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PKR is a protein kinase that is activated by binding of dsRNA to its N-terminal regulatory domain. As a consequence of its activation, PKR phosphorylates its eukaryotic initiation factor-2 alpha subunit (eIF-2 alpha), triggering shut-off of translation and initiation of cell death, apoptosis. As a result of its pro-apoptotic function, PKR is implicated in the development of many diseases, including neurodegenerative and infectious diseases. PKR is also activated by pathogens, such as HIV-1, and this activation results in the switch of viral replication from translation to gene expression. Here, we describe the design, synthesis and evaluation of a novel peptide inhibitor of PKR that has shown promising in vitro inhibition of the enzyme.Genetics of excitatory synaptic transmission in the central nervous system.
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