High-affinity response-selective C-terminal analogs of C5a anaph

Details High-affinity response-selective C-terminal analogs of C5a anaph High-affinity response-selective C-terminal analogs of C5a anaph

1994-08-31

1997-12-09

Davenport, Avis M.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

8 to 10 amino acid residues in defined sequence

514 15, A61K 3800, A61K 3802, C07K 500, C07K 700

Patent

active

056962304

ABSTRACT:
High-affinity response-selective C-terminal analogs of C5a anaphylatoxin are provided. Whereas natural C5a has considerable flexibility in the C-terminal region, the analogs of the invention possess a backbone conformation which is constrained at the C-terminus to a .beta.-turn. The stabilized .beta.-turn confers a marked increase in in potency of the analogs; the particular .beta.-turn motif further confers the capability to selectively elicit certain biological responses associated with C5a. Exemplary compounds of the invention are decapeptide analogs of the formula: A1-Ser-Phe-Lys-A2-A3-A4-A5-A6-A7, with the constrained .beta.-turn being localized in the region of A4-A7.

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