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Effects of Glycosylation and d-Amino Acid Substitution on the Antitumor and Antibacterial Activities of Bee Venom Peptide HYL.
Bioconjugate Chemistry ( IF 4.7 ) Pub Date : 2020-08-10 , DOI: 10.1021/acs.bioconjchem.0c00355
Ming-Hao Wu 1, 2 , Su Ai 1, 2 , Qing Chen 1, 2 , Xiang-Yan Chen 1, 2 , Hong-Jin Li 1 , Yu-Lei Li 1 , Xia Zhao 1, 2
Affiliation  

Glycosylation is a promising strategy for modulating the physicochemical properties of peptides. However, the influence of glycosylation on the biological activities of peptides remains unknown. Here, we chose the bee venom peptide HYL as a model peptide and 12 different monosaccharides as model sugars to study the effects of glycosylation site, number, and monosaccharide structure on the biochemical properties, activities, and cellular selectivities of HYL derivatives. Some analogues of HYL showed improvement not only in cell selectivity and proteolytic stability but also in antitumor and antimicrobial activity. Moreover, we found that the helicity of glycopeptides can affect its antitumor activity and proteolytic stability, and the α-linked d-monosaccharides can effectively improve the antitumor activity of HYL. Therefore, it is possible to design peptides with improved properties by varying the number, structure, and position of monosaccharides. What’s more, the glycopeptides HYL-31 and HYL-33 show a promising prospect for antitumor and antimicrobial drugs development, respectively. In addition, we found that the d-lysine substitution strategy can significantly improve the proteolytic stability of HYL. Our new approach provides a reference or guidance for the research of novel antitumor and antimicrobial peptide drugs.

中文翻译:

糖基化和d-氨基酸取代对蜂毒肽HYL的抗肿瘤和抗菌活性的影响。

糖基化是调节肽的理化性质的有前途的策略。然而,糖基化对肽的生物学活性的影响仍然未知。在这里,我们选择蜂毒肽HYL作为模型肽,并选择12种不同的单糖作为模型糖,以研究糖基化位点,数目和单糖结构对HYL衍生物的生化特性,活性和细胞选择性的影响。HYL的某些类似物不仅显示出细胞选择性和蛋白水解稳定性的改善,而且还显示出抗肿瘤和抗菌活性的改善。此外,我们发现糖肽的螺旋结构会影响其抗肿瘤活性和蛋白水解稳定性,以及α-连接的d-单糖可有效提高HYL的抗肿瘤活性。因此,可以通过改变单糖的数目,结构和位置来设计具有改善的性质的肽。此外,糖肽HYL-31和HYL-33分别显示出抗肿瘤和抗菌药物开发的前景。另外,我们发现d-赖氨酸取代策略可以显着提高HYL的蛋白水解稳定性。我们的新方法为新型抗肿瘤和抗菌肽药物的研究提供了参考或指导。
更新日期:2020-08-10
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