Differential expression of the efflux pumps p-glycoprotein and multidrug resistance-associated protein in human monocyte-derived dendritic cells

2001 ◽  
Vol 62 (10) ◽  
pp. 1073-1080 ◽  
Author(s):  
B Laupèze ◽  
L Amiot ◽  
N Bertho ◽  
J.M Grosset ◽  
G Lehne ◽  
...  
Molecules ◽  
2020 ◽  
Vol 25 (15) ◽  
pp. 3364 ◽  
Author(s):  
Bruno M. F. Gonçalves ◽  
David S. P. Cardoso ◽  
Maria-José U. Ferreira

Multidrug resistance (MDR) in cancer is one of the main limitations for chemotherapy success. Numerous mechanisms are behind the MDR phenomenon wherein the overexpression of the ATP-binding cassette (ABC) transporter proteins P-glycoprotein (P-gp), breast cancer resistance protein (BCRP) and multidrug resistance protein 1 (MRP1) is highlighted as a prime factor. Natural product-derived compounds are being addressed as promising ABC transporter modulators to tackle MDR. Flavonoids and terpenoids have been extensively explored in this field as mono or dual modulators of these efflux pumps. Nitrogen-bearing moieties on these scaffolds were proved to influence the modulation of ABC transporters efflux function. This review highlights the potential of semisynthetic nitrogen-containing flavonoid and terpenoid derivatives as candidates for the design of effective MDR reversers. A brief introduction concerning the major role of efflux pumps in multidrug resistance, the potential of natural product-derived compounds in MDR reversal, namely natural flavonoid and terpenoids, and the effect of the introduction of nitrogen-containing groups are provided. The main modifications that have been performed during last few years to generate flavonoid and terpenoid derivatives, bearing nitrogen moieties, such as aliphatic, aromatic and heterocycle amine, amide, and related functional groups, as well as their P-gp, MRP1 and BCRP inhibitory activities are reviewed and discussed.


2005 ◽  
Vol 175 (10) ◽  
pp. 6570-6579 ◽  
Author(s):  
Anne Lehtonen ◽  
Ville Veckman ◽  
Tuomas Nikula ◽  
Riitta Lahesmaa ◽  
Leena Kinnunen ◽  
...  

2011 ◽  
Vol 508 (2) ◽  
pp. 212-216 ◽  
Author(s):  
Claudia Skazik ◽  
Ruth Heise ◽  
Hagen Ott ◽  
Katharina Czaja ◽  
Yvonne Marquardt ◽  
...  

2012 ◽  
Vol 8 ◽  
pp. 1700-1704 ◽  
Author(s):  
Torsten Dittrich ◽  
Nils Hanekop ◽  
Nacera Infed ◽  
Lutz Schmitt ◽  
Manfred Braun

The inhibition of ABC (ATP binding cassette) transporters is considered a powerful tool to reverse multidrug resistance. Zosuquidar featuring a difluorocyclopropyl-annulated dibenzosuberyl moiety has been found to be an inhibitor of the P-glycoprotein, one of the best-studied multidrug efflux pumps. Twelve 5-oxyisoquinoline derivatives, which are analogues of zosuquidar wherein the dibenzosuberyl-piperazine moiety is replaced by either a diarylaminopiperidine or a piperidone-derived acetal or thioacetal group, have been synthesized as pure enantiomers. Their inhibitory power has been evaluated for the bacterial multidrug-resistance ABC transporter LmrCD and fungal Pdr5. Four of the newly synthesized compounds reduced the transport activity to a higher degree than zosuquidar, being up to fourfold more efficient than the lead compound in the case of LmrCD and about two times better for Pdr5.


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