Synthesis and Characterization of Phenylboronic Acid-Modified Insulin With Glucose-Dependent Solubility.

Synthesis and Characterization of Phenylboronic Acid-Modified Insulin With Glucose-Dependent Solubility.
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DOI:
10.3389/fchem.2022.859133
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发表时间:
2022
影响因子:
5.5
通讯作者:
Chou DH
Chou DH
中科院分区:
化学3区
文献类型:
--
作者:
Lin NP;Zheng N;Purushottam L;Zhang YW;Chou DH

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葡萄糖反应性胰岛素是一种很有前途的调节血糖水平的方法。我们之前的研究表明,将两个氟苯硼酸(FPBA)残基连接到甘精胰岛素的c端B链上会导致葡萄糖依赖性的溶解度。在此,我们证明了将FPBA从B链移至A链增加了基线溶解度而不影响其效力。此外,增加FPBA基团的数量导致葡萄糖依赖性溶解度增加。
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.
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