Proteins > Hydroxycarboxylic acid receptor 2
Page last updated: 2024-08-07 13:40:04
Hydroxycarboxylic acid receptor 2
A hydroxycarboxylic acid receptor 2 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q8TDS4]
Synonyms
G-protein coupled receptor 109A;
G-protein coupled receptor HM74A;
Niacin receptor 1;
Nicotinic acid receptor
Research
Bioassay Publications (32)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 15 (46.88) | 29.6817 |
| 2010's | 16 (50.00) | 24.3611 |
| 2020's | 1 (3.13) | 2.80 |
Compounds (21)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Discovery of novel pyrrole derivatives as potent agonists for the niacin receptor GPR109A.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 30, Issue:10, 2020
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Discovery of coumarin-dihydroquinazolinone analogs as niacin receptor 1 agonist with in-vivo anti-obesity efficacy.European journal of medicinal chemistry, , May-25, Volume: 152, 2018
Synthesis and Characterization of Fatty Acid Conjugates of Niacin and Salicylic Acid.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Affinity and kinetics study of anthranilic acids as HCA2 receptor agonists.Bioorganic & medicinal chemistry, , Jul-15, Volume: 23, Issue:14, 2015
SAR studies of C2 ethers of 2H-pyrano[2,3-d]pyrimidine-2,4,7(1H,3H)-triones as nicotinic acid receptor (NAR) agonist.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 22, Issue:2, 2012
Discovery of SCH 900271, a Potent Nicotinic Acid Receptor Agonist for the Treatment of Dyslipidemia.ACS medicinal chemistry letters, , Jan-12, Volume: 3, Issue:1, 2012
Identification of Hydroxybenzoic Acids as Selective Lactate Receptor (GPR81) Agonists with Antilipolytic Effects.ACS medicinal chemistry letters, , Aug-09, Volume: 3, Issue:8, 2012
(1aR,5aR)1a,3,5,5a-Tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid (MK-1903): a potent GPR109a agonist that lowers free fatty acids in humans.Journal of medicinal chemistry, , Apr-26, Volume: 55, Issue:8, 2012
Discovery of a potent nicotinic Acid receptor agonist for the treatment of dyslipidemia.ACS medicinal chemistry letters, , Feb-10, Volume: 2, Issue:2, 2011
GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 20, Issue:15, 2010
Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).Bioorganic & medicinal chemistry letters, , May-01, Volume: 20, Issue:9, 2010
Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 20, Issue:11, 2010
Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.Journal of medicinal chemistry, , Mar-25, Volume: 53, Issue:6, 2010
Anthranilic acid replacements in a niacin receptor agonist.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 20, Issue:11, 2010
5-N,N-Disubstituted 5-aminopyrazole-3-carboxylic acids are highly potent agonists of GPR109b.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 2009
GPR109a agonists. Part 1: 5-Alkyl and 5-aryl-pyrazole-tetrazoles as agonists of the human orphan G-protein coupled receptor GPR109a.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
Pyrazole acids as niacin receptor agonists for the treatment of dyslipidemia.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
Molecular modeling aided design of nicotinic acid receptor GPR109A agonists.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
Analogues of acifran: agonists of the high and low affinity niacin receptors, GPR109a and GPR109b.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 17, Issue:20, 2007
Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor.Journal of medicinal chemistry, , Dec-13, Volume: 50, Issue:25, 2007
Nicotinic acid receptor agonists differentially activate downstream effectors.The Journal of biological chemistry, , Jun-22, Volume: 282, Issue:25, 2007
Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 17, Issue:24, 2007
Agonist lead identification for the high affinity niacin receptor GPR109a.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 17, Issue:17, 2007
Agonist lead identification for the high affinity niacin receptor GPR109a.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 17, Issue:17, 2007
Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 17, Issue:20, 2007
Nicotinic acid receptor agonists differentially activate downstream effectors.The Journal of biological chemistry, , Jun-22, Volume: 282, Issue:25, 2007
Affinity and kinetics study of anthranilic acids as HCA2 receptor agonists.Bioorganic & medicinal chemistry, , Jul-15, Volume: 23, Issue:14, 2015
5-N,N-Disubstituted 5-aminopyrazole-3-carboxylic acids are highly potent agonists of GPR109b.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 2009
Nicotinic acid receptor agonists.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Analogues of acifran: agonists of the high and low affinity niacin receptors, GPR109a and GPR109b.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
Agonist lead identification for the high affinity niacin receptor GPR109a.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 17, Issue:17, 2007
Nicotinic acid receptor agonists differentially activate downstream effectors.The Journal of biological chemistry, , Jun-22, Volume: 282, Issue:25, 2007
(1aR,5aR)1a,3,5,5a-Tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid (MK-1903): a potent GPR109a agonist that lowers free fatty acids in humans.Journal of medicinal chemistry, , Apr-26, Volume: 55, Issue:8, 2012
GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 20, Issue:15, 2010
Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).Bioorganic & medicinal chemistry letters, , May-01, Volume: 20, Issue:9, 2010
GPR109a agonists. Part 1: 5-Alkyl and 5-aryl-pyrazole-tetrazoles as agonists of the human orphan G-protein coupled receptor GPR109a.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
Enables
This protein enables 1 target(s):
| Target | Category | Definition |
|---|
| nicotinic acid receptor activity | molecular function | Combining with nicotinic acid to initiate a change in cell activity. [GOC:mah, PMID:12522134] |
Located In
This protein is located 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] |
| cell junction | cellular component | A cellular component that forms a specialized region of connection between two or more cells, or between a cell and the extracellular matrix, or between two membrane-bound components of a cell, such as flagella. [GOC:aruk, GOC:bc, GOC:mah, http://www.vivo.colostate.edu/hbooks/cmb/cells/pmemb/junctions_a.html, ISBN:0198506732, PMID:26820516, PMID:28096264] |
Active In
This protein is active 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] |
Involved In
This protein is involved in 5 target(s):
| Target | Category | Definition |
|---|
| neutrophil apoptotic process | biological process | Any apoptotic process in a neutrophil, any of the immature or mature forms of a granular leukocyte that in its mature form has a nucleus with three to five lobes connected by slender threads of chromatin, and cytoplasm containing fine inconspicuous granules and stainable by neutral dyes. [CL:0000775, GOC:add, GOC:mtg_apoptosis, PMID:12752675, PMID:12960266] |
| positive regulation of neutrophil apoptotic process | biological process | Any process that activates or increases the frequency, rate, or extent of neutrophil apoptotic process. [GOC:add, GOC:mtg_apoptosis] |
| negative regulation of lipid catabolic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the chemical reactions and pathways resulting in the breakdown of lipids. [GOC:ai] |
| positive regulation of adiponectin secretion | biological process | Any process that activates or increases the frequency, rate or extent of the regulated release of adiponectin from a cell. [GOC:BHF, GOC:mah] |
| 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] |