Top ▲

SST5 receptor

Click here for help

Target not currently curated in GtoImmuPdb

Target id: 359

Nomenclature: SST5 receptor

Family: Somatostatin receptors

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 364 16p13.3 SSTR5 somatostatin receptor 5 29,51
Mouse 7 362 17 12.62 cM Sstr5 somatostatin receptor 5 17,22
Rat 7 363 10q12 Sstr5 somatostatin receptor 5 27
Previous and Unofficial Names Click here for help
SOMATO
Database Links Click here for help
Specialist databases
GPCRdb ssr5_human (Hs), ssr5_mouse (Mm), ssr5_rat (Rn)
Other databases
Alphafold P35346 (Hs), O08858 (Mm), P30938 (Rn)
ChEMBL Target CHEMBL1792 (Hs), CHEMBL2733 (Mm), CHEMBL4318 (Rn)
DrugBank Target P35346 (Hs)
Ensembl Gene ENSG00000162009 (Hs), ENSMUSG00000050824 (Mm), ENSRNOG00000018834 (Rn)
Entrez Gene 6755 (Hs), 20609 (Mm), 25354 (Rn)
Human Protein Atlas ENSG00000162009 (Hs)
KEGG Gene hsa:6755 (Hs), mmu:20609 (Mm), rno:25354 (Rn)
OMIM 182455 (Hs)
Orphanet ORPHA119872 (Hs)
Pharos P35346 (Hs)
RefSeq Nucleotide NM_001053 (Hs), NM_011425 (Mm), NM_012882 (Rn)
RefSeq Protein NP_001044 (Hs), NP_035555 (Mm), NP_037014 (Rn)
UniProtKB P35346 (Hs), O08858 (Mm), P30938 (Rn)
Wikipedia SSTR5 (Hs)
Natural/Endogenous Ligands Click here for help
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 go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I]LTT-SRIF-28 Peptide Ligand is labelled Ligand is radioactive Mm Full agonist 11.0 pKd 15
⤷ pKd 11.0 [15]
[125I]Tyr10-CST14 Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 10.3 pKd 41,43
⤷ pKd 10.3 [41,43]
[125I]Tyr10-CST14 Peptide Ligand is labelled Ligand is radioactive Mm Full agonist 10.2 pKd 15
⤷ pKd 10.2 [15]
[125I]Tyr11-SRIF-14 Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 10.0 pKd 28
⤷ pKd 10.0 [28]
[125I]Tyr11-SRIF-14 Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Rn Full agonist 10.0 pKd 28
⤷ pKd 10.0 [28]
[125I]LTT-SRIF-28 Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 9.2 – 10.5 pKd 36,41,43
⤷ pKd 10.5 [41,43]
pKd 9.2 [36]
SRIF-28 {Sp: Human, Mouse, Rat} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 9.2 – 10.3 pKi 5,11,25,30,41-43
⤷ pKi 9.2 – 10.3 [5,11,25,30,41-43]
L-817,818 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.4 pKi 36
⤷ pKi 9.4 [36]
CST-17 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 8.5 – 10.2 pKi 11,41,43
⤷ pKi 8.5 – 10.2 [11,41,43]
SRIF-14 {Sp: Human, Mouse, Rat} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 8.4 – 9.9 pKi 5,11,25,30,32,36,41-43,52
⤷ pKi 8.4 – 9.9 [5,11,25,30,32,36,41-43,52]
cortistatin-14 {Sp: Mouse, Rat} Peptide Click here for species-specific activity table Hs Full agonist 8.4 – 9.7 pKi 41-43
⤷ pKi 8.4 – 9.7 [41-43]
BIM 23268 Peptide Hs Full agonist 8.7 pKi 25
⤷ pKi 8.7 [25]
lanreotide Peptide Approved drug Primary target of this compound Click here for species-specific activity table Hs Full agonist 7.4 – 9.3 pKi 5,25,30,41-43
⤷ pKi 7.4 – 9.3 [5,25,30,41-43]
octreotide Peptide Approved drug Click here for species-specific activity table Hs Full agonist 7.2 – 9.5 pKi 5,25,30,41-43,52
