Frontiers in Chemistry (Mar 2022)

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

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

DOI
https://doi.org/10.3389/fchem.2022.859133
Journal volume & issue
Vol. 10

Abstract

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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.

Keywords