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Target not currently curated in GtoImmuPdb
Target id: 357
Nomenclature: SST3 receptor
Family: Somatostatin receptors
Annotation status:
Annotated and expert reviewed. Please contact us if you can help with updates.
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Gene and Protein Information ![]() |
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class A G protein-coupled receptor | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 7 | 418 | 22q13.1 | SSTR3 | somatostatin receptor 3 | 4,46-47 |
Mouse | 7 | 428 | 15 E1 | Sstr3 | somatostatin receptor 3 | 49 |
Rat | 7 | 428 | 7q34 | Sstr3 | somatostatin receptor 3 | 24 |
Previous and Unofficial Names ![]() |
SRIF1C | somatostatin receptor 28 | SSR-28 |
Database Links ![]() |
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Specialist databases | |
GPCRDB | ssr3_human (Hs), ssr3_mouse (Mm), ssr3_rat (Rn) |
Other databases | |
ChEMBL Target | CHEMBL2028 (Hs), CHEMBL2238 (Mm), CHEMBL3340 (Rn) |
Ensembl Gene | ENSG00000183473 (Hs), ENSMUSG00000044933 (Mm), ENSRNOG00000007332 (Rn) |
Entrez Gene | 6753 (Hs), 20607 (Mm), 171044 (Rn) |
Human Protein Atlas | ENSG00000183473 (Hs) |
KEGG Gene | hsa:6753 (Hs), mmu:20607 (Mm), rno:171044 (Rn) |
OMIM | 182453 (Hs) |
RefSeq Nucleotide | NM_001051 (Hs), NM_009218 (Mm), NM_133522 (Rn) |
RefSeq Protein | NP_001042 (Hs), NP_033244 (Mm), NP_598206 (Rn) |
UniProtKB | P32745 (Hs), P30935 (Mm), P30936 (Rn) |
Wikipedia | SSTR3 (Hs) |
Natural/Endogenous Ligands ![]() |
cortistatin-14 {Sp: Mouse, Rat} |
CST-17 {Sp: Human} |
SRIF-14 {Sp: Human, Mouse, Rat} |
SRIF-28 {Sp: Human, Mouse, Rat} |
Comments: SRIF-14 and SRIF-28 are the active fragments of precursor somatostatin |
Download all structure-activity data for this target as a CSV file
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Key to terms and symbols | View all chemical structures | Click column headers to sort | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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View species-specific agonist tables |
Antagonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Primary Transduction Mechanisms ![]() |
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Transducer | Effector/Response |
Gi/Go family | Adenylate cyclase inhibition |
References: 16,38,49 |
Tissue Distribution ![]() |
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Expression Datasets ![]() |
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Functional Assays ![]() |
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Physiological Functions ![]() |
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1. Arena S, Pattarozzi A, Corsaro A, Schettini G, Florio T. (2005) Somatostatin receptor subtype-dependent regulation of nitric oxide release: involvement of different intracellular pathways. Mol. Endocrinol., 19 (1): 255-67. [PMID:15388796]
2. Bruns C, Raulf F, Hoyer D, Schloos J, Lübbert H, Weckbecker G. (1996) Binding properties of somatostatin receptor subtypes. Metab. Clin. Exp., 45 (8 Suppl 1): 17-20. [PMID:8769372]
3. Cardoso A, el Ghamrawy C, Gautron JP, Horvat B, Gautier N, Enjalbert A, Krantic S. (1998) Somatostatin increases mitogen-induced IL-2 secretion and proliferation of human Jurkat T cells via sst3 receptor isotype. J. Cell. Biochem., 68 (1): 62-73. [PMID:9407314]
4. Corness JD, Demchyshyn LL, Seeman P, Van Tol HH, Srikant CB, Kent G, Patel YC, Niznik HB. (1993) A human somatostatin receptor (SSTR3), located on chromosome 22, displays preferential affinity for somatostatin-14 like peptides. FEBS Lett., 321 (2-3): 279-84. [PMID:8097479]
