconomy—i4HB. D. Gomes also acknowledges the doctoral fellowship from FCT (ref: 2020.06792.BD). This work was also supported by the Ramalingaswami Fellowship (BT/RLF/Re-entry/64/2017), Department of Biotechnology, Govt. of India (V.K.). Publisher Copyright: © 2022 by the authors. Licensee MDPI, Basel, Switzerland.Cervical cancer is the fourth leading cause of death in women worldwide, with 99% of cases associated with a human papillomavirus (HPV) infection. Given that HPV prophylactic vaccines do not exert a therapeutic effect in individuals previously infected, have low coverage of all HPV types, and have poor accessibility in developing countries, it is unlikely that HPV-associated cancers will be eradicated in the coming years. Therefore, there is an emerging need for the development of anti-HPV drugs. Considering HPV E6’s oncogenic role, this protein has been proposed as a relevant target for cancer treatment. In the present work, we employed in silico tools to discover potential E6 inhibitors, as well as biochemical and cellular assays to understand the action of selected compounds in HPV-positive cells (Caski and HeLa) vs. HPV-negative (C33A) and non-carcinogenic (NHEK) cell lines. In fact, by molecular docking and molecular dynamics simulations, we found three phenolic compounds able to dock in the E6AP binding pocket of the E6 protein. In particular, lucidin and taxifolin were able to inhibit E6-mediated p53 degradation, selectively reduce the viability, and induce apoptosis in HPV-positive cells. Altogether, our data can be relevant for discovering promising leads for the development of specific anti-HPV drugs.UCIBIO - Applied Molecular Biosciences UnitDQ - Departamento de QuímicaRUNGomes, DianaYaduvanshi, ShivaniSilvestre, SamuelDuarte, Ana PaulaSantos, Adriana O.Soares, Christiane P.Kumar, VeerendraPassarinha, LuísSousa, Ângela2022-09-22T22:38:57Z2022-06-082022-06-08T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article24application/pdfhttp://hdl.handle.net/10362/143976eng2072-6694PURE: 46648124https://doi.org/10.3390/cancers14122834info:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2024-03-11T05:23:03Zoai:run.unl.pt:10362/143976Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-20T03:51:15.417556Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse
dc.title.none.fl_str_mv Taxifolin and Lucidin as Potential E6 Protein Inhibitors
p53 Function Re-Establishment and Apoptosis Induction in Cervical Cancer Cells
title Taxifolin and Lucidin as Potential E6 Protein Inhibitors
spellingShingle Taxifolin and Lucidin as Potential E6 Protein Inhibitors
Gomes, Diana
cervical cancer
E6 protein inhibitors
human papillomavirus
in silico tools
lucidin
molecular docking
p53
taxifolin
Oncology
Cancer Research
SDG 3 - Good Health and Well-being
title_short Taxifolin and Lucidin as Potential E6 Protein Inhibitors
title_full Taxifolin and Lucidin as Potential E6 Protein Inhibitors
title_fullStr Taxifolin and Lucidin as Potential E6 Protein Inhibitors
title_full_unstemmed Taxifolin and Lucidin as Potential E6 Protein Inhibitors
title_sort Taxifolin and Lucidin as Potential E6 Protein Inhibitors
author Gomes, Diana
author_facet Gomes, Diana
Yaduvanshi, Shivani
Silvestre, Samuel
Duarte, Ana Paula
Santos, Adriana O.
Soares, Christiane P.
Kumar, Veerendra
Passarinha, Luís
Sousa, Ângela
author_role author
author2 Yaduvanshi, Shivani
Silvestre, Samuel
Duarte, Ana Paula
Santos, Adriana O.
Soares, Christiane P.
Kumar, Veerendra
Passarinha, Luís
Sousa, Ângela
author2_role author
author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv UCIBIO - Applied Molecular Biosciences Unit
DQ - Departamento de Química
RUN
dc.contributor.author.fl_str_mv Gomes, Diana
Yaduvanshi, Shivani
Silvestre, Samuel
Duarte, Ana Paula
Santos, Adriana O.
Soares, Christiane P.
Kumar, Veerendra
Passarinha, Luís
Sousa, Ângela
dc.subject.por.fl_str_mv cervical cancer
E6 protein inhibitors
human papillomavirus
in silico tools
lucidin
molecular docking
p53
taxifolin
Oncology
Cancer Research
SDG 3 - Good Health and Well-being
topic cervical cancer
E6 protein inhibitors
human papillomavirus
in silico tools
lucidin
molecular docking
p53
taxifolin
Oncology
Cancer Research
SDG 3 - Good Health and Well-being
description This work was supported by the Foundation for Science and Technology (FCT), through funds from the State Budget, and by the European Regional Development Fund through the “Pro-grama Operacional Regional do Centro (Centro 2020)—Sistema de Apoio à Investigação Científica e Tecnológica—Programas Integrados de IC&DT” (Project Centro-01-0145-FEDER-000019—C4—Centro de Competências em Cloud Computing). project LA/P/0140/2020 of the Associate Laboratory Institute for Health and Bioeconomy—i4HB. D. Gomes also acknowledges the doctoral fellowship from FCT (ref: 2020.06792.BD). This work was also supported by the Ramalingaswami Fellowship (BT/RLF/Re-entry/64/2017), Department of Biotechnology, Govt. of India (V.K.). Publisher Copyright: © 2022 by the authors. Licensee MDPI, Basel, Switzerland.
publishDate 2022
dc.date.none.fl_str_mv 2022-09-22T22:38:57Z
2022-06-08
2022-06-08T00:00:00Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://hdl.handle.net/10362/143976
url http://hdl.handle.net/10362/143976
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 2072-6694
PURE: 46648124
https://doi.org/10.3390/cancers14122834
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
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application/pdf
dc.source.none.fl_str_mv reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron:RCAAP
instname_str Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron_str RCAAP
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reponame_str Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
collection Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
repository.name.fl_str_mv Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
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