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Addressing Drug Resistance in Cancer with Macromolecular Chemotherapeutic Agents
Journal of the American Chemical Society ( IF 14.4 ) Pub Date : 2018-03-05 , DOI: 10.1021/jacs.7b11468 Nathaniel H. Park 1 , Wei Cheng 2 , Fritz Lai 3 , Chuan Yang 2 , Paola Florez de Sessions 4 , Balamurugan Periaswamy 4 , Collins Wenhan Chu 4 , Simone Bianco 1 , Shaoqiong Liu 2 , Shrinivas Venkataraman 2 , Qingfeng Chen 3 , Yi Yan Yang 2 , James L. Hedrick 1
Journal of the American Chemical Society ( IF 14.4 ) Pub Date : 2018-03-05 , DOI: 10.1021/jacs.7b11468 Nathaniel H. Park 1 , Wei Cheng 2 , Fritz Lai 3 , Chuan Yang 2 , Paola Florez de Sessions 4 , Balamurugan Periaswamy 4 , Collins Wenhan Chu 4 , Simone Bianco 1 , Shaoqiong Liu 2 , Shrinivas Venkataraman 2 , Qingfeng Chen 3 , Yi Yan Yang 2 , James L. Hedrick 1
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Drug resistance to chemotherapeutics is a recurrent issue plaguing many cancer treatment regimens. To circumvent resistance issues, we have designed a new class of macromolecules as self-contained chemotherapeutic agents. The macromolecular chemotherapeutic agents readily self-assemble into well-defined nanoparticles and show excellent activity in vitro against multiple cancer cell lines. These cationic polymers function by selectively binding and lysing cancer cell membranes. As a consequence of this mechanism, they exhibit significant potency against drug-resistant cancer cells and cancer stem cells, prevent cancer cell migration, and do not induce resistance onset following multiple treatment passages. Concurrent experiments with the small-molecule chemotherapeutic, doxorubicin, show aggressive resistance onset in cancer cells, a lack of efficacy against drug-resistant cancer cell lines, and a failure to prevent cancer cell migration. Additionally, the polymers showed anticancer efficacy in a hepatocellular carcinoma patient derived xenograft mouse model. Overall, these results demonstrate a new approach to designing anticancer therapeutics utilizing macromolecular compounds.
中文翻译：
用大分子化疗药物解决癌症的耐药性
对化疗药物的耐药性是困扰许多癌症治疗方案的反复出现的问题。为了规避耐药性问题，我们设计了一类新的大分子作为独立的化学治疗剂。大分子化学治疗剂很容易自组装成明确定义的纳米颗粒，并在体外对多种癌细胞系显示出优异的活性。这些阳离子聚合物通过选择性结合和裂解癌细胞膜发挥作用。由于这种机制，它们对耐药癌细胞和癌症干细胞表现出显着的效力，防止癌细胞迁移，并且在多次治疗后不会诱导耐药性发作。与小分子化疗药物多柔比星同时进行的实验显示癌细胞具有侵袭性耐药性，缺乏针对耐药癌细胞系的功效，以及未能阻止癌细胞迁移。此外，该聚合物在源自肝细胞癌患者的异种移植小鼠模型中显示出抗癌功效。总的来说，这些结果证明了一种利用大分子化合物设计抗癌疗法的新方法。
更新日期：2018-03-05
中文翻译：
用大分子化疗药物解决癌症的耐药性
对化疗药物的耐药性是困扰许多癌症治疗方案的反复出现的问题。为了规避耐药性问题，我们设计了一类新的大分子作为独立的化学治疗剂。大分子化学治疗剂很容易自组装成明确定义的纳米颗粒，并在体外对多种癌细胞系显示出优异的活性。这些阳离子聚合物通过选择性结合和裂解癌细胞膜发挥作用。由于这种机制，它们对耐药癌细胞和癌症干细胞表现出显着的效力，防止癌细胞迁移，并且在多次治疗后不会诱导耐药性发作。与小分子化疗药物多柔比星同时进行的实验显示癌细胞具有侵袭性耐药性，缺乏针对耐药癌细胞系的功效，以及未能阻止癌细胞迁移。此外，该聚合物在源自肝细胞癌患者的异种移植小鼠模型中显示出抗癌功效。总的来说，这些结果证明了一种利用大分子化合物设计抗癌疗法的新方法。
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