Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

PLAU (P00749) - Overview - Molecular Target Synopsis

Protein


PLAU, Urokinase-type plasminogen activator
Enzyme Classification 3.4.21.73
UniProt P00749

Also Known as UROK_HUMAN, PLAU

Specifically cleaves the zymogen plasminogen to form the active enzyme plasmin. Found in high and low molecular mass forms. Each consists of two chains, A and B. The high molecular mass form contains a long chain A which is cleaved to yield a short chain A. Forms heterodimer with SERPINA5. Binds LRP1B; binding is followed by internalization and degradation. Interacts with MRC2. Interacts with PLAUR.

6NMB
TRANEXAMIC ACID IS AN ACTIVE SITE INHIBITOR OF UROKINASE PLASMINOGEN ACTIVATOR
RCSB/PDB
Inspect Structure
See all 3D Structures for PLAU

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: PLAU is active in the following subcellular-locations: secreted.
GO terms: PLAU is active in the following subcellular-locations: cell surface, extracellular exosome, extracellular region, extracellular space, focal adhesion, plasma membrane, specific granule membrane, tertiary granule membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project PLAU has gain in 5 cell-lines, loss in 2 cell-lines and no signal in 997 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HOP_92, ACHN, SN12C

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HCC515, M059J, Hs 675.T

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: SK-N-SH, HSMM, HMEC

(see details)

3D Structures


For PLAU there are:
139 structures (179 chains) solved
91 are solved in complex with at least one small molecule ligand
2 are solved with an approved drug

PLAU is solved in complex with the approved drug(s):

AMH/TRANEXAMIC ACID (6NMB_A, 6NMB_B, 6NMB_C, 6NMB_D),
AMR/AMILORIDE (1F5L_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


PLAU has been screened with 1580 compounds (2079 bioactivities), 434 compounds have bioactivities that show binding affinity of <= 500nM (574 bioactivities). (see details)