Use of the Npys thiol protection in solid phase peptide synthesis. Application to direct peptide-protein conjugation through cysteine residues

Int J Pept Protein Res. 1989 Aug;34(2):124-8. doi: 10.1111/j.1399-3011.1989.tb01500.x.

Abstract

The protection of the thiol function of cysteine with the 3-nitro-2-pyridylsulfenyl (Npys) group has been successfully applied in the solid phase synthesis of nine peptides. A reexamination of the chemical stability of the protecting group has shown that, while Npys is essentially suitable for standard Boc/benzyl synthesis conditions, it is inadequate for the Fmoc strategy. Its proven stability to "high" HF acidolysis can not be extended to "low-high" conditions without significant thiol deprotection. On the other hand, the Npys group is quite compatible with standard photolytical cleavage conditions. The stability of Npys to HF and its thiol-activating character allow its application in peptide-carrier protein conjugation reactions by specific coupling through cysteine residues in the peptide.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Chromatography, High Pressure Liquid
  • Cysteine*
  • Indicators and Reagents
  • Molecular Sequence Data
  • Nitro Compounds
  • Peptides / chemical synthesis*
  • Pyridines

Substances

  • Indicators and Reagents
  • Nitro Compounds
  • Peptides
  • Pyridines
  • Cysteine