Page last updated: 2024-08-07 16:33:03
Somatostatin receptor type 5
A somatostatin receptor type 5 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P35346]
Synonyms
SS-5-R;
SS5-R;
SS5R
Research
Bioassay Publications (24)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (4.17) | 18.2507 |
| 2000's | 18 (75.00) | 29.6817 |
| 2010's | 5 (20.83) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (13)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| obelin | Homo sapiens (human) | Kd | 1.7783 | 1 | 1 |
| l 363301 | Homo sapiens (human) | Kd | 0.0076 | 1 | 1 |
| somatostatin | Homo sapiens (human) | EC50 | 0.0001 | 2 | 2 |
Benzoxazole piperidines as selective and potent somatostatin receptor subtype 5 antagonists.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 19, Issue:21, 2009
Discovery of the first nonpeptidic, small-molecule, highly selective somatostatin receptor subtype 5 antagonists: a chemogenomics approach.Journal of medicinal chemistry, , Dec-13, Volume: 50, Issue:25, 2007
Novel sst(4)-selective somatostatin (SRIF) agonists. 3. Analogues amenable to radiolabeling.Journal of medicinal chemistry, , Dec-18, Volume: 46, Issue:26, 2003
Novel sst(4)-selective somatostatin (SRIF) agonists. 1. Lead identification using a betide scan.Journal of medicinal chemistry, , Dec-18, Volume: 46, Issue:26, 2003
Novel sst(4)-selective somatostatin (SRIF) agonists. 2. Analogues with beta-methyl-3-(2-naphthyl)alanine substitutions at position 8.Journal of medicinal chemistry, , Dec-18, Volume: 46, Issue:26, 2003
N-Methylated sst2 Selective Somatostatin Cyclic Peptide Analogue as a Potent Candidate for Treating Neurogenic Inflammation.ACS medicinal chemistry letters, , Jul-14, Volume: 2, Issue:7, 2011
A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential.Journal of medicinal chemistry, , Jun-05, Volume: 46, Issue:12, 2003
A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential.Journal of medicinal chemistry, , Jun-05, Volume: 46, Issue:12, 2003
Design, synthesis, and biological activities of potent and selective somatostatin analogues incorporating novel peptoid residues.Journal of medicinal chemistry, , Jul-16, Volume: 41, Issue:15, 1998
Ligand design for somatostatin receptor isoforms 4 and 5.European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
[DOTA]Somatostatin-14 analogs and their (111)In-radioligands: effects of decreasing ring-size on sst1-5 profile, stability and tumor targeting.European journal of medicinal chemistry, , Feb-12, Volume: 73, 2014
A tetradecapeptide somatostatin dicarba-analog: Synthesis, structural impact and biological activity.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 24, Issue:1, 2014
N-imidazolebenzyl-histidine substitution in somatostatin and in its octapeptide analogue modulates receptor selectivity and function.Journal of medicinal chemistry, , Sep-08, Volume: 54, Issue:17, 2011
Discovery of iodinated somatostatin analogues selective for hsst2 and hsst5 with excellent inhibition of growth hormone and prolactin release from rat pituitary cells.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
3-Thio-1,2,4-triazoles, novel somatostatin sst2/sst5 agonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 15, Issue:15, 2005
Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.Journal of medicinal chemistry, , Sep-08, Volume: 48, Issue:18, 2005
Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.Journal of medicinal chemistry, , Jan-27, Volume: 48, Issue:2, 2005
A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential.Journal of medicinal chemistry, , Jun-05, Volume: 46, Issue:12, 2003
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Identification of potent non-peptide somatostatin antagonists with sst(3) selectivity.Journal of medicinal chemistry, , Aug-30, Volume: 44, Issue:18, 2001
Novel non-peptide ligands for the somatostatin sst3 receptor.Bioorganic & medicinal chemistry letters, , Apr-23, Volume: 11, Issue:8, 2001
Synthesis of substituted imidazopyrazines as ligands for the human somatostatin receptor subtype 5.Bioorganic & medicinal chemistry letters, , Mar-12, Volume: 11, Issue:5, 2001
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| neuropeptide binding | molecular function | Interacting selectively and non-covalently and stoichiometrically with neuropeptides, peptides with direct synaptic effects (peptide neurotransmitters) or indirect modulatory effects on the nervous system (peptide neuromodulators). [http://www.wormbook.org/chapters/www_neuropeptides/neuropeptides.html] |
| somatostatin receptor activity | molecular function | Combining with somatostatin to initiate a change in cell activity. Somatostatin is a peptide hormone that regulates the endocrine system by signaling via G protein-coupled somatostatin receptors. Somatostatin has two active forms produced by proteolytic cleavage: a 14 amino acid peptide (SST-14) and a 28 amino acid peptide (SST-28). [GOC:ai, GOC:bf, Wikipedia:Somatostatin] |
Located In
This protein is located in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| neuron projection | cellular component | A prolongation or process extending from a nerve cell, e.g. an axon or dendrite. [GOC:jl, http://www.cogsci.princeton.edu/~wn/] |
Involved In
This protein is involved in 8 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of a nucleotide cyclase activity and a subsequent change in the concentration of a cyclic nucleotide. [GOC:mah, GOC:signaling, ISBN:0815316194] |
| negative regulation of cell population proliferation | biological process | Any process that stops, prevents or reduces the rate or extent of cell proliferation. [GOC:go_curators] |
| positive regulation of cytokinesis | biological process | Any process that activates or increases the frequency, rate or extent of the division of the cytoplasm of a cell, and its separation into two daughter cells. [GOC:mah] |
| somatostatin signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by somatostatin binding to a somatostatin receptor (SSTR), and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:bf, GOC:nhn, GOC:signaling, PMID:18006219, Wikipedia:Somatostatin] |
| cellular response to glucocorticoid stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a glucocorticoid stimulus. Glucocorticoids are hormonal C21 corticosteroids synthesized from cholesterol with the ability to bind with the cortisol receptor and trigger similar effects. Glucocorticoids act primarily on carbohydrate and protein metabolism, and have anti-inflammatory effects. [GOC:mah] |
| neuropeptide signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by a neuropeptide binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:mah, ISBN:0815316194] |
| regulation of insulin secretion | biological process | Any process that modulates the frequency, rate or extent of the regulated release of insulin. [GOC:ai] |