Dihidro-β-Agarofuran Sesquiterpenes: A New Class of Reversal Agents of the Multidrug Resistance Phenotype Mediated by P-Glycoprotein in the Protozoan Parasite Leishmania

2005 ◽  
Vol 11 (24) ◽  
pp. 3125-3139 ◽  
Author(s):  
F. Cortes-Selva ◽  
I. Jimenez ◽  
F. Munoz-Martinez ◽  
M. Campillo ◽  
I. Bazzocchi ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Protozoan Parasite ◽  
Resistance Phenotype ◽  
Reversal Agents ◽  
New Class ◽  
P Glycoprotein ◽  
Parasite Leishmania

Multidrug Resistance Phenotype Mediated by the P-Glycoprotein-Like Transporter in Leishmania: A Search for Reversal Agents

2002 ◽  
Vol 3 (4) ◽  
pp. 311-333 ◽  
Author(s):  
J. Perez-Victoria ◽  
A. Pietro ◽  
D. Barron ◽  
A. Ravelo ◽  
S. Castanys ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Resistance Phenotype ◽  
Reversal Agents ◽  
P Glycoprotein

Bis-pyranobenzoquinones as a New Family of Reversal Agents of the Multidrug Resistance Phenotype Mediated by P-Glycoprotein in Mammalian Cells and the Protozoan ParasiteLeishmania

2008 ◽  
Vol 51 (22) ◽  
pp. 7132-7143 ◽  
Author(s):  
Sandra Jiménez-Alonso ◽  
Antonio L. Pérez-Lomas ◽  
Ana Estévez-Braun ◽  
Francisco Muñoz Martinez ◽  
Haydee Chávez Orellana ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Mammalian Cells ◽  
Resistance Phenotype ◽  
Reversal Agents ◽  
New Family ◽  
P Glycoprotein

IsomericN,N-Bis(cyclohexanol)amine Aryl Esters:  The Discovery of a New Class of Highly Potent P-Glycoprotein (Pgp)-dependent Multidrug Resistance (MDR) Inhibitors

2007 ◽  
Vol 50 (4) ◽  
pp. 599-602 ◽  
Author(s):  
Elisabetta Teodori ◽  
Cecilia Martelli ◽  
Milena Salerno ◽  
Nacira Darghal ◽  
Silvia Dei ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
New Class ◽  
P Glycoprotein

Trabectedin (ET-743, Yondelis™) is a substrate for P-glycoprotein, but only high expression of P-glycoprotein confers the multidrug resistance phenotype

2006 ◽  
Vol 25 (1) ◽  
pp. 1-7 ◽  
Author(s):  
Jan-Hendrik Beumer ◽  
Tessa Buckle ◽  
Mariet Ouwehand ◽  
Niels E. F. Franke ◽  
Luis Lopez-Lazaro ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
High Expression ◽  
Resistance Phenotype ◽  
P Glycoprotein

Design, synthesis and biological evaluation of novel triazole-core reversal agents against P-glycoprotein-mediated multidrug resistance

RSC Advances ◽  
2016 ◽  
Vol 6 (31) ◽  
pp. 25819-25828 ◽  
Author(s):  
Bo Zhang ◽  
Tianxiao Zhao ◽  
Jie Zhou ◽  
Qianqian Qiu ◽  
Yuxuan Dai ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Click Chemistry ◽  
Biological Evaluation ◽  
Glycoprotein P ◽  
Design Synthesis ◽  
Reversal Agents ◽  
P Glycoprotein ◽  
Synthesis And Biological Evaluation

We designed and synthesized a novel series of P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) inhibitors bearing a triazolphenethyl–tetrahydroisoquinoline scaffold through click chemistry.

scholarly journals Characterization of an ABCG-Like Transporter from the Protozoan Parasite Leishmania with a Role in Drug Resistance and Transbilayer Lipid Movement

2008 ◽  
Vol 52 (10) ◽  
pp. 3573-3579 ◽  
Author(s):  
Esther Castanys-Muñoz ◽  
José María Pérez-Victoria ◽  
Francisco Gamarro ◽  
Santiago Castanys
Keyword(s):  
Drug Resistance ◽  
Plasma Membrane ◽  
Treatment Failure ◽  
Tumor Cells ◽  
Abc Transporters ◽  
Protozoan Parasite ◽  
Protozoan Parasites ◽  
Resistance Phenotype ◽  
Parasite Leishmania

ABSTRACT Leishmaniasis treatment is hampered by the increased appearance of treatment failure. ATP-binding cassette (ABC) transporters are usually involved in drug resistance both in tumor cells and in microorganisms. Here we report the characterization of an ABCG-like transporter, LiABCG6, localized mainly at the plasma membrane in Leishmania protozoan parasites. When overexpressed, this half-transporter confers significant resistance to the leishmanicidal agents miltefosine and sitamaquine. This resistance phenotype is mediated by a reduction in intracellular drug accumulation. LiABCG6 also reduces the accumulation of short-chain fluorescent phospholipid analogues of phosphatidylcholine, phosphatidylethanolamine, and phosphatidylserine. As a whole, these results suggest that LiABCG6 could be implicated in phospholipid trafficking and drug resistance.

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