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DrugBank target: P00747

DrugBank target: P00747 (PLMN_HUMAN)     

Example drug-target structure: 1b2i

( There are 30 structures corresponding to this UniProt sequence in the PDB. Click the orange, plus icon above for a list. )

Plasminogen

Plasmin heavy chain A, Activation peptide, Angiostatin, Plasmin heavy chain A, short form, Plasmin light chain B.

Function

Plasmin dissolves the fibrin of blood clots and acts as a proteolytic factor in a variety of other processes including embryonic development, tissue remodeling, tumor invasion, and inflammation. In ovulation, weakens the walls of the Graafian follicle. It activates the urokinase-type plasminogen activator, collagenases and several complement zymogens, such as C1 and C5. Cleavage of fibronectin and laminin leads to cell detachment and apoptosis. Also cleaves fibrin, thrombospondin and von Willebrand factor. Its role in tissue remodeling and tumor invasion may be modulated by CSPG4. Binds to cells., Angiostatin is an angiogenesis inhibitor that blocks neovascularization and growth of experimental primary and metastatic tumors in vivo..

Enzyme

3.4.21.7   [EC->PDB]   [IntEnz]   [ExPASy]   [KEGG]  

Catalytic activity

Preferential cleavage: Lys-|-Xaa > Arg-|-Xaa; higher selectivity than trypsin. Converts fibrin into soluble products.

Disease(s)

Plasminogen deficiency (PLGD) [MIM:217090]: A disorder characterized by decreased serum plasminogen activity. Two forms of the disorder are distinguished: type 1 deficiency is additionally characterized by decreased plasminogen antigen levels and clinical symptoms, whereas type 2 deficiency, also known as dysplasminogenemia, is characterized by normal, or slightly reduced antigen levels, and absence of clinical manifestations. Plasminogen deficiency type 1 results in markedly impaired extracellular fibrinolysis and chronic mucosal pseudomembranous lesions due to subepithelial fibrin deposition and inflammation. The most common clinical manifestation of type 1 deficiency is ligneous conjunctivitis in which pseudomembranes formation on the palpebral surfaces of the eye progresses to white, yellow-white, or red thick masses with a wood-like consistency that replace the normal mucosa. Note=The disease is caused by mutations affecting the gene represented in this entry.

Schematic diagram of Pfam domains in target sequence plus wiring diagrams of PDB structures containing drug molecules

1b2i
1cea

Key:    PfamA domain  Secondary structure  Bound drug molecule

Sequence length: 809 a.a.

Approved drugs / biotech drugs targeting this protein

The DrugBank database identifies 2 drugs and 7 biotech drugs for this target protein:

 

 

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Generic name: DB06692 aprotinin
Formula: C284H432N84O79S7
Structure: There are no structures of this molecule in the PDB.

 

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Generic name: DB00031 tenecteplase
Formula: C2561H3919N747O781S40
Structure: There are no structures of this molecule in the PDB.

 

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Generic name: DB00015 reteplase
Formula: C1736H2671N499O522S22
Structure: There are no structures of this molecule in the PDB.

 

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Generic name: DB00009 alteplase
Formula: C2569H3928N746O781S40
Structure: There are no structures of this molecule in the PDB.

 

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Generic name: DB00086 streptokinase
Formula: C2100H3278N566O669S4
Structure: There are no structures of this molecule in the PDB.

 

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Generic name: DB00013 urokinase
Formula: C1376H2145N383O406S18
Structure: There are no structures of this molecule in the PDB.
Generic name: DB00302 tranexamic acid
AMH
Formula: C8H15No2
Structure: There are 2 PDB structures containing this molecule and all are bound to the above target protein.

 

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Generic name: DB00029 anistreplase
Formula: C2569H3928N746O781S40
Structure: There are no structures of this molecule in the PDB.
Generic name: DB00513 aminocaproic acid
ACA
Formula: C6H13No2
Structure: There are 36 PDB structures containing this molecule of which 3 are bound to the above target protein.

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