Grf analogs

• Main Authors: JOACHIM SPEISS, WYLIE WALKER VALE JR, JEAN EDOUARD FREDERIC RIVER
• Format: Patent
• Language: English
• Published: 23.05.1985
• Edition: 4
• Subjects: CHEMISTRY; FODDER; FOODS OR FOODSTUFFS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; THEIR TREATMENT, NOT COVERED BY OTHER CLASSES

Human pancreatic GRF analogs which are extremely potent in stimulating the release of pituitary GH in mammals and which have the formula: H-R1-Ala-Asp-Ala-Ile-Phe-Thr-R8-Ser-R10- Arg-R12-R13-Leu-R15-Gln- Leu-R18-Ala-Arg-Lys-Leu-Leu-R24-R25- Ile-R27-R28-Arg-Gln-Gln- Glu-R34-Asn-Gln-Glu-R38-R39-R40-Arg-R42- R43-R44-Y wherein R1 is Tyr, Met, D-Tyr, Phe, D-Phe, Leu, D-His or His; R8 is Ser or Asn; R10 is Tyr, Phe or D-Tyr; R12 is Arg or Lys; R13 is Ile or Val; R15 is Gly or D-Ala; R18 is Tyr or Ser; R24 is His or Gln; R25 is Glu orAsp; R27 is selected from the group consisting of the D- and L-isomers of Ala, Nle, Ile, Leu, Met and Val; R28 is Ser, Asn or D-Ala; R34 is Arg or Ser; R38 is Gln or Arg; R39 is Arg or Gly; R40 is Ser or Ala; R42 is Phe or Ala; R43 is Asn or Arg; R44 is a natural amino acid or des-R44; and Y signifies the carboxyl moiety of the amino acid residue at the C-terminus and is the radical -COOR, -CRO, -CONHNHR, -CON(R)(R min ) or -CH2OR, with R and R min being lower alkyl, fluoro lower alkyl or hydrogen, provided however that when R1 is Tyr, then R27 is other than Met, R8 is Ser, R12 is Arg, R13 is Ile, R18 is Tyr, R24 is His, R25 is Glu, R28 is Asn, R34 is Arg, R34 is Gln, R39 is Arg, R40 is Ser, R42 is Phe or R43 is Asn; provided further that any or all of residues 28 through 44 can be deleted to provide a biologically active fragment; or a nontoxic salt of the foregoing. These peptides or biologically active fragments thereof, which will generally extend from the N-terminal to the vicinity of a residue between positions 27 and 32, as well as nontoxic salts of any of the foregoing, may be administered to animals, including humans, and may be used in aquiculture.