Conotoxins

Details Conotoxins Conotoxins

1982-06-04

1984-05-08

Phillips, Delbert R.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

C07C10352

Patent

active

044473567

ABSTRACT:
The present invention provides bioactive peptides of generic formula ##STR1## These peptides are extremely potent inhibitors of synaptic transmission at the neuromuscular junction, while at the same time lacing demonstrable inhibition of either nerve or muscle action potential propagation. The peptides are termed conotoxins herein. Naturally occurring conotoxins include conotoxin GI, GIA and GII. In conotoxin GI, U is Glu, V.sub.4 is Asn, V.sub.5 is Pro, V.sub.6 is Ala, W is Gly, X is Arg, Y is His, Z is Tyr, V.sub.12 is Ser and R is --NH.sub.2. Conotoxin GIA is identical to GI except R is --Gly--Lys--NH.sub.2. Conotoxin GII is identical to GI except that V.sub.4 is His, Z is Phe, and X is Lys. Conotoxin MI is identical to GI except that U is Gly-Arg, X is Lys and Y is Asn.

REFERENCES:
J. Biol. Chem. (1981) 256, 4734-4740.
Arch. Biochem. & Biophys. (1978) 190, 539-548.
Biochemistry, 684, 2171-2172.
J. Biol. Chem. 256, No. 10, (1981) 4734-4740.
FEBS Letters 148, No. 2, (1982) 260-262.

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