Proteins > Type-2 angiotensin II receptor
Page last updated: 2024-08-07 16:46:57
Type-2 angiotensin II receptor
An angiotensin II receptor 2 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P50052]
Synonyms
Angiotensin II type-2 receptor;
AT2
Research
Bioassay Publications (30)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 4 (13.33) | 18.2507 |
| 2000's | 13 (43.33) | 29.6817 |
| 2010's | 9 (30.00) | 24.3611 |
| 2020's | 4 (13.33) | 2.80 |
Compounds (29)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| ipsapirone | Homo sapiens (human) | EC50 | 0.0676 | 1 | 1 |
| flesinoxan | Homo sapiens (human) | EC50 | 0.0066 | 1 | 1 |
| bexarotene | Homo sapiens (human) | Kd | 0.0360 | 1 | 1 |
| alitretinoin | Homo sapiens (human) | Kd | 0.0425 | 2 | 2 |
| nrx 194204 | Homo sapiens (human) | Kd | 0.0036 | 1 | 1 |
| agn 194204 | Homo sapiens (human) | Kd | 0.0025 | 1 | 1 |
Structural determinants of subtype selectivity and functional activity of angiotensin II receptors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 26, Issue:4, 2016
Nonpeptidic angiotensin II AT₁ receptor antagonists derived from 6-substituted aminocarbonyl and acylamino benzimidazoles.European journal of medicinal chemistry, , Volume: 69, 2013
Design, synthesis and biological evaluation of 6-substituted aminocarbonyl benzimidazole derivatives as nonpeptidic angiotensin II AT1 receptor antagonists.European journal of medicinal chemistry, , Volume: 49, 2012
Synopsis of some recent tactical application of bioisosteres in drug design.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist.Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Using conformational constraints at position 6 of Angiotensin II to generate compounds with enhanced AT2R selectivity and proteolytic stability.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 43, 2021
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Structural determinants of subtype selectivity and functional activity of angiotensin II receptors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 26, Issue:4, 2016
Angiotensin II pseudopeptides containing 1,3,5-trisubstituted benzene scaffolds with high AT2 receptor affinity.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
AT2-selective angiotensin II analogues containing tyrosine-functionalized 5,5-bicyclic thiazabicycloalkane dipeptide mimetics.Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
A selective AT2 receptor ligand with a gamma-turn-like mimetic replacing the amino acid residues 4-5 of angiotensin II.Journal of medicinal chemistry, , Feb-12, Volume: 47, Issue:4, 2004
Multiple binding modes for the receptor-bound conformations of cyclic AII agonists.Journal of medicinal chemistry, , Jun-25, Volume: 36, Issue:13, 1993
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.Bioorganic & medicinal chemistry, , Dec-15, Volume: 18, Issue:24, 2010
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.Journal of medicinal chemistry, , Sep-03, Volume: 36, Issue:18, 1993
Synthesis and characterization of a new RXR agonist based on the 6-tert-butyl-1,1-dimethylindanyl structure.Bioorganic & medicinal chemistry letters, , Sep-16, Volume: 12, Issue:18, 2002
Enantioselective syntheses of potent retinoid X receptor ligands: differential biological activities of individual antipodes.Journal of medicinal chemistry, , Jul-05, Volume: 44, Issue:14, 2001
Structural determinants of subtype selectivity and functional activity of angiotensin II receptors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 26, Issue:4, 2016
Saralasin and Sarile Are AT2 Receptor Agonists.ACS medicinal chemistry letters, , Oct-09, Volume: 5, Issue:10, 2014
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: deBioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Multiple binding modes for the receptor-bound conformations of cyclic AII agonists.Journal of medicinal chemistry, , Jun-25, Volume: 36, Issue:13, 1993
[no title available]Bioorganic & medicinal chemistry, , 07-15, Volume: 66, 2022
[no title available]Bioorganic & medicinal chemistry, , 07-01, Volume: 65, 2022
Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist.Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
First reported nonpeptide AT1 receptor agonist (L-162,313) acts as an AT2 receptor agonist in vivo.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.Journal of medicinal chemistry, , Feb-02, Volume: 39, Issue:3, 1996
Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist.Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
First reported nonpeptide AT1 receptor agonist (L-162,313) acts as an AT2 receptor agonist in vivo.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.Journal of medicinal chemistry, , Feb-02, Volume: 39, Issue:3, 1996
The Other Angiotensin II Receptor: ATJournal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
Structural determinants of subtype selectivity and functional activity of angiotensin II receptors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 26, Issue:4, 2016
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.Journal of medicinal chemistry, , Feb-02, Volume: 39, Issue:3, 1996
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| angiotensin type II receptor activity | molecular function | An angiotensin receptor activity that acts via Gi protein coupling and cGMP (NO) generation, and may also act via additional signaling mechanisms. [GOC:mah, PMID:10977869] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| receptor antagonist activity | molecular function | The activity of a gene product that interacts with a receptor to decrease the ability of the receptor agonist to bind and activate the receptor. [GOC:ceb, ISBN:0198506732] |
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 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 25 target(s):
| Target | Category | Definition |
|---|
| blood vessel remodeling | biological process | The reorganization or renovation of existing blood vessels. [GOC:hjd] |
