uPAR (urokinase plasminogen activator receptor)
A protein that helps cancer cells break through surrounding tissue and spread. Higher amounts on a tumour are linked to more aggressive disease, and a PET tracer built on a small peptide can measure how much of it a tumour has.
Overview
uPAR is a glycosylphosphatidylinositol-anchored cell-surface receptor for urokinase-type plasminogen activator (uPA); the uPA/uPAR system focuses proteolytic activity (activation of plasmin, which degrades extracellular matrix) at the cell surface, driving tumour cell invasion, matrix remodelling and metastasis. uPAR overexpression is an established biomarker of tumour aggressiveness across several common cancers, including prostate, breast, bladder and glioma, and correlates with independent prognostic information beyond PSA and Gleason score in prostate cancer.
The PET ligand 68Ga-NOTA-AE105 (and the earlier 64Cu-DOTA-AE105), based on the high-affinity peptide antagonist AE105, has been evaluated in first-in-human and phase 2 studies in prostate cancer, breast cancer, bladder cancer and glioma. In localised prostate cancer, tumour SUVmax on 68Ga-NOTA-AE105 PET correlated significantly with Gleason score (Spearman ρ = 0.55), and a SUVmax cut-off achieved 96% sensitivity for detecting Gleason score ≥3+4, raising the possibility of uPAR PET reducing the number of repeat biopsies needed in active surveillance. In glioma, uPAR-PET uptake was associated with worse overall and progression-free survival.
As a target, uPAR's strength is a genuine link to tumour aggressiveness and metastatic potential across multiple tumour types, giving it prognostic as well as localising value. Its main limitation to date is that all published clinical PET data come from small studies run predominantly by one research group, so multicentre validation is still needed, and no uPAR-targeted therapeutic radioligand has reached clinical use.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · A protein that helps cancer cells break through surrounding tissue and spread. Higher amounts on a tumour are linked to more aggressive disease, and a PET tracer built on a small peptide can measure how much of it a tumour has.
- 1 · What it is
A protein that helps cancer cells break through surrounding tissue and spread. Higher amounts on a tumour are linked to more aggressive disease, and a PET tracer built on a small peptide can measure how much of it a tumour has.
- 2 · What goes wrong in cancer
A GPI-anchored cell-surface receptor for urokinase-type plasminogen activator that focuses proteolytic activity at the cell surface, activating plasmin to degrade extracellular matrix and drive tumour invasion and metastasis.
- 3 · How drugs use it
No product in this corpus aims at uPAR (urokinase plasminogen activator receptor) yet. Because it sits on the outside of the cell, it can be reached from the bloodstream: antibodies flag the cell, ADCs deliver a toxin, radioligands deliver radiation, and CAR-T or bispecifics bring a T cell.
External identifiers
Biology
A GPI-anchored cell-surface receptor for urokinase-type plasminogen activator that focuses proteolytic activity at the cell surface, activating plasmin to degrade extracellular matrix and drive tumour invasion and metastasis. Its overexpression is an established biomarker of tumour aggressiveness in prostate, breast, bladder cancer and glioma.
- Prostate cancer: uPAR expression correlates with Gleason score and aggressiveness
- Glioma: uPAR-PET uptake associated with tumour grade and worse survival
- Breast cancer and urinary bladder cancer: uPAR overexpression linked to invasive and metastatic potential
- Normal tissue: low background expression, contributing to good image contrast
Latest papers
topQuery for this target: (TITLE:"uPAR" OR ABSTRACT:"uPAR" OR TITLE:"urokinase plasminogen activator receptor" OR ABSTRACT:"urokinase plasminogen activator receptor" OR TITLE:"PLAUR" OR ABSTRACT:"PLAUR") AND (radiopharmaceutical OR radioligand OR radionuclide OR theranostic OR "nuclear medicine" OR "molecular imaging" OR radiotracer OR scintigraphy OR cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about uPAR (urokinase plasminogen activator receptor), not a curated reading list.
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