Skip to main content

N- and Cα-Methylation in Biologically Active Peptides: Synthesis, Structural and Functional Aspects

Buy Article:

$63.00 plus tax (Refund Policy)


Numerous backbone constraints can be used to develop pseudopeptides or pseudomimetics of biologically active peptides. Among those, N- and Cα-methyl amino acids that can be incorporated by solidphase peptide synthesis in a bioactive sequence represent important tools to restrict and ψ angles of peptide backbone.

This review will focus on the chemical syntheses of N- and Cα-methyl amino acids, their effects on peptide conformation and structure, and their role on the peptide stability towards enzymatic degradation and on the biological activities of the resulting analogues.

Keywords: amino acid; backbone constraint; biological activity; methylation; n-methylation; organic synthesis; peptide; structure

Document Type: Review Article


Affiliations: UMR 7613 CNRSUniversite Pierre & Marie Curie, Structure and Function of Bioactive Molecules, Case courrier 182, 4 place Jussieu, 75005 Paris, France.

Publication date: November 1, 2004

More about this publication?
  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

Access Key

Free Content
Free content
New Content
New content
Open Access Content
Open access content
Subscribed Content
Subscribed content
Free Trial Content
Free trial content
Cookie Policy
Cookie Policy
Ingenta Connect website makes use of cookies so as to keep track of data that you have filled in. I am Happy with this Find out more