| regulation of systemic arterial blood pressure by circulatory renin-angiotensin | biological process | The process in which angiotensinogen metabolites in the bloodstream modulate the force with which blood passes through the circulatory system. The process begins when renin is released and cleaves angiotensinogen. [ISBN:0721643949] |
| angiotensin-mediated vasodilation involved in regulation of systemic arterial blood pressure | biological process | The process that increases the diameter of a blood vessel via the renin-angiotensin system. [GOC:pr, ISBN:0323031951, PMID:10425188] |
| brain renin-angiotensin system | biological process | The process in which an angiotensin-mediated signaling system present in the brain regulates the force with which blood passes through the circulatory system. [PMID:2909574] |
| cell surface receptor signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a receptor located on the cell surface. The pathway ends with regulation of a downstream cellular process, e.g. transcription. [GOC:signaling] |
| 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 cGMP nucleotide second messenger | biological process | The series of molecular signals generated as a consequence of a G protein-coupled receptor binding to its physiological ligand, followed by activation of guanylyl cyclase (GC) activity and a subsequent increase in the concentration of cyclic GMP (cGMP). [GOC:mah, GOC:signaling, ISBN:0815316194] |
| brain development | biological process | The process whose specific outcome is the progression of the brain over time, from its formation to the mature structure. Brain development begins with patterning events in the neural tube and ends with the mature structure that is the center of thought and emotion. The brain is responsible for the coordination and control of bodily activities and the interpretation of information from the senses (sight, hearing, smell, etc.). [GOC:dph, GOC:jid, GOC:tb, UBERON:0000955] |
| regulation of blood pressure | biological process | Any process that modulates the force with which blood travels through the circulatory system. The process is controlled by a balance of processes that increase pressure and decrease pressure. [GOC:dph, GOC:mtg_cardio, ISBN:0721643949] |
| negative regulation of heart rate | biological process | Any process that stops, prevents or reduces the frequency or rate of heart contraction. [GOC:dph, GOC:tb] |
| negative regulation of cell growth | biological process | Any process that stops, prevents, or reduces the frequency, rate, extent or direction of cell growth. [GOC:go_curators] |
| positive regulation of phosphoprotein phosphatase activity | biological process | Any process that activates or increases the activity of a phosphoprotein phosphatase. [GOC:mah] |
| regulation of metanephros size | biological process | Any process that modulates the size of a metanephric kidney. [GOC:bf] |
| exploration behavior | biological process | The specific behavior of an organism in response to a novel environment or stimulus. [GOC:BHF, GOC:pr, PMID:11682103, PMID:9767169] |
| nitric oxide-cGMP-mediated signaling | biological process | An intracellular signaling cassette in which the signal is passed on within the cell by nitric oxide (NO) activating soluble guanylyl cyclase (sGC). Includes synthesis of nitric oxide, guanylyl cyclase activity, and downstream effectors that further transmit the signal within the cell following activation by cGMP. [GOC:signaling, PMID:21549190, PMID:22019632] |
| angiotensin-activated signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by angiotensin II binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:BHF, GOC:mtg_cardiac_conduct_nov11, GOC:nhn, GOC:signaling, PMID:10977869] |
| vasodilation | biological process | An increase in the internal diameter of blood vessels, especially arterioles or capillaries, due to relaxation of smooth muscle cells that line the vessels, and usually resulting in a decrease in blood pressure. [GOC:pr, ISBN:0192800981] |
| negative regulation of blood vessel endothelial cell migration | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the migration of the endothelial cells of blood vessels. [GOC:go_curators] |
| positive regulation of DNA-templated transcription | biological process | Any process that activates or increases the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
| negative regulation of neurotrophin TRK receptor signaling pathway | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the neurotrophin TRK receptor signaling pathway. [GOC:ai] |
| neuron apoptotic process | biological process | Any apoptotic process in a neuron, the basic cellular unit of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the nervous system. [CL:0000540, GOC:mtg_apoptosis] |
| positive regulation of metanephric glomerulus development | biological process | Any process that increases the rate, frequency or extent of metanephric glomerulus development, the progression of the metanephric glomerulus over time from its initial formation until its mature state. The metanephric glomerulus is a capillary tuft surrounded by Bowman's capsule in nephrons of the vertebrate kidney, or metanephros. [GOC:mtg_kidney_jan10] |
| positive regulation of branching involved in ureteric bud morphogenesis | biological process | Any process that increases the rate, frequency or extent of branching involved in ureteric bud morphogenesis, the process in which the branching structure of the ureteric bud is generated and organized. The ureteric bud is an epithelial tube that grows out from the metanephric duct. The bud elongates and branches to give rise to the ureter and kidney collecting tubules. [GOC:dph, GOC:tb, GOC:yaf] |
| positive regulation of extrinsic apoptotic signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of extrinsic apoptotic signaling pathway. [GOC:mtg_apoptosis] |
| inflammatory response | biological process | The immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732] |