Academic Journal
Crossing of the Cystic Barriers of Toxoplasma gondii by the Fluorescent Coumarin Tetra-Cyclopeptide
| العنوان: | Crossing of the Cystic Barriers of Toxoplasma gondii by the Fluorescent Coumarin Tetra-Cyclopeptide |
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| المؤلفون: | Dard, Céline, Leforestier, Baptiste, Francisco Hilário, Flaviane, Traoré, Mohamed Dit Mady, Lespinasse, Marie-Ange, Pérès, Basile, Molina, Marie-Carmen, Pereira de Freitas, Rossimiriam, Milet, Anne, Maubon, Danièle, Wong, Yung-Sing |
| المساهمون: | Institute for Advanced Biosciences / Institut pour l'Avancée des Biosciences (Grenoble) (IAB), Centre Hospitalier Universitaire CHU Grenoble (CHUGA)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Etablissement français du sang - Auvergne-Rhône-Alpes (EFS)-Centre National de la Recherche Scientifique (CNRS)-Université Grenoble Alpes (UGA), Département de Chimie Moléculaire (DCM), Institut de Chimie - CNRS Chimie (INC-CNRS)-Centre National de la Recherche Scientifique (CNRS)-Université Grenoble Alpes (UGA), Département de pharmacochimie moléculaire (DPM), Universidade Federal de Minas Gerais = Federal University of Minas Gerais Belo Horizonte, Brazil (UFMG), Labex Arcane, ANR-17-EURE-0003,CBH-EUR-GS,CBH-EUR-GS(2017) |
| المصدر: | ISSN: 1420-3049 ; Molecules ; https://hal.science/hal-03692230 ; Molecules, 2021, 26 (24), pp.7506. ⟨10.3390/molecules26247506⟩. |
| بيانات النشر: | CCSD MDPI |
| سنة النشر: | 2021 |
| المجموعة: | Université Grenoble Alpes: HAL |
| مصطلحات موضوعية: | cyclopeptides, histone deacetylase, Toxoplasma gondii, bradyzoite, cell-permeable agent, molecular dynamics, [CHIM.THER]Chemical Sciences/Medicinal Chemistry, [SDV.MP.PAR]Life Sciences [q-bio]/Microbiology and Parasitology/Parasitology |
| الوصف: | International audience ; FR235222 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. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | English |
| Relation: | PUBMEDCENTRAL: PMC8708940 |
| DOI: | 10.3390/molecules26247506 |
| الاتاحة: | https://hal.science/hal-03692230 https://hal.science/hal-03692230v1/document https://hal.science/hal-03692230v1/file/molecules-26-07506-v2.pdf https://doi.org/10.3390/molecules26247506 |
| Rights: | info:eu-repo/semantics/OpenAccess |
| رقم الانضمام: | edsbas.D83C398E |
| قاعدة البيانات: | BASE |
| DOI: | 10.3390/molecules26247506 |
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