Department of Chemistry, Laboratory of Organic Chemistry, University of Ioannina, Ioannina, Greece.
Methods Mol Biol. 2021;2207:327-338. doi: 10.1007/978-1-0716-0920-0_23.
Cancer constitutes a major threat to humanity, while its incidence and mortality rates are increasing rapidly worldwide. To tackle cancer, numerous strategies have been exploited, including the development of peptide-drug conjugates (PDCs), which are considered an appealing approach to selectively populate malignant tumors with toxic substances. The general architecture of a PDC usually includes three parts: the tumor-targeting peptide, the cytotoxic drug, and the biodegradable linker. Due to the fact that peptides possess fast renal clearance, affecting the bioavailability of the PDC, a nanodrug formation concept can be exploited to ameliorate this pitfall. Herein, we present methodologies to develop PDCs, along with certain basic principles governing such constructs. In addition, we highlight possible problems that may appear during the synthesis of PDCs, as also solutions to overcome them.
癌症对人类构成重大威胁，而其发病率和死亡率在全球范围内迅速上升。为了应对癌症，人们已经开发了许多策略，包括开发肽药物偶联物（PDCs），这被认为是一种有吸引力的方法，可以选择性地将有毒物质输送到恶性肿瘤中。PDC 的一般结构通常包括三个部分：肿瘤靶向肽、细胞毒性药物和可生物降解的连接子。由于肽具有快速的肾脏清除作用，影响 PDC 的生物利用度，因此可以利用纳米药物形成的概念来改善这一缺陷。本文介绍了开发 PDC 的方法，以及这些结构的一些基本原则。此外，我们还强调了在 PDC 合成过程中可能出现的问题，以及解决这些问题的方法。
