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A new generation of MDR modulating agents with dual activity: P-gp inhibitor and iNOS inducer agents
- Source :
- Toxicology in vitro : an international journal published in association with BIBRA. 25(1)
- Publication Year :
- 2010
-
Abstract
- MultiDrug Resistance (MDR) is due to the ability of some ATPase transporters to efflux chemotherapeutic agents out from tumor cells decreasing the endocellular concentration for the pharmacological effect, causing cancer cells chemoresistance. In the present work, a set of MDR modulating agents (MC89, MC70, PB28, IG9) able to modulate transmembrane ATP-dependent transporter, P-glycoprotein (P-gp), and also to induce inducible nitric oxide synthase (iNOS) expression in a panel of tumor cell lines are presented. All selected compounds, known as potent P-gp modulating agents, stimulated nitric oxide (NO) via iNOS in U937, Caco-2 and MCF7-Adr cell lines. The results displayed a new pharmacological strategy to revert MDR and lead to develop a new class of MDR reverting agents devoid of the limits of P-gp inhibitors third generation.
- Subjects :
- ATP Binding Cassette Transporter, Subfamily B
Nitric Oxide Synthase Type II
ATP-binding cassette transporter
Antineoplastic Agents
Pharmacology
Toxicology
Nitric Oxide
Nitric oxide
chemistry.chemical_compound
Cell Line, Tumor
Neoplasms
Humans
ATP Binding Cassette Transporter, Subfamily B, Member 1
Molecular Targeted Therapy
Enzyme Inhibitors
P-glycoprotein
biology
Chemistry
General Medicine
Drug Resistance, Multiple
Up-Regulation
Multiple drug resistance
Nitric oxide synthase
Kinetics
Cell culture
Drug Resistance, Neoplasm
Enzyme Induction
Cancer cell
biology.protein
Efflux
Signal Transduction
Subjects
Details
- ISSN :
- 18793177
- Volume :
- 25
- Issue :
- 1
- Database :
- OpenAIRE
- Journal :
- Toxicology in vitro : an international journal published in association with BIBRA
- Accession number :
- edsair.doi.dedup.....c748daa8803c9c117587c700b7c76d6e