Product Name: PKR (443-457) pT446+pT451+pY454+pS456
Product Number: PE-04AXB80
Size: | 200 µg | | Price: | 28.00 |
| 1 mg | | $US | 56.00 |
Peptide Name: PKR (443-457) pT446+pT451+pY454+pS456
Product Use: This phosphopeptide may be useful as a substrate for screening the phosphatase activity of protein phosphatases. The peptide sequence is located in the protein kinase catalytic domain activation T-loop between subdomains VII and VIII. T446 phosphorylation stimulates phosphotransferase activity. T451, Y454 and S456 phosphorylation are predicted to be inhibitory.
Peptide Production Method: Solid-phase peptide synthesis
Peptide Origin: Homo sapiens
Peptide Sequence: GKR-pT-RSKG-pT-LR-pY-M-pS-P
Peptide Modifications N Terminus: Free amino
Peptide Modifications C Terminus: βAla-Cys
Peptide Modifications Other: Phosphorylated
Peptide Molecular Mass Calculated: 2273.2 Da
Peptide Purity Percent after Synthesis and Purification: ~50
Peptide Appearance: White powder
Peptide Form: Solid
Storage Conditions: -20°C
Storage Stability: Not stable
Scientific Background: PKR (PRKR, EIF2AK1) is a protein-serine/threonine kinase of the Other group and PEK family. It has an antiviral activity on various ranges of DNA and RNA viruses such as hepatitis C virus, hepatitis B virus, measles virus, and herpes simplex virus 1. It is activated by autophosphorylation after binding to dsRNA (generated during virus infection) in the presence of ATP. Besides double stranded RNA (dsRNA), heparin is a potent activator of the kinase. Binding to dsRNA is required for dimerization leading to autophosphorylation in the activation loop and stimulation of function. Activity is markedly stimulated by manganese ions. Autophosphorylation at S83, T88, T89, T90, Y101, Y162, S242, T255, T258, Y293 T446, T451, and S456 increase the phosphotransferase activity of EIF2AK2. Once activated, PKR can phosphorylate translation initiation factor EIF2S1, which in turn will inhibit protein synthesis. It can be inhibited by vaccinia virus protein E3, possibly via dsRNA sequestering. It has a role in p53-mediated responses to genotoxic stress. Since the protein has a crucial role for inflammation activation, it can be a potential therapeutic target to treat inflammation.