Article
Agonist-specific requirement for a glutamate in transmembrane helix 1 of the oxytocin receptor.
Molecular and cellular endocrinology - 10 Feb 2011
Wootten Denise L, Simms John, Massoura Amelia J, Trim Julie E, Wheatley Mark
Abstract excerpt
Defining key differences between agonist and antagonist binding to hormone receptors is important and will aid rational drug design. Glu(1.35) in transmembrane helix 1 (TM1) of the human oxytocin receptor (OTR) is absolutely conserved in all OTRs cloned to date. We establish that Glu(1.35) is critical for high affinity binding of agonists (full and partial) but is not required for antagonist binding (peptide or...
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