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

具有葡萄糖依赖性溶解度的苯硼酸修饰胰岛素的合成与表征

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作者:Nai-Pin Lin, Nan Zheng, Landa Purushottam, Yi Wolf Zhang, Danny Hung-Chieh Chou

Abstract

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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