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Modifying Ligand-Induced and Constitutive Signaling of the Human 5-HT₄ Receptor

Figure 1

Human 5-HT₄-based RASSLs.

A signal peptide and the FLAG epitope were added to the N-terminus of the human 5-HT₄ receptor. A D¹⁰⁰A mutation was introduced by site-directed mutagenesis to create the G_s-coupled RASSL (Rs1). An additional point mutation (D⁶⁶A, D⁶⁶N, or W²⁷²A) was added to Rs1 to modulate constitutive signaling. Rs1.1 is the Rs1-C-5-HT_2C chimera with enhanced G_q signaling. Rs1.2 is Rs1 with an extra D⁶⁶A mutation that decreased constitutive G_s signaling. Rs1.3 is the Rs1-i3-5-HT_1A chimera with G_i signaling. The junctions in Rs1.1 and Rs1.3 indicate ends of domain swapping where the 5-HT₄ has been replaced by 5-HT_2C or 5-HT_1A, respectively.

doi: https://doi.org/10.1371/journal.pone.0001317.g001