Proteinase-activated receptor 1

A proteinase-activated receptor 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P25116]

Synonyms

PAR-1;
Coagulation factor II receptor;
Thrombin receptor

Research

Bioassay Publications (15)

Timeframe	Studies on this Protein(%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	1 (6.67)	18.2507
2000's	2 (13.33)	29.6817
2010's	11 (73.33)	24.3611
2020's	1 (6.67)	2.80

Compounds (15)

Drugs with Inhibition Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
omega-n-methylarginine	Homo sapiens (human)	IC50	0.0018	1	2
vu0099704	Homo sapiens (human)	IC50	10.0000	1	1
2-bromo-N-[3-(1-oxopropylamino)phenyl]benzamide	Homo sapiens (human)	IC50	3.2082	2	3
2-bromo-N-[3-(1-oxobutylamino)phenyl]benzamide	Homo sapiens (human)	IC50	0.6035	2	4
sch 79797	Homo sapiens (human)	IC50	0.0560	2	2
morphine	Homo sapiens (human)	Ki	0.0022	1	1
tapentadol	Homo sapiens (human)	Ki	0.1600	1	1
rwj-56110	Homo sapiens (human)	IC50	0.4400	1	1
vorapaxar	Homo sapiens (human)	IC50	0.0626	8	8
vorapaxar	Homo sapiens (human)	Ki	0.0077	5	5
e 5555	Homo sapiens (human)	IC50	0.0323	1	2
AZ3451	Homo sapiens (human)	IC50	50.0000	1	1

Drugs with Activation Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
ultram	Homo sapiens (human)	EC50	1.3000	1	2
morphine	Homo sapiens (human)	EC50	0.0037	1	2
tapentadol	Homo sapiens (human)	EC50	0.6700	1	2
o-demethyltramadol	Homo sapiens (human)	EC50	0.1200	1	2

Drugs with Other Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one	Homo sapiens (human)	Imax	25.0000	2	2
zstk474	Homo sapiens (human)	Imax	1.3750	2	2

Enables

This protein enables 6 target(s):

Target	Category	Definition
G-protein alpha-subunit binding	molecular function	Binding to a G-protein alpha subunit. The alpha subunit binds a guanine nucleotide. [GOC:hjd]
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]
signaling receptor binding	molecular function	Binding to one or more specific sites on a receptor molecule, a macromolecule that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:bf, GOC:ceb, ISBN:0198506732]
protein binding	molecular function	Binding to a protein. [GOC:go_curators]
thrombin-activated receptor activity	molecular function	A G protein-coupled receptor activity that is activated by cleavage by thrombin, which exposes a tethered ligand corresponding to the new N-terminus, which binds to the receptor and activates it. [GOC:ai, GOC:pg, PMID:20423334]
G-protein beta-subunit binding	molecular function	Binding to a G-protein beta subunit. [GOC:mah]

Located In

This protein is located in 10 target(s):

Target	Category	Definition
extracellular region	cellular component	The space external to the outermost structure of a cell. For cells without external protective or external encapsulating structures this refers to space outside of the plasma membrane. This term covers the host cell environment outside an intracellular parasite. [GOC:go_curators]
early endosome	cellular component	A membrane-bounded organelle that receives incoming material from primary endocytic vesicles that have been generated by clathrin-dependent and clathrin-independent endocytosis; vesicles fuse with the early endosome to deliver cargo for sorting into recycling or degradation pathways. [GOC:mah, NIF_Subcellular:nlx_subcell_20090701, PMID:19696797]
late endosome	cellular component	A prelysosomal endocytic organelle differentiated from early endosomes by lower lumenal pH and different protein composition. Late endosomes are more spherical than early endosomes and are mostly juxtanuclear, being concentrated near the microtubule organizing center. [NIF_Subcellular:nlx_subcell_20090702, PMID:11964142, PMID:2557062]
Golgi apparatus	cellular component	A membrane-bound cytoplasmic organelle of the endomembrane system that further processes the core oligosaccharides (e.g. N-glycans) added to proteins in the endoplasmic reticulum and packages them into membrane-bound vesicles. The Golgi apparatus operates at the intersection of the secretory, lysosomal, and endocytic pathways. [ISBN:0198506732]
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]
caveola	cellular component	A membrane raft that forms small pit, depression, or invagination that communicates with the outside of a cell and extends inward, indenting the cytoplasm and the cell membrane. Examples include flask-shaped invaginations of the plasma membrane in adipocytes associated with caveolin proteins, and minute pits or incuppings of the cell membrane formed during pinocytosis. Caveolae may be pinched off to form free vesicles within the cytoplasm. [GOC:mah, ISBN:0721662544, PMID:16645198]
cell surface	cellular component	The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm]
platelet dense tubular network	cellular component	A network of membrane-bounded compartments found in blood platelets, where they regulate platelet activation by sequestering or releasing calcium. The dense tubular network exists as thin elongated membranes in resting platelets, and undergoes a major ultrastructural change, to a rounded vesicular form, upon addition of thrombin. [PMID:1322202]
neuromuscular junction	cellular component	The junction between the axon of a motor neuron and a muscle fiber. In response to the arrival of action potentials, the presynaptic button releases molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane of the muscle fiber, leading to a change in post-synaptic potential. [GOC:nln]
postsynaptic membrane	cellular component	A specialized area of membrane facing the presynaptic membrane on the tip of the nerve ending and separated from it by a minute cleft (the synaptic cleft). Neurotransmitters cross the synaptic cleft and transmit the signal to the postsynaptic membrane. [ISBN:0198506732]

