RU49953: a non-hormonal steroid derivative that potently inhibits P-glycoprotein and reverts cellular multidrug resistance

2003 ◽  
Vol 60 (3) ◽  
pp. 526-535 ◽  
Author(s):  
F. J. Perez-Victoria ◽  
G. Conseil ◽  
F. Munoz-Martinez ◽  
J. M. Perez-Victoria ◽  
G. Dayan ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
P Glycoprotein ◽  
Hormonal Steroid ◽  
Steroid Derivative

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

scholarly journals Overcoming multidrug-resistance in vitro and in vivo using the novel P-glycoprotein inhibitor 1416

2012 ◽  
Vol 32 (6) ◽  
pp. 559-566 ◽  
Author(s):  
Yan Xu ◽  
Feng Zhi ◽  
Guangming Xu ◽  
Xiaolei Tang ◽  
Sheng Lu ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Cancer Chemotherapy ◽  
Antitumour Activity ◽  
Multidrug Resistant ◽  
The Novel ◽  
Mice Model ◽  
P Glycoprotein ◽  
Channel Currents

MDR (multidrug-resistance) represents a major obstacle to successful cancer chemotherapy and is usually accomplished by overexpression of P-gp (P-glycoprotein). Much effort has been devoted to developing P-gp inhibitors to modulate MDR. However, none of the inhibitors on the market have been successful. 1416 [1-(2,6-dimethylphenoxy)-2-(3,4-dimethoxyphenylethylamino)propane hydrochloride (phenoprolamine hydrochloride)] is a new VER (verapamil) analogue with a higher IC50 for blocking calcium channel currents than VER. In the present paper, we examined the inhibition effect of 1416 on P-gp both in vitro and in vivo. 1416 significantly enhanced cytotoxicity of VBL (vinblastine) in P-gp-overexpressed human multidrug-resistant K562/ADM (adriamycin) and KBV cells, but had no such effect on the parent K562 and KB cells. The MDR-modulating function of 1416 was further confirmed by increasing intracellular Rh123 (rhodanmine123) content in MDR cells. Human K562/ADM xenograft-nude mice model verified that 1416 potentiates the antitumour activity of VBL in vivo. RT-PCR (reverse transcriptase-PCR) and FACS analysis demonstrated that the expression of MDR1/P-gp was not affected by 1416 treatment. All these observations suggest that 1416 could be a promising agent for overcoming MDR in cancer chemotherapy.

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