Chloroquine-Containing HPMA Copolymers as Polymeric Inhibitors of Cancer Cell Migration Mediated by the CXCR4/SDF-1 Chemokine Axis.

Chloroquine-Containing HPMA Copolymers as Polymeric Inhibitors of Cancer Cell Migration Mediated by the CXCR4/SDF-1 Chemokine Axis.
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含氯喹的 HPMA 共聚物作为 CXCR4/SDF-1 趋化因子轴介导的癌细胞迁移的聚合物抑制剂。

DOI:
10.1021/acsmacrolett.5b00857
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发表时间:
2016
期刊:
影响因子:
7.015
通讯作者:
Oupický,David
Oupický,David
中科院分区:
化学1区
文献类型:
--
作者:
Yu,Fei;Xie,Ying;Wang,Yan;Peng,Zheng-Hong;Li,Jing;Oupický,David

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通过甲基丙烯酰化羟氯喹与HPMA共聚,首次合成了含氯喹的HPMA共聚物(pCQ)。与羟氯喹相比,共聚物显示出较低的细胞毒性。用pCQ处理癌细胞导致趋化因子受体CXCR 4的表面表达降低。pCQ共聚物显示出对CXCR 4/SDF 1介导的癌细胞迁移的有效抑制,这与商业小分子CXCR 4拮抗剂AMD 3100完全相当。报道的pCQ代表了独特和简单的聚合物药物,具有作为组合抗转移疗法的一部分的潜在用途。
Chloroquine-containing HPMA copolymers (pCQs) were synthesized for the first time by copolymerization of methacryloylated hydroxychloroquine and HPMA. The copolymers showed lower cytotoxicity when compared with hydroxychloroquine. Treatment of cancer cells with pCQ resulted in decreased surface expression of chemokine receptor CXCR4. The pCQ copolymers showed effective inhibition of CXCR4/SDF1-mediated cancer cell migration that was fully comparable with a commercial small-molecule CXCR4 antagonist AMD3100. The reported pCQ represent unique and simple polymeric drugs with potential use as part of a combination antimetastatic therapies.
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