39
views
0
recommends
+1 Recommend
0 collections
    0
    shares
      • Record: found
      • Abstract: found
      • Article: not found

      Advances in Fmoc solid‐phase peptide synthesis

      review-article

      Read this article at

      ScienceOpenPublisherPMC
      Bookmark
          There is no author summary for this article yet. Authors can add summaries to their articles on ScienceOpen to make them more accessible to a non-specialist audience.

          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. Copyright © 2015 European Peptide Society and John Wiley & Sons, Ltd.

          Related collections

          Most cited references125

          • Record: found
          • Abstract: found
          • Article: not found

          The diverse functions of histone lysine methylation.

          Covalent modifications of histone tails have fundamental roles in chromatin structure and function. One such modification, lysine methylation, has important functions in many biological processes that include heterochromatin formation, X-chromosome inactivation and transcriptional regulation. Here, we summarize recent advances in our understanding of how lysine methylation functions in these diverse biological processes, and raise questions that need to be addressed in the future.
            Bookmark
            • Record: found
            • Abstract: found
            • Article: not found

            Future directions for peptide therapeutics development.

            The notable expansion of peptide therapeutics development in the late 1990s and the 2000s led to an unprecedented number of marketing approvals in 2012 and has provided a robust pipeline that should deliver numerous approvals during the remainder of the 2010s. To document the current status of the pipeline, we collected data for peptide therapeutics in clinical studies and regulatory review, as well as those recently approved. In this Foundation review, we provide an overview of the pipeline, including therapeutic area and molecular targets, with a focus on glucagon-like peptide 1 receptor agonists. Areas for potential expansion, for example constrained peptides and peptide-drug conjugates, are profiled. Copyright © 2013 Elsevier Ltd. All rights reserved.
              Bookmark
              • Record: found
              • Abstract: found
              • Article: not found

              Solid phase peptide synthesis utilizing 9-fluorenylmethoxycarbonyl amino acids.

              9-Fluorenylmethoxycarbonyl (Fmoc) amino acids were first used for solid phase peptide synthesis a little more than a decade ago. Since that time, Fmoc solid phase peptide synthesis methodology has been greatly enhanced by the introduction of a variety of solid supports, linkages, and side chain protecting groups, as well as by increased understanding of solvation conditions. These advances have led to many impressive syntheses, such as those of biologically active and isotopically labeled peptides and small proteins. The great variety of conditions under which Fmoc solid phase peptide synthesis may be carried out represents a truly "orthogonal" scheme, and thus offers many unique opportunities for bioorganic chemistry.
                Bookmark

                Author and article information

                Journal
                J Pept Sci
                J. Pept. Sci
                10.1002/(ISSN)1099-1387
                PSC
                Journal of Peptide Science
                John Wiley and Sons Inc. (Hoboken )
                1075-2617
                1099-1387
                20 January 2016
                January 2016
                : 22
                : 1 ( doiID: 10.1002/psc.v22.1 )
                : 4-27
                Affiliations
                [ 1 ]Novabiochem, Merck & Cie Im Laternenacker 5 8200 SchaffhausenSwitzerland
                [ 2 ]Novabiochem, Merck Chemicals Ltd Padge Road Beeston NG9 2JRUK
                [ 3 ]The Francis Crick Institute 215 Euston Road London NW1 2BEUK
                Author notes
                [*] [* ]Correspondence to: John Offer, The Francis Crick Institute, 215 Euston road, London, NW1 2BE, UK. E‐mail: john.offer@ 123456crick.ac.uk
                Article
                PSC2836 PSC-15-0129
                10.1002/psc.2836
                4745034
                26785684
                739785b3-b5e7-4a79-baf6-f989ae6a7c16
                Copyright © 2015 European Peptide Society and John Wiley & Sons, Ltd.

                Open access.

                History
                : 05 October 2015
                : 20 October 2015
                Page count
                Pages: 24
                Categories
                Review
                Reviews
                Custom metadata
                2.0
                psc2836
                January 2016
                Converter:WILEY_ML3GV2_TO_NLMPMC version:4.7.6 mode:remove_FC converted:05.02.2016

                solid‐phase peptide synthesis,fmoc/tbu,aspartimide,peptide thioester,post‐translational modification,protecting group,racemisation

                Comments

                Comment on this article