Saltar para:
Logótipo
Comuta visibilidade da coluna esquerda
Você está em: Início > Publicações > Visualização > Tryptophanol-derived oxazoloisoindolinone fluorescent probes for cellular localization studies of p53 activators

Publicações

Tryptophanol-derived oxazoloisoindolinone fluorescent probes for cellular localization studies of p53 activators

Título
Tryptophanol-derived oxazoloisoindolinone fluorescent probes for cellular localization studies of p53 activators
Tipo
Artigo em Revista Científica Internacional
Ano
2024-01-01
Autores
Lucilia Saraiva
(Autor)
FFUP
Revista
Título: Bioorganic ChemistryImportada do Authenticus Pesquisar Publicações da Revista
Vol. 153
ISSN: 0045-2068
Editora: Elsevier
Indexação
Publicação em ISI Web of Knowledge ISI Web of Knowledge - 0 Citações
Publicação em Scopus Scopus - 0 Citações
Outras Informações
ID Authenticus: P-017-AJP
Abstract (EN): The protein p53 is a transcription factor with several key roles in cells, including acting as a tumour suppressor. In most human cancers its tumour suppressor function is inactivated, either through inhibition by negative regulators or by mutation in the TP53 gene. Thus, there is a high interest in developing molecules able to activate p53 tumour suppressor activity. Tryptophanol-derived isoindolinones are known to act as wild-type and mutant p53 activators. Specifically, SLMP53-1 is a non-fluorescent wild-type and mutant p53 R280K reactivator, with potent in vivo anti-tumour activity in HCT116 and MDA-MB-231 mice xenograft models. With the aim of studying tryptophanol-derived isoindolinones intracellular localization by fluorescence microscopy, three SLMP53-1 based fluorescent probes were prepared. Here we report the design, synthesis, photophysical characterization, antiproliferative activity and cell localization studies of these fluorescent probes. The previously described structure-activity relationships of the SLMP53-1 scaffold set the basis for the design the fluorescent probes. The probes were prepared by connecting a small fluorophore (dansyl or 7-nitrobenzofurazan) to the indole nitrogen of the tryptophanol-derived oxazoloisoindolinone SLMP53-1 through two different linkers. The antiproliferative activity and cell localization studies of the three fluorescent probes were performed in HCT116 cells. The three probes showed enhanced internalization when compared with their fluorophorelinker intermediates, good photo-stability and high affinity for the endoplasmic reticulum, indicating the potential involvement of endoplasmic reticulum in the mechanism of action of tryptophanol-derived oxazoloisoindolinones.
Idioma: Inglês
Tipo (Avaliação Docente): Científica
Nº de páginas: 11
Documentos
Não foi encontrado nenhum documento associado à publicação.
Publicações Relacionadas

Da mesma revista

3-Arylcoumarins as highly potent and selective monoamine oxidase B inhibitors: Which chemical features matter? (2020)
Artigo em Revista Científica Internacional
Mellado, M; Mella, J; Gonzalez, C; Vina, D; Uriarte, E; Matos, MJ
Synthesis, molecular docking and cholinesterase inhibitory activity of hydroxylated 2-phenylbenzofuran derivatives (2019)
Artigo em Revista Científica Internacional
Fais, A; Kumar, A; Medda, R; Pintus, F; Delogu, F; Matos, MJ; Era, B; Delogu, GL
Novel pyridine-2,4,6-tricarbohydrazide derivatives: Design, synthesis, characterization and in vitro biological evaluation as alpha- and beta-glucosidase inhibitors (2014)
Artigo em Revista Científica Internacional
Riaz, S; Khan, IU; Yar, M; Ashraf, M; Rehman, TU; Shaukat, A; Jamal, SB; Duarte, VCM; Alves, MJ
Novel propargylamine-based inhibitors of cholinesterases and monoamine oxidases: Synthesis, biological evaluation and docking study (2021)
Artigo em Revista Científica Internacional
Krátký, M; Vu, QA; ¦t¿pánková, ¦; Maruca, A; Silva, TB; Ambro¸, M; Pflégr, V; Rocca, R; Svr¿ková, K; Alcaro, S; Fernanda Borges; Vin¨ová, J

Ver todas (18)

Recomendar Página Voltar ao Topo
Copyright 1996-2025 © Faculdade de Direito da Universidade do Porto  I Termos e Condições  I Acessibilidade  I Índice A-Z
Página gerada em: 2025-10-14 às 14:30:04 | Política de Privacidade | Política de Proteção de Dados Pessoais | Denúncias | Livro Amarelo Eletrónico