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A galactosidase-responsive doxorubicin-folate conjugate for selective targeting of acute myelogenous leukemia blasts
Jonathan Clarhaut
1, 2, *
Sylvain Fraineau
3
Joëlle Guilhot
1, 2
Elodie Péraudeau
1, 2, 3
Isabelle Tranoy-Opalinski
4
Mikaël Thomas
4
Brigitte Renoux
4
Edouard Randriamalala
5
Patrick Bois
3
Aurelien Chatelier
3
Arnaud Monvoisin
3
Laurent Cronier
3
Sébastien Papot
4
François Guilhot
1, 2, 5
*
Corresponding author
Jonathan Clarhaut 1, 2
Mail :
Correspondent author
Sylvain Fraineau 3
Author
Joëlle Guilhot 1, 2
Author
Elodie Péraudeau 1, 2, 3
Author
Isabelle Tranoy-Opalinski 4
Mail :
Author IdHAL : isabelle-tranoy
Mikaël Thomas 4
Author
Brigitte Renoux 4
Author
Edouard Randriamalala 5
Author
Patrick Bois 3
Author
Aurelien Chatelier 3
Author
Arnaud Monvoisin 3
Author
Laurent Cronier 3
Author
Sébastien Papot 4
Author
François Guilhot 1, 2, 5
Author
1
Inserm CIC 0802 (France)
- CHU Poitiers - Centre hospitalier universitaire de Poitiers (2 Rue de la Milétrie, 86021 Poitiers - France)
2
Université de Poitiers (15, rue de l'Hôtel Dieu - 86034 Poitiers Cedex - France)
3
IPBC - Institut de Physiologie et Biologie Cellulaires (Poitiers - France)
- CNRS - Centre National de la Recherche Scientifique : FRE3511 (France)
- Université de Poitiers : FRE3511 (15, rue de l'Hôtel Dieu - 86034 Poitiers Cedex - France)
4
Synthèse Organique (E5) (Bâtiment B28 - 4 rue Michel Brunet
TSA 51106
86073 Poitiers Cedex 9 - France)
- IC2MP - Institut de Chimie des Milieux et Matériaux de Poitiers (4 RUE MICHEL BRUNET BAT B27 - CHIMIE 86022 POITIERS CEDEX - France)
- Université de Poitiers (15, rue de l'Hôtel Dieu - 86034 Poitiers Cedex - France)
- CNRS - Centre National de la Recherche Scientifique : UMR7285 (France)
5
Department of Oncology-Hematology and Cell Therapy (CHU de Poitiers La Miletrie 86000 POITIERS - France)
- CHU Poitiers - Centre hospitalier universitaire de Poitiers (2 Rue de la Milétrie, 86021 Poitiers - France)
Abstract : Cytarabine combined with an anthracycline or an anthracenedione represents the usual intensive induction therapy for the treatment of AML. However, this protocol induces severe side effects and treatment-related mortality due to the lack of selectivity of these cytotoxic agents. In this paper, we present the study of the first galactosidase-responsive molecular "Trojan Horse" programmed for the delivery of doxorubicin exclusively inside AML blasts over-expressing the folate receptor (FR). This targeting system allows the selective killing of AML blasts without affecting normal endothelial, cardiac or hematologic cells from healthy donors suggesting that FDC could reduce adverse events usually recorded with anthracyclines.
Document type :
Journal articles
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https://www.hal.inserm.fr/inserm-02444614
Contributor : Sylvain Fraineau <>
Submitted on : Saturday, January 18, 2020 - 11:19:47 AM
Last modification on : Monday, March 16, 2020 - 3:04:02 PM
Contributor : Sylvain Fraineau <>
Submitted on : Saturday, January 18, 2020 - 11:19:47 AM
Last modification on : Monday, March 16, 2020 - 3:04:02 PM
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Identifiers
- HAL Id : inserm-02444614, version 1
- DOI : 10.1016/j.leukres.2013.04.026
- PUBMED : 23726264
Collections
UNIV-POITIERS | IC2MP | INC-CNRS | 2IC | CNRS
Citation
Jonathan Clarhaut, Sylvain Fraineau, Joëlle Guilhot, Elodie Péraudeau, Isabelle Tranoy-Opalinski, et al.. A galactosidase-responsive doxorubicin-folate conjugate for selective targeting of acute myelogenous leukemia blasts. Leukemia Research, Elsevier, 2013, 37 (8), pp.948 - 955. ⟨10.1016/j.leukres.2013.04.026⟩. ⟨inserm-02444614⟩
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