5. Engström M, Tomperi J, El-Darwish K, Ahman M, Savola JM, Wurster S. (2005) Superagonism at the human somatostatin receptor subtype 4. J. Pharmacol. Exp. Ther., 312 (1): 332-8. [PMID:15333679]
6. Erchegyi J, Hoeger CA, Low W, Hoyer D, Waser B, Eltschinger V, Schaer JC, Cescato R, Reubi JC, Rivier JE. (2005) Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. J Med Chem, 48: 507-514. [PMID:15658864]
7. Feuerbach D, Fehlmann D, Nunn C, Siehler S, Langenegger D, Bouhelal R, Seuwen K, Hoyer D. (2000) Cloning, expression and pharmacological characterisation of the mouse somatostatin sst(5) receptor. Neuropharmacology, 39 (8): 1451-62. [PMID:10818261]
8. Florio T, Morini M, Villa V, Arena S, Corsaro A, Thellung S, Culler MD, Pfeffer U, Noonan DM, Schettini G et al.. (2003) Somatostatin inhibits tumor angiogenesis and growth via somatostatin receptor-3-mediated regulation of endothelial nitric oxide synthase and mitogen-activated protein kinase activities. Endocrinology, 144 (4): 1574-84. [PMID:12639942]
9. Ginj M, Chen J, Walter MA, Eltschinger V, Reubi JC, Maecke HR. (2005) Preclinical evaluation of new and highly potent analogues of octreotide for predictive imaging and targeted radiotherapy. Clin. Cancer Res., 11 (3): 1136-45. [PMID:15709181]
10. He S, Ye Z, Truong Q, Shah S, Du W, Guo L, Dobbelaar PH, Lai Z, Liu J, Jian T et al.. (2012) The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes. ACS Med Chem Lett, 3 (6): 484-9. [PMID:24900499]
11. Hervieu G, Emson PC. (1999) Visualisation of somatostatin receptor sst(3) in the rat central nervous system. Brain Res. Mol. Brain Res., 71 (2): 290-303. [PMID:10521583]
12. Hocart SJ, Jain R, Murphy WA, Taylor JE, Morgan B, Coy DH. (1998) Potent antagonists of somatostatin: synthesis and biology. J. Med. Chem., 41 (7): 1146-54. [PMID:9544214]
13. Hoyer D, Vassout A, Gentsch C, Enz A, Vigouret JM, Jaton A, Schoeffter P, Kelly P, Wrynn A, Hurth K, Troxler T. (2004) Functional characterization of NVP ACQ090, a somatostatin sst3 receptor antagonist. Soc Neuroscience Abs,: -.
14. Händel M, Schulz S, Stanarius A, Schreff M, Erdtmann-Vourliotis M, Schmidt H, Wolf G, Höllt V. (1999) Selective targeting of somatostatin receptor 3 to neuronal cilia. Neuroscience, 89 (3): 909-26. [PMID:10199624]
15. Iwanaga T, Miki T, Takahashi-Iwanaga H. (2011) Restricted expression of somatostatin receptor 3 to primary cilia in the pancreatic islets and adenohypophysis of mice. Biomed. Res., 32 (1): 73-81. [PMID:21383513]
16. Kaupmann K, Bruns C, Hoyer D, Seuwen K, Lubbert H. (1993) Distribution and second messenger coupling of four somatostatin receptor subtypes expressed in brain. FEBS Lett, 331: 53-59. [PMID:8405411]
17. Kreienkamp HJ, Hönck HH, Richter D. (1997) Coupling of rat somatostatin receptor subtypes to a G-protein gated inwardly rectifying potassium channel (GIRK1). FEBS Lett., 419 (1): 92-4. [PMID:9426226]
18. Kreuzer OJ, Krisch B, Déry O, Bunnett NW, Meyerhof W. (2001) Agonist-mediated endocytosis of rat somatostatin receptor subtype 3 involves beta-arrestin and clathrin coated vesicles. J. Neuroendocrinol., 13 (3): 279-87. [PMID:11207943]
19. Lesche S, Lehmann D, Nagel F, Schmid HA, Schulz S. (2009) Differential effects of octreotide and pasireotide on somatostatin receptor internalization and trafficking in vitro. J. Clin. Endocrinol. Metab., 94 (2): 654-61. [PMID:19001514]
