TY - JOUR
T1 - International union of basic and clinical pharmacology. CV. somatostatin receptors
T2 - Structure, function, ligands, and new nomenclature
AU - Günther, Thomas
AU - Tulipano, Giovanni
AU - Dournaud, Pascal
AU - Bousquet, Corinne
AU - Csaba, Zsolt
AU - Kreienkamp, Hans Jürgen
AU - Lupp, Amelie
AU - Korbonits, Márta
AU - Castaño, Justo P.
AU - Wester, Hans Jürgen
AU - Culler, Michael
AU - Melmed, Shlomo
AU - Schulz, Stefan
N1 - Publisher Copyright:
© 2018 The Author(s).
PY - 2018/10/1
Y1 - 2018/10/1
N2 - Somatostatin, also known as somatotropin-release inhibitory factor, is a cyclopeptide that exerts potent inhibitory actions on hormone secretion and neuronal excitability. Its physiologic functions are mediated by five G protein–coupled receptors (GPCRs) called somatostatin receptor (SST)1–5. These five receptors share common structural features and signaling mechanisms but differ in their cellular and subcellular localization and mode of regulation. SST 2 and SST 5 receptors have evolved as primary targets for pharmacological treatment of pituitary adenomas and neuroendocrine tumors. In addition, SST 2 is a prototypical GPCR for the development of peptide-based radiopharmaceuticals for diagnostic and therapeutic interventions. This review article summarizes findings published in the last 25 years on the physiology, pharmacology, and clinical applications related to SSTs. We also discuss potential future developments and propose a new nomenclature.
AB - Somatostatin, also known as somatotropin-release inhibitory factor, is a cyclopeptide that exerts potent inhibitory actions on hormone secretion and neuronal excitability. Its physiologic functions are mediated by five G protein–coupled receptors (GPCRs) called somatostatin receptor (SST)1–5. These five receptors share common structural features and signaling mechanisms but differ in their cellular and subcellular localization and mode of regulation. SST 2 and SST 5 receptors have evolved as primary targets for pharmacological treatment of pituitary adenomas and neuroendocrine tumors. In addition, SST 2 is a prototypical GPCR for the development of peptide-based radiopharmaceuticals for diagnostic and therapeutic interventions. This review article summarizes findings published in the last 25 years on the physiology, pharmacology, and clinical applications related to SSTs. We also discuss potential future developments and propose a new nomenclature.
UR - http://www.scopus.com/inward/record.url?scp=85054104530&partnerID=8YFLogxK
U2 - 10.1124/pr.117.015388
DO - 10.1124/pr.117.015388
M3 - Article
C2 - 30232095
AN - SCOPUS:85054104530
SN - 0031-6997
VL - 70
SP - 763
EP - 835
JO - Pharmacological reviews
JF - Pharmacological reviews
IS - 4
ER -