C-terminal modification peptide analysis method

Abstract

The invention provides a C-terminal modification peptide analysis method. The method is characterized by including steps: 1) coupling an amino at one end of a diamino compound to solid-phase synthesized resin; 2) adopting an Fmoc solid-phase peptide synthesis strategy to sequentially couple amino acids to an amino at the other end of the diamino compound so as to obtain fully-protected polypeptide resin; 3) splitting fully-protected polypeptides from resin to obtain the fully-protected polypeptides; 4) removing protecting groups from the fully-protected polypeptides to obtain targeted C-terminal modification peptides; or 5) coupling the fully-protected polypeptides with carboxylic modification groups to obtain the targeted C-terminal modification peptides. The C-terminal modification peptide analysis method has advantages of simplicity in operation, energy saving, environmental friendliness, yield increase and the like.

Description

technical field [0001] A synthetic method for preparing C-terminal modified peptides. Background technique [0002] Peptide modification, as an important means to change the main chain structure and side chain groups of the peptide chain, plays an increasingly important role in changing the physical and chemical properties of peptide compounds and solving their effective utilization in vivo. There have been a large number of literature reports. , the modified polypeptide drug can significantly reduce immunogenicity, reduce side effects, increase water solubility, prolong the action time in vivo, change its biodistribution, etc., and significantly improve the efficacy of the drug. [0003] At present, the chemical modification of the C-terminus of polypeptides is becoming a research hotspot, and the introduction of some small molecule drugs at the C-terminus has become a new research direction. For the modification of the C-terminus of the polypeptide, the modification of th...

AI Technical Summary

Problems solved by technology

For the modification of the C-terminus of the polypeptide, the modification of the amino group is generally completed by directly performing an amide bond reaction with the carboxyl group at the C-terminus of the peptide chain in the liquid phase; A diamino-type Linker is introduced between the C-terminal carboxyl group of the peptide chain and the modified carboxyl group. This method will undoubtedly increase the difficulty of chemical synthesis of this type of peptide, because it generally undergoes two amide bond reactions in the liquid phase, so that It will greatly increase the difficulty of the post-processing of the synthesis, and will greatly reduce the yield of the target peptide

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