N-Methylation of Peptides: A Key Chemical Strategy for Making Oral Peptide Drugs
N-methylation of peptide bonds dramatically improves oral bioavailability, proteolytic stability, and membrane permeability of peptides — the chemical modification strategy behind several successful oral peptide drugs including cyclosporine.
Quick Facts
What This Study Found
N-methylation of peptide backbone amides improves oral bioavailability, proteolytic stability, membrane permeability, and conformational rigidity — the key chemical modification enabling oral peptide drugs, validated by cyclosporine and being applied to new therapeutic peptides.
Key Numbers
How They Did This
review study.
Why This Research Matters
Relevant for peptide-design, bioavailability, cyclic-peptides.
The Bigger Picture
Advances peptide research.
What This Study Doesn't Tell Us
See abstract.
Questions This Raises
- ?Further research needed.
- ?Clinical translation to evaluate.
Trust & Context
- Key Stat:
- Key finding N-methylation of peptide backbone amides improves oral bioavailability, proteolytic stability, membrane permeability, and conformational rigidity — th
- Evidence Grade:
- moderate evidence.
- Study Age:
- Published in 2008.
- Original Title:
- N-methylation of peptides: a new perspective in medicinal chemistry.
- Published In:
- Accounts of chemical research, 41(10), 1331-42 (2008)
- Authors:
- Chatterjee, Jayanta(2), Gilon, Chaim(4), Hoffman, Amnon(5), Kessler, Horst
- Database ID:
- RPEP-01320
Evidence Hierarchy
Summarizes existing research on a topic.
What do these levels mean? →Frequently Asked Questions
What was studied?
N-Methylation of Peptides: A Key Chemical Strategy for Making Oral Peptide Drugs
What was found?
N-methylation of peptide bonds dramatically improves oral bioavailability, proteolytic stability, and membrane permeability of peptides — the chemical modification strategy behind several successful oral peptide drugs including cyclosporine.
Read More on RethinkPeptides
Cite This Study
https://rethinkpeptides.com/research/RPEP-01320APA
Chatterjee, Jayanta; Gilon, Chaim; Hoffman, Amnon; Kessler, Horst. (2008). N-methylation of peptides: a new perspective in medicinal chemistry.. Accounts of chemical research, 41(10), 1331-42. https://doi.org/10.1021/ar8000603
MLA
Chatterjee, Jayanta, et al. "N-methylation of peptides: a new perspective in medicinal chemistry.." Accounts of chemical research, 2008. https://doi.org/10.1021/ar8000603
RethinkPeptides
RethinkPeptides Research Database. "N-methylation of peptides: a new perspective in medicinal ch..." RPEP-01320. Retrieved from https://rethinkpeptides.com/research/chatterjee-2008-nmethylation-of-peptides-a
Access the Original Study
Study data sourced from PubMed, a service of the U.S. National Library of Medicine, National Institutes of Health.
This study breakdown was produced by the RethinkPeptides research team. We analyze and report published research findings without making health recommendations. All interpretations are based solely on the published abstract and study data.