Crossing of the cystic barriers of Toxoplasma gondii by the fluorescent coumarin tetra-cyclopeptide.
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Data
2021
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Resumo
FR235222 is a natural tetra-cyclopeptide with a strong inhibition effect on histone deacety-
lases, effective on mammalian cells as well as on intracellular apicomplexan parasites, such as Toxo-
plasma gondii, in the tachyzoite and bradyzoite stages. This molecule is characterized by two parts: the
zinc-binding group, responsible for the binding to the histone deacetylase, and the cyclic tetrapeptide
moiety, which plays a crucial role in cell permeability. Recently, we have shown that the cyclic
tetrapeptide coupled with a fluorescent diethyl-amino-coumarin was able to maintain properties of
cellular penetration on human cells. Here, we show that this property can be extended to the crossing
of the Toxoplasma gondii cystic cell wall and the cell membrane of the parasite in its bradyzoite form,
while maintaining a high efficacy as a histone deacetylase inhibitor. The investigation by molecular
modeling allows a better understanding of the penetration mechanism.
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Histone deacetylase, Bradyzoite, Cell-permeable agent, Molecular dynamics
Citação
DARD, C. et al. Crossing of the cystic barriers of Toxoplasma gondii by the fluorescent coumarin tetra-cyclopeptide. Molecules, v. 26, n. 24, artigo 7506, 2021. Disponível em: <https://www.mdpi.com/1420-3049/26/24/7506>. Acesso em: 11 out. 2022.