Synthesis of carbon-14-labelled peptides

J Labelled Comp Radiopharm. 2019 Sep;62(11):713-717. doi: 10.1002/jlcr.3777. Epub 2019 Aug 1.

Abstract

Carbon-14 (14 C)-labelled active pharmaceutical ingredients (APIs) and investigational medicinal products (IMPs) are required for phase 0/I to phase III mass balance and micro-dosing clinical trials. In some cases, this may involve the synthesis of 14 C-labelled peptides, and the analysis can be performed by accelerated mass spectrometry (AMS). The 14 C-peptide is typically prepared by the solid-phase peptide synthesis (SPPS) approach using custom-made glassware for the key coupling steps. Further modification of the purified 14 C-peptide can then be performed.

Keywords: accelerated mass spectrometry; biomolecules; carbon-14 peptides; solid-phase peptide synthesis.

MeSH terms

  • Biotinylation
  • Carbon Radioisotopes / chemistry*
  • Chemistry Techniques, Synthetic
  • Disulfides / chemistry
  • Isotope Labeling
  • Models, Molecular
  • Peptides / chemical synthesis*
  • Peptides / chemistry*
  • Protein Conformation

Substances

  • Carbon Radioisotopes
  • Disulfides
  • Peptides
  • Carbon-14