Epidermal growth factor receptor (EGFR) inhibitor PD153035 reverses ABCG2-mediated multidrug resistance in non-small cell lung cancer: In vitro and in vivo

被引：49

作者：

Zhang, Guan-Nan ^{[1
]}

Zhang, Yun-Kai ^{[1
]}

Wang, Yi-Jun ^{[1
]}

Gupta, Pranav ^{[1
]}

Ashby, Charles R., Jr. ^{[1
]}

Alqahtani, Saeed ^{[2
]}

Deng, Tongjin ^{[1
,5
]}

Bates, Susan E. ^{[3
]}

Kaddoumi, Amal ^{[2
]}

Wurpel, John N. D. ^{[1
]}

Lei, Yi-Xiong ^{[4
]}

Chen, Zhe-Sheng ^{[1
]}

机构：

[1] St Johns Univ, Coll Pharm & Hlth Sci, Dept Pharmaceut Sci, Queens, NY 11439 USA

[2] Univ Louisiana Monroe, Sch Pharm, Dept Basic Pharmaceut Sci, Monroe, LA 71201 USA

[3] Columbia Univ, Med Ctr, Div Hematol Oncol, New York, NY 10032 USA

[4] Guangzhou Med Univ, Sch Publ Hlth, Dept Prevent Med, Guangzhou 511436, Guangdong, Peoples R China

[5] Bayside High Sch, New York, NY 11361 USA

来源：

CANCER LETTERS | 2018年 / 424卷

关键词：

PD153035; Tyrosine kinase inhibitor; Multidrug resistance; EGFR inhibitor; ABCG2; TYROSINE KINASE INHIBITOR; G MEMBER 2; DRUG-RESISTANCE; PACLITAXEL RESISTANCE; PROTEIN BCRP/ABCG2; ABCG2; EXPRESSION; P-GLYCOPROTEIN; TRANSPORTERS; TOPOTECAN; POLYMORPHISMS;

D O I：

10.1016/j.canlet.2018.02.040

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

One of the major mediators of multidrug resistance (MDR) in non-small cell lung cancer (NSCLC) is the overexpression of ATP-binding cassette subfamily G member 2 (ABCG2). In this study, we conducted in vitro and in vivo experiments to determine whether PD153035, an inhibitor of EGFR, could reverse ABCG2-mediated MDR in human NSCLC and transfected cells overexpressing ABCG2. The efficacy of SN-38, topotecan, and mitoxantrone (MX) were significantly increased by PD153035, PD153035 significantly reversed ABCG2-mediated MDR by attenuating the efflux activity of this transporter. In addition, PD153035 significantly down-regulated the expression of the ABCG2 transporter protein. Furthermore, a combination of PD153035 and topotecan, exhibited significant synergistic anticancer activity against mice xenografted with human H460/MX20 cells. These results, provided that they can be extrapolated to humans, suggest that the combination of topotecan and PD153035 could be a promising therapeutic strategy to attenuate the resistance to topotecan, as well as other anticancer drugs, mediated by the overexpression of ABCG2. (C) 2018 Elsevier B.V. All rights reserved.

引用

页码：19 / 29

页数：11

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