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Synthesis and Characterization of an A6-A11 Methylene Thioacetal Human Insulin Analogue with Enhanced Stability.

ABSTRACT: Insulin has been a life-saving drug for millions of people with diabetes. However, several challenges exist which limit therapeutic benefits and reduce patient convenience. One key challenge is the fibrillation propensity, which necessitates refrigeration for storage. To address this limitation, we chemically synthesized and evaluated a methylene thioacetal human insulin analogue (SCS-Ins). The synthesized SCS-Ins showed enhanced serum stability and aggregation resistance while retaining bioactivity compared with native insulin.

SUBMITTER: Zheng N

PROVIDER: S-EPMC7217704 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature

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Synthesis and Characterization of an A6-A11 Methylene Thioacetal Human Insulin Analogue with Enhanced Stability.

Zheng Nan N Karra Prasoona P VandenBerg Michael A MA Kim Jin Hwan JH Webber Matthew J MJ Holland William L WL Chou Danny Hung-Chieh DH

Journal of medicinal chemistry 20191213 24

Insulin has been a life-saving drug for millions of people with diabetes. However, several challenges exist which limit therapeutic benefits and reduce patient convenience. One key challenge is the fibrillation propensity, which necessitates refrigeration for storage. To address this limitation, we chemically synthesized and evaluated a methylene thioacetal human insulin analogue (SCS-Ins). The synthesized SCS-Ins showed enhanced serum stability and aggregation resistance while retaining bioacti ...[more]

PMID: 31804076

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