Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – 15 to 23 amino acid residues in defined sequence
Patent
1997-05-15
1999-02-02
Loring, Susan A.
Chemistry: natural resins or derivatives; peptides or proteins;
Peptides of 3 to 100 amino acid residues
15 to 23 amino acid residues in defined sequence
530300, 530327, 530857, A61K 3800, A61K 3804
Patent
active
058666826
ABSTRACT:
This invention relates to relatively short peptides about 14-17 residues in length, which are naturally available in minute amounts in the venom of the cone snails or analogs to the naturally available peptides, and which include two cyclizing disulfide linkages. More specifically, the present invention is directed to conopeptides having the general formula: Gly-Cys-Cys-Ser-Tyr-Xaa.sub.1 -Xaa.sub.1 -Cys-Phe-Ala-Thr-Asn-Xaa.sub.2 -Xaa.sub.3 -Xaa.sub.4 -Cys (SEQ ID NO: 1), wherein Xaa.sub.1 is Pro or Hyp (trans-4-hydroxy-Pro), Xaa.sub.2 is Ser, Pro or Hyp, Xaa.sub.3 is Gly or Asp and Xaa.sub.4 is a Tyr or des- Xaa.sub.4. The disulfide bridges are between the first and third between the second fourth cysteine residues. The C-terminal end is preferably amidated. The invention further relates to the specific peptides AuIA: Gly-Cys-Cys-Ser-Tyr-Pro-Pro-Cys-Phe-Ala-Thr-Asn-Ser-Asp-Tyr-Cys (SEQ ID NO:2); AuIB: Gly-Cys-Cys-Ser-Tyr-Pro-Pro-Cys-Phe-Ala-Thr-Asn-Pro-Asp-Cys (SEQ ID NO:3); and AuIC: Gly-Cys-Cys-Ser-Tyr-Pro-Pro-Cys-Phe-Ala-Thr-Asn-Ser-Gly-Tyr-Cys (SEQ ID NO:4). The invention also includes pharmaceutically acceptable salts of the conopeptides.
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Cartier G. Edward
Luo Siqin
McIntosh J. Michael
Olivera Baldomero M.
Yoshikami Doju
Loring Susan A.
University of Utah Research Foundation
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