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PEPTID, THAT AFFECTS THE FUNCTION OF THE HYPPHYPHIC Gland

机译:PEPTID,影响下丘脑功能

摘要

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.
机译:人胰腺GRF类似物,在刺激哺乳动物垂体GH释放方面非常有效,其分子式为: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其中R1是Tyr,Met,D-Tyr,Phe,D-Phe,Leu,D-His或His; R8是Ser或Asn; R10是Tyr,Phe或D-Tyr; R12是Arg或Lys; R13是Ile或Val; R15是Gly或D-Ala; R18是Tyr或Ser; R24是他的或Gln; R25是Glu或Asp; R27选自由Ala,Nle,Ile,Leu,Met和Val的D-和L-异构体组成的组; R28是Ser,Asn或D-Ala; R34是Arg或Ser; R38是Gln或Arg; R39是Arg或Gly; R40是Ser或Ala; R42是苯丙氨酸或丙氨酸; R43是Asn或Arg; R44是天然氨基酸或des-R44; Y表示在C末端的氨基酸残基的羧基部分,并且是基团-COOR,-CRO,-CONHNHR,-CON(R)(R min)或-CH 2OR,其中R和R min是低级烷基。 (氟代低级烷基或氢),但前提是当R1为Tyr时,R27不是Met,R8为Ser,R12为Arg,R13为Ile,R18为Tyr,R24为His,R25为Glu,R28为Asn, R34为Arg,R34为Gln,R39为Arg,R40为Ser,R42为Phe或R43为Asn;进一步提供的是,可以删除任何或所有残基28至44,以提供生物活性片段;或上述物质的无毒盐。这些肽或其生物活性片段,通常会从N端延伸至位置27和32之间的残基附近,以及上述任何一种的无毒盐,可以施用于动物,包括人,和可用于水产养殖。

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