Modulation of the spacer in N,N-bis(alkanol)amine aryl ester heterodimers led to the discovery of a series of highly potent P-glycoprotein-based multidrug resistance (MDR) modulators

2019 ◽  
Vol 172 ◽  
pp. 71-94 ◽  
Author(s):  
Silvia Dei ◽  
Laura Braconi ◽  
Alfonso Trezza ◽  
Marta Menicatti ◽  
Marialessandra Contino ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
P Glycoprotein ◽  
Alkanol Amine ◽  
Aryl Ester

Structure−Activity Relationships Studies in a Series ofN,N-Bis(alkanol)amine Aryl Esters as P-Glycoprotein (Pgp) Dependent Multidrug Resistance (MDR) Inhibitors†

2010 ◽  
Vol 53 (4) ◽  
pp. 1755-1762 ◽  
Author(s):  
Cecilia Martelli ◽  
Marcella Coronnello ◽  
Silvia Dei ◽  
Dina Manetti ◽  
Francesca Orlandi ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
P Glycoprotein ◽  
Alkanol Amine

scholarly journals Dual P-Glycoprotein and CA XII Inhibitors: A New Strategy to Reverse the P-gp Mediated Multidrug Resistance (MDR) in Cancer Cells

Molecules ◽  
2020 ◽  
Vol 25 (7) ◽  
pp. 1748 ◽  
Author(s):  
Elisabetta Teodori ◽  
Laura Braconi ◽  
Silvia Bua ◽  
Andrea Lapucci ◽  
Gianluca Bartolucci ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Cancer Cells ◽  
Glycoprotein P ◽  
Reversal Effect ◽  
P Glycoprotein ◽  
New Strategy ◽  
Uptake Test ◽  
New Compounds ◽  
Alkanol Amine ◽  
Mdr Reversal

A new series of N,N-bis(alkanol)amine aryl diesters was synthesized and studied as dual P-glycoprotein (P-gp) and carbonic anhydrase XII inhibitors (CA XII). These hybrids should be able to synergistically overcome P-gp mediated multidrug resistance (MDR) in cancer cells. It was reported that the efflux activity of P-gp could be modulated by CA XII, as the pH reduction caused by CA XII inhibition produces a significant decrease in P-gp ATPase activity. The new compounds reported here feature both P-gp and CA XII binding moieties. These hybrids contain a N,N-bis(alkanol)amine diester scaffold found in P-glycoprotein ligands and a coumarin or benzene sulfonamide moiety to target CA XII. Many compounds displayed a dual activity against P-gp and CA XII being active in the Rhd 123 uptake test on K562/DOX cells and in the hCA XII inhibition test. On LoVo/DOX cells, that overexpress both P-gp and CA XII, some coumarin derivatives showed a high MDR reversal effect in Rhd 123 uptake and doxorubicin cytotoxicity enhancement tests. In particular, compounds 7 and 8 showed higher activity than verapamil and were more potent on LoVo/DOX than on K562/DOX cells overexpressing only P-gp. They can be considered as valuable candidates for selective P-gp/CA XII inhibition in MDR cancer cells.

Transfection with Protein Kinase Cα Confers Increased Multidrug Resistance to MCF-7 Cells Expressing P-Glycoprotein

1991 ◽  
Vol 3 (6) ◽  
pp. 181-189 ◽  
Author(s):  
Gang Yu ◽  
Shakeel Ahmad ◽  
Angelo Aquino ◽  
Craig R. Fairchild ◽  
Jane B. Trepel ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Protein Kinase ◽  
P Glycoprotein ◽  
Protein Kinase Cα ◽  
Mcf 7

scholarly journals Modulation of the expression of a multidrug resistance gene (mdr-1/P-glycoprotein) by differentiating agents

1989 ◽  
Vol 264 (30) ◽  
pp. 18031-18040
Author(s):  
L A Mickley ◽  
S E Bates ◽  
N D Richert ◽  
S Currier ◽  
S Tanaka ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Resistance Gene ◽  
Multidrug Resistance Gene ◽  
P Glycoprotein ◽  
Differentiating Agents ◽  
Mdr 1

Designing potent inhibitors against the multidrug resistance P-glycoprotein

2021 ◽  
pp. 1-13
Author(s):  
Shafi Mahmud ◽  
Md. Jahirul Islam ◽  
Md. Rimon Parves ◽  
Md. Arif Khan ◽  
Lamiya Tabussum ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
P Glycoprotein

scholarly journals Retraction Note: Flavonoids modulate multidrug resistance through wnt signaling in P-glycoprotein overexpressing cell lines

BMC Cancer ◽  
2021 ◽  
Vol 21 (1) ◽  
Author(s):  
S. Mohana ◽  
M. Ganesan ◽  
N. Rajendra Prasad ◽  
D. Ananthakrishnan ◽  
D. Velmurugan
Keyword(s):  
Multidrug Resistance ◽  
Wnt Signaling ◽  
Cell Lines ◽  
P Glycoprotein ◽  
Overexpressing Cell

An amendment to this paper has been published and can be accessed via the original article.

scholarly journals Reversal of multidrug resistance by calcium channel blocker SR33557 without photoaffinity labeling of P-glycoprotein.

1991 ◽  
Vol 266 (29) ◽  
pp. 19858-19864
Author(s):  
J.P. Jaffrézou ◽  
J.M. Herbert ◽  
T. Levade ◽  
M.N. Gau ◽  
P. Chatelain ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Calcium Channel ◽  
Calcium Channel Blocker ◽  
Channel Blocker ◽  
Photoaffinity Labeling ◽  
P Glycoprotein
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