Somatostatin receptor 5 explained

Somatostatin receptor type 5 is a protein that in humans is encoded by the SSTR5 gene.^[1]

Somatostatin acts at many sites to inhibit the release of many hormones and other secretory proteins. The biological effects of somatostatin are probably mediated by a family of G protein-coupled receptors that are expressed in a tissue-specific manner. SSTR5 is a member of the superfamily of receptors having seven transmembrane segments.^[2]

Ligands

Agonists

• L-817818 ^[3]
• Zavolosotine ^[4]

See also

• Somatostatin receptor

Further reading

• Yamada Y, Post SR, Wang K, etal . Cloning and functional characterization of a family of human and mouse somatostatin receptors expressed in brain, gastrointestinal tract, and kidney. . Proc. Natl. Acad. Sci. U.S.A. . 89 . 1 . 251–5 . 1992 . 1346068 . 10.1073/pnas.89.1.251 . 48214 . 1992PNAS...89..251Y . free .
• Montminy MR, Goodman RH, Horovitch SJ, Habener JF . Primary structure of the gene encoding rat preprosomatostatin. . Proc. Natl. Acad. Sci. U.S.A. . 81 . 11 . 3337–40 . 1984 . 6145156 . 10.1073/pnas.81.11.3337 . 345502 . 1984PNAS...81.3337M . free .
• Panetta R, Greenwood MT, Warszynska A, etal . Molecular cloning, functional characterization, and chromosomal localization of a human somatostatin receptor (somatostatin receptor type 5) with preferential affinity for somatostatin-28. . Mol. Pharmacol. . 45 . 3 . 417–27 . 1994 . 7908405 .
• O'Carroll AM, Raynor K, Lolait SJ, Reisine T . Characterization of cloned human somatostatin receptor SSTR5. . Mol. Pharmacol. . 46 . 2 . 291–8 . 1994 . 8078491 .
• Yamada Y, Kagimoto S, Kubota A, etal . Cloning, functional expression and pharmacological characterization of a fourth (hSSTR4) and a fifth (hSSTR5) human somatostatin receptor subtype. . Biochem. Biophys. Res. Commun. . 195 . 2 . 844–52 . 1993 . 8373420 . 10.1006/bbrc.1993.2122 .
• Yamada Y, Stoffel M, Espinosa R, etal . Human somatostatin receptor genes: localization to human chromosomes 14, 17, and 22 and identification of simple tandem repeat polymorphisms. . Genomics . 15 . 2 . 449–52 . 1993 . 8449518 . 10.1006/geno.1993.1088 .
• Fukusumi S, Kitada C, Takekawa S, etal . Identification and characterization of a novel human cortistatin-like peptide. . Biochem. Biophys. Res. Commun. . 232 . 1 . 157–63 . 1997 . 9125122 . 10.1006/bbrc.1997.6252 .
• Ain KB, Taylor KD, Tofiq S, Venkataraman G . Somatostatin receptor subtype expression in human thyroid and thyroid carcinoma cell lines. . J. Clin. Endocrinol. Metab. . 82 . 6 . 1857–62 . 1997 . 10.1210/jcem.82.6.4013 . 9177396 . 25337792 . free .
• de Lecea L, Ruiz-Lozano P, Danielson PE, etal . Cloning, mRNA expression, and chromosomal mapping of mouse and human preprocortistatin. . Genomics . 42 . 3 . 499–506 . 1997 . 9205124 . 10.1006/geno.1997.4763 .
• Jaïs P, Terris B, Ruszniewski P, etal . Somatostatin receptor subtype gene expression in human endocrine gastroentero-pancreatic tumours. . Eur. J. Clin. Invest. . 27 . 8 . 639–44 . 1997 . 9279525 . 10.1046/j.1365-2362.1997.1740719.x . 23503397 .
• Hukovic N, Panetta R, Kumar U, etal . The cytoplasmic tail of the human somatostatin receptor type 5 is crucial for interaction with adenylyl cyclase and in mediating desensitization and internalization. . J. Biol. Chem. . 273 . 33 . 21416–22 . 1998 . 9694905 . 10.1074/jbc.273.33.21416 . free .
