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Protein / target

Tissue-type plasminogen activator

Encoded byPLATP00750Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
8
Approved medicines
Open Targets target-level
View by indication →
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Serine-type endopeptidase

Strongest disease association

Pulmonary Embolism

Via encoding gene PLAT · Genetic evidence · score 0.19

Therapeutic position

Established drug target

Small molecules

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function overview

Converts the abundant, but inactive, zymogen plasminogen to plasmin by hydrolyzing a single Arg-Val bond in plasminogen.

View complete UniProt function annotation

Converts the abundant, but inactive, zymogen plasminogen to plasmin by hydrolyzing a single Arg-Val bond in plasminogen. By controlling plasmin-mediated proteolysis, it plays an important role in tissue remodeling and degradation, in cell migration and many other physiopathological events. During oocyte activation, plays a role in cortical granule reaction in the zona reaction, which contributes to the block to polyspermy (By similarity)

Subcellular location

Secreted, extracellular space
Domains and Gene Ontology detail (29)

Domains & features

Fibronectin type-IEGF-likeKringle 1Kringle 2Peptidase S1

Gene Ontology

  • Capical part of cell
  • Ccell surface
  • Ccytoplasm
  • Cextracellular exosome
  • Cextracellular region
  • Cextracellular space
  • Cglutamatergic synapse
  • CSchaffer collateral - CA1 synapse
  • Csecretory granule
  • Fphosphoprotein binding
  • Fserine-type endopeptidase activity
  • Fsignaling receptor binding

562 aa · 63 kDa · 4 isoforms

Biological roles

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Cell migrationUniProt · GOSynaptic signallingGOGrowth-factor signallingGOProteolysisUniProt · GOHaemostasisGO
View supporting evidence

Cell migration

  • ·Converts the abundant, but inactive, zymogen plasminogen to plasmin by hydrolyzing a sin…
  • ·smooth muscle cell migration

Synaptic signalling

  • ·glutamatergic synapse
  • ·Schaffer collateral - CA1 synapse
  • ·trans-synaptic signaling by BDNF, modulating synaptic transmission

Growth-factor signalling

  • ·platelet-derived growth factor receptor signaling pathway

Proteolysis

  • ·Converts the abundant, but inactive, zymogen plasminogen to plasmin by hydrolyzing a sin…
  • ·serine-type endopeptidase activity
  • ·negative regulation of proteolysis
  • ·proteolysis

Haemostasis

  • ·blood coagulation
  • ·fibrinolysis
  • ·negative regulation of fibrinolysis

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Approved medicines with mapped indications

1 medicine · 6 areas

Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.

Eye Diseases1 medicine
Heart Failure1 medicine
Myocardial Infarction1 medicine
Pulmonary Embolism1 medicine
Stroke1 medicine
Thrombosis1 medicine

8 medicines meet Open Targets' target-level approved-medicine definition; the 1 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.

Drugs targeting this protein

1

How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.

alteplase
Narrow target profileApprovedExogenous protein

Tissue-type plasminogen activator exogenous protein

Indicated for Eye Diseases, Heart Failure, Myocardial Infarction, Pulmonary Embolism

Direct interaction with this protein · Only this protein recorded as a target

ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.

Translational evidence

Open Targets 26

Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.

Strongest disease associations · via encoding gene PLAT

Gene-level evidence surfaced through the gene PLAT that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.

Pulmonary Embolism
0.77Well supported

Clinical evidence dominant · Open Targets 0.61

Myocardial Infarction
0.73Moderately supported

Clinical evidence dominant · Open Targets 0.59

Stroke
0.65Moderately supported

Clinical evidence dominant · Open Targets 0.51

Heart Failure
0.58Moderately supported

Clinical evidence dominant · Open Targets 0.47

Ischemic Stroke
0.58Moderately supported

Clinical evidence dominant · Open Targets 0.45

View evidence synthesis (5)
Pulmonary EmbolismWell supported
0.77
agreement 0.670.88
Clinical76%Genetic21%Literature3%

Open Targets aggregate 0.61 · 3 independent evidence families

Myocardial InfarctionModerately supported
0.73
agreement 0.580.89
Clinical92%Literature8%

Open Targets aggregate 0.59 · 2 independent evidence families

StrokeModerately supported
0.65
agreement 0.500.81
Clinical80%Literature20%

Open Targets aggregate 0.51 · 2 independent evidence families

Heart FailureModerately supported
0.58
agreement 0.430.74
Clinical94%Literature6%

Open Targets aggregate 0.47 · 2 independent evidence families

Ischemic StrokeModerately supported
0.58
agreement 0.430.74
Clinical80%Literature20%

Open Targets aggregate 0.45 · 2 independent evidence families

The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the per-type scores above show the calculation.