⤷ pKi 7.2 – 9.5 [5,25,30,41-43,52]
L-362,855 Peptide Click here for species-specific activity table Hs Full agonist 7.2 – 9.2 pKi 25,41-43
⤷ pKi 7.2 – 9.2 [25,41-43]
BIM 23056 Peptide Click here for species-specific activity table Hs Full agonist 6.7 – 8.3 pKi 25,30,41-43
⤷ pKi 6.7 – 8.3 [25,30,41-43]
zavolosotine Small molecule or natural product Hs Agonist >9.0 pEC50 14
⤷ pEC50 >9.0 (EC50 <1x10-9 M) [14]
pasireotide Peptide Approved drug Primary target of this compound Click here for species-specific activity table Hs Full agonist 9.8 pIC50 37
⤷ pIC50 9.8 [37]
[111In]DOTA-BOC-ATE Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.4 pIC50 16
⤷ pIC50 8.4 [16]
[111In]DOTA-NOC-ATE Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.4 pIC50 16
⤷ pIC50 8.4 [16]
[111In,90Y]DOTA-NOC Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.0 pIC50 49
⤷ pIC50 8.0 [49]
[111In,90Y]DOTA-TOC Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 6.7 pIC50 49
⤷ pIC50 6.7 [49]
veldoreotide Peptide Click here for species-specific activity table Hs Agonist - - 2
⤷ [2]
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
S5A1 Small molecule or natural product Hs Antagonist 9.3 pKi 13
⤷ pKi 9.3 (Ki 5.4x10-10 M) [13]
BIM 23056 Peptide Click here for species-specific activity table Hs Antagonist 7.4 – 8.3 pKi
⤷ pKi 7.4 – 8.3
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family Adenylyl cyclase inhibition
Potassium channel
Calcium channel
Comments:  GRK2-mediated agonist-selective phosphorylation and PP1γ-mediated dephosphorylation of threonine 333 (T333) regulates rapid internalization and recycling.
References:  31,39
Tissue Distribution Click here for help
Other structures: kidney
Species:  Human
Technique:  Immunohistochemistry
References:  23,48
Pancreatic islets: Mainly in beta-cells, co-localised with insulin. Moderately expressed in alpha-cells, co-localised with glucagon. Also predominant in delta-cells, co-localised with somatostatin.
Species:  Human
Technique:  immunocytochemistry.
References:  21
CNS: basal forebrain
Species:  Human
Technique:  Immunohistochemistry
References:  44
Anterior pituitary: GH- and ACTH producing cells, neuroendocrine cells of the intestine, pancreatic islets
Species:  Human
Technique:  Immunohistochemistry
References:  19
Endocrine system: anterior pituitary, endocrine pancreas, adrenal cortex, adrenal medulla, thyroid gland, ovary, testis, neuroendocrine / enterochromaffin-like cells of the GI mucosa
Species:  Human
Technique:  Immunohistochemistry
References:  23,48
Gastrointestinal tract: parotid gland
Species:  Human
Technique:  Immunohistochemistry
References:  23,48
Immune system: lymphocytes in the germinal center of lymph follicles, macrophages
Species:  Human
Technique:  Immunohistochemistry
References:  23,48
Pituitary: Somatotrophs (secrete GH), thyrotrophs (secrete TSH), lactotrophs (secrete PRL) as well as gonadotrophs and corticotrophs.
Species:  Rat
Technique:  double label in situ hybridisation.
References:  9
Expression Datasets Click here for help