20. Liew CW, Vockel M, Glassmeier G, Brandner JM, Fernandez-Ballester GJ, Schwarz JR, Schulz S, Buck F, Serrano L, Richter D et al.. (2009) Interaction of the human somatostatin receptor 3 with the multiple PDZ domain protein MUPP1 enables somatostatin to control permeability of epithelial tight junctions. FEBS Lett., 583 (1): 49-54. [PMID:19071123]
21. Lin CY, Varma MG, Joubel A, Madabushi S, Lichtarge O, Barber DL. (2003) Conserved motifs in somatostatin, D2-dopamine, and alpha 2B-adrenergic receptors for inhibiting the Na-H exchanger, NHE1. J. Biol. Chem., 278 (17): 15128-35. [PMID:12566440]
22. Lupp A, Nagel F, Doll C, Röcken C, Evert M, Mawrin C, Saeger W, Schulz S. (2012) Reassessment of sst3 somatostatin receptor expression in human normal and neoplastic tissues using the novel rabbit monoclonal antibody UMB-5. Neuroendocrinology, 96 (4): 301-10. [PMID:22414742]
23. Meyerhof W. (1998) The elucidation of somatostatin receptor functions: a current view. Rev. Physiol. Biochem. Pharmacol., 133: 55-108. [PMID:9600011]
24. Meyerhof W, Wulfsen I, Schönrock C, Fehr S, Richter D. (1992) Molecular cloning of a somatostatin-28 receptor and comparison of its expression pattern with that of a somatostatin-14 receptor in rat brain. Proc. Natl. Acad. Sci. U.S.A., 89 (21): 10267-71. [PMID:1279674]
25. Murray RD, Kim K, Ren SG, Chelly M, Umehara Y, Melmed S. (2004) Central and peripheral actions of somatostatin on the growth hormone-IGF-I axis. J. Clin. Invest., 114 (3): 349-56. [PMID:15286801]
26. Patel YC, Srikant CB. (1994) Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5). Endocrinology, 135 (6): 2814-7. [PMID:7988476]
27. Pfeiffer M, Koch T, Schröder H, Klutzny M, Kirscht S, Kreienkamp HJ, Höllt V, Schulz S. (2001) Homo- and heterodimerization of somatostatin receptor subtypes. Inactivation of sst(3) receptor function by heterodimerization with sst(2A). J. Biol. Chem., 276 (17): 14027-36. [PMID:11134004]
28. Poitout L, Roubert P, Contour-Galcéra MO, Moinet C, Lannoy J, Pommier J, Plas P, Bigg D, Thurieau C. (2001) Identification of potent non-peptide somatostatin antagonists with sst(3) selectivity. J. Med. Chem., 44 (18): 2990-3000. [PMID:11520208]
29. Raynor K, Murphy WA, Coy DH, Taylor JE, Moreau JP, Yasuda K, Bell GI, Reisine T. (1993) Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides. Mol. Pharmacol., 43 (6): 838-44. [PMID:8100350]
30. Reardon DB, Wood SL, Brautigan DL, Bell GI, Dent P, Sturgill TW. (1996) Activation of a protein tyrosine phosphatase and inactivation of Raf-1 by somatostatin. Biochem. J., 314 ( Pt 2): 401-4. [PMID:8670047]
31. Reubi JC, Eisenwiener KP, Rink H, Waser B, Mäcke HR. (2002) A new peptidic somatostatin agonist with high affinity to all five somatostatin receptors. Eur. J. Pharmacol., 456 (1-3): 45-9. [PMID:12450568]
32. Reubi JC, Schaer JC, Wenger S, Hoeger C, Erchegyi J, Waser B, Rivier J. (2000) SST3-selective potent peptidic somatostatin receptor antagonists. Proc. Natl. Acad. Sci. U.S.A., 97 (25): 13973-8. [PMID:11095748]
33. Rohrer SP, Birzin ET, Mosley RT, Berk SC, Hutchins SM, Shen DM, Xiong Y, Hayes EC, Parmar RM, Foor F et al.. (1998) Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry. Science, 282 (5389): 737-40. [PMID:9784130]
34. Roth A, Kreienkamp HJ, Meyerhof W, Richter D. (1997) Phosphorylation of four amino acid residues in the carboxyl terminus of the rat somatostatin receptor subtype 3 is crucial for its desensitization and internalization. J. Biol. Chem., 272 (38): 23769-74. [PMID:9295322]
35. Schindler M, Harrington KA, Humphrey PP, Emson PC. (1995) Cellular localisation and co-expression of somatostatin receptor messenger RNAs in the human brain. Brain Res. Mol. Brain Res., 34 (2): 321-6. [PMID:8750836]
