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sst5 receptor

Family: Somatostatin receptors

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Agonists
Antagonists
Transduction Mechanisms
Tissue Distribution
Expression Datasets
Functional Assays
Physiological Functions
Physiological Consequences of Altering Gene Expression
Phenotypes, Alleles and Disease Models
Clinically-Relevant Mutations and Pathophysiology
References
Gene and Protein Information
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 29,48
Mouse 7 362 17 A3.3 Sstr5 somatostatin receptor 5 16,22
Rat 7 363 10q12 Sstr5 somatostatin receptor 5 27
Previous and Unofficial Names
SSTR5
SSTR4
SRIF1B
SRIF1
SOMATO
Smstr5
SS-5-R
SS5-R
SS5R
Somatostatin receptor subtype 5
somatostatin receptor type 5
sst5
Database Links
ChEMBL Target 11265 (Hs), 10347 (Mm), 12791 (Rn)
DrugBank Target 3872 (Hs)
Ensembl ENSG00000162009 (Hs), ENSMUSG00000050824 (Mm), ENSRNOG00000018834 (Rn)
Entrez Gene 6755 (Hs), 20609 (Mm), 25354 (Rn)
GeneCards SSTR5 (Hs)
GenitoUrinary Development Molecular Anatomy Project Sstr5 (Mm)
HomoloGene 20287 (Hs)
Human Protein Reference Database 01677 (Hs)
InterPro P35346 (Hs), O08858 (Mm), P30938 (Rn)
KEGG Gene hsa:6755 (Hs), mmu:20609 (Mm), rno:25354 (Rn)
OMIM 182455 (Hs)
Orphanet Gene ORPHA119872 (Hs)
PharmGKB Gene PA36158 (Hs)
PhosphoSitePlus P35346 (Hs), O08858 (Mm), P30938 (Rn)
Protein Ontology (PRO) PRO:000001672 (Hs)
RefSeq Nucleotide NM_001053 (Hs), NM_011425 (Mm), NM_012882 (Rn)
RefSeq Protein NP_001044 (Hs), NP_035555 (Mm), NP_037014 (Rn)
TreeFam ENSG00000162009 (Hs), ENSMUSG00000050824 (Mm), ENSRNOG00000018834 (Rn)
UniGene Hs. 449840 (Hs)
UniProt P35346 (Hs), O08858 (Mm), P30938 (Rn)
Wikipedia sst5 receptor
Somatostatin receptors
Search for 3D structures on the PDB
Search by keyword: Somatostatin receptors sst5 receptor Search by accession number: P30938, P35346, O08858
Natural/Endogenous Ligand(s)
CST-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
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[125I]LTT-SRIF-28 Mm Full agonist 11.0 pKd 14
[125I]LTT-SRIF-28 Hs Full agonist 10.5 pKd 41-42
[125I]Tyr10-CST14 Hs Full agonist 10.3 pKd 41-42
[125I]Tyr10-CST14 Mm Full agonist 10.2 pKd 14
[125I]Tyr11-SRIF-14 Hs Full agonist 10.0 pKd 28
[125I]Tyr11-SRIF-14 Rn Full agonist 10.0 pKd 28
[125I]CGP 23996 Mm Full agonist 9.8 pKd 14
[125I]Tyr3 SMS 201-995 Hs Full agonist 9.64 pKd 40,42
[125I]CGP 23996 Hs Full agonist 9.5 pKd 40,42
[125I]Tyr3 SMS 201-995 Mm Full agonist 9.4 pKd 14
[125I]LTT-SRIF-28 Hs Full agonist 9.2 pKd 35
BIM 23056 Mm Full agonist 7.5 – 7.9 pKd 14
L-363,301 Rn Full agonist 7.0 – 8.3 pKd 14
SRIF-28 {Sp: Human, Mouse, Rat} Mm Full agonist 9.8 – 9.9 pKi 14
SRIF-28 {Sp: Human, Mouse, Rat} Hs Full agonist 9.2 – 10.3 pKi 6,11,24,30,40-42
BIM 23059 Hs Full agonist 9.6 pKi 30
BIM 23313 Hs Full agonist 9.6 pKi 24
L-817,818 Hs Full agonist 9.4 pKi 35
