Tissue-type plasminogen activator

A tissue-type plasminogen activator that is encoded in the genome of human. [PRO:DNx, UniProtKB:P00750]

Synonyms

t-PA;
t-plasminogen activator;
tPA;
EC 3.4.21.68

Research

Bioassay Publications (33)

Timeframe	Studies on this Protein(%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	5 (15.15)	18.2507
2000's	19 (57.58)	29.6817
2010's	8 (24.24)	24.3611
2020's	1 (3.03)	2.80

Compounds (31)

Drugs with Inhibition Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
gallic acid	Homo sapiens (human)	IC50	6.6000	1	1
5-(n,n-hexamethylene)amiloride	Homo sapiens (human)	IC50	10.0000	1	1
benzamidine	Homo sapiens (human)	Ki	910.0000	1	1
bis(5-amidino-2-benzimidazolyl)methane	Homo sapiens (human)	Ki	2.3000	1	1
gabexate	Homo sapiens (human)	IC50	15.3600	1	1
hexachlorophene	Homo sapiens (human)	IC50	3.8000	1	1
1,2,5,8-tetrahydroxy anthraquinone	Homo sapiens (human)	IC50	4.4000	1	1
phenylguanidine	Homo sapiens (human)	Ki	733.0000	1	1
amiloride	Homo sapiens (human)	IC50	163.3333	3	3
amiloride	Homo sapiens (human)	Ki	345.7667	1	3
epigallocatechin gallate	Homo sapiens (human)	IC50	0.0910	1	1
sennoside A	Homo sapiens (human)	IC50	51.0000	1	1
mci 9038	Homo sapiens (human)	Ki	87.8000	1	1
dx 9065	Homo sapiens (human)	Ki	21.0000	1	1
efegatran	Homo sapiens (human)	IC50	10.5170	2	2
melagatran	Homo sapiens (human)	Ki	1.2050	2	2
beta-naphthamidine	Homo sapiens (human)	Ki	100.0000	2	2
razaxaban	Homo sapiens (human)	Ki	17.6500	4	4
dabigatran	Homo sapiens (human)	Ki	45.3600	1	1
benzamidine	Homo sapiens (human)	Ki	247.0769	3	13
Epigallocatechin 3,5-Digallate	Homo sapiens (human)	IC50	0.3300	1	1
bms 740808	Homo sapiens (human)	Ki	2.8000	1	1
bms-262084	Homo sapiens (human)	IC50	8.2500	1	1
uk-356,202	Homo sapiens (human)	Ki	0.0170	1	1
n-alpha-(2,4,6-triisopropyl-phenylsulfonyl)-3-amidino-(l)-phenyl-alanine-4-ethoxycarbonyl-piperazide hydrochloride	Homo sapiens (human)	Ki	4.9000	1	1
gw 813893	Homo sapiens (human)	IC50	25.1000	1	1
lb 30057	Homo sapiens (human)	Ki	27.2000	1	1
a-317567	Homo sapiens (human)	Ki	6.2300	1	1
betrixaban	Homo sapiens (human)	IC50	10.0000	1	1
rpr 120844	Homo sapiens (human)	Ki	8.6000	1	1
rpx7009	Homo sapiens (human)	IC50	1,000.0000	1	1

Drugs with Other Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
dpc 423	Homo sapiens (human)	Activity	45,000.0000	1	1

Enables

This protein enables 4 target(s):

Target	Category	Definition
serine-type endopeptidase activity	molecular function	Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain by a catalytic mechanism that involves a catalytic triad consisting of a serine nucleophile that is activated by a proton relay involving an acidic residue (e.g. aspartate or glutamate) and a basic residue (usually histidine). [GOC:mah, https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE]
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]
phosphoprotein binding	molecular function	Binding to a phosphorylated protein. [GOC:ai]

