Crossing of the cystic barriers of Toxoplasma gondii by the fluorescent coumarin tetra-cyclopeptide

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dc.creatorCéline Dard
dc.creatorBaptiste Leforestier
dc.creatorFlaviane Francisco Hilário
dc.creatorMohamed Dit Mady Traoré
dc.creatorMarie-Ange Lespinasse
dc.creatorBasile Pérès
dc.creatorMarie-Carmen Molina
dc.creatorRossimiriam Pereira de Freitas
dc.creatorAnne Milet
dc.creatorDanièle Maubon
dc.creatorYung-Sing Wong
dc.date.accessioned2024-08-06T23:05:03Z
dc.date.accessioned2025-09-09T00:58:26Z
dc.date.available2024-08-06T23:05:03Z
dc.date.issued2021
dc.description.sponsorshipCNPq - Conselho Nacional de Desenvolvimento Científico e Tecnológico
dc.description.sponsorshipFAPEMIG - Fundação de Amparo à Pesquisa do Estado de Minas Gerais
dc.description.sponsorshipCAPES - Coordenação de Aperfeiçoamento de Pessoal de Nível Superior
dc.description.sponsorshipOutra Agência
dc.format.mimetypepdf
dc.identifier.doihttps://doi.org/10.3390/molecules26247506
dc.identifier.issn1420-3049
dc.identifier.urihttps://hdl.handle.net/1843/73163
dc.languageeng
dc.publisherUniversidade Federal de Minas Gerais
dc.relation.ispartofMolecules
dc.rightsAcesso Aberto
dc.subjectToxoplasma gondii
dc.subjectDinâmica molecular
dc.subjectPeptídios
dc.subjectMoléculas
dc.subject.otherCyclopeptides
dc.subject.otherHistone deacetylase
dc.subject.otherToxoplasma gondii
dc.subject.otherBradyzoite
dc.subject.otherCell-permeable agent
dc.subject.otherMolecular dynamics
dc.titleCrossing of the cystic barriers of Toxoplasma gondii by the fluorescent coumarin tetra-cyclopeptide
dc.typeArtigo de periódico
local.citation.issue24
local.citation.spage7506
local.citation.volume26
local.description.resumoFR235222 is a natural tetra-cyclopeptide with a strong inhibition effect on histone deacetylases, effective on mammalian cells as well as on intracellular apicomplexan parasites, such as Toxoplasma 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.
local.identifier.orcidhttps://orcid.org/0000-0002-5843-0842
local.identifier.orcidhttps://orcid.org/0000-0001-8547-6021
local.identifier.orcidhttps://orcid.org/0000-0002-0784-6450
local.identifier.orcidhttps://orcid.org/0000-0001-6974-3724
local.identifier.orcidhttps://orcid.org/0000-0002-1480-4451
local.identifier.orcidhttps://orcid.org/0000-0002-9080-7638
local.identifier.orcidhttps://orcid.org/0000-0003-1038-9681
local.publisher.countryBrasil
local.publisher.departmentICX - DEPARTAMENTO DE QUÍMICA
local.publisher.initialsUFMG
local.url.externahttps://www.mdpi.com/1420-3049/26/24/7506

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