Fig. 1: Octreotide and paltusotine activate SSTR2 at the nanomolar level.
From: Prospect of acromegaly therapy: molecular mechanism of clinical drugs octreotide and paltusotine
a The chemical structures of octreotide and paltusotine; similar moieties are highlighted in pink. b, c The efficacy of octreotide- and paltusotine-induced SSTR2 Gi signaling (b) and β-arrestin recruitment (c). Data represent mean ± SEM from three independent experiments. d Internalization of SSTR2 in HEK293 cells treated with octreotide and paltusotine measured by ELISA assays by detecting the expression of SSTR2 on the cell surface. Data represent mean ± SEM from three independent experiments. e, f eGFP-tagged SSTR2 plasmid was transfected in HEK293 cells and then cells were treated with octreotide (e) or paltusotine (f) for 30 min. The cells were analyzed by confocal fluorescence microscopy (green, eGFP-SSTR2; blue, DAPI). Scale bar, 50 μm.