Show »

Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

There should be a chart of expression data here, you may need to enable JavaScript!
Functional Assays Click here for help
Measurement of GH, TSH and PRL secretion from human fetal pituitary cells.
Species:  Human
Tissue:  Primary human fetal pituitary cells.
Response measured:  Reduction in GH and TSH secretion, no change to PRL secretion.
References:  38
Measurement of gastric acid secretion in vivo using rats.
Species:  Rat
Tissue:  In vivo.
Response measured:  Inhibition of gastric acid secretion.
References:  24
Measurement of PLC activity in CHO-K1 cells stably transfected with human sst5 receptors.
Species:  Human
Tissue:  CHO-K1 cells.
Response measured:  Stimulation of PLC activity.
References:  50
Measurement of PLC activity in CCL39 cells stably transfected with human sst5 receptors.
Species:  Human
Tissue:  CCL39 cells.
Response measured:  Stimulation of PLC activity.
References:  40
Measurement of Ca2+ currents in AtT-20 cells expressing sst5 receptors.
Species:  Mouse
Tissue:  AtT-20 cell line (mouse anterior pituitary).
Response measured:  Coupling to L-type Ca2+ current.
References:  46
Measurement of AC activity (cAMP levels) in CHO-K1 cells stably transfected with human sst5 receptors.
Species:  Human
Tissue:  CHO-K1 cells.
Response measured:  Inhibition of AC activity at low agonist concentrations, and activation of AC activity at higher concentrations, via different transduction pathways.
References:  6
Measurement of AC activity (cAMP levels) in CCL39 cells stably transfected with human sst5 receptors.
Species:  Human
Tissue:  CCL39 cells.
Response measured:  Inhibition of AC activity.
References:  39
Measurement of GIRK currents (inward potassium currents) in Xenopus oocyte cells stably transfected with rat sst5 receptors and GIRK1 channels.
Species:  Rat
Tissue:  Xenopus oocytes.
Response measured:  Activation of GIRK currents.
References:  20
Measurement of GH release from GC cells (growth cells) from a rat somatotroph tumour, treated with a sst1/sst2 subtype selective agonist.
Species:  Rat
Tissue:  GC cells (growth cells) from a rat somatotroph tumour endogenously expressing all 5 sst receptor subtypes.
Response measured:  Reduction in GH secretion.
References:  7
Physiological Functions Click here for help
Inhibition of GH release (synergistic with sst2).
Species:  Human
Tissue:  Primary fetal pituitary cell culture.
References:  34
Inhibition of insulin release.
Species:  Mouse
Tissue:  Pancreas.
References:  45
Antiproliferation.
Species:  Human
Tissue:  Umbilical vein endothelial cells.
References:  1
Physiological Consequences of Altering Gene Expression Click here for help
Mice lacking the sst5 receptor show subtype-selective sexually dimorphic changes in the brain and pancreatic islets. They show an up-regulation of sst2 and sst3 receptors, and a down-regulation of sst4 receptors in the female sst5 knock-out brain, but not the male. They show a reduction in SRIF mRNA and SRIF-like immunoreactivity in the male sst5 knock-out brain, but not the female. They show an up-regulation of sst1, sst2 and sst3 receptors in male sst5 knock-out pancreatic islets, but only an increase in sst3 in female sst5 knock-out islets. They show a reduction in SRIF-like immunoreactivity in male sst5 knock-out mice, but no change in female.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  33
Mice lacking the sst5 receptor appeared to be healthy, with no obvious phenotypic abnormalities. However, they show an increase in insulin levels and a reduction in the SRIF-induced inhibition of insulin secretion from the pancreatic islets. They show a decrease in blood glucose and plasma insulin levels, and increased leptin and glucagon concentrations compared with the wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  45
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

Show »

Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Sstr5tm1Hawi|Sstr5tm1Xpw|Tg(Ins2-cre)1Heed Sstr5tm1Hawi/Sstr5tm1Xpw,Tg(Ins2-cre)1Heed/0
involves: 129S7/SvEvBrd * C57BL/6 * CBA		 MGI:3603308  MGI:894282  MP:0003839 abnormal insulin clearance PMID: 15919085 
Sstr5tm1Hawi Sstr5tm1Hawi/Sstr5tm1Hawi
involves: 129S7/SvEvBrd * C57BL/6J		 MGI:894282  MP:0001262 decreased body weight PMID: 12511609 
Sstr5tm1Hawi Sstr5tm1Hawi/Sstr5tm1Hawi
involves: 129S7/SvEvBrd * C57BL/6J		 MGI:894282  MP:0005560 decreased circulating glucose level PMID: 12511609 
Sstr5tm1Hawi|Sstr5tm1Xpw|Tg(Ins2-cre)1Heed Sstr5tm1Hawi/Sstr5tm1Xpw,Tg(Ins2-cre)1Heed/0
involves: 129S7/SvEvBrd * C57BL/6 * CBA		 MGI:3603308  MGI:894282  MP:0005560 decreased circulating glucose level PMID: 15919085 
Sstr5tm1Hawi Sstr5tm1Hawi/Sstr5tm1Hawi
involves: 129S7/SvEvBrd * C57BL/6J		 MGI:894282  MP:0002727 decreased circulating insulin level PMID: 12511609 
Sstr5tm1Hawi|Sstr5tm1Xpw|Tg(Ins2-cre)1Heed Sstr5tm1Hawi/Sstr5tm1Xpw,Tg(Ins2-cre)1Heed/0
involves: 129S7/SvEvBrd * C57BL/6 * CBA		 MGI:3603308  MGI:894282  MP:0003059 decreased insulin secretion PMID: 15919085 
Sstr5tm1Kum Sstr5tm1Kum/Sstr5tm1Kum
involves: 129/Sv * C57BL/6J		 MGI:894282  MP:0003339 decreased pancreatic beta cell number PMID: 15223137 
Sstr5tm1Hawi|Sstr5tm1Xpw|Tg(Ins2-cre)1Heed Sstr5tm1Hawi/Sstr5tm1Xpw,Tg(Ins2-cre)1Heed/0
involves: 129S7/SvEvBrd * C57BL/6 * CBA		 MGI:3603308  MGI:894282  MP:0009181 decreased pancreatic delta cell number PMID: 15919085 
Sstr5tm1Hawi|Sstr5tm1Xpw|Tg(Ins2-cre)1Heed Sstr5tm1Hawi/Sstr5tm1Xpw,Tg(Ins2-cre)1Heed/0
involves: 129S7/SvEvBrd * C57BL/6 * CBA		 MGI:3603308  MGI:894282  MP:0005293 impaired glucose tolerance PMID: 15919085 
Sstr5tm1Hawi Sstr5tm1Hawi/Sstr5tm1Hawi
involves: 129S7/SvEvBrd * C57BL/6J		 MGI:894282  MP:0005292 improved glucose tolerance PMID: 12511609 
Sstr5tm1Hawi Sstr5tm1Hawi/Sstr5tm1Hawi
involves: 129S7/SvEvBrd * C57BL/6J		 MGI:894282  MP:0002712 increased circulating glucagon level PMID: 12511609 
Sstr5tm1Hawi|Sstr5tm1Xpw|Tg(Ins2-cre)1Heed Sstr5tm1Hawi/Sstr5tm1Xpw,Tg(Ins2-cre)1Heed/0
involves: 129S7/SvEvBrd * C57BL/6 * CBA		 MGI:3603308  MGI:894282  MP:0002079 increased circulating insulin level PMID: 15919085 
Sstr5tm1Hawi Sstr5tm1Hawi/Sstr5tm1Hawi
involves: 129S7/SvEvBrd * C57BL/6J		 MGI:894282  MP:0005669 increased circulating leptin level PMID: 12511609 
Sstr5tm1Hawi Sstr5tm1Hawi/Sstr5tm1Hawi
involves: 129S7/SvEvBrd * C57BL/6J		 MGI:894282  MP:0003058 increased insulin secretion PMID: 12511609 
Sstr5tm1Hawi|Sstr5tm1Xpw|Tg(Ins2-cre)1Heed Sstr5tm1Hawi/Sstr5tm1Xpw,Tg(Ins2-cre)1Heed/0
involves: 129S7/SvEvBrd * C57BL/6 * CBA		 MGI:3603308  MGI:894282  MP:0003058 increased insulin secretion PMID: 15919085 
Sstr5tm1Hawi Sstr5tm1Hawi/Sstr5tm1Hawi
involves: 129S7/SvEvBrd * C57BL/6J		 MGI:894282  MP:0002891 increased insulin sensitivity PMID: 12511609 
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Acromegaly
Disease Ontology: DOID:2449
OMIM: 102200
Orphanet: ORPHA963
Comments:  A point mutation of the sst5 caused activation of the MAPK cascade. The result was an acromegalic patient resistant to somatostatin treatment. The replacement of Arg240 with Trp within the 3rd cytoplasmic loop altered G-protein coupling, changing an inhibitory signal (to MAPK) into a stimulatory one.
References:  3
Click column headers to sort
Type Species Amino acid change Nucleotide change Description Reference
Missense Human R240W 3
Disease:  Pituitary adenoma, growth hormone-secreting, 1; PAGH1
Synonyms: Growth hormone secreting pituitary adenoma [Disease Ontology: DOID:6255]
Disease Ontology: DOID:6255
OMIM: 102200
Drugs:  Pasireotide significantly decreases cortisol levels in patients with Cushing´s disease in a Phase 3 study.
References:  8
Biologically Significant Variants Click here for help
Type:  Splice variant
Species:  Human
Description:  Two differently truncated sst5 variants (sstTMD5/sstTMD4) show a different expression pattern in normal tissue and pituitary tumors. Both splice variants are functionally active and show a predominant intracellular localization. Sst5TMD is selectively activated by somatostatin compared with cortistatin, while sst5TMD4 is exclusively activated by cortistatin and not somatostatin. The details of the transcripts provided by the authors are sst5TM5(DQ448303) and sst5TMD4 (DQ448304).
References:  10

