Calmodulin-Dependent Protein Kinase (CaM Kinase) Inhibitors


Many effects of Ca2+ are mediated by Ca2+/calmodulin(CaM)- dependent protein kinases (CaM kinases). CaM kinases constitute a family of structurally related enzymes that include phosphorylase kinase, myosin light chain kinase, and CaM kinases I-IV. CaM kinase II, one of the best-studied multifunctional enzymes, is found in high concentrations in neuronal synapses, and in some regions of the brain it may constitute up to 2% of the total protein content. Activation of CaM kinase II has been linked to memory and learning processes in the vertebrate nervous system. CaM kinase II is a complex of about 12 subunits that exist in four differentially expressed forms (a, b, g, and d). The a and b isoforms are most abundant in neurons, whereas d or g isoforms are expressed in most tissues. The d isoform is the most prominent isoform in cardiomyocytes. In the inactive state there is a strong interaction between the inhibitory and catalytic domains of the enzyme. The binding of Ca2+/CaM allows the catalytic domain to phosphorylate the inhibitory domain. Once activated, CaM kinase II retains significant activity even after the withdrawal of Ca2+, thereby prolonging the duration of kinase activity. Several synthetic and naturally occurring compounds have been shown to bind CaM in a Ca2+-dependent manner and block the activation of CaM-dependent enzymes. These compounds have been extensively used in investigating the mechanism of Ca2+-binding and activation in biological systems.

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Fukunaga, K., and Miyamoto, E. 1999. Jap. J. Pharmacol. 79, 7.
Kemp, B.E., et al. 1994. In Protein Kinases (Woodgett, J.R., ed.), Oxford Univ. Press, N.Y. pp 30-67.

Produkte in dieser Kategorie
Artikelnummer Produkte
208710 [Ala286]-Ca2+/Calmodulin Kinase II Inhibitor 281-301 
189480 Autocamtide-2 Related Inhibitory Peptide - Calbiochem 
189484 Autocamtide-2 Related Inhibitory Peptide II - Calbiochem 
189485 Autocamtide-2 Related Inhibitory Peptide II, Cell-permeable - Calbiochem 
189482 Autocamtide-2 Related Inhibitory Peptide, Myristoylated - Calbiochem 
208711 Ca2+/Calmodulin Kinase II Inhibitor 281-309 - Calbiochem 
208734 Calmodulin Binding Domain - CAS 115044-69-4 - Calbiochem 
208920 Calmodulin Kinase IINtide - Calbiochem 
208921 Calmodulin Kinase IINtide, Myristoylated - Calbiochem 
208922 CaMKII Inhibitor, CK59 - CAS 140651-18-9 - Calbiochem 
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