Target intelligence / Profile preview

Calcium/calmodulin-dependent protein kinase II (CaMKII)

Target
CaMKII
Molecular classification
Serine/threonine-specific protein kinase, Enzyme
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Overview

Calcium/calmodulin-dependent protein kinase II (CaMKII) is a family of multifunctional serine/threonine-specific protein kinases that play a central role in calcium signaling pathways. CaMKII is widely expressed across many tissues and cell types, with particularly high abundance in the brain, heart, and skeletal muscle. It exists as a multimeric holoenzyme typically composed of 12 or 14 subunits. Activation occurs when intracellular calcium levels rise, leading to binding of calmodulin (CaM) to the regulatory domain and subsequent autophosphorylation. CaMKII regulates numerous cellular processes, including neuronal function, cardiac function, immune system function, and gene transcription. Dysregulation or aberrant activation has been linked to Alzheimer's disease, Angelman syndrome, and cardiac arrhythmias. Inhibition of CaMKII shows therapeutic potential for improving cardiac performance and reducing arrhythmic risk.

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Mechanism of action

CaMKII inhibition

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Biological functions

Synaptic plasticityCardiac contractility regulationT-cell signalingCalcium signalingGene transcriptionGlycogen metabolism
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Disease associations

Alzheimer's diseaseAngelman syndromeCardiac arrhythmiasHeart failure

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