• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>RSC Advances >Synthesis and biological evaluation of an epidermal growth factor receptor-targeted peptide-conjugated phthalocyanine-based photosensitiser
【24h】

Synthesis and biological evaluation of an epidermal growth factor receptor-targeted peptide-conjugated phthalocyanine-based photosensitiser

机译：表皮生长因子受体靶向肽 - 共轭酞菁光敏蛋白的合成与生物学评价

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

A peptide-conjugated zinc(ii) phthalocyanine containing the epidermal growth factor receptor-targeted heptapeptide QRHKPRE has been prepared. The conjugate labelled as ZnPc-QRH* can selectively bind to the cell membrane of HT29 human colorectal adenocarcinoma cells in 10 min followed by internalisation upon prolonged incubation via receptor-mediated endocytosis, leading to localisation in lysosomes eventually. By manipulating the incubation time, the subcellular localisation of the conjugate can be varied and the cell-death pathways induced upon irradiation can also be altered. It has been found that photosensitisation initiated at the cell membrane and in the lysosomes would trigger cell death mainly through necrosis and apoptosis respectively. Intravenous administration of the conjugate into HT29 tumour-bearing nude mice resulted in higher accumulation in the tumour than in most major organs. The selective binding of this conjugate to tumour has also been demonstrated by comparing the results with those of the analogue with a scrambled peptide sequence (EPRQRHK). The overall results indicate that ZnPc-QRH* is a promising EGFR-targeted photosensitiser for photodynamic therapy.
机译：制备了含有表皮生长因子受体靶向七肽QRHKPRE的肽 - 共轭锌（II）酞菁。标记为ZnPC-QRH *的缀合物可以在10分钟内选择性地与HT29人结肠腺癌细胞的细胞膜结合，然后通过受体介导的内吞作用延长孵育后的内化，从而最终导致溶酶体局部化。通过操纵孵育时间，可以改变缀合物的亚细胞定位，并且在照射时也可以改变诱导的细胞死亡途径。已经发现，在细胞膜和溶酶体中发起的光敏性会分别通过坏死和细胞凋亡引发细胞死亡。静脉内给予缀合物进入HT29肿瘤裸鼠导致肿瘤中的较高积累而不是大多数主要器官。通过将结果与用炒肽序列（EPRQRHK）的结果进行比较，还通过将结果与类似物的结果进行比较来证明该缀合物与肿瘤的选择性结合。总体结果表明，ZnPC-QRH *是用于光动力治疗的有前途的EGFR靶向光囊炎。

著录项

  • 来源
    《RSC Advances》 |2019年第36期|共11页
  • 作者

    Xue Evelyn Y.; Wong Roy C. H.; Wong Clarence T. T.; Fong Wing-Ping; Ng Dennis K. P.;

  • 作者单位

    Chinese Univ Hong Kong Dept Chem Shatin Hong Kong Peoples R China;

    Chinese Univ Hong Kong Dept Chem Shatin Hong Kong Peoples R China;

    Chinese Univ Hong Kong Dept Chem Shatin Hong Kong Peoples R China;

    Chinese Univ Hong Kong Sch Life Sci Shatin Hong Kong Peoples R China;

    Chinese Univ Hong Kong Dept Chem Shatin Hong Kong Peoples R China;

  • 收录信息
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 化学;
  • 关键词

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号