School of Pharmacy, Faculty of Medical Sciences, Newcastle University, Newcastle upon Tyne NE1 7RU, UK.
Department of Chemical Engineering, Imperial College London, London SW7 2AZ, UK.
Biomolecules. 2024 Feb 22;14(3):264. doi: 10.3390/biom14030264.
Peptides continue to gain significance in the pharmaceutical arena. Since the unveiling of insulin in 1921, the Food and Drug Administration (FDA) has authorised around 100 peptides for various applications. Peptides, although initially derived from endogenous sources, have evolved beyond their natural origins, exhibiting favourable therapeutic effectiveness. Medicinal chemistry has played a pivotal role in synthesising valuable natural peptide analogues, providing synthetic alternatives with therapeutic potential. Furthermore, key chemical modifications have enhanced the stability of peptides and strengthened their interactions with therapeutic targets. For instance, selective modifications have extended their half-life and lessened the frequency of their administration while maintaining the desired therapeutic action. In this review, I analyse the FDA approval of natural peptides, as well as engineered peptides for diabetes treatment, growth-hormone-releasing hormone (GHRH), cholecystokinin (CCK), adrenocorticotropic hormone (ACTH), and α-melanocyte stimulating hormone (α-MSH) peptide analogues. Attention will be paid to the structure, mode of action, developmental journey, FDA authorisation, and the adverse effects of these peptides.
肽在药物领域的重要性不断增加。自 1921 年胰岛素问世以来,美国食品和药物管理局 (FDA) 已批准了大约 100 种用于各种用途的肽。肽虽然最初来源于内源性来源,但已经超越了其自然起源,表现出良好的治疗效果。药物化学在合成有价值的天然肽类似物方面发挥了关键作用,提供了具有治疗潜力的合成替代品。此外,关键的化学修饰提高了肽的稳定性,并增强了它们与治疗靶点的相互作用。例如,选择性修饰延长了它们的半衰期,减少了给药频率,同时保持了所需的治疗作用。在这篇综述中,我分析了 FDA 对用于治疗糖尿病、生长激素释放激素 (GHRH)、胆囊收缩素 (CCK)、促肾上腺皮质激素 (ACTH) 和 α-黑素细胞刺激素 (α-MSH) 肽类似物的天然肽和工程肽的批准情况。将重点关注这些肽的结构、作用模式、开发历程、FDA 批准情况以及它们的不良反应。