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Journal articles
Iodination increases the activity of verapamil derivatives in reversing PGP multidrug resistance.
Régis Barattin
1
Bastien Gerby
2
Kevin Bourges
2
Gaëlle Hardy
3
Jose Olivares
4
Jean Boutonnat
2
Christophe Arnoult
2, 5
Amaury Du Moulinet d'Hardemare
1, *
Xavier Ronot
2, *
Jose Olivares 4
Author
Jean Boutonnat 2
Author
Christophe Arnoult 2, 5
Author IdHAL : christophe-arnoult ORCID : https://orcid.org/0000-0002-3753-5901
Amaury Du Moulinet d'Hardemare 1
Correspondent author
Xavier Ronot 2
Correspondent author
1
DCM - Département de Chimie Moléculaire (301, rue de la Chimie 38041 GRENOBLE CEDEX 9
570, rue de la Chimie 38041 GRENOBLE CEDEX 9 - France)
- UJF - Université Joseph Fourier - Grenoble 1 (BP 53 - 38041 Grenoble Cedex 9 - France)
- CNRS - Centre National de la Recherche Scientifique : UMR5250 (France)
2
AGIM - AGeing and IMagery (Faculté de médecine de Grenoble, 38700 La Tronche - France)
- UPMF - Université Pierre Mendès France - Grenoble 2 (BP 47 - 38040 Grenoble Cedex 9 - France)
- UJF - Université Joseph Fourier - Grenoble 1 (BP 53 - 38041 Grenoble Cedex 9 - France)
- EPHE - École pratique des hautes études (4-14 Rue Ferrus, 75014 Paris - France)
- PSL - Université Paris sciences et lettres (60 rue Mazarine 75006 Paris - France)
- CNRS - Centre National de la Recherche Scientifique : FRE3405 (France)
3
HP2 - Laboratoire de Pharmacologie (Faculté de médecine, La Tronche - France)
- CHU Grenoble (France)
- Hôpital Michallon (CHU Grenoble-Alpes - France)
4
LBFA - Laboratoire de bioénergétique fondamentale et appliquée (CS 40700, F-38058 Grenoble Cedex 9 - France)
- UJF - Université Joseph Fourier - Grenoble 1 (BP 53 - 38041 Grenoble Cedex 9 - France)
- INSERM - Institut National de la Santé et de la Recherche Médicale : U1055 (101, rue de Tolbiac, 75013 Paris - France)
5
GIN - Grenoble Institut des Neurosciences (UJF - Site Santé La Tronche - BP 170 - 38042 Grenoble Cedex 9 - France)
- UJF - Université Joseph Fourier - Grenoble 1 (BP 53 - 38041 Grenoble Cedex 9 - France)
- INSERM - Institut National de la Santé et de la Recherche Médicale : U836 (101, rue de Tolbiac, 75013 Paris - France)
Abstract : Iodinated derivatives of verapamil were synthesized and tested as P-glycoprotein (Pgp)-mediated multidrug resistance (MDR) reversal agents. The ability of these compounds to revert MDR was evaluated on daunorubicin-resistant K562 cells, by measuring the intracellular accumulation of rhodamine 123, a fluorescent probe of Pgp transport activity. One of the investigated compounds (16c) was found to be a more potent MDR reversal agent than verapamil and cyclosporin A, used as reference molecules. Further in vitro studies showed that compound 16c restored daunorubicin activity and, when used alone, did not induce cell death, cell cycle perturbation and modification of calcium channel activity in comparison with verapamil.
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https://www.hal.inserm.fr/inserm-00520132
Contributor : Marco Canepari <>
Submitted on : Wednesday, September 22, 2010 - 12:04:43 PM
Last modification on : Thursday, May 20, 2021 - 4:50:02 PM
Long-term archiving on: : Friday, December 2, 2016 - 3:57:13 AM
Contributor : Marco Canepari <>
Submitted on : Wednesday, September 22, 2010 - 12:04:43 PM
Last modification on : Thursday, May 20, 2021 - 4:50:02 PM
Long-term archiving on: : Friday, December 2, 2016 - 3:57:13 AM
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- HAL Id : inserm-00520132, version 1
- PUBMED : 20682982
Citation
Régis Barattin, Bastien Gerby, Kevin Bourges, Gaëlle Hardy, Jose Olivares, et al.. Iodination increases the activity of verapamil derivatives in reversing PGP multidrug resistance.. Anticancer Research, International Institute of Anticancer Research, 2010, 30 (7), pp.2553-9. ⟨inserm-00520132⟩
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