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Table 1 Effect of ERK5-IN-1 on enhancing efficacy of chemothereapeutic agents in ABCB1- and ABCG2-overexpressing cells

From: Reversal of ABCB1-related multidrug resistance by ERK5-IN-1

Compounds

IC50 ± SD (μmol/L) (fold-reversal)

KB

KBv200 (ABCB1)

Vincristine

0.00131 ± 0.00009

(1.00)

0.18606 ± 0.03569

(1.00)

+  0.1 μM ERK5-IN-1

0.00122 ± 0.00008

(1.08)

0.11322 ± 0.01575 *

(1.64)

+  0.2 μM ERK5-IN-1

0.00074 ± 0.00010 **

(1.78)

0.07330 ± 0.00529 **

(2.54)

+  0.4 μM ERK5-IN-1

0.00066 ± 0.00004 **

(2.00)

0.02260 ± 0.01838 **

(8.23)

+  10 μM Verapamil

0.00141 ± 0.00025

(0.93)

0.00055 ± 0.00008 **

(337.99)

Paclitaxel

0.00329 ± 0.00055

(1.00)

0.19882 ± 0.01985

(1.00)

+  0.1 μM ERK5-IN-1

0.00299 ± 0.00071

(1.10)

0.09600 ± 0.01963 *

(2.07)

+  0.2 μM ERK5-IN-1

0.00346 ± 0.00075

(0.95)

0.06959 ± 0.00393 *

(2.86)

+  0.4 μM ERK5-IN-1

0.00275 ± 0.00023

(1.20)

0.01793 ± 0.00351 **

(11.09)

+  10 μM Verapamil

0.00306 ± 0.00021

(1.08)

0.00124 ± 0.00135 **

(160.50)

Cisplatin

0.15037 ± 0.02336

(1.00)

1.30926 ± 0.06360

(1.00)

+  0.4 μM ERK5-IN-1

0.15123 ± 0.03312

(0.99)

1.30950 ± 0.09836

(1.00)

 

MCF-7

MCF-7/adr (ABCB1)

Doxorubicin

0.20569 ± 0.08712

(1.00)

7.17759 ± 1.37837

(1.00)

+  0.1 μM ERK5-IN-1

0.18715 ± 0.03454

(1.10)

1.77472 ± 0.19202 **

(4.04)

+  0.2 μM ERK5-IN-1

0.12307 ± 0.01691

(1.67)

1.32842 ± 0.77573 **

(5.40)

+  0.4 μM ERK5-IN-1

0.12114 ± 0.04427

(1.70)

0.94483 ± 0.11191 **

(7.60)

+  10 μM Verapamil

0.19548 ± 0.01487

(1.05)

0.27687 ± 0.05879 **

(25.92)

Cisplatin

5.03363 ± 0.10899

(1.00)

8.48499 ± 0.19816

(1.00)

+  0.4 μM ERK5-IN-1

4.90850 ± 0.07421

(1.03)

7.72168 ± 0.93519

(1.10)

 

HEK293/Vector

HEK293/ABCB1

Doxorubicin

0.12555 ± 0.00745

(1.00)

0.92581 ± 0.11863

(1.00)

+  0.1 μM ERK5-IN-1

0.11298 ± 0.05714

(1.11)

0.29031 ± 0.06122 **

(3.19)

+  0.2 μM ERK5-IN-1

0.10177 ± 0.00585 *

(1.23)

0.27352 ± 0.05309 **

(3.38)

+  0.4 μM ERK5-IN-1

0.08744 ± 0.01173 **

(1.44)

0.19985 ± 0.00635 **

(4.63)

+  10 μM Verapamil

0.13465 ± 0.02525

(0.93)

0.05056 ± 0.01142 **

(18.31)

Cisplatin

2.48910 ± 0.39760

(1.00)

3.58743 ± 0.43037

(1.00)

+  0.4 μM ERK5-IN-1

2.58130 ± 0.27812

(0.96)

3.41328 ± 0.32569

(1.05)

 

S1

S1-MI-80 (ABCG2)

Mitoxantrone

0.04168 ± 0.00444

(1.00)

14.10528 ± 0.46080

(1.00)

+  0.1 μM ERK5-IN-1

0.03865 ± 0.00137

(1.07)

12.15908 ± 2.02744

(1.16)

+  0.2 μM ERK5-IN-1

0.03508 ± 0.00114

(1.19)

11.46149 ± 0.31168

(1.23)

+  0.4 μM ERK5-IN-1

0.03265 ± 0.00026

(1.27)

11.45988 ± 1.95085

(1.23)

+  2.5 μM FTC

0.03616 ± 0.00510

(1.15)

0.80305 ± 0.07874**

(17.56)

  1. Cell viability was determined by MTT assay as described in Materials and Methods. Data represent means ± SD of at least three independent experiments. The fold-reversal of MDR was calculated by dividing the IC50 for cells with the chemotherapeutic agents in the absence of ERK5-IN-1 by that obtained in the presence of ERK5-IN-1. VRP (definite inhibitor of ABCB1) and FTC (definite inhibitor of ABCG2) were used as the positive control. * P < 0.05, ** P < 0.01, both for values versus that obtained in the absence of inhibitor
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Journal of Experimental & Clinical Cancer Research

ISSN: 1756-9966

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