KISS1R receptor agonist compounds and use thereof for inducing ovulation in mammals
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United States of America Patent
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Feb 6, 2018
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app pub date -
Jan 31, 2014
filing date -
Jan 31, 2013
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Abstract
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.
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