Cyclic CRF agonists

Details Cyclic CRF agonists Cyclic CRF agonists

1995-12-19

1998-12-01

Tsang, Cecilia J.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Corticotropin ; related peptides

530317, 930 21, 930 70, 930260, 514 9, 514 2, 514805, A61K 3828, A61K 3812, C07K 14695, C07K 764

Patent

active

058440747

ABSTRACT:
Novel cyclic CRF agonist peptides have the amino acid sequence: (cyclo 30-33)Ac-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-D-Phe-His-Leu-Leu-Arg-Glu-Val-Leu -Glu-Nle-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-R.sub.30 -Ala-R.sub.32 -R.sub.33 -Asn-Arg-Lys-Leu-Nle-Glu-Ile-Ile-NH.sub.2 wherein R.sub.30 is Glu or Cys; R.sub.32 is His or a D-amino acid such as D-His, D-Arg or similar; R.sub.33 is Lys, Orn or Cys. The N-terminus may be extended by Ser-Glu-Glu. Lys may be substituted for Arg.sup.23, and its side chain connected by a lactam bridge to Glu.sup.20 to form a bicyclic peptide. Certain disclosed CRF agonists include: Glu.sup.30, Lys.sup.33 !r/hCRF(4-41), Glu.sup.30, Orn.sup.33 !r/hCRF(4-41), D-His.sup.32 !r/hCRF(4-41), Lys.sup.23,33, Glu.sup.30, D-His.sup.32 !-r/hCRF(4-41), Glu.sup.30, imBzlD-His.sup.32, Lys.sup.33 !r/hCRF(4-41) and D-Arg.sup.32, Lys.sup.33 !r/hCRF(4-41). Nle.sup.21,38, Glu.sup.30, D-His.sup.32, Lys.sup.33 !r/hCRF and (cyclo D-His.sup.32, Lys.sup.33 !r/hCRF(3-41) are useful in screening for more potent agonists.

REFERENCES:
patent: 5439885 (1995-08-01), Kornreich et al.
patent: 5493006 (1996-02-01), de Miranda et al.
Gulyas et al., "Potent, structurally constrained agonists and competitive antagonists of corticotropin-releasing factor", P.N.A.S., vol. 92, pp. 10575-10579 (Nov. 1995).
Miranda, A. et al. Conformationally restricted competitive a factor. J. Med. Chem. 37, 1450-1459, Oct. 1994.

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