title: Advances in Fmoc solid-phase peptide synthesis.
abstract: Today, Fmoc SPPS is the method of choice for peptide synthesis. Very-high-quality Fmoc building blocks are available at low cost because of the economies of scale arising from current multiton production of therapeutic peptides by Fmoc SPPS. Many modified derivatives are commercially available as Fmoc building blocks, making synthetic access to a broad range of peptide derivatives straightforward. The number of synthetic peptides entering clinical trials has grown continuously over the last decade, and recent advances in the Fmoc SPPS technology are a response to the growing demand from medicinal chemistry and pharmacology. Improvements are being continually reported for peptide quality, synthesis time and novel synthetic targets. Topical peptide research has contributed to a continuous improvement and expansion of Fmoc SPPS applications.
authors.affiliation: Novabiochem, Merck & Cie, Im Laternenacker 5, 8200, Schaffhausen, Switzerland.
authors.forename: Raymond
authors.initials: R
authors.lastname: Behrendt
authors.affiliation: Novabiochem, Merck Chemicals Ltd, Padge Road, Beeston, NG9 2JR, UK.
authors.forename: Peter
authors.initials: P
authors.lastname: White
authors.affiliation: The Francis Crick Institute, 215 Euston Road, London, NW1 2BE, UK.
authors.forename: John
authors.initials: J
authors.lastname: Offer
mesh_terms: D000596:Amino Acids / Q000737:chemistry*; D001224:Aspartic Acid / Q000031:analogs & derivatives / Q000737:chemistry; D002460:Cell Line; D004847:Epithelial Cells / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D005449:Fluorenes / Q000737:chemistry*; D006031:Glycosylation; D006801:Humans; D008745:Methylation; D010455:Peptides / Q000138:chemical synthesis* / Q000494:pharmacology; D010766:Phosphorylation; D017368:Protein Prenylation; D011499:Protein Processing, Post-Translational; D060327:Solid-Phase Synthesis Techniques / Q000379:methods*
chemical_list: D000596:Amino Acids; D005449:Fluorenes; D010455:Peptides; D001224:Aspartic Acid; C075871:aspartimide
keywords: Fmoc/tBu; aspartimide; peptide thioester; post-translational modification; protecting group; racemisation; solid-phase peptide synthesis