Show all associations
Pulmonary Embolism0.61
Myocardial Infarction0.59
Stroke0.51
Heart Failure0.47
ST Elevation Myocardial Infarction0.46
Ischemic Stroke0.45

Drug development

8 compounds recorded · 8 approved

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines. Distinct from the 1 drug that targets this protein in Forefront's canonical graph (1 with a mapped approved indication, shown above): these count different sets and are not a subset relation.

View all recorded compounds (8)
MONTEPLASEApproval
LANOTEPLASEPreapproval
RETEPLASEApproval
TENECTEPLASEApproval
PAMITEPLASEApproval
ALTEPLASEApproval
AMINOCAPROIC ACIDApproval
DUTEPLASEApproval

Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.

Tractability

Small moleculesStrong

Approved Drug and Structure with Ligand support this modality.

AntibodiesEmerging

Feasibility evidence (go cc high conf and uniprot loc med conf) — no clinical-stage drug of this modality recorded.

Protein degradersEmerging

Feasibility evidence (half-life data and small molecule binder) — no clinical-stage drug of this modality recorded.

Other modalitiesStrong

Approved Drug support this modality.

View underlying tractability evidence (11)
SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · Med-Quality PocketSM · Druggable FamilyAB · GO CC high confAB · UniProt loc med confAB · UniProt SigP or TMHMMPR · Half-life DataPR · Small Molecule BinderOC · Approved Drug

Raw Open Targets tractability assessment buckets, by modality.

Safety-related annotations

regulation of gene expressionToxCast

Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.

Clinical trials

30

Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.

View all trials (26)

RECRUITING · via alteplase · NCT05736757

ClinicalTrials.gov via the drug-target graph.

What's happening now

6

Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for a drug that targets this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.

  1. Trial status changed2026-08-12

    Intra-arterial Alteplase for Acute Ischemic Stroke After Mechanical Thrombectomy (PEARL): A Multicenter, Prospective, Open-label, Blinded Endpoint, Randomized Controlled Trial

    Status changed to Completed · ClinicalTrials.gov · via alteplase

  2. Product recall2024-05-20

    Recall (Class II): ALTEPLASE

    fda · safety · fda · via alteplase

  3. New publication2020-08-01
    Intrapleural Fibrinolytic Therapy versus Early Medical Thoracoscopy for Treatment of Pleural Infection. Randomized Controlled Clinical Trial.

    Annals of the American Thoracic Society · 2020 · 44 citations · Europe PMC · via alteplase

  4. New publication2015-02-11
    Endovascular therapy for ischemic stroke with perfusion-imaging selection.

    The New England journal of medicine · 2015 · 4,231 citations · Europe PMC · via alteplase

  5. New publication2010-01-14
    Effects of 0.6 mg/kg intravenous alteplase on vascular and clinical outcomes in middle cerebral artery occlusion: Japan Alteplase Clinical Trial II (J-ACT II).

    Stroke · 2010 · 121 citations · Europe PMC · via alteplase

  6. New publication2006-06-08
    Alteplase at 0.6 mg/kg for acute ischemic stroke within 3 hours of onset: Japan Alteplase Clinical Trial (J-ACT).

    Stroke · 2006 · 313 citations · Europe PMC · via alteplase

Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.

Related family literature

1

Papers about “Serine Proteases” — a broader family this protein belongs to. Shown as context; not counted as papers specifically about this protein.

Lipoprotein(a) as a Risk Factor for Cardiovascular Diseases: Pathophysiology and Treatment Perspectives.

Vinci P · International journal of environmental research and public health · 2023

via Serine Proteases

Europe PMC literature, reached through curated HGNC family membership. Membership is a taxonomic relationship — it does not imply this protein participates in every mechanism these papers discuss.