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Double Sequential Encrypted Targeting Sequence: A New Concept for Bone Cancer Treatment

机译：双顺序加密靶向序列：骨癌治疗的新概念

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摘要

The selective transportation of therapeutic agents to tumoral cells is usually achieved by their conjugation with targeting moieties able to recognize these cells. Unfortunately, simple and static targeting systems usually show a lack in selectivity. Herein, a double sequential encrypted targeting system is proposed as a stimuli-responsive targeting analogue for selectivity enhancement. The system is able to recognize diseased bone tissue in the first place, and once there, a hidden secondary targeting group is activated by the presence of an enzyme overproduced in the malignant tissue (cathepsin K), thereby triggering the recognition of diseased cells. Transporting the cell targeting agent in a hidden conformation that contains a high selective tissular primary targeting, could avoid not only its binding to similar cell receptors but also the apparition of the binding-site barrier effect, which can enhance the penetration of the therapeutic agent within the affected zone. This strategy could be applied not only to conjugate drugs but also to drug-loaded nanocarriers to improve the efficiency for bone cancer treatments.
机译：通过它们的缀合物与能够识别这些细胞的靶向部分的缀合通常可以实现治疗剂对肿瘤细胞的选择性运输。不幸的是，简单且静态的靶向系统通常缺乏选择性。这里，提出了一种双顺序加密的靶向系统作为用于选择性增强的刺激响应靶向模拟。该系统能够首先识别患病的骨组织，并且在那里，通过在恶性组织（组织蛋白蛋白k）中过度引发的酶存在，激活隐藏的二次靶向组，从而引发对患病细胞的识别。将细胞靶向剂在含有高选择性组织初级靶向的隐藏构象中，可以避免其与类似细胞受体的结合，而且可以避免结合位点阻挡效果的幻影，这可以增强治疗剂内的渗透受影响的区域。该策略不仅可以应用于缀合物药物，还可以应用于含药的纳米载体，以提高骨癌治疗的效率。

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  • 来源
    《Chemistry: A European journal》 |2017年第30期|共6页
  • 作者

    Gonzalo Villaverde; Valentina Nairi; Alejandro Baeza; María Vallet-Regí;

  • 作者单位

    Depto. Química Inorgánica y Bioinorgánica Facultad de Farmacia Universidad Complutense de Madrid. Plaza Ramon y CajaLs/n. Instituto de Investigacijn Sanitaria Hospital 12 de Octubre i+12 ? Centro de Investigacijn Biomédica en Red de Bioingeniería Biomat;

    Depto. Química Inorgánica y Bioinorgánica Facultad de Farmacia Universidad Complutense de Madrid. Plaza Ramon y CajaLs/n. Instituto de Investigacijn Sanitaria Hospital 12 de Octubre i+12 ? Centro de Investigacijn Biomédica en Red de Bioingeniería Biomat;

    Depto. Química Inorgánica y Bioinorgánica Facultad de Farmacia Universidad Complutense de Madrid. Plaza Ramon y CajaLs/n. Instituto de Investigacijn Sanitaria Hospital 12 de Octubre i+12 ? Centro de Investigacijn Biomédica en Red de Bioingeniería Biomat;

    Depto. Química Inorgánica y Bioinorgánica Facultad de Farmacia Universidad Complutense de Madrid. Plaza Ramon y CajaLs/n. Instituto de Investigacijn Sanitaria Hospital 12 de Octubre i+12 ? Centro de Investigacijn Biomédica en Red de Bioingeniería Biomat;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 应用化学;
  • 关键词

    cancer; drug delivery; dual targeting; encrypted peptide; stimuli-responsive targeting;

    机译：癌症;药物递送;双重靶向;加密肽;刺激响应靶向;

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