Document Detail


Iodination increases the activity of verapamil derivatives in reversing PGP multidrug resistance.
MedLine Citation:
PMID:  20682982     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Regis Barattin; Bastien Gerby; Kevin Bourges; Gaëlle Hardy; Jose Olivares; Jean Boutonnat; Christophe Arnoult; Amaury D U Moulinet D'Hardemare; Xavier Ronot
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Anticancer research     Volume:  30     ISSN:  1791-7530     ISO Abbreviation:  Anticancer Res.     Publication Date:  2010 Jul 
Date Detail:
Created Date:  2010-08-04     Completed Date:  2010-08-30     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8102988     Medline TA:  Anticancer Res     Country:  Greece    
Other Details:
Languages:  eng     Pagination:  2553-9     Citation Subset:  IM    
Affiliation:
University of Grenoble I, Department of Molecular Chemistry, UMR CNRS 5250, F-38041, Grenoble Cedex 9, France.
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MeSH Terms
Descriptor/Qualifier:
Animals
Calcium Channel Blockers / pharmacology
Calcium Channels, L-Type / metabolism
Cell Cycle / drug effects
Cyclosporine / pharmacology
Daunorubicin / pharmacology
Drug Resistance, Neoplasm
Drug Synergism
Humans
K562 Cells
Male
Myocytes, Cardiac / drug effects,  metabolism
P-Glycoprotein / antagonists & inhibitors*,  metabolism
Rats
Rats, Wistar
Rhodamine 123 / pharmacokinetics
Verapamil / analogs & derivatives*,  pharmacology
Chemical
Reg. No./Substance:
0/Calcium Channel Blockers; 0/Calcium Channels, L-Type; 0/P-Glycoprotein; 20830-81-3/Daunorubicin; 52-53-9/Verapamil; 59865-13-3/Cyclosporine; 62669-70-9/Rhodamine 123

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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