Costa Lia, Sousa Emília, Fernandes Carla
Laboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal.
Interdisciplinary Centre of Marine and Environmental Research (CIIMAR), Edifício do Terminal de Cruzeiros do Porto de Leixões, Av. General Norton de Matos s/n, 4050-208 Matosinhos, Portugal.
Pharmaceuticals (Basel). 2023 Jul 12;16(7):996. doi: 10.3390/ph16070996.
Cyclic peptides are molecules that are already used as drugs in therapies approved for various pharmacological activities, for example, as antibiotics, antifungals, anticancer, and immunosuppressants. Interest in these molecules has been growing due to the improved pharmacokinetic and pharmacodynamic properties of the cyclic structure over linear peptides and by the evolution of chemical synthesis, computational, and in vitro methods. To date, 53 cyclic peptides have been approved by different regulatory authorities, and many others are in clinical trials for a wide diversity of conditions. In this review, the potential of cyclic peptides is presented, and general aspects of their synthesis and development are discussed. Furthermore, an overview of already approved cyclic peptides is also given, and the cyclic peptides in clinical trials are summarized.
环肽是一类已被用作药物的分子，用于多种经批准的具有不同药理活性的治疗，例如作为抗生素、抗真菌剂、抗癌药物和免疫抑制剂。由于环肽结构相对于线性肽具有更好的药代动力学和药效学性质，以及化学合成、计算和体外方法的发展，人们对这些分子的兴趣一直在增加。迄今为止，已有53种环肽被不同监管机构批准，还有许多其他环肽正在针对多种病症进行临床试验。在本综述中，介绍了环肽的潜力，并讨论了其合成和开发的一般方面。此外，还给出了已批准环肽的概述，并总结了正在进行临床试验的环肽。
