The dynamic changes of life activity and protein are closely related. In many cases , certain proteins complete
or change its function through various modifications. In a large number of protein post-translational modifications,protein phosphorylation is one of the most important.
It is the process that through the protein kinase (Protein kinase, PK) - mediated the enzymatic reaction to
transfer the phosphate group from one compound to another compound [1] (Figure 1),which is a common
way of regulating presence of organisms. Nowadays more than 30% of all human proteins can be modified by phosphorylation, which plays an important role in transfer cell signal and has close relationship with many
processes in life activities . This research has become a hot topic in protein science.Phosphorylation peptides
(mainly refer to the modificated peptides that hydroxyl groups in the side chain of tyrosine, serine and threonine residues were phosphorylated to generate peptide modified acidic phosphate) is an essential tool for the research of protein phosphorylation process. In the past few years ,the synthesis of phosphorylated polypeptides has attracted considerable interests. Now the mature synthesis route has been determined .
Generally speaking ,two main strategies: Global phosphorylation and Building block approach, as shown in Figure 2. The former is to hydroxyl phosphorylate on the solid carrier of serine, Threonine or tyrosine side chain after the synthesis of peptide . While the latter one is that the appropriately protected phosphorylated amino acids will be led directly into peptide sequences, which is more simple than the former one and has become the preferred strategies of phosphorylated peptides synthesis now.
Side chain single benzyl protected amino acids :
Fmoc-AA(PO(OBzl)OH)-OH (AA = Ser, Thr or Tyr) is widely used as raw materials in the monomer construction of phosphorylation peptide.
The problem in the synthesis of multiple phosphorylation sites will become particularly serious, even directly lead to the synthesis of a failure.
Successful case:
Sequence:NH2-TERD(pS)D(pT)DVEEDSRPPGRPAEVHLERAQPFGFID(pS)D(pS)DAEEEY-CONH2，four phosphorylation sites.
HPLC Analyse:
MS Analyse:
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