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酶指导的自组装(EISA)有助于疏水性肽的自组装和水凝胶形成。

Enzyme-instructed self-assembly (EISA) assists the self-assembly and hydrogelation of hydrophobic peptides.

机构信息

Key Laboratory of Bioactive Materials, Ministry of Education, State Key Laboratory of Medicinal Chemical Biology, College of Life Sciences, Nankai University, Tianjin 300071, P. R. China.

Key Laboratory of Bioactive Materials, Ministry of Education, College of Life Sciences, Nankai University, Tianjin 300071, P. R. China.

出版信息

J Mater Chem B. 2022 May 4;10(17):3242-3247. doi: 10.1039/d2tb00182a.

DOI:10.1039/d2tb00182a
PMID:35437539
Abstract

Enzyme-instructed self-assembly (EISA) has several advantages in the preparation of supramolecular self-assembly materials for biomedical applications. In this study, we demonstrated that the enzyme-instructed self-assembly (EISA) strategy could assist the self-assembly and hydrogelation of two hydrophobic and bioactive peptides, tyroservatide (YSV) and laminin pentapeptide (YIGSR). We first synthesized the peptide derivatives of Nap-GFFYSV (peptide 1) and Nap-GFFYIGSR (peptide 2) and found that both peptides could not self-assemble into hydrogels due to their poor solubility. We therefore designed the phosphorylated precursors of the two hydrophobic peptides, Nap-GFFpYSV (precursor 1) and Nap-GFFpYIGSR (precursor 2), respectively, which had good solubility and can be dephosphorylated by alkaline phosphatase (ALP) to form supramolecular hydrogels. In addition, we found that the EISA could also occur on the surface of cells that overexpress ALP. The EISA strategy was a powerful method to generate hydrogels of hydrophobic compounds. We envision the big promise of the strategy in the preparation of biomaterials and nanomaterials of hydrophobic bioactive molecules.

摘要

酶指导的自组装(EISA)在制备用于生物医学应用的超分子自组装材料方面具有多个优势。在本研究中,我们证明了酶指导的自组装(EISA)策略可以辅助两种疏水性和生物活性肽,即酪丝亮肽(YSV)和层粘连蛋白五肽(YIGSR)的自组装和水凝胶化。我们首先合成了 Nap-GFFYSV(肽 1)和 Nap-GFFYIGSR(肽 2)的肽衍生物,发现由于它们的溶解度较差,这两种肽都不能自组装成水凝胶。因此,我们分别设计了两种疏水性肽的磷酸化前体,即 Nap-GFFpYSV(前体 1)和 Nap-GFFpYIGSR(前体 2),它们具有良好的溶解度,并可以通过碱性磷酸酶(ALP)去磷酸化形成超分子水凝胶。此外,我们发现 EISA 也可以在过表达 ALP 的细胞表面发生。EISA 策略是生成疏水性化合物水凝胶的有力方法。我们设想该策略在制备疏水性生物活性分子的生物材料和纳米材料方面具有广阔的前景。

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