Tivozanib reverses multidrug resistance mediated by ABCB1 (P-glycoprotein) and ABCG2 (BCRP).
Tivozanib reverses multidrug resistance mediated by ABCB1 (P-glycoprotein) and ABCG2 (BCRP).
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Tivozanib 可逆转 ABCB1（P-糖蛋白）和 ABCG2（BCRP）介导的多药耐药性。
DOI：
10.2217/fon.13.253
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发表时间：
2014-08
期刊：
影响因子：
--
通讯作者：
Chen X
中科院分区：
文献类型：
--
作者：
Yang D;Kathawala RJ;Chufan EE;Patel A;Ambudkar SV;Chen ZS;Chen X
This study aimed to investigate the mechanism of reversal of multidrug resistance mediated by ABC transporters with tivozanib (AV-951 and KRN-951). Tivozanib is a potent inhibitor of VEGF-1, −2 and −3 receptors. ABCB1- and ABCG2-overexpressing cell lines were treated with respective substrate antineoplastic agents in the presence or absence of tivozanib. The results indicate that tivozanib can significantly reverse ABCB1-mediated resistance to paclitaxel, vinblastine and colchicine, as well as ABCG2-mediated resistance to mitoxantrone, SN-38 and doxorubicin. Drug efflux assays showed that tivozanib increased the intracellular accumulation of substrates by inhibiting the ABCB1 and ABCG2 efflux activity. Furthermore, at a higher concentration, tivozanib inhibited the ATPase activity of both ABCB1 and ABCG2 and inhibited the photolabeling of ABCB1 or ABCG2. We conclude that tivozanib at noncytotoxic concentrations has the previously unknown activity of reversing multidrug resistance mediated by ABCB1 and ABCG2 transporters.
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影响因子：
--
作者：
Kathawala RJ;Wang YJ;Ashby CR Jr;Chen ZS
通讯作者：
Chen ZS
影响因子：
11.2
作者：
Dai CL;Tiwari AK;Wu CP;Su XD;Wang SR;Liu DG;Ashby CR Jr;Huang Y;Robey RW;Liang YJ;Chen LM;Shi CJ;Ambudkar SV;Chen ZS;Fu LW
通讯作者：
Fu LW
影响因子：
3.8
作者：
Mayer, Erica L.;Scheulen, M. E.;Dickler, M. N.
通讯作者：
Dickler, M. N.
DOI：
10.1111/j.1742-4658.2011.08235.x
发表时间：
2011-09
期刊：
The FEBS journal
影响因子：
--
作者：
Chen ZS;Tiwari AK
通讯作者：
Tiwari AK
转移性肾细胞癌的靶向治疗：当前治疗和未来方向。
影响因子：
4.9
作者：
Heng, Daniel Y C;Kollmannsberger, Christian;Chi, Kim N
通讯作者：
Chi, Kim N