2020
DOI: 10.1186/s13046-020-01604-z
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Inhibition of lysine acetyltransferases impairs tumor angiogenesis acting on both endothelial and tumor cells

Abstract: Background: Understanding the signalling pathways involved in angiogenesis, and developing anti-angiogenic drugs are one of the major focuses on cancer research. Herein, we assessed the effect of CPTH6, a lysine acetyltransferase inhibitor and anti-tumoral compound, on angiogenesis-related properties of both endothelial and cancer cells. Methods: The in vitro effect of CPTH6 on protein acetylation and anti-angiogenic properties on endothelial and lung cancer cells was evaluated via wound healing, trans-well in… Show more

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Cited by 6 publications
(4 citation statements)
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“…Zebrafish larvae at 72 hpf, previously exposed to control conditions or 100 mg/L BRB for 48 h, were fixed in 4% PFA in PBS for 2 h at RT and stained for endogenous alkaline phosphatase, in line with a previous work 66 . Briefly, after fixation, larvae were washed 3 times in PBS containing 0.1% Tween-20 (PBST).…”
Section: Methodsmentioning
confidence: 99%
“…Zebrafish larvae at 72 hpf, previously exposed to control conditions or 100 mg/L BRB for 48 h, were fixed in 4% PFA in PBS for 2 h at RT and stained for endogenous alkaline phosphatase, in line with a previous work 66 . Briefly, after fixation, larvae were washed 3 times in PBS containing 0.1% Tween-20 (PBST).…”
Section: Methodsmentioning
confidence: 99%
“…By observing the development of ISV and SIV after the intervention, researchers can evaluate the antiangiogenic activity of compounds. Currently, an increasing number of botanical extracts [110][111][112][113][114][115][116][117][118] and synthetic compounds [119][120][121][122][123] with cytotoxic effects are being evaluated for their antiangiogenic activity in zebrafish. Some of these compounds have demonstrated potential as anticancer agents.…”
Section: Zebrafish In Screening For Antiangiogenic Drugsmentioning
confidence: 99%
“…Padrões irregulares na atividade das HAT podem ocorrer tanto pela repressão gênica geral, quando há perda dessa atividade acetiltransferase ou por sua alta expressão, e ambos estão associados ao câncer. Alguns exemplos da desregulação das HAT foram relatados em diversos tumores como, mutação de HAT p300; hiperacetilação de histonas em amostras orais de pacientes com carcinoma hepatocelular e escamoso; translocação de genes HAT; acetilação de lisina dependente de ligante do receptor do fator de crescimento endotelial vascular 2 (VEGFR2), e superexpressão de AIB-1, uma HAT coativadora de um receptor nuclear de hormônio (TRISCIUOGLIO et al, 2012;DI MARTILE et al, 2020;EICH et al, 2020).…”
Section: Alvos Terapêuticos Das Epi-drogas: "Enzimas Writers: Escrito...unclassified
“…CPTH6, um derivado tiazólico, é um inibidor da enzima HAT Gcn5/PCAF que inibe a acetilação das histonas H3 e H4 (TRISCIUOGLIO et al, 2012). Foi demonstrado que CPTH6 apresenta capacidade de reduzir a acetilação das histonas em células cancerosas, inibir viabilidade celular e autorenovação de CTT, bem como diminuir o crescimento in vivo de tumores derivados de células-tronco de câncer de pulmão (DI MARTILE et al, 2016;DI MARTILE et al, 2020). Delphinidin, inibe a atividade da HAT p300/CBP, o que previne a hiperacetilação de p65, regulando a função nuclear de NF-ƘB (SEONG et al, 2011).…”
Section: Alvos Terapêuticos Das Epi-drogas: "Enzimas Writers: Escrito...unclassified