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 46 target(s):

Target	Category	Definition
connective tissue replacement involved in inflammatory response wound healing	biological process	The series of events leading to growth of connective tissue when loss of tissues that are incapable of regeneration occurs, or when fibrinous exudate cannot be adequately cleared, as part of an inflammatory response. [GOC:jal, PMID:9639571]
negative regulation of glomerular filtration	biological process	Any process that stops, prevents, or reduces the frequency, rate or extent of glomerular filtration. Glomerular filtration is the processs whereby blood is filtered by the glomerulus into the renal tubule. [GOC:mtg_cardio]
activation of cysteine-type endopeptidase activity involved in apoptotic process	biological process	Any process that initiates the activity of the inactive enzyme cysteine-type endopeptidase in the context of an apoptotic process. [GOC:al, GOC:dph, GOC:jl, GOC:mtg_apoptosis, GOC:tb, PMID:14744432, PMID:18328827, Wikipedia:Caspase]
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]
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]
phospholipase C-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 phospholipase C (PLC) and a subsequent increase in the intracellular concentration of inositol trisphosphate (IP3) and diacylglycerol (DAG). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194]
positive regulation of cytosolic calcium ion concentration	biological process	Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai]
protein kinase C-activating G protein-coupled receptor signaling pathway	biological process	The series of molecular signals generated as a consequence of a G protein-coupled receptor binding to its physiological ligand, where the pathway proceeds with activation of protein kinase C (PKC). PKC is activated by second messengers including diacylglycerol (DAG). [GOC:mah, GOC:signaling]
establishment of synaptic specificity at neuromuscular junction	biological process	The biological process in which a synapse between a motor neuron and a muscle is initially formed. [GOC:isa_complete]
positive regulation of cell population proliferation	biological process	Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators]
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]
response to wounding	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 stimulus indicating damage to the organism. [GOC:go_curators]
anatomical structure morphogenesis	biological process	The process in which anatomical structures are generated and organized. Morphogenesis pertains to the creation of form. [GOC:go_curators, ISBN:0521436125]
platelet activation	biological process	A series of progressive, overlapping events triggered by exposure of the platelets to subendothelial tissue. These events include shape change, adhesiveness, aggregation, and release reactions. When carried through to completion, these events lead to the formation of a stable hemostatic plug. [http://www.graylab.ac.uk/omd/]
regulation of blood coagulation	biological process	Any process that modulates the frequency, rate or extent of blood coagulation. [GOC:mah]
positive regulation of blood coagulation	biological process	Any process that activates or increases the frequency, rate or extent of blood coagulation. [GOC:mah]
positive regulation of cell migration	biological process	Any process that activates or increases the frequency, rate or extent of cell migration. [GOC:go_curators]
response to lipopolysaccharide	biological process	Any process that results in a change in state or activity of an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:add, ISBN:0721601464]
regulation of interleukin-1 beta production	biological process	Any process that modulates the frequency, rate, or extent of interleukin-1 beta production. [GOC:mah]
positive regulation of interleukin-6 production	biological process	Any process that activates or increases the frequency, rate, or extent of interleukin-6 production. [GOC:mah]
positive regulation of interleukin-8 production	biological process	Any process that activates or increases the frequency, rate, or extent of interleukin-8 production. [GOC:mah]
positive regulation of collagen biosynthetic process	biological process	Any process that activates or increases the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of collagen, any of a group of fibrous proteins of very high tensile strength that form the main component of connective tissue in animals. [GOC:mah]
positive regulation of Rho protein signal transduction	biological process	Any process that activates or increases the frequency, rate or extent of Rho protein signal transduction. [GOC:bf]
dendritic cell homeostasis	biological process	The process of regulating the proliferation and elimination of dendritic cells such that the total number of dendritic cells within a whole or part of an organism is stable over time in the absence of an outside stimulus. [CL:0000451, GOC:uh, PMID:12570827, PMID:19176316]
