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摘要
HER2受体因具有致瘤性而成为癌症研究中被大量研究的对象。特别指出的是,trastuzumab (Herceptin,一种人源化抗HER2抗体)对乳腺癌的治疗显现出多种临床治疗效果。并且,由于HER2 受体含有accesinvolvement sible胞外结构域,该受体被认为是受体介导的抗癌治疗的理想给药靶点之一。目前,单克隆抗体及其片段,affibody和一些多肽已被用作靶向剂向HER2阳性肿瘤细胞输送多种药物。尤其是对大量多肽分子进行快速可靠的筛选使获得高特异性受体靶向成分成为可能。因此,能否通过制备一个简化合成模型并利用该良好受体靶点模拟物对配体进行可靠筛选,将对选择性HER2靶向多肽分子的开发具有战略价值。在此,我们阐述了HER2靶向抗癌治疗的重要性。我们也就受体的合成和有效模拟作了报告,并揭示它们将成为特异性HER2配体筛选的有用工具。
关键词: 药物传递系统,HER2受体,筛选方法,选择性配体,合成受体片段,癌症靶向治疗
Current Medicinal Chemistry
Title:HER2-Mediated Anticancer Drug Delivery: Strategies to Prepare Targeting Ligands Highly Specific for the Receptor
Volume: 22 Issue: 21
Author(s): Enrica Calce, Luca Monfregola, Michele Saviano and Stefania De Luca
Affiliation:
关键词: 药物传递系统,HER2受体,筛选方法,选择性配体,合成受体片段,癌症靶向治疗
摘要: HER2 receptor, for its involvement in tumorigenesis, has been largely studied as topic in cancer research. In particular, the employment of trastuzumab (Herceptin), a humanized anti-HER2 antibody, showed several clinical benefits in the therapy against the breast cancer. Moreover, for its accessible extracellular domain, this receptor is considered an ideal target to deliver anticancer drugs for the receptormediated anticancer therapy. By now, monoclonal antibody and its fragments, affibody, and some peptides have been employed as targeting agents in order to deliver various drugs to HER2 positive tumor cells. In particular, the ability to perform a fast and reliable screening of a large number of peptide molecules would make possible the selection of highly specific compounds to the receptor target. In this regard, the availability of preparing a simplified synthetic model which is a good mimetic of the receptor target and can be used in a reliable screening method of ligands would be of a strategic importance for the development of selective HER2-targeting peptide molecules. Herein, we illustrate the importance of HER2-targeted anticancer therapies. We also report on a synthetic and effective mimetic of the receptor, which revealed to be a useful tool for the selection of specific HER2 ligands.
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Cite this article as:
Enrica Calce, Luca Monfregola, Michele Saviano and Stefania De Luca , HER2-Mediated Anticancer Drug Delivery: Strategies to Prepare Targeting Ligands Highly Specific for the Receptor, Current Medicinal Chemistry 2015; 22 (21) . https://dx.doi.org/10.2174/0929867322666150521091103
DOI https://dx.doi.org/10.2174/0929867322666150521091103 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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