References

Show »

1. Adams RL, Adams IP, Lindow SW, Atkin SL. (2004) Inhibition of endothelial proliferation by the somatostatin analogue SOM230. Clin Endocrinol (Oxf), 61 (4): 431-6. [PMID:15473874]

2. Afargan M, Janson ET, Gelerman G, Rosenfeld R, Ziv O, Karpov O, Wolf A, Bracha M, Shohat D, Liapakis G et al.. (2001) Novel long-acting somatostatin analog with endocrine selectivity: potent suppression of growth hormone but not of insulin. Endocrinology, 142 (1): 477-86. [PMID:11145612]

3. Ballarè E, Persani L, Lania AG, Filopanti M, Giammona E, Corbetta S, Mantovani S, Arosio M, Beck-Peccoz P, Faglia G et al.. (2001) Mutation of somatostatin receptor type 5 in an acromegalic patient resistant to somatostatin analog treatment. J Clin Endocrinol Metab, 86 (8): 3809-14. [PMID:11502816]

4. Baumbach WR, Carrick TA, Pausch MH, Bingham B, Carmignac D, Robinson IC, Houghten R, Eppler CM, Price LA, Zysk JR. (1998) A linear hexapeptide somatostatin antagonist blocks somatostatin activity in vitro and influences growth hormone release in rats. Mol Pharmacol, 54 (5): 864-73. [PMID:9804621]

5. 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]

6. Carruthers AM, Warner AJ, Michel AD, Feniuk W, Humphrey PP. (1999) Activation of adenylate cyclase by human recombinant sst5 receptors expressed in CHO-K1 cells and involvement of Galphas proteins. Br J Pharmacol, 126 (5): 1221-9. [PMID:10205012]

7. Cervia D, Zizzari P, Pavan B, Schuepbach E, Langenegger D, Hoyer D, Biondi C, Epelbaum J, Bagnoli P. (2003) Biological activity of somatostatin receptors in GC rat tumour somatotrophs: evidence with sst1-sst5 receptor-selective nonpeptidyl agonists. Neuropharmacology, 44 (5): 672-85. [PMID:12668053]

