Title : Histidine(7.36(305)) in the conserved peptide receptor activation domain of the gonadotropin releasing hormone receptor couples peptide binding and receptor activation.

Pub. Date : 2015 Feb 15

PMID : 25583361






8 Functional Relationships(s)
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1 We investigated GnRH interactions with the His(7.36(305)) residue of the GnRH receptor, using functional and computational analysis of modified GnRH receptors and peptides. Histidine gonadotropin releasing hormone 1 Homo sapiens
2 We investigated GnRH interactions with the His(7.36(305)) residue of the GnRH receptor, using functional and computational analysis of modified GnRH receptors and peptides. Histidine gonadotropin releasing hormone 1 Homo sapiens
3 We investigated GnRH interactions with the His(7.36(305)) residue of the GnRH receptor, using functional and computational analysis of modified GnRH receptors and peptides. Histidine gonadotropin releasing hormone 1 Homo sapiens
4 Non-polar His(7.36(305)) substitutions decreased receptor affinity for GnRH four- to forty-fold, whereas GnRH signaling potency was more decreased (~150-fold). Histidine gonadotropin releasing hormone 1 Homo sapiens
5 Uncharged polar His(7.36(305)) substitutions decreased GnRH potency, but not affinity. Histidine gonadotropin releasing hormone 1 Homo sapiens
6 [2-Nal(3)]-GnRH retained high affinity at receptors with non-polar His(7.36(305)) substitutions, supporting a role for His(7.36(305)) in recognizing Trp(3) of GnRH. Histidine gonadotropin releasing hormone 1 Homo sapiens
7 [2-Nal(3)]-GnRH retained high affinity at receptors with non-polar His(7.36(305)) substitutions, supporting a role for His(7.36(305)) in recognizing Trp(3) of GnRH. Histidine gonadotropin releasing hormone 1 Homo sapiens
8 Results suggest that His(7.36(305)) of the GnRH receptor forms two distinct interactions that determine binding to Trp(3) and couple agonist binding to the conserved transmembrane domain network that activates GPCRs. Histidine gonadotropin releasing hormone 1 Homo sapiens