具有葡萄糖依赖性溶解性的苯基硼酸修饰胰岛素的合成与表征
Synthesis and Characterization of Phenylboronic Acid-Modified Insulin With Glucose-Dependent Solubility.
作者信息
Lin Nai-Pin, Zheng Nan, Purushottam Landa, Zhang Yi Wolf, Chou Danny Hung-Chieh
机构信息
Department of Pediatrics, Division of Diabetes and Endocrinology, Stanford University, Stanford, CA, United States.
Department of Biochemistry, University of Utah, Salt Lake City, UT, United States.
出版信息
Front Chem. 2022 Mar 16;10:859133. doi: 10.3389/fchem.2022.859133. eCollection 2022.
Glucose-responsive insulin represents a promising approach to regulate blood glucose levels. We previously showed that attaching two fluorophenylboronic acid (FPBA) residues to the C-terminal B chain of insulin glargine led to glucose-dependent solubility. Herein, we demonstrated that relocating FPBA from B chain to A chain increased the baseline solubility without affecting its potency. Furthermore, increasing the number of FPBA groups led to increased glucose-dependent solubility.
葡萄糖响应性胰岛素是调节血糖水平的一种有前景的方法。我们之前表明，将两个氟代苯硼酸（FPBA）残基连接到甘精胰岛素的C末端B链上会导致葡萄糖依赖性溶解度。在此，我们证明将FPBA从B链重新定位到A链可提高基线溶解度而不影响其效力。此外，增加FPBA基团的数量会导致葡萄糖依赖性溶解度增加。
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