8. Colao A, Petersenn S, Newell-Price J, Findling JW, Gu F, Maldonado M, Schoenherr U, Mills D, Salgado LR, Biller BM et al.. (2012) A 12-month phase 3 study of pasireotide in Cushing's disease. N Engl J Med, 366 (10): 914-24. [PMID:22397653]

9. Day R, Dong W, Panetta R, Kraicer J, Greenwood MT, Patel YC. (1995) Expression of mRNA for somatostatin receptor (sstr) types 2 and 5 in individual rat pituitary cells. A double labeling in situ hybridization analysis. Endocrinology, 136 (11): 5232-5. [PMID:7588263]

10. Durán-Prado M, Gahete MD, Martínez-Fuentes AJ, Luque RM, Quintero A, Webb SM, Benito-López P, Leal A, Schulz S, Gracia-Navarro F et al.. (2009) Identification and characterization of two novel truncated but functional isoforms of the somatostatin receptor subtype 5 differentially present in pituitary tumors. J Clin Endocrinol Metab, 94 (7): 2634-43. [PMID:19401364]

11. 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]

12. 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]

13. Farb TB, Adeva M, Beauchamp TJ, Cabrera O, Coates DA, Meredith TD, Droz BA, Efanov A, Ficorilli JV, Gackenheimer SL et al.. (2017) Regulation of Endogenous (Male) Rodent GLP-1 Secretion and Human Islet Insulin Secretion by Antagonism of Somatostatin Receptor 5. Endocrinology, 158 (11): 3859-3873. [PMID:28938487]

14. Ferrara-Cook C, Krasner AS. (2022) Somatostatin receptor type 5 agonist for the treatment of hyperinsulinism. Patent number: WO2022177988A1. Assignee: Crinetics Pharmaceuticals. Priority date: 16/02/2016. Publication date: 25/08/2022.

15. 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]

16. 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]

17. Gordon DF, Woodmansee WW, Lewis SR, James RA, Wood WM, Ridgway EC. (1999) Cloning of the mouse somatostatin receptor subtype 5 gene: promoter structure and function. Endocrinology, 140 (12): 5598-608. [PMID:10579323]

18. Hocart SJ, Jain R, Murphy WA, Taylor JE, Coy DH. (1999) Highly potent cyclic disulfide antagonists of somatostatin. J Med Chem, 42 (11): 1863-71. [PMID:10354394]

19. Kaemmerer D, Lupp A, Peter L, Fischer E, Schulz S, Klöppel G, Hommann M. (2013) Correlation of monoclonal and polyclonal somatostatin receptor 5 antibodies in pancreatic neuroendocrine tumors. Int J Clin Exp Pathol, 6 (1): 49-54. [PMID:23236542]

20. 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]

21. Kumar U, Sasi R, Suresh S, Patel A, Thangaraju M, Metrakos P, Patel SC, Patel YC. (1999) 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. [PMID:9892225]

22. Lublin AL, Diehl NL, Hochgeschwender U. (1997) Isolation and characterization of the gene encoding the type 5 mouse (Mus musculus) somatostatin receptor (msst5). Gene, 195 (1): 63-6. [PMID:9300821]

23. Lupp A, Hunder A, Petrich A, Nagel F, Doll C, Schulz S. (2011) Reassessment of sst(5) somatostatin receptor expression in normal and neoplastic human tissues using the novel rabbit monoclonal antibody UMB-4. Neuroendocrinology, 94 (3): 255-64. [PMID:21952553]

24. Martínez V, Coy DH, Lloyd KC, Taché Y. (1996) Intracerebroventricular injection of somatostatin sst5 receptor agonist inhibits gastric acid secretion in rats. Eur J Pharmacol, 296 (2): 153-60. [PMID:8838451]

25. Meyerhof W. (1998) The elucidation of somatostatin receptor functions: a current view. Rev Physiol Biochem Pharmacol, 133: 55-108. [PMID:9600011]

26. Nunn C, Schoeffter P, Langenegger D, Hoyer D. (2003) Functional characterisation of the putative somatostatin sst2 receptor antagonist CYN 154806. Naunyn Schmiedebergs Arch Pharmacol, 367 (1): 1-9. [PMID:12616335]

