PDF(Pubmed)
Abstract：
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.
摘要：
肽在制药领域继续获得重要意义。自1921年胰岛素问世以来，美国食品和药物管理局（FDA）已授权约100种肽用于各种应用。肽，虽然最初来自内生来源，已经超越了它们的自然起源，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，提供具有治疗潜力的合成替代品。此外，关键的化学修饰增强了肽的稳定性，并加强了它们与治疗靶标的相互作用。例如,选择性修饰延长了它们的半衰期并减少了它们的给药频率,同时保持了所需的治疗作用。在这次审查中,我分析了FDA批准的天然肽，以及用于糖尿病治疗的工程肽，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-黑素细胞刺激激素(α-MSH)肽类似物。将注意结构，行动模式,发展之旅,FDA授权,以及这些肽的副作用。
