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胸腺五肽(TP5)由胸腺生成素活性中心的5个氨基酸组成,作为免疫平衡调节剂广泛应用于临床。TP5在体内稳定性差、易被酶解、半衰期极短,导致其所具有的生物活性在临床应用中难以充分发挥。通过结构修饰研发TP5衍生物,提高产物的体内抗酶解能力及生物利用度,更好地发挥其生物活性,是研发新型高效免疫平衡调节剂的重要方向。文中针对TP5进行结构修饰的研究进展,包括氨基酸序列的调整与取代、端基化学修饰与肽键替换、反转类似物及环肽的设计与合成、TP5偶合物的研制等。
Thymopentin (TP5) is composed of 5 amino acids of thymopoietin active center and is widely used clinically as an immune balance regulator. TP5 in vivo stability is poor, easy to be enzymatic hydrolysis, very short half-life, resulting in its biological activity in clinical applications is difficult to give full play. It is an important direction to research and develop a novel and effective immune balance regulator by developing TP5 derivatives through structural modification to improve the anti-enzymatic activity and bioavailability of the product in vivo and to exert its biological activity better. In this paper, structural modifications of TP5 are reviewed, including the adjustment and substitution of amino acid sequences, the chemical modification of end groups and the substitution of peptide bonds, the design and synthesis of reversed analogs and cyclic peptides, and the development of TP5 conjugates.