EphA4 receptor tyrosine kinase inhibitor (Kd
= 0.8 μ
M); inhibits EphA4-EphrinA5 interactions (IC50
= 6.34 μ
M). Prevents Aβ
O induced synaptic damage, dendritic spine loss and prevents the blocking of LTP in hippocampal CA3-CA1 transmissions. Exhibits a long half life in cell culture media (8 and 12 hours in PC3 and C2C12 media respectively). Neuroprotective.
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Distinctive binding of three antagonistic peptides to the ephrin-binding pocket of the EphA4 receptor.
Lamberto et al.
Biochem. J., 2012;445:47
EphA4 activation of c-Abl mediates synaptic loss and LTP blockade caused by amyloid-β oligomers.
Vargas et al.
PLoS One., 2014;9:e92309