Target intelligence / Profile preview

Somatostatin Receptor (SSTR)

Target
SSTR
Molecular classification
G protein-coupled receptor, GPCR, Receptor
01

Overview

Somatostatin receptors (SSTRs) are a family of G protein-coupled receptors (GPCRs) that mediate the effects of somatostatin, a cyclic peptide hormone involved in regulating neurotransmission, hormone secretion, and cell proliferation. There are five known subtypes: SSTR1, SSTR2, SSTR3, SSTR4, and SSTR5. These subtypes are differentially distributed throughout the central nervous system (CNS) and peripheral tissues. They regulate multiple physiological processes including hormone secretion, neuronal activity, and cell proliferation. SSTR expression increases significantly in certain pathological states like neuroendocrine tumors, making them important diagnostic markers and therapeutic targets. Synthetic analogs are used for treating acromegaly and neuroendocrine tumors.

Other names
Somatostatin receptorsSST receptorsSSTR1SSTR2SSTR3SSTR4SSTR5
02

Mechanism of action

Activation typically inhibits adenylyl cyclase through inhibitory G-proteins (Gαi/o), reducing cAMP levels. Some subtypes also modulate ion channels or activate phosphotyrosine phosphatases or MAPK pathways to control cell cycle progression and apoptosis.

03

Biological functions

Signal transductionInhibition of growth hormone releaseSuppression of insulin secretionSuppression of glucagon secretionInhibition of gastric acid secretionModulation of neuronal activityRegulation of cell proliferationApoptosisImmune response
04

Disease associations

Neuroendocrine tumorsAcromegalyCushing's diseaseCancerColorectal carcinomas
05

Safety considerations

Potential side effects associated with somatostatin analogsTherapeutic challenges in targeting specific SSTR subtypes
06

Interacting drugs

Octreotide

3 more in the full profile.

07

Biomarkers

SSTR expression levels in neuroendocrine tumorsSST2 expression in pituitary tumors

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