Bioactive Mimetics of Conotoxins and other Venom Peptides.
Ziconotide (Prialt®), a synthetic version of the peptide ω-conotoxin MVIIA found in the venom of a fish-hunting marine cone snail Conus magnus, is one of very few drugs effective in the treatment of intractable chronic pain. However, its intrathecal mode of delivery and narrow therapeutic window cause complications for patients. This review will summarize progress in the development of small molecule, non-peptidic mimics of Conotoxins and a small number of other venom peptides. This will include a description of how some of the initially designed mimics have been modified to improve their drug-like properties.
CSIRO Manufacturing, Bag 10, Clayton South, VIC 3169, Australia. peter.duggan@csiro.au.|School of Chemical and Physical Sciences, Flinders University, Adelaide, SA 5042, Australia. peter.duggan@csiro.au.
Peter J
PJ
Duggan
School of Chemistry, Monash University, Clayton, VIC 3800, Australia. kellie.tuck@monash.edu.
Kellie L
KL
Tuck
D000595:Amino Acid Sequence; D000818:Animals; D002121:Calcium Channel Blockers / Q000737:chemistry* / Q000494:pharmacology; D020864:Calcium Channels, N-Type / Q000378:metabolism; D045744:Cell Line, Tumor; D006801:Humans; D008958:Models, Molecular; D008969:Molecular Sequence Data; D015394:Molecular Structure; D008978:Mollusk Venoms / Q000737:chemistry* / Q000494:pharmacology; D018408:Patch-Clamp Techniques; D057786:Peptidomimetics / Q000737:chemistry* / Q000494:pharmacology; D020960:omega-Conotoxins / Q000737:chemistry* / Q000494:pharmacology
D002121:Calcium Channel Blockers; D020864:Calcium Channels, N-Type; D008978:Mollusk Venoms; D057786:Peptidomimetics; D020960:omega-Conotoxins; C053423:Conus magus toxin; C078452:ziconotide
Cav2.2; N-type calcium channel; conotoxins; peptidomimetics; toxins; venom peptides