27. O'Carroll AM, Lolait SJ, König M, Mahan LC. (1992) Molecular cloning and expression of a pituitary somatostatin receptor with preferential affinity for somatostatin-28. Mol Pharmacol, 42 (6): 939-46. [PMID:1362243]

28. O'Carroll AM, Raynor K, Lolait SJ, Reisine T. (1994) Characterization of cloned human somatostatin receptor SSTR5. Mol Pharmacol, 46 (2): 291-8. [PMID:8078491]

29. Panetta R, Greenwood MT, Warszynska A, Demchyshyn LL, Day R, Niznik HB, Srikant CB, Patel YC. (1994) 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. [PMID:7908405]

30. 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]

31. Petrich A, Mann A, Kliewer A, Nagel F, Strigli A, Märtens JC, Pöll F, Schulz S. (2013) Phosphorylation of threonine 333 regulates trafficking of the human sst5 somatostatin receptor. Mol Endocrinol, 27 (4): 671-82. [PMID:23418396]

32. 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]

33. Ramírez JL, Grant M, Norman M, Wang XP, Moldovan S, de Mayo FJ, Brunicardi C, Kumar U. (2004) Deficiency of somatostatin (SST) receptor type 5 (SSTR5) is associated with sexually dimorphic changes in the expression of SST and SST receptors in brain and pancreas. Mol Cell Endocrinol, 221 (1-2): 105-19. [PMID:15223137]

34. Ren SG, Taylor J, Dong J, Yu R, Culler MD, Melmed S. (2003) Functional association of somatostatin receptor subtypes 2 and 5 in inhibiting human growth hormone secretion. J Clin Endocrinol Metab, 88 (9): 4239-45. [PMID:12970293]

35. 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]

36. 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]

37. 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]

38. 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]

39. 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]

40. 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]

41. 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]

42. Siehler S, Seuwen K, Hoyer D. (1998) [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors. Eur J Pharmacol, 348 (2-3): 311-20. [PMID:9652348]

43. 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]

44. Stroh T, Kreienkamp HJ, Beaudet A. (1999) Immunohistochemical distribution of the somatostatin receptor subtype 5 in the adult rat brain: predominant expression in the basal forebrain. J Comp Neurol, 412 (1): 69-82. [PMID:10440710]

45. Strowski MZ, Kohler M, Chen HY, Trumbauer ME, Li Z, Szalkowski D, Gopal-Truter S, Fisher JK, Schaeffer JM, Blake AD et al.. (2003) Somatostatin receptor subtype 5 regulates insulin secretion and glucose homeostasis. Mol Endocrinol, 17 (1): 93-106. [PMID:12511609]

46. Tallent M, Liapakis G, O'Carroll AM, Lolait SJ, Dichter M, Reisine T. (1996) Somatostatin receptor subtypes SSTR2 and SSTR5 couple negatively to an L-type Ca2+ current in the pituitary cell line AtT-20. Neuroscience, 71 (4): 1073-81. [PMID:8684611]

47. 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]

48. Unger N, Ueberberg B, Schulz S, Saeger W, Mann K, Petersenn S. (2012) Differential expression of somatostatin receptor subtype 1-5 proteins in numerous human normal tissues. Exp Clin Endocrinol Diabetes, 120 (8): 482-9. [PMID:22976314]

49. 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]

50. Wilkinson GF, Feniuk W, Humphrey PP. (1997) Characterization of human recombinant somatostatin sst5 receptors mediating activation of phosphoinositide metabolism. Br J Pharmacol, 121 (1): 91-6. [PMID:9146892]

51. Yamada Y, Kagimoto S, Kubota A, Yasuda K, Masuda K, Someya Y, Ihara Y, Li Q, Imura H, Seino S et al.. (1993) 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. [PMID:8373420]

52. 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 USA, 95 (18): 10836-41. [PMID:9724791]

Contributors

Show »

How to cite this page