Low molecular weight non-peptide mimics of omega-conotoxin GVIA.
We report the synthesis and biological activity of a low molecular weight non-peptidic mimic of the analgesic peptide omega-conotoxin GVIA. The molecular weight of this compound presents a reduction by 193g/mol compared to a previously reported lead. This compound exhibits an EC(50) of 5.8microM and is accessible in only six synthetic steps compared to the original lead (13 steps). We also report several improvements to the original synthetic route.
Duggan
Peter J
PJ
CSIRO Molecular and Health Technologies, Clayton, VIC, Australia.
Lewis
Richard J
RJ
Phei Lok
Y
Y
Lumsden
Natalie G
NG
Tuck
Kellie L
KL
Yang
Aijun
A
D000595:Amino Acid Sequence; D000818:Animals; D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D020864:Calcium Channels, N-Type / Q000737:chemistry / Q000378:metabolism; D008970:Molecular Weight; D051381:Rats; D020866:omega-Conotoxin GVIA / Q000737:chemistry*
D002121:Calcium Channel Blockers; D020864:Calcium Channels, N-Type; D020866:omega-Conotoxin GVIA