Deigin Vladislav I, Poluektova Elena A, Beniashvili Allan G, Kozin Sergey A, Poluektov Yuri M
Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, 142290 Moscow, Russia.
Department of Propaedeutics of Internal Diseases, Gastroenterology and Hepatology, I.M. Sechenov First Moscow State Medical University (Sechenov University), 119991 Moscow, Russia.
Pharmaceutics. 2022 Mar 27;14(4):716. doi: 10.3390/pharmaceutics14040716.
Peptides are low-molecular-weight substances that participate in numerous important physiological functions, such as human growth and development, stress, regulation of the emotional state, sexual behavior, and immune responses. Their mechanisms of action are based on receptor-ligand interactions, which result in highly selective effects. These properties and low toxicity enable them to be considered potent drugs. Peptide preparations became possible at the beginning of the 20th century after a method was developed for selectively synthesizing peptides; however, after synthesis of the first peptide drugs, several issues related to increasing the stability, bioavailability, half-life, and ability to move across cell membranes remain unresolved. Here, we briefly review the history of peptide production and development in the biochemical industry and outline potential areas of peptide biopharmaceutical applications and modern approaches for creating pharmaceuticals based on synthetic peptides and their analogs. We also focus on original peptide drugs and the approaches used for their development by the Russian Federation.
肽是参与众多重要生理功能的低分子量物质,如人类生长发育、应激反应、情绪状态调节、性行为和免疫反应等。它们的作用机制基于受体 - 配体相互作用,从而产生高度选择性的效应。这些特性和低毒性使它们被视为有效的药物。在20世纪初开发出一种选择性合成肽的方法后,肽制剂成为可能;然而,在首批肽类药物合成后,与提高稳定性、生物利用度、半衰期以及跨细胞膜转运能力相关的几个问题仍未得到解决。在此,我们简要回顾生化行业中肽生产和开发的历史,并概述肽生物制药应用的潜在领域以及基于合成肽及其类似物制造药物的现代方法。我们还关注原创肽类药物以及俄罗斯联邦用于其开发的方法。