Cyclic CRF antagonists

Details Cyclic CRF antagonists Cyclic CRF antagonists

1995-11-10

1999-02-23

Tsang, Cecilia

Chemistry: molecular biology and microbiology

Measuring or testing process involving enzymes or...

Involving antigen-antibody binding, specific binding protein...

530306, 530317, 514 2, 514 9, 514805, 930 21, 930 70, 930260, G01N 3353, A61K 3828, A61K 3812, C07K 500

Patent

active

058742271

ABSTRACT:
Novel cyclic CRF antagonist peptides have the amino acid sequence: ##STR1## wherein Y is Ac, H, Ac-Thr or H-Thr; R.sub.30 is Glu or Cys; R.sub.32 is His or preferably a basic and/or aromatic D-amino acid such as D-His or D-Arg; R.sub.33 is Lys, Orn or Cys. The N-terminus may be extended by Leu or Asp-Leu. CML may be substituted for Leu.sup.27, and D-Tyr may be substituted for D-Phe to facilitate labelling. 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. Disclosed CRF antagonists include: !r/hCRF(12-41), Lys.sup.33 !r/hCRF(11-41), Glu.sup.30 !-r/hCRF(12-41), Lys.sup.33 !r/hCRF(12-41), D-His.sup.32, Lys.sup.33 !r/hCRF(12-41) and Lys.sup.33 !r/hCRF(12-41). Nle.sup.21,38, Glu.sup.30, D-His.sup.32, Lys.sup.33 !r/hCRF(12-41) are useful in drug screening assays.

REFERENCES:
patent: 5439885 (1995-08-01), Kornreich et al.
patent: 5493006 (1996-02-01), De Miranda et al.
Miranda, et al., Conformationally Restricted Competitive Antagonists of Human/Rat Corticotropin-Releasing Factor, vol. 37, pp. 1450-1459, 1994.
Rivier, et al., Synthetic Competitive Antagonists of Corticotropin Releasing Factor: Effect on ACTH Secretion in the Rat, vol. 224, pp. 889-891, May 25, 1984.
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).

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