positive regulation of canonical NF-kappaB signal transduction	biological process	Any process that activates or increases the frequency, rate or extent of a canonical NF-kappaB signaling cascade. [GOC:jl]
positive regulation of cysteine-type endopeptidase activity involved in apoptotic process	biological process	Any process that activates or increases the activity of a cysteine-type endopeptidase involved in the apoptotic process. [GOC:jl, GOC:mtg_apoptosis]
positive regulation of MAPK cascade	biological process	Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators]
negative regulation of neuron apoptotic process	biological process	Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process in neurons. [GOC:go_curators, GOC:mtg_apoptosis]
positive regulation of GTPase activity	biological process	Any process that activates or increases the activity of a GTPase. [GOC:jl, GOC:mah]
cell-cell junction maintenance	biological process	The maintenance of junctions between cells. [GOC:ai]
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]
positive regulation of vasoconstriction	biological process	Any process that activates or increases the frequency, rate or extent of vasoconstriction. [GOC:go_curators]
positive regulation of smooth muscle contraction	biological process	Any process that activates or increases the frequency, rate or extent of smooth muscle contraction. [GOC:go_curators]
positive regulation of receptor signaling pathway via JAK-STAT	biological process	Any process that activates or increases the frequency, rate or extent of the JAK-STAT signaling pathway activity. [GOC:bf]
regulation of synaptic plasticity	biological process	A process that modulates synaptic plasticity, the ability of synapses to change as circumstances require. They may alter function, such as increasing or decreasing their sensitivity, or they may increase or decrease in actual numbers. [GOC:dph, GOC:jid, GOC:tb, PMID:11891290]
homeostasis of number of cells within a tissue	biological process	Any biological process involved in the maintenance of the steady-state number of cells within a population of cells in a tissue. [GOC:isa_complete]
release of sequestered calcium ion into cytosol	biological process	The process in which calcium ions sequestered in the endoplasmic reticulum, Golgi apparatus or mitochondria are released into the cytosolic compartment. [GOC:dph, GOC:hjd, GOC:mtg_lung, PMID:1814929]
positive regulation of release of sequestered calcium ion into cytosol	biological process	Any process that activates or increases the frequency, rate or extent of the release into the cytosolic compartment of calcium ions sequestered in the endoplasmic reticulum or mitochondria. [GOC:ai]
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	biological process	Any process that activates or increases the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai]
positive regulation of calcium ion transport	biological process	Any process that activates or increases the frequency, rate or extent of the directed movement of calcium ions into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai]
regulation of sensory perception of pain	biological process	Any process that modulates the frequency, rate or extent of the sensory perception of pain, the series of events required for an organism to receive a painful stimulus, convert it to a molecular signal, and recognize and characterize the signal. [GOC:ai]
platelet dense granule organization	biological process	A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of a platelet dense granule. A platelet dense granule is an electron-dense granule occurring in blood platelets that stores and secretes adenosine nucleotides and serotonin. They contain a highly condensed core consisting of serotonin, histamine, calcium, magnesium, ATP, ADP, pyrophosphate and membrane lysosomal proteins. [GOC:dph, PMID:11487378]
positive regulation of ERK1 and ERK2 cascade	biological process	Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:mah]
thrombin-activated receptor signaling pathway	biological process	A G protein-coupled receptor signaling pathway initiated by thrombin binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:mah, PMID:1672265]
trans-synaptic signaling by endocannabinoid, modulating synaptic transmission	biological process	Cell-cell signaling between presynapse and postsynapse, via the release and reception of endocannabinoid ligands, that modulates the synaptic transmission properties of the synapse. [GOC:dos, PMID:21531987]
negative regulation of renin secretion into blood stream	biological process	Any process that stops, prevents or reduces the frequency, rate or extent of renin secretion into blood stream. [GOC:TermGenie]