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Diversity of the Neurotoxic Conus Peptides
Table 3.
Therapeutic Applications of Conopeptides
| Clinical application | Conopeptide | Sequence | Target | Clinical status | References |
|---|---|---|---|---|---|
| Z, pyroglutamate; O, 4-trans-hydroxyproline; γ, γ-carboxyglutamate; T, O-glycosylated threonine; *, C-terminal amidation; nAChR, nicotinic acetylcholine receptor; NMDAR, N-methyl-D-aspartate receptor. A derivative of χ-MrIA, rather than the native peptide, advanced to human clinical trials. | |||||
| Pain | ω-MVIIA (Ziconitide, Prialt®) | CKGKGAKCSRLMYDCCTGSCRSGKC* | Ca2+ channel (CaV2.2) | FDA approved | (35, 36, 42) |
| Pain | ω-CVID (AM336) | CKSKGAKCSKLMYDCCSGSCSGTVGRC* | Ca2+ channel (CaV2.2) | Phase I | (43–45) |
| Pain | Contulakin-G (CGX-1160) | ZSEEGGSNATKKPYIL | Neurotensin receptor | Phase I | (46) |
| Pain | α-Vc1.1 (ACV1) | GCCSDPRCNYDHPEIC* | nAChR (α9α10) | Phase I | (13, 47, 48) |
| Pain | χ-MrIA (Xen2174) | NGVCCGYKLCHOC | Norepinephrine transporter | Phase I | (49) |
| Pain/Neuro-protection | Conantokin-G (CGX-1007) | GEγγLQγNQγLIRγKSN* | NMDA receptor (NR2B) | Preclinical | (50–53) |
| Epilepsy | Conantokin-G (CGX-1007) | GEγγLQγNQγLIRγKSN* | NMDA receptor (NR2B) | Phase I | (50–52, 54) |
| Pain | μ-conotoxins | Various | Na+ channels | Preclinical | (55, 56) |
| Myocardial infarction | κ-PVIIA (CGX-1051) | CRIONQKCFQHLDDCCSRKCNRFNKCV | K+ channel (KV1) | Preclinical | (57, 58) |
