Proteins > Glucose-dependent insulinotropic receptor
Page last updated: 2024-08-07 18:47:01
Glucose-dependent insulinotropic receptor
A glucose-dependent insulinotropic receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q8TDV5]
Synonyms
G-protein coupled receptor 119
Research
Bioassay Publications (17)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (5.88) | 29.6817 |
| 2010's | 13 (76.47) | 24.3611 |
| 2020's | 3 (17.65) | 2.80 |
Compounds (4)
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| psn 632408 | Homo sapiens (human) | Activity | 0.6300 | 1 | 1 |
Design and biological evaluation of tetrahydropyridine derivatives as novel human GPR119 agonists.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 30, Issue:4, 2020
[no title available]Bioorganic & medicinal chemistry, , 08-07, Volume: 26, Issue:14, 2018
Novel 5-nitropyrimidine derivatives bearing endo-azabicyclic alcohols/amines as potent GPR119 agonists.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
Synthesis and biological evaluation of pyrimidine derivatives with diverse azabicyclic ether/amine as novel GPR119 agonist.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 27, Issue:11, 2017
Synthesis and biological evaluation of novel 2,4-disubstituted quinazoline analogues as GPR119 agonists.Bioorganic & medicinal chemistry, , Mar-01, Volume: 21, Issue:5, 2013
Synthesis and biological evaluation of 5-nitropyrimidine analogs with azabicyclic substituents as GPR119 agonists.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 23, Issue:5, 2013
Novel acylethanolamide derivatives that modulate body weight through enhancement of hypothalamic pro-opiomelanocortin (POMC) and/or decreased neuropeptide Y (NPY).Journal of medicinal chemistry, , Mar-14, Volume: 56, Issue:5, 2013
Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists.ACS medicinal chemistry letters, , Jun-09, Volume: 7, Issue:6, 2016
G Protein-Coupled Receptor 119 (GPR119) Agonists for the Treatment of Diabetes: Recent Progress and Prevailing Challenges.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 24, Issue:23, 2014
Discovery of structurally novel, potent and orally efficacious GPR119 agonists.Bioorganic & medicinal chemistry letters, , May-15, Volume: 24, Issue:10, 2014
Discovery of a potent G-protein-coupled receptor 119 agonist for the treatment of type 2 diabetes.Bioorganic & medicinal chemistry, , 04-01, Volume: 35, 2021
[no title available]European journal of medicinal chemistry, , Feb-15, Volume: 188, 2020
One-pot synthesis of novel tert-butyl-4-substituted phenyl-1H-1,2,3-triazolo piperazine/piperidine carboxylates, potential GPR119 agonists.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 29, Issue:23, 2019
Discovery of novel xanthine compounds targeting DPP-IV and GPR119 as anti-diabetic agents.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
Discovery of structurally novel, potent and orally efficacious GPR119 agonists.Bioorganic & medicinal chemistry letters, , May-15, Volume: 24, Issue:10, 2014
Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control.Bioorganic & medicinal chemistry letters, , May-15, Volume: 21, Issue:10, 2011
Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119.Journal of medicinal chemistry, , Sep-11, Volume: 51, Issue:17, 2008
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| G protein-coupled receptor activity | molecular function | Combining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR] |
| phosphatidylcholine binding | molecular function | Binding to a phosphatidylcholine, a glycophospholipid in which a phosphatidyl group is esterified to the hydroxyl group of choline. [GOC:mah, ISBN:0198506732] |
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] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| receptor complex | cellular component | Any protein complex that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:go_curators] |
Involved In
This protein is involved in 3 target(s):
| Target | Category | Definition |
|---|
| insulin secretion | biological process | The regulated release of proinsulin from secretory granules accompanied by cleavage of proinsulin to form mature insulin. In vertebrates, insulin is secreted from B granules in the B cells of the vertebrate pancreas and from insulin-producing cells in insects. [GOC:mah, ISBN:0198506732] |
| adenylate cyclase-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of adenylyl cyclase activity which results in an increase in the intracellular concentration of cyclic AMP (cAMP). This pathway is negatively regulated by phosphodiesterase, which cleaves cAMP and terminates the signaling. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
| regulation of metabolic process | biological process | Any process that modulates the frequency, rate or extent of the chemical reactions and pathways within a cell or an organism. [GOC:go_curators] |