自然启发和医学相关的短肽

M. G. Ciulla, M. Civera, S. Sattin, Kamal Kumar
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引用次数: 1

摘要

多肽是自然药物的重要组成部分,作为天然生物信使,在多种信号通路中发挥着重要作用。虽然大自然已经掌握了大肽和短肽的创造、应用和破坏的循环,以造福宿主生物,但有机和药物化学家凭借他们的能力和小步,在肽合成领域取得了重大进展,并将其开发为治疗方法。与它们的大对应物,即蛋白质相比,短肽具有几个优点,从易于合成到其物理化学性质。然而,治疗肽在体内应用的真正挑战是克服其低血浆利用率和快速酶降解。本文简要介绍了具有重要医学意义的短肽的相关领域以及将这些短肽转化为治疗药物的最新进展。本文还介绍了用于克服肽分子固有局限性的重要努力和策略,从而促进其在临床阶段向批准药物的进展。
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Nature-inspired and medicinally relevant short peptides
Peptides constitute an important component of Nature’s pharmacy and they play a significant role in several signaling pathways acting as natural biological messengers. While nature has mastered the cycle of creation, application, and destruction of large and short peptides to the benefit of the host organism, organic and medicinal chemists have in their capacity and small steps, made big developments in the field of peptide synthesis as well as in developing them as therapeutics. In comparison to their big counterparts, i.e. proteins, short peptides encompass several advantages, from the ease of synthesis to their physico-chemical properties. However, the real challenge for in vivo application of therapeutic peptides is to overcome their low plasma availability and their fast enzymatic degradation. This review briefly covers the relevant areas of medicinally important short peptides and the recent developments made to turn these peptides into therapeutics. Also presented in this article are important efforts and strategies used to overcome some of the inherent limitations of peptidic molecules and thereby facilitate their progression in the clinical phases towards approved drugs.
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