Figure 6.
Summary of the synthetic agonist peptide and small molecule agonist ligand pharmacology (Figure 2 and Table 4) at the wild type (WT) hMC4R and the F51L, E61K, I69T, D90N, Y157S, A219V, and C271R hMC4Rs. The ligands were full agonists at the wild type hMC4R and displayed different combinations of a) no stimulatory activity (up to 100 μM concentrations), b) partial agonist efficacy as normalized to the forskolin control (defined as 1.0 on the Y-axis), and c) to full agonist activity. Notable results include the THIQ small molecule to reach a full agonist response at the Y157S.