Structure and Activity of N-Methylated Peptides

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Peptides typically display high potency and target selectivity, making them valuable leads in the development of new therapeutics. Indeed, many peptides have made the transition to clinical use, including cyclosporine (cyclosporin A) [1, 2], gonadotropin-releasing hormone (also known as luteinizing-hormone releasing hormone) agonists and antagonists [3, 4], somatostatin analogs [3, 4], exenatide [5], ziconotide [6], andglatiramer acetate [7], to name just a few. Nonetheless, converting lead peptides to drugs represents a considerable challenge. Many peptides lack oral bioavailability as a consequence of their susceptibility to proteolysis in the gut, inefficient transport across the intestinal wall, proteolytic degradation in the bloodstream, and rapid clearance by the kidney.
Original languageEnglish
Title of host publicationAmino Acids, Peptides and Proteins in Organic Chemistry
Subtitle of host publicationAnalysis and Function of Amino Acids and Peptides
EditorsAndrew B. Hughes
Place of PublicationWeinheim Germany
PublisherWiley-VCH Verlag GmbH & Co. KGaA
Number of pages12
ISBN (Electronic)9783527631858
ISBN (Print)9783527321049
Publication statusPublished - 28 Nov 2011


  • Conformation
  • Energy calculation
  • N-methylation
  • Nuclear magnetic resonance
  • Peptide
  • X-ray crystallography

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