GeXIVA

GeXIVA is a synthetic 28-amino-acid peptide toxin (αO-conotoxin GeXIVA) originally discovered in the venom of the marine mollusk Conus generalis. It is a potent and selective antagonist of the α9α10 nicotinic acetylcholine receptor (nAChR) subtype, acting by voltage-dependent blockade, likely at a site allosterically coupled to a voltage-sensitive domain. GeXIVA, especially the [1,2] disulfide isomer, has demonstrated potent analgesic effects in multiple animal models of neuropathic pain and chemotherapy-induced peripheral neuropathy, with a favorable safety profile (nonaddictive, without motor side effects). Preclinical studies also suggest anticancer activities, particularly in breast and cervical cancer models. GeXIVA has three possible isomeric forms, with [1,2] showing the highest activity toward α9α10 nAChRs.

Other names

α-conotoxin GeXIVAαO-conotoxin GeXIVAGeXIVA[1,2]GeXIVA[1,4]