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KISS1R receptor agonist compounds and use thereof for inducing ovulation in mammals

机译:KISS1R受体激动剂化合物及其在哺乳动物中诱导排卵的用途

摘要

A KISS1R agonist peptide compound capable of inducing ovulation in a female mammal is provided. The compound is a pseudopeptide having the C-terminal sequence: -XaaΨ[Tz]Xaa2-Xaa3-Xaa4-NH2 (SEQ ID NO: 3), where Ψ[Tz] represents a 1,4-disubstituted 1,2,3-triazole group replacing the peptide bond between the Xaa1 residue and the Xaa2 residue, Xaa1 is Gly or Ala, Xaa2 is Leu or an aliphatic α-aminoacyl analog residue, Xaa3 is Arg, Arg(Me) or a positively charged α-aminoacyl analog residue, and Xaa4 is Tyr, Phe, Trp or an α-aminoacyl analog residue such as aryl alanine; or an analog of the pseudopeptide in which the amide peptide bond between Xaa2 and Xaa3 and/or between Xaa3 and Xaa4 is replaced with an isosteric bond, or a salt thereof.
机译:提供了一种能够在雌性哺乳动物中诱导排卵的KISS1R激动剂肽化合物。该化合物是具有C端序列的伪肽:-XaaΨ[Tz] Xaa2-Xaa3-Xaa4-NH 2 (SEQ ID NO:3),其中Ψ[Tz]代表1,4 -二取代的1,2,3-三唑基团取代了Xaa1残基和Xaa2残基之间的肽键,Xaa1是Gly或Ala,Xaa2是Leu或脂族α-氨酰基类似物残基,Xaa3是Arg,Arg(Me)或带正电荷的α-氨基酰基类似物残基,Xaa4是Tyr,Phe,Trp或α-氨基酰基类似物残基,例如芳基丙氨酸;或其盐,其中Xaa2与Xaa3之间和/或Xaa3与Xaa4之间的酰胺肽键被等排键取代的假肽的类似物或其盐。

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