TAT-CN21 – TAT Conjugated Peptides

TatCN21 is an inhibitor peptide for the calcium/calmodulin-dependent protein kinase II (CaMKII), a ubiquitously-expressed multifunctional serine/threonine protein kinase. TatCN21 blocks both autonomous and stimulated CaMKII activity with high selectivity. CaMKII is highly expressed in brain tissue where it regulates several processes including: neurotransmitter synthesis/release, neuronal plasticity- excitability and calcium homeostasis. Glutamate clearance by astrocytes is an essential part of normal excitatory neurotransmission, and accumulation of glutamate in the central nervous system is associated with many neurodegenerative disorders. CaMKII regulates glutamate homeostasis: CaMKII inhibition results in diminished glutamate uptake, dysregulated calcium homeostasis, release of the gliotransmitter ATP and compromise neuronal survival. Loss of CaMKII signalling may be an important factor in excitotoxicity. Peptide was obtained by linking the 11 amino acid human HIV Tat transporter to a 21 amino acid sequence corresponding to the CN21.