Page last updated: 2024-08-07 16:26:30
Somatostatin receptor type 1
A somatostatin receptor type 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P30872]
Synonyms
SS-1-R;
SS1-R;
SS1R;
SRIF-2
Research
Bioassay Publications (20)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 1 (5.00) | 18.2507 |
2000's | 14 (70.00) | 29.6817 |
2010's | 5 (25.00) | 24.3611 |
2020's | 0 (0.00) | 2.80 |
Compounds (11)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
obelin | Homo sapiens (human) | Kd | 0.0102 | 1 | 1 |
l 363301 | Homo sapiens (human) | Kd | 4.5700 | 1 | 1 |
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. 2. Analogues with beta-methyl-3-(2-naphthyl)alanine substitutions at position 8.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
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
A tetradecapeptide somatostatin dicarba-analog: Synthesis, structural impact and biological activity.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 24, Issue:1, 2014
[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
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
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
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
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
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
Enables
This protein enables 3 target(s):
Target | Category | Definition |
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] |
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] |
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 11 target(s):
Target | Category | Definition |
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] |
glutamate receptor signaling pathway | biological process | The series of molecular signals initiated by the binding of glutamate to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:mah, GOC:signaling, PMID:9131252] |
spermatogenesis | biological process | The developmental process by which male germ line stem cells self renew or give rise to successive cell types resulting in the development of a spermatozoa. [GOC:jid, ISBN:9780878933846, PMID:28073824, PMID:30990821] |
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] |
cerebellum development | biological process | The process whose specific outcome is the progression of the cerebellum over time, from its formation to the mature structure. The cerebellum is the portion of the brain in the back of the head between the cerebrum and the pons. In mice, the cerebellum controls balance for walking and standing, modulates the force and range of movement and is involved in the learning of motor skills. [GO_REF:0000021, GOC:cls, GOC:dgh, GOC:dph, GOC:jid, ISBN:0838580343] |
forebrain development | biological process | The process whose specific outcome is the progression of the forebrain over time, from its formation to the mature structure. The forebrain is the anterior of the three primary divisions of the developing chordate brain or the corresponding part of the adult brain (in vertebrates, includes especially the cerebral hemispheres, the thalamus, and the hypothalamus and especially in higher vertebrates is the main control center for sensory and associative information processing, visceral functions, and voluntary motor functions). [http://www2.merriam-webster.com/cgi-bin/mwmednlm?book=Medical&va=forebrain] |
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] |
response to starvation | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a starvation stimulus, deprivation of nourishment. [GOC:go_curators] |
cellular response to leukemia inhibitory factor | 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 leukemia inhibitory factor stimulus. [PMID:12801913] |
cellular response to estradiol 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 stimulus by estradiol, a C18 steroid hormone hydroxylated at C3 and C17 that acts as a potent estrogen. [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] |