• Sharma K, Patel YC, Srikant CB . C-terminal region of human somatostatin receptor 5 is required for induction of Rb and G1 cell cycle arrest. . Mol. Endocrinol. . 13 . 1 . 82–90 . 1999 . 9892014 . 10.1210/mend.13.1.0220 . free .
• Kumar U, Sasi R, Suresh S, etal . Subtype-selective expression of the five somatostatin receptors (hSSTR1-5) in human pancreatic islet cells: a quantitative double-label immunohistochemical analysis. . Diabetes . 48 . 1 . 77–85 . 1999 . 9892225 . 10.2337/diabetes.48.1.77 .
• Rocheville M, Lange DC, Kumar U, etal . Subtypes of the somatostatin receptor assemble as functional homo- and heterodimers. . J. Biol. Chem. . 275 . 11 . 7862–9 . 2000 . 10713101 . 10.1074/jbc.275.11.7862 . free .
• Rocheville M, Lange DC, Kumar U, etal . Receptors for dopamine and somatostatin: formation of hetero-oligomers with enhanced functional activity. . Science . 288 . 5463 . 154–7 . 2000 . 10753124 . 10.1126/science.288.5463.154 . 2000Sci...288..154R .
• Daniels RJ, Peden JF, Lloyd C, etal . Sequence, structure and pathology of the fully annotated terminal 2 Mb of the short arm of human chromosome 16. . Hum. Mol. Genet. . 10 . 4 . 339–52 . 2001 . 11157797 . 10.1093/hmg/10.4.339 . free .
• Ballarè E, Persani L, Lania AG, etal . Mutation of somatostatin receptor type 5 in an acromegalic patient resistant to somatostatin analog treatment. . J. Clin. Endocrinol. Metab. . 86 . 8 . 3809–14 . 2001 . 10.1210/jcem.86.8.7787 . 11502816 . 17616592 . free .
• Pasquali D, Notaro A, Esposito D, etal . [Somatostatin receptor genes expression and effects of octreotide on orbital fibroblasts from Graves' ophthalmopathy] . Minerva Endocrinol. . 26 . 3 . 175–9 . 2002 . 11753241 .
• Papotti M, Bongiovanni M, Volante M, etal . Expression of somatostatin receptor types 1-5 in 81 cases of gastrointestinal and pancreatic endocrine tumors. A correlative immunohistochemical and reverse-transcriptase polymerase chain reaction analysis. . Virchows Arch. . 440 . 5 . 461–75 . 2002 . 12021920 . 10.1007/s00428-002-0609-x . 28584328 .

External links

• Web site: Somatostatin Receptors: sst₅ . IUPHAR Database of Receptors and Ion Channels . International Union of Basic and Clinical Pharmacology . 2008-12-09 . 2016-03-03 . https://web.archive.org/web/20160303184415/http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2435 . dead .

Notes and References

1. Takeda J, Fernald AA, Yamagata K, Le Beau MM, Bell GI . Localization of human somatostatin receptor 5 gene (SSTR5) to chromosome band 16p13.3 by fluorescence in situ hybridization . Genomics . 26 . 3 . 638–9 . Aug 1995 . 7607700 . 10.1016/0888-7543(95)80195-R .
2. Web site: Entrez Gene: SSTR5 somatostatin receptor 5.
3. Zhang Y, Wu N, Li Q, Hu X, Wang L, Sun JG, Wang Z, Sun XH. Neuroprotective effect of the somatostatin receptor 5 agonist L-817,818 on retinal ganglion cells in experimental glaucoma. Exp Eye Res. 2021 Mar;204:108449.
4. https://patents.google.com/patent/WO2022177988A1 Ferrara-Cook C, Krasner AS. Somatostatin receptor type 5 agonist for the treatment of hyperinsulinism. WO 2022/177988