Difference in receptor- binding contributes to difference in biological activity between the unique guinea pig GnRH and mammalian GnRH

Publication year: 2011 Source: Neuroscience Letters, Available online 8 December 2011 Chang-Qing Gao, Jean-Marc Kaufmanb, Frank Eertmans, Willem Dhooge, Norbert Fraeyman In the current study, we compared thein vitropotency of a unique form of gonadotropin-releasing hormone (GnRH) present in the brain of the guinea pig (gpGnRH) with that of mammalian GnRH (mGnRH) as well as their binding affinities to the GnRH receptor. In gpGnRH, the highly conserved histidine in position 2 (His) and leucine in position 7 (Leu) are substituted by tyrosine and valine, respectively.In vivo, gpGnRH was shown to be less potent than mGnRH, possibly in part because of higher susceptibility to enzymatic degradation

Publication year: 2011 Source: Neuroscience Letters, Available online 8 December 2011 Chang-Qing Gao, Jean-Marc Kaufmanb, Frank Eertmans, Willem Dhooge, Norbert Fraeyman In the current study, we compared thein vitropotency of a unique form of gonadotropin-releasing hormone (GnRH) present in the brain of the guinea pig (gpGnRH) with that of mammalian GnRH (mGnRH) as well as their binding affinities to the GnRH receptor. In gpGnRH, the highly conserved histidine in position 2 (His) and leucine in position 7 (Leu) are substituted by tyrosine and valine, respectively.In vivo, gpGnRH was shown to be less potent than mGnRH, possibly in part because of higher susceptibility to enzymatic degradation

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Difference in receptor- binding contributes to difference in biological activity between the unique guinea pig GnRH and mammalian GnRH