GRF analogs II

Details GRF analogs II GRF analogs II

1985-06-10

1986-12-02

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530325, C07K 710, A61K 3724

Patent

active

046265236

ABSTRACT:
Human pancreatic GRF(hpGRF) and rat hypothalamic GRF(rhGRF) have been earlier characterized and synthesized. The invention provides synthetic peptides which are extremely potent in stimulating the release of pituitary GH in animals, including humans, which are resistant to enzymatic degradation in the body, and which have the sequence: R.sub.1 -Ala-R.sub.3 -Ala-Ile-Phe-Thr-R.sub.8 -Ser-R.sub.10 -Arg-R.sub.12 -R.sub.13 -Leu-R.sub.15 -Gln-Leu-R.sub.18 -Ala-Arg-Lys-Leu-Leu-R.sub.24 -R.sub.25 -Ile-R.sub.27 -R.sub.28 -Arg-Gln-Gln-Gly-Glu-R.sub.34 -Asn-Gln-Glu-R.sub.38 -R.sub.39 -R.sub.40 -Arg-R.sub.42 -R.sub.43 -R.sub.44 -Y wherein R.sub.1 is Tyr, D-Tyr, Met, Phe, D-Phe, pCl-Phe, Leu, His or D-His having either a C.sup.a Me or N.sup.a Me substitution; R.sub.3 is Asp or D-Asp; R.sub.8 is Ser, Asn, D-Ser or D-Asn; R.sub.10 is Tyr or D-Tyr; R.sub.12 is Arg or Lys; R.sub.13 is Ile or Val; R.sub.15 is Gly or D-Ala; R.sub.18 is Tyr or Ser; R.sub.24 is His or Gln; R.sub.25 is Glu or Asp; R.sub.27 is Met, Ala, Nle, Ile, Leu, Nva or Val; R.sub.28 is Asn or Ser; R.sub.34 is Arg or Ser; R.sub.38 is Gln or Arg; R.sub.39 is Arg or Gly; R.sub.40 is Ser or Ala; R.sub.42 is Phe or Ala; R.sub.43 is Asn or Arg; R.sub.44 is a natural amino acid. Any or all of the residues between R.sub.28 and R.sub.44, inclusive, can be deleted, and the carboxyl moiety of the amino acid residue at the C-terminus can be the radical --COOR,--CRO,--CONHNHR,--CON(R) (R') or --CH.sub.2 OR, with R and R' being lower alkyl, fluoro lower alkyl or hydrogen. These peptides as well as nontoxic salts thereof may be administered to animals, including humans and cold-blooded animals, to stimulate the release of GH and may be used diagnostically.

REFERENCES:
patent: 4518586 (1985-05-01), Rivier et al.
Esch et al., Biochemical and Biophysical Research Communications, vol. 109, No. 1, 152-158 (1982).
Esch et al. The J. of Biol. Chem., vol. 258, No. 3, 1806-1812 (1983).
Spiess et al., Nature, vol. 303, 532-535 (1983).
Rivier et al., Nature, vol. 300, 276-279 (1980).
Thorner et al., The Lancet, 24-28 (1983).
Spiess et al., Biochemistry, 21, 6037-6040 (1982).
Guillemin et al., Science, vol. 218, 585-587 (1982).
Yue et al., Diabetes, vol. 24, No. 7, 625-632 (1975).
Lance, et al., "Super-Active Analogs of Growth Hormone-Releasing Factor (1-29)-Amide", 2/29/84, Biochem. & Biophys. Res. Comm., vol. 119, No. 1, pp. 265-272.

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