• 肽瑞禾

用肽藥物偶聯物靶向癌細胞上的肽結合受體

更新日期:6月 2


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引用 | Wiley Online Library報導


Targeting of peptide‐binding receptors on cancer cells with peptide‐drug conjugates

Abstract 專門解決癌細胞上的細胞表面分子有助於靶向癌症治療,從而提供選擇性破壞惡性細胞的潛力,同時保留健康組織。因此,大大減少了腫瘤患者的不良副作用。肽結合受體經常在癌細胞上過度表達,因此是選擇性腫瘤治療的有希望的靶點。在這篇綜述中,總結了用於抗癌藥物遞送的肽結合受體,重點是肽配體作為遞送劑。第一部分介紹了一些研究最多的肽結合受體,以及生長素釋放肽受體和 Y 1受體被引入作為癌症治療的最新靶點。

此外,概述了用於靶向癌細胞的受體的非肽小分子。在第二部分中,描述了用於在癌症治療中遞送治療性貨物的肽綴合物。指定了受體靶向肽的基本特性,並介紹了經典肽-藥物偶聯物與毒劑、用於放射性核素治療的放射性標記肽和用於硼中子捕獲治療的硼化肽領域的最新進展。 Specifically addressing cell surface molecules on cancer cells facilitates targeted cancer therapies that offer the potential to selectively destroy malignant cells, while sparing healthy tissue. Thus, undesired side-effects in tumor patients are highly reduced. Peptide-binding receptors are frequently overexpressed on cancer cells and therefore promising targets for selective tumor therapy. In this review, peptide-binding receptors for anti-cancer drug delivery are summarized with a focus on peptide ligands as delivery agents. In the first part, some of the most studied peptide-binding receptors are presented, and the ghrelin receptor and the Y1 receptor are introduced as more recent targets for cancer therapy. Furthermore, nonpeptidic small molecules for receptor targeting on cancer cells are outlined. In the second part, peptide conjugates for the delivery of therapeutic cargos in cancer therapy are described. The essential properties of receptor-targeting peptides are specified, and recent developments in the fields of classical peptide-drug conjugates with toxic agents, radiolabeled peptides for radionuclide therapy, and boronated peptides for boron neutron capture therapy are presented.


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