Voltage-gated calcium channel auxiliary subunit α2δ and uses thereof

摘要

The present invention relates to a target / receptor of a gabapentinoid compound known to exert a therapeutic effect in voltage-gated calcium channel auxiliary subunit α2δ-1, eg, epilepsy and neuropathic pain. Gabapentinoids are known to exert their action through the binding arginine (R) in the RRR motif located at the N-terminus of α2δ-1. The present invention describes novel binding sites for gabapentinoids located within the VGCC_a2 domain and within the IKAK amino acid sequence of α2δ-1. This newly identified amino acid binding site is useful for identifying and characterizing new compounds with therapeutic properties in neuropathic pain and other diseases and conditions that include α2δ-1.