SSTR2 signals via activation of G-protein and engages β-arrestin to mediate distinct cellular signaling events and has been proved to be a valuable drug target for the treatment of acromegaly, however, subtype selectivity of SSTRs and signal bias properties of different types of ligands (peptide octreotide and small molecule paltusotine) hinder the development of effective drugs targeting SSTR2. The gene discussed is SSTR2; the disease is acromegaly.