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Peptides for cancer therapy: A drug-development opportunity and a drug-delivery challenge

机译:用于癌症治疗的肽:药物开发机会和药物输送挑战

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摘要

Therapeutic peptides (TPs) are a class of peptide-based agents capable of eliciting a therapeutic response by modulation of targets within or on the surface of cells. TPs are advantageous because they are amenable to rational design, they have high specificity for their targets and can be made to target almost any protein of interest, including proteins for which we have no small-molecule drugs. Owing to this versatility, TPs have a great potential for cancer therapy in an age of personalized medicine, in which we need novel drugs to target the many novel pathways being discovered as tumor drivers. However, in order to utilize TPs as drugs, many obstacles must be overcome. TPs have short half-lives in systemic circulation, are easily degraded by proteases in plasma and target cells, are often cleared by the reticuloendothelial system and can be immunogenic. This article will discuss ways of overcoming many of these hurdles by utilizing macromolecular peptide delivery systems and tumor-targeting agents.
机译:治疗性肽(TPs)是一类基于肽的药物,能够通过调节细胞表面内或表面上的靶标引发治疗反应。 TPs具有优势,因为它们易于合理设计,对靶标具有高度特异性,并且可以使其靶向几乎所有目标蛋白质,包括我们没有小分子药物的蛋白质。由于这种多功能性,TPs在个性化医学时代具有巨大的癌症治疗潜力,在该时代,我们需要新型药物来靶向被发现为肿瘤驱动因子的许多新型途径。然而,为了将TP用作药物,必须克服许多障碍。 TP在全身循环中的半衰期很短,很容易被血浆和靶细胞中的蛋白酶降解,通常被网状内皮系统清除并具有免疫原性。本文将讨论通过利用大分子肽递送系统和肿瘤靶向剂克服许多这些障碍的方法。

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