ArticleACS chemical biology2018
Chemically Precise Glycoengineering Improves Human Insulin.
Article in ACS chemical biology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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The trial behind it
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Who cites it
17 citing papers in PubMed, 43 citations in OpenAlex.
- Re-engineering insulin for oral delivery: structural modifications, advanced formulation strategies, and future directions.Drug delivery · 2026Review
- Site-Specific Abiraterone Protein-Drug Conjugates via Hedgehog Autoprocessing.ACS applied materials & interfaces · 2026Article
- Deciphering the significant impact of natural glycosylation on human insulin.Acta pharmaceutica Sinica. B · 2025Article
- Rapid synthesis of glycosylated insulins by flow-based peptide synthesis.Chemical science · 2025Article
- Glycosylation shapes the efficacy and safety of diverse protein, gene and cell therapies.Biotechnology advances · 2023Review
- Article
- Current advances and future prospects in production of recombinant insulin and other proteins to treat diabetes mellitus.Biotechnology letters · 2022Review
- Identifying signatures of proteolytic stability and monomeric propensity in O-glycosylated insulin using molecular simulation.Journal of computer-aided molecular design · 2022Article
- Strategies for Glycoengineering Therapeutic Proteins.Frontiers in chemistry · 2022Review
- Facile synthesis of insulin fusion derivatives through sortase A ligation.Acta pharmaceutica Sinica. B · 2021Article
- Exploring a combined Escherichia coli-based glycosylation and in vitro transglycosylation approach for expression of glycosylated interferon alpha.Bioorganic & medicinal chemistry · 2021Article
- Improving the Pharmacodynamics and In Vivo Activity of ENPP1-Fc Through Protein and Glycosylation Engineering.Clinical and translational science · 2021Article
- Chemical Glycosylation and Its Application to Glucose Homeostasis-Regulating Peptides.Frontiers in chemistry · 2021Review
- Protein Glycoengineering: An Approach for Improving Protein Properties.Frontiers in chemistry · 2020Review
- Synthesis and Characterization of an A6-A11 Methylene Thioacetal Human Insulin Analogue with Enhanced Stability.Journal of medicinal chemistry · 2019Article
- Chemical biology of glycoproteins: From chemical synthesis to biological impact.Methods in enzymology · 2019Article
- Article
Corrections and comments
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Authors and funding
15 authors at 2 institutions in 2 countries.
Funding
Abstract
Diabetes is a leading cause of death worldwide and results in over 3 million annual deaths. While insulin manages the disease well, many patients fail to comply with injection schedules, and despite significant investment, a more convenient oral formulation of insulin is still unavailable. Studies suggest that glycosylation may stabilize peptides for oral delivery, but the demanding production of homogeneously glycosylated peptides has hampered transition into the clinic. We report here the first total synthesis of homogeneously glycosylated insulin. After characterizing a series of insulin glycoforms with systematically varied O-glycosylation sites and structures, we demonstrate that O-mannosylation of insulin B-chain Thr27 reduces the peptide's susceptibility to proteases and self-association, both critical properties for oral dosing, while maintaining full activity. This work illustrates the promise of glycosylation as a general mechanism for regulating peptide activity and expanding its therapeutic use.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.