A dendritic β-galactosidase-responsive folate–monomethylauristatin E conjugate
| Autor: | Pauline Poinot, Elodie Péraudeau, Jérôme Alsarraf, Jonathan Clarhaut, Isabelle Tranoy-Opalinski, Brigitte Renoux, Sébastien Papot |
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| Přispěvatelé: | Institut de Chimie des Milieux et Matériaux de Poitiers (IC2MP), Institut national des sciences de l'Univers (INSU - CNRS)-Centre National de la Recherche Scientifique (CNRS)-Université de Poitiers-Institut de Chimie du CNRS (INC), Centre hospitalier universitaire de Poitiers (CHU Poitiers), Signalisation et Transports Ioniques Membranaires (STIM), Université de Poitiers-Université de Tours-Centre National de la Recherche Scientifique (CNRS), INSERM CIC 0802 (INSERM - CHU de Poitiers), Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre hospitalier universitaire de Poitiers (CHU Poitiers)-Université de Poitiers, Université de Poitiers-Institut national des sciences de l'Univers (INSU - CNRS)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Université de Poitiers-Université de Tours (UT)-Centre National de la Recherche Scientifique (CNRS) |
| Rok vydání: | 2015 |
| Předmět: |
Antineoplastic Agents
[SDV.CAN]Life Sciences [q-bio]/Cancer 010402 general chemistry 01 natural sciences Catalysis Drug Delivery Systems Folic Acid Monomethylauristatin E Escherichia coli Materials Chemistry [CHIM]Chemical Sciences Humans ComputingMilieux_MISCELLANEOUS 010405 organic chemistry Chemistry Folate Receptors GPI-Anchored Metals and Alloys Galactosides General Chemistry beta-Galactosidase Endocytosis 3. Good health 0104 chemical sciences Surfaces Coatings and Films Electronic Optical and Magnetic Materials Cancer cell Drug delivery Ceramics and Composites Cancer research Oligopeptides HeLa Cells Conjugate |
| Zdroj: | Chemical Communications Chemical Communications, Royal Society of Chemistry, 2015, 51 (87), pp.15792-15795. ⟨10.1039/c5cc05294g⟩ Chemical Communications, Royal Society of Chemistry, 2015, 51 (87), pp.15792-15795. ⟨10.1039/C5CC05294G⟩ |
| ISSN: | 1364-548X 1359-7345 |
| Popis: | We report the study of a new drug delivery system programmed for the selective internalisation and the subsequent enzyme-catalysed release of two monomethylauristatin E molecules inside FR-positive cancer cells. This targeting device is the most potent β-galactosidase-responsive folate-drug conjugate developed so far, killing cancer cells expressing a medium level of FR at low nanomolar concentrations. |
| Databáze: | OpenAIRE |
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