Phosphorylation Modification

 

Research on phosphorylated proteins and peptides can help people elucidate the mechanism of the above process and further understand the nature of life activities. In recent years, with the continuous development of proteomics technology, the study of protein phosphorylation has received more and more widespread attention. Many natural toxins and pathogens also exert their effects by changing the phosphorylation status of intracellular proteins.

Phosphorylated polypeptides mainly refer to the Ser, Tyr and Thr The side chain hydroxyl group of the residue is modified into an acid phosphate polypeptide. So far, the phosphorylation modification of polypeptides mainly involves post-phosphorylation method and Two synthesis methods:

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When modified by the monomer method, the phosphorylated amino acid is difficult to condense with the peptide chain due to the steric hindrance caused by the larger side chain modification group, and subsequent amino acid introduction will be more difficult. Especially when it contains multiple phosphorylation site modifications, the synthesis will become extremely difficult, and the final product has complex components, is difficult to separate, and has an extremely low yield. Therefore, when multiple sites in the peptide chain are phosphorylated, the post-phosphorylation method can be considered. The main synthesis process is to selectively remove the side chain protecting groups of the amino acids to be labeled after the polypeptide synthesis is completed. For Tyr, Thr Amino acids with unprotected side chains can be used directly for the reaction. Side chain protecting group at 1% TFA/DCM It can be quantitatively removed under certain conditions. During post-phosphorylation, bis benzyl phosphoramidite can be used. The tetrazole generates the phosphoramidite tetrazole active intermediate, which is connected to the hydroxyl group, and then oxidized under peroxyacid conditions to generate a phosphoryl group to complete the reaction.

 

  • We provide pSer, pTyr, pThr and D-pSer, D-pTyr, D-pThr Phosphorylation modification services.
  • Phosphorylation modifications of 2 sites, 3 sites, 4 sites, and 5 sites can be performed simultaneously.

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Phosphorylated peptidesSynthetic case (Thr(HPO3), Tyr(HPO3), Ser(HPO3) wait)
1. There are 4 phosphorylation sites in the sequence (xxxpSpTxxxpSxxxpTx), The purity is 95% and the completion cycle is 3 weeks.

HPLC analyze

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MS Atlas

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