Other

Youhei Soma

Stephen B H Kent

Compositions and methods related to ester insulin or derivatives thereof are provided. The compositions include Glu-Threster insulin, in which side chains of Gluand Throf native human insulin or an insulin analogue such as insulin lispro are covalently linked via a single ester bond. The ester insulin is efficiently folded, forming the desired disulfides. The Thr-Gluester bond can be cleaved in vitro or in vivo to give the desired folded insulin with full biological activity. The ester insulin is readily prepared by total chemical synthesis, and amendable to cost-effective, large scale manufacturing. Also provided are pharmaceutical compositions and kits for use in practicing the subject methods. Also provided are methods of using the subject compositions and kits in the treatment of a variety of different disease conditions, particularly glucose metabolic disorders such as diabetes and obesity.

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Tokyo, Japan

Youhei Soma