Located In

This protein is located in 8 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]
cytoplasm	cellular component	The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]
cell surface	cellular component	The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm]
secretory granule	cellular component	A small subcellular vesicle, surrounded by a membrane, that is formed from the Golgi apparatus and contains a highly concentrated protein destined for secretion. Secretory granules move towards the periphery of the cell and upon stimulation, their membranes fuse with the cell membrane, and their protein load is exteriorized. Processing of the contained protein may take place in secretory granules. [GOC:mah, ISBN:0198506732]
apical part of cell	cellular component	The region of a polarized cell that forms a tip or is distal to a base. For example, in a polarized epithelial cell, the apical region has an exposed surface and lies opposite to the basal lamina that separates the epithelium from other tissue. [GOC:mah, ISBN:0815316194]
extracellular exosome	cellular component	A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894]
Schaffer collateral - CA1 synapse	cellular component	A synapse between the Schaffer collateral axon of a CA3 pyramidal cell and a CA1 pyramidal cell. [PMID:16399689]
glutamatergic synapse	cellular component	A synapse that uses glutamate as a neurotransmitter. [GOC:dos]

Active In

This protein is active in 1 target(s):

Target	Category	Definition
extracellular space	cellular component	That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684]

Part Of

This protein is part of 1 target(s):

Target	Category	Definition
serine protease inhibitor complex	cellular component	A heterodimeric protein complex that contains a serine protease inhibitor and a protease; formation of the complex inhibits serine protease activity. [GOC:ans, PMID:6323392]

Involved In

This protein is involved in 13 target(s):

Target	Category	Definition
response to hypoxia	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 lowered oxygen tension. Hypoxia, defined as a decline in O2 levels below normoxic levels of 20.8 - 20.95%, results in metabolic adaptation at both the cellular and organismal level. [GOC:hjd]
proteolysis	biological process	The hydrolysis of proteins into smaller polypeptides and/or amino acids by cleavage of their peptide bonds. [GOC:bf, GOC:mah]
blood coagulation	biological process	The sequential process in which the multiple coagulation factors of the blood interact, ultimately resulting in the formation of an insoluble fibrin clot; it may be divided into three stages: stage 1, the formation of intrinsic and extrinsic prothrombin converting principle; stage 2, the formation of thrombin; stage 3, the formation of stable fibrin polymers. [PMID:30700128]
negative regulation of plasminogen activation	biological process	Any process that decreases the rate, frequency or extent of plasminogen activation. Plasminogen activation is the process in which plasminogen is processed to plasmin. [GOC:BHF, GOC:dph, GOC:tb]
plasminogen activation	biological process	The process in which inactive plasminogen is processed to active plasmin. This process includes cleavage at an internal Arg-Val site to form an N-terminal A-chain and C-terminal B-chain held together by a disulfide bond, and can include further proteolytic cleavage events to remove the preactivation peptide. [PMID:9548733]
protein modification process	biological process	The covalent alteration of one or more amino acids occurring in proteins, peptides and nascent polypeptides (co-translational, post-translational modifications). Includes the modification of charged tRNAs that are destined to occur in a protein (pre-translation modification). [GOC:bf, GOC:jl]
fibrinolysis	biological process	A process that solubilizes fibrin in the bloodstream of a multicellular organism, chiefly by the proteolytic action of plasmin. [GOC:jl, PMID:15842654]
negative regulation of proteolysis	biological process	Any process that stops, prevents, or reduces the frequency, rate or extent of the hydrolysis of a peptide bond or bonds within a protein. [GOC:go_curators]
negative regulation of fibrinolysis	biological process	Any process that stops, prevents, or reduces the frequency, rate or extent of fibrinolysis, an ongoing process that solubilizes fibrin, resulting in the removal of small blood clots. [GOC:ai]
prevention of polyspermy	biological process	The negative regulation of fertilization process that takes place as part of egg activation, ensuring that only a single sperm fertilizes the egg. [GOC:dph]
trans-synaptic signaling by BDNF, modulating synaptic transmission	biological process	Cell-cell signaling between presynapse and postsynapse, via the vesicular release and reception of brain derived neurotrophic factor (BDNF), that modulates the synaptic transmission properties of the synapse. [GOC:dos]
platelet-derived growth factor receptor signaling pathway	biological process	The series of molecular signals initiated by a ligand binding to a platelet-derived growth factor receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb]
smooth muscle cell migration	biological process	The orderly movement of a smooth muscle cell from one site to another, often during the development of a multicellular organism. [CL:0000192, GOC:mtg_muscle]

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