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

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 FPB...

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Detalles Bibliográficos
Autores principales: Lin, Nai-Pin, Zheng, Nan, Purushottam, Landa, Zhang, Yi Wolf, Chou, Danny Hung-Chieh
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8965884/
https://www.ncbi.nlm.nih.gov/pubmed/35372263
http://dx.doi.org/10.3389/fchem.2022.859133
Descripción
Sumario: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.