Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Corticotropin ; related peptides
Patent
1991-06-14
1993-09-14
Cashion, Jr., Merrell C.
Chemistry: natural resins or derivatives; peptides or proteins;
Peptides of 3 to 100 amino acid residues
Corticotropin ; related peptides
530317, 530321, 530324, 530325, 930 21, 930 70, 930260, C07K 738, C07K 760, C07K 710
Patent
active
052450090
ABSTRACT:
Disclosed are improved CRF peptide antagonists such as those having the formula: Y-D-Phe-R.sub.13 -Leu-Leu-Arg-R.sub.17 -R.sub.18 -Leu-R.sub.20 -Nle-R.sub.22 -R.sub.23 -R.sub.24 -R.sub.25 -R.sub.26 -Leu-R.sub.28 -R.sub.29 -Gln-R.sub.31 -R.sub.32 -R.sub.33 -R.sub.34 -Arg-R.sub.36 -R.sub.37 -Nle-R.sub.39 -R.sub.40 -R.sub.41 -NH.sub.2 wherein Y is Ac or hydrogen; R.sub.13 is His, Tyr or Glu; R.sub.17 is Cys, Glu, Asn or Lys; R.sub.18 is Val, Nle or Met; R.sub.20 is D-Cys, Glu, D-Glu, Aib or D-Ala; R.sub.22 is Ala, Aib, Thr, Asp or Glu; R.sub.23 is Arg, Orn, Har or Lys; R.sub.24 is Ala or Aib; R.sub.25 is Asp or Glu; R.sub.26 is Gln, Asn or Lys; R.sub.28 is Ala or Aib; R.sub.29 is Gln, Aib or Glu, R.sub.31 is Ala or Aib; R.sub.32 is His, Aib, Gly, Tyr or Ala; R.sub.33 is Ser, Aib, Asn, Leu, Thr or Ala; R.sub.34 is Asn or Aib; R.sub.36 is Lys, Orn, Arg, Har or Leu; R.sub.37 is Leu or Try; R.sub.39 is Glu, Aib or Asp; R.sub.40 is Ile, Aib, Thr, Glu, Ala, Val, Leu, Nle, Phe, Nva, Gly or Gln; and R.sub.41 is Ala, Ile, Gly, Val, Leu, Nle, Phe, Nva or Gln. Specific CRF antagonists disclosed include [D-Phe.sup.12, D-Ala.sup.20, Nle.sup.21,38,]-rCRF(12-41), [D-Phe.sup.12, Nle.sup.21,38, Aib.sup.33 ]-rCRF(12-41) and (c 17-20) [D-Phe.sup.12, Cys.sup.17, D-Cys.sup.20, Nle.sup.21,38 ]-rCRF(12-41).
REFERENCES:
patent: 3761459 (1973-09-01), Pless
patent: 3770715 (1973-11-01), Tesser et al.
patent: 4415558 (1983-11-01), Vale et al.
patent: 4489163 (1984-12-01), Rivier et al.
patent: 4594329 (1986-06-01), Vale et al.
patent: 4605642 (1986-08-01), Rivier et al.
Rivier et al., Proc. Natl. Acad. Sci. USA, vol. 80, pp. 4851-4855, (Aug. 1983).
Rivier et al., Science, vol. 224, pp. 889-891, (May. 22, 1984).
Shibabara et al., The EMBO Journal, vol. 2(5), pp. 775-779, (1983).
Rittel, Proceedings of the Biochemical Society, 56p, vol. 125, (1971).
Hulligen et al., Acta Endocrinologica, vol. 75, pp. 24-32, (1974).
Hernandez Jean-Francois
Kornreich Wayne D.
Rivier Catherine L.
Rivier Jean E. F.
Vale, Jr. Wylie W.
Cashion Jr. Merrell C.
The Salk Institute for Biological Studies
Wessendorf T. D.
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