36. Schmid HA, Schoeffter P. (2004) Functional activity of the multiligand analog SOM230 at human recombinant somatostatin receptor subtypes supports its usefulness in neuroendocrine tumors. Neuroendocrinology, 80 Suppl 1: 47-50. [PMID:15477717]
37. Shimon I, Taylor JE, Dong JZ, Bitonte RA, Kim S, Morgan B, Coy DH, Culler MD, Melmed S. (1997) Somatostatin receptor subtype specificity in human fetal pituitary cultures. Differential role of SSTR2 and SSTR5 for growth hormone, thyroid-stimulating hormone, and prolactin regulation. J. Clin. Invest., 99 (4): 789-98. [PMID:9045884]
38. Siehler S, Hoyer D. (1999) Characterisation of human recombinant somatostatin receptors. 3. Modulation of adenylate cyclase activity. Naunyn Schmiedebergs Arch Pharmacol, 360: 510-521. [PMID:10598790]
39. Siehler S, Hoyer D. (1999) Characterisation of human recombinant somatostatin receptors. 4. Modulation of phospholipase C activity. Naunyn Schmiedebergs Arch. Pharmacol., 360 (5): 522-32. [PMID:10598791]
40. Siehler S, Seuwen K, Hoyer D. (1998) [125I]Tyr10-cortistatin14 labels all five somatostatin receptors. Naunyn Schmiedebergs Arch. Pharmacol., 357 (5): 483-9. [PMID:9650799]
41. Siehler S, Seuwen K, Hoyer D. (1999) Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies. Naunyn Schmiedebergs Arch. Pharmacol., 360 (5): 488-99. [PMID:10598788]
42. Tower-Gilchrist C, Lee E, Sztul E. (2011) Endosomal trafficking of the G protein-coupled receptor somatostatin receptor 3. Biochem. Biophys. Res. Commun., 413 (4): 555-60. [PMID:21925142]
43. Tulipano G, Soldi D, Bagnasco M, Culler MD, Taylor JE, Cocchi D, Giustina A. (2002) Characterization of new selective somatostatin receptor subtype-2 (sst2) antagonists, BIM-23627 and BIM-23454. Effects of BIM-23627 on GH release in anesthetized male rats after short-term high-dose dexamethasone treatment. Endocrinology, 143: 1218-1224. [PMID:11897676]
44. Viollet C, Bodenant C, Prunotto C, Roosterman D, Schaefer J, Meyerhof W, Epelbaum J, Vaudry H, Leroux P. (1997) Differential expression of multiple somatostatin receptors in the rat cerebellum during development. J. Neurochem., 68 (6): 2263-72. [PMID:9166718]
45. Wild D, Schmitt JS, Ginj M, Mäcke HR, Bernard BF, Krenning E, De Jong M, Wenger S, Reubi JC. (2003) DOTA-NOC, a high-affinity ligand of somatostatin receptor subtypes 2, 3 and 5 for labelling with various radiometals. Eur. J. Nucl. Med. Mol. Imaging, 30 (10): 1338-47. [PMID:12937948]
46. Yamada Y, Reisine T, Law SF, Ihara Y, Kubota A, Kagimoto S, Seino M, Seino Y, Bell GI, Seino S. (1992) Somatostatin receptors, an expanding gene family: cloning and functional characterization of human SSTR3, a protein coupled to adenylyl cyclase. Mol. Endocrinol., 6 (12): 2136-42. [PMID:1337145]
47. Yamada Y, Stoffel M, Espinosa 3rd R, Xiang KS, Seino M, Seino S, Le Beau MM, Bell GI. (1993) Human somatostatin receptor genes: localization to human chromosomes 14, 17, and 22 and identification of simple tandem repeat polymorphisms. Genomics, 15 (2): 449-52. [PMID:8449518]
48. Yang L, Berk SC, Rohrer SP, Mosley RT, Guo L, Underwood DJ, Arison BH, Birzin ET, Hayes EC, Mitra SW et al.. (1998) Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2. Proc. Natl. Acad. Sci. U.S.A., 95 (18): 10836-41. [PMID:9724791]
49. Yasuda K, Rens-Domiano S, Breder CD, Law SF, Saper CB, Reisine T, Bell GI. (1992) Cloning of a novel somatostatin receptor, SSTR3, coupled to adenylylcyclase. J Biol Chem, 267: 20422-20428. [PMID:1328199]