CST-17 {Sp: Human} Hs Full agonist 8.5 – 10.2 pKi 11,41-42
CST-17 {Sp: Human} Mm Full agonist 8.8 – 9.8 pKi 14
SRIF-14 {Sp: Human, Mouse, Rat} Hs Full agonist 8.4 – 9.9 pKi 6,11,24,30-31,35,40-42,49
CST-14 {Sp: Mouse, Rat} Mm Full agonist 8.7 – 9.4 pKi 14
CST-14 {Sp: Mouse, Rat} Hs Full agonist 8.4 – 9.7 pKi 40-42
SRIF-28 {Sp: Human, Mouse, Rat} Rn Full agonist 9.0 pKi 24
BIM 23023 Hs Full agonist 8.4 – 9.4 pKi 24,30
BIM 23050 Hs Full agonist 8.8 pKi 30
octreotide Mm Full agonist 7.7 – 9.9 pKi 14
BIM 23268 Hs Full agonist 8.7 pKi 24
BIM 23052 Rn Full agonist 8.6 pKi 24
BIM 23060 Hs Full agonist 8.6 pKi 30
BIM 23052 Hs Full agonist 7.4 – 9.6 pKi 24,40-42
BIM 23268 Rn Full agonist 8.5 pKi 24
CGP 23996 Mm Full agonist 8.0 – 8.9 pKi 14
MK-678 Hs Full agonist 6.6 – 10.2 pKi 6,24,30,40-42,49
SRIF-14 {Sp: Human, Mouse, Rat} Mm Full agonist 7.7 – 9.1 pKi 14
SRIF-14 {Sp: Human, Mouse, Rat} Rn Full agonist 8.4 pKi 24
L-363,301 Hs Full agonist 7.2 – 9.5 pKi 41-42
lanreotide Hs Full agonist 7.4 – 9.3 pKi 6,24,30,40-42
octreotide Hs Full agonist 7.2 – 9.5 pKi 6,24,30,40-42,49
vapreotide Hs Full agonist 7.3 – 9.2 pKi 6,24,30,40-42
L-362,855 Hs Full agonist 7.2 – 9.2 pKi 24,40-42
L-362,855 Mm Full agonist 7.7 – 8.7 pKi 14
vapreotide Rn Full agonist 8.2 pKi 24
BIM 23313 Rn Full agonist 8.0 pKi 24
BIM 23023 Rn Full agonist 7.8 pKi 24
octreotide Rn Full agonist 7.8 pKi 24
CGP 23996 Hs Full agonist 6.6 – 8.7 pKi 40-42
lanreotide Rn Full agonist 7.6 pKi 24
MK-678 Mm Full agonist 6.7 – 8.5 pKi 14
BIM 23030 Mm Full agonist 7.1 – 8.0 pKi 14
BIM 23056 Hs Full agonist 6.7 – 8.3 pKi 24,30,40-42
L-362,855 Rn Full agonist 7.3 pKi 24
MK-678 Rn Full agonist 7.1 pKi 24
BIM 23030 Hs Full agonist 5.6 – 7.4 pKi 42
BIM 23056 Rn Full agonist 6.3 pKi 24
SOM-230 Hs Full agonist 9.8 pIC50 36
KE 108 Hs Full agonist 9.2 pIC50 34
BOC-ATE Hs Full agonist 8.4 pIC50 15
[111In]DOTA-BOC-ATE Hs Full agonist 8.4 pIC50 15
[111In]DOTA-NOC-ATE Hs Full agonist 8.4 pIC50 15
Des-AA5-[D-Trp8]SRIF Hs Full agonist 8.2 – 8.4 pIC50 13
BIM 23197 Hs Full agonist 8.0 pIC50 37
[111In]DOTA-NOC Hs Full agonist 8.0 pIC50 46
[111In,90Y]DOTA-NOC Hs Full agonist 8.0 pIC50 46
NOC-ATE Hs Full agonist 7.8 pIC50 15
[111In,90Y]DOTA-LAN Hs Full agonist 7.8 pIC50 46
[111In,90Y]DOTA-OC Hs Full agonist 7.2 pIC50 46
[111In,90Y]DOTA-TOC Hs Full agonist 6.7 pIC50 46
View species-specific agonist tables
Antagonists
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[L-Tyr8]CYN 154806 Hs Antagonist 7.3 – 9.1 pKi 26
BIM 23056 Hs Antagonist 7.4 – 8.3 pKi
PRL-2970 Hs Antagonist 7.3 pKi 17
[D-Tyr8]CYN 154806 Hs Antagonist 6.4 – 8.0 pKi 26
[D-Tyr8]CYN 154806 Mm Antagonist 6.6 – 7.5 pKi 14
[L-Tyr8]CYN 154806 Mm Antagonist 6.2 – 7.2 pKi 14
AC-178,335 Rn Antagonist 6.6 pKi 4
PRL-2915 Hs Antagonist 6.3 pKi 17
BIM 23627 Hs Antagonist 7.1 pIC50 45
BIM 23454 Hs Antagonist 6.9 pIC50 45
View species-specific antagonist tables

