Bradykinin analogs with non-peptide bond

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Bradykinin; kallidin; related peptides

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530328, 530332, A61K 3800, C07K 500, C07K 700, C07K 1700

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active

057506469

ABSTRACT:
A linear peptide which is an analog of a naturally occurring, biologically active peptide having an active site and a binding site responsible for the binding of the peptide to a receptor on a target cell, cleavage of a peptide bond in the active site to the naturally occurring peptide being unnecessary for in vivo biological activity, the analog having a non-peptide bond instead of a peptide bond between an amino acid of the active site and an adjacent amino acid, and having the same binding site as the naturally occurring peptide, so that the analog is capable of acting as a competitive inhibitor of the naturally occurring peptide by binding to the receptor and, by virtue of the non-peptide bond, failing to exhibit the in vivo activity of the naturally occurring peptide.

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Martinez et al, J. Med. Chem., vol. 28, pp. 1874-1879, (1985).
Nagain et al, Peptides, vol. 8, pp. 1023-1028, (1987).
Rodriguez et al, J. Med. Chem., vol. 30 pp. 1366-1373, (1987).
Sasaki et al, J. Med. Chem., vol. 30, pp. 1162-1166, (1987).
Dubmevil et al, Drug Design and Delivery, vol. 2, pp. 49-54, (1987).

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