Human grf peptide analogs

C - Chemistry – Metallurgy – 07 – K

Patent

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530/7.1

C07K 14/60 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1243016

Human Pancreatic GRF ABSTRACT OF THE DISCLOSURE Two surprisingly active fragments of human pancreatic GRF have been synthesized, along with an analog which exhibitss good biological activity. The synthetic peptides are extremely potent in stimulating the release of pituitary GH in humans and nonhuman animals and have the general formula: H-Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-Val- Leu-R15-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp- Ile-Met-Ser-Arg-Gln-Gln-Gly-Glu-Ser-Asn-Gln-Glu-Arg-Gly- R40-Y wherein R15 is Gly or D-Ala, R40 is Ala or des-R40, and Y signifies the carboxyl moiety of the amino acid residue at the C-terminal and is the radical -COOR1,-CR10,-CONHNHR1,-CON(R1)(R2) or -CH2OR1, with R1 and R2 being lower alkyl or hydrogen. The two fragments include the 29 or 32 N-terminal residues and are each amidated at the C-terminus. These peptides, as well as nontoxic salts thereof, may be administered therapeutically to animals, including humans.

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