Explore drug-target interactions for this set of compounds using iPHACE

Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
References:  39
Secondary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family
Gq/G11 family 		Phospholipase C stimulation
Potassium channel
Calcium channel
Comments:  PLC activation is via the Gq G-protein. Activation of K+ channels and inhibition of Ca2+ is via Gi/Go G-proteins.
References:  2,19,38,44,47
Tissue Distribution
Small intestine, heart, adrenal, cerebellum, pituitary, placenta, skeletal muscle.
Species:  Human
Technique:  RT-PCR.
References:  28
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:  20
Whole placenta and cytotrophoblast cells.
Species:  Human
Technique:  RT-PCR.
References:  7
Pituitary.
Species:  Human
Technique:  RT-PCR.
References:  25
High levels in the hypothalamus and preoptic area. Medium levels in the hippocampus, striatum, amygdala, olfactory tubule, midbrain, olfactory bulb and cortex.
Species:  Rat
Technique:  Nuclease protection analysis.
References:  5
Pituitary.
Species:  Rat
Technique:  Nuclease protection analysis.
References:  5
Aorta.
Species:  Rat
Technique:  RT-PCR and immunocytochemistry.
References:  18
Fundic gastric mucosa of the stomach.
Species:  Rat
Technique:  RT-PCR.
References:  21
Pituitary.
Species:  Rat
Technique:  RT-PCR.
References:  10,12
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:  10
Spleen.
Species:  Rat
Technique:  Nuclease protection analysis.
References:  5
Expression Datasets

Click here to show/hide data

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]

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Functional Assays
Measurement of gastric acid secretion in vivo using rats.
Species:  Rat
Tissue:  In vivo.
Response measured:  Inhibition of gastric acid secretion.
References:  23
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:  37
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:  47
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:  38
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:  44
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:  8
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:  19
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:  9
Physiological Functions
Inhibition of GH release (synergistic with sst2).
Species:  Human
Tissue:  Primary fetal pituitary cell culture.
References:  33
Inhibition of insulin release.
Species:  Mouse
Tissue:  Pancreas.
References:  43
Antiproliferation.
Species:  Human
Tissue:  Umbilical vein endothelial cells.
References:  1
Physiological Consequences of Altering Gene Expression
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:  32
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:  43
Phenotypes, Alleles and Disease Models Mouse data from MGI

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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
Disease:  Acromegaly
OMIM:  102200
Orphanet:  963
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 Molecular location Description Reference
single nucleotide polymorphism Human R240W 3

REFERENCES

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To cite this database page, please use the following:

Jacques Epelbaum, Wasyl Feniuk, Anthony Harmar, Rebecca Hills, Daniel Hoyer, Patrick P. A. Humphrey, Wolfgang Meyerhof, Anne-Marie O'Carroll, Yogesh C. Patel, Terry Reisine, Jean-Claude Reubi, Marcus Schindler, Agnes Schonbrunn, John E. Taylor, Annamaria Vezzani.
Somatostatin receptors: sst5 receptor. Last modified on 15/02/2013. Accessed on 22/05/2013. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=359.


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