Heparin binds PKR

Stable Identifier
Reaction [binding]
Homo sapiens
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Heparin is a mixture of glycosaminoglycan polymers of different sizes and is commercially available as mixtures of predominantly hexamers, octamers, or hexadecamers (Hep-6, Hep-8, Hep-16). PKR (EIF2AK2) binds Hep-8 and Hep-16, but not Hep-6, leading to its dimerization and autophosphorylaton. This activation has also been shown to occur following treatment of vascular smooth muscle cells with heparin, resulting in antiproliferative effects through PKR-mediated signaling. These results indicate that PKR can be activated by small molecules and is a viable target for the development of novel antiviral agents (George et al, 1996; Patel et al, 2002; Fasciano et al, 2005; Anderson et al, 2011).
Literature References
PubMed ID Title Journal Year
21978664 Heparin activates PKR by inducing dimerization

Lary, JW, Anderson, E, Cole, JL, Pierre-Louis, WS, Wong, CJ

J Mol Biol 2011
12231563 Contribution of double-stranded RNA-activated protein kinase toward antiproliferative actions of heparin on vascular smooth muscle cells

Handy, I, Patel, CV, Patel, RC

Arterioscler Thromb Vasc Biol 2002
8661426 Characterization of the heparin-mediated activation of PKR, the interferon-inducible RNA-dependent protein kinase

McCormack, SJ, Svahn, CM, George, CX, Samuel, CE, Thomis, DC

Virology 1996
15752359 Identification of the heparin-binding domains of the interferon-induced protein kinase, PKR

Handy, I, Fasciano, S, Hutchins, B, Patel, RC

FEBS J 2005
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