Leu3a binding peptides

Details Leu3a binding peptides Leu3a binding peptides

C - Chemistry, Metallurgy

07

K

530/7.08

C07K 7/14 (2006.01) C07K 7/08 (2006.01) C07K 14/73 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2036997

A peptide having the general formula (I), R1-Ser-Lys-Leu-Asn-Asp-Arg-Ala-Asp-Ser-Arg-Arg- Ser-Leu-Trp-Asp-R2 (I) wherein R1 is H-, H-Pro-, H-Gly-Pro, H-Lys-Gly-Pro-, H-Thr-Lys- Gly-Pro-, H-Leu-Thr-Lys-Gly-Pro-, H-Phe-Leu-Thr-Lys-Gly-Pro-, H- Ser-Phe-Leu-Thr-Lys-Gly-Pro-, H-Gly-Ser-Phe-Leu-Thr-Lys-Gly-Pro-, H-Gln-Gly-Ser-Phe-Leu-Thr-Lys-Gly-Pro-, H-Asn-Gln-Gly-Ser-Phe- Leu-Thr-Lys-Gly-Pro-, or H-Gly-Asn-Gln-Gly-Ser-Phe-Leu-Thr-Lys- Gly-Pro-, and R2 is -OH, -Gln-OH, -Gln-Gly-OH, -Gln-Gly-Asn-OH, or -Gln-Gly-Asn-Phe-OH, with the proviso that R1 is not H-Thr- Lys-Gly-Pro- when R2 is -Gln-Gly-Asn-Phe-OH, or a pharmaceuti- cally acceptable salt thereof. The peptide of the formula (I) exhibits the inhibitory activity in an enzyme-immunoassay (EIA), using Leu3a (anti-CD4 monoclonal antibody) and a membrane fraction of a human T cell line (for example, MOLT4 cell, or CCRF-CEM cell). L/D peptide, i.e., the peptide wherein at least one of the amino acids consituting the peptide of the formula (I) is substituted by a D-amino acid, has improved stability in blood while maintaining the above inhibitory acitivty, and is useful as a physiological agent. The peptide of the formula (I) and the L/D peptide are expected to exhibit physiological activities, particularly an anti-autoimmunity and an inhibitory action for implantation rejection.

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