Uniprot accession / id : P22777  OR   Uniprot accession / id : P05121  OR   Uniprot accession / id : A0A024QYT5
 
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Entry Information
Entry status  (1)
REL
(30)
 
Experimental methods  (1)
X-ray diffraction
(30)
 
Authors  (130)
Declerck PJ
(10)
Strelkov SV
(8)
Sillen M
(6)
Andreasen PA
(5)
Jensen JK
(4)
Weeks SD
(4)
Florova G
(3)
Gettins PG
(3)
Huang M
(3)
Idell S
(3)
Komissarov AA
(3)
Lawrence DA
(3)
Zhou X
(3)
Bucci JC
(2)
Buckley DI
(2)
Carrell RW
(2)
Deinum J
(2)
Dewilde M
(2)
Emal CD
(2)
Gils A
(2)
Graham H
(2)
Hong ZB
(2)
Huang MD
(2)
Huntington JA
(2)
Li S-H
(2)
Li SH
(2)
Lin ZH
(2)
Matthews DJ
(2)
Miyata T
(2)
Morth JP
(2)
Nissen P
(2)
Pannu NS
(2)
Peterson CB
(2)
Read RJ
(2)
Reinke AA
(2)
Sanders KL
(2)
Stein PE
(2)
Stout TJ
(2)
Stuckey JA
(2)
Thompson LC
(2)
Vaughan DE
(2)
Whisstock JC
(2)
Yuan C
(2)
Aertgeerts K
(1)
Al-Senaidy A
(1)
Baek K
(1)
Bauer M
(1)
Berkenpas MB
(1)
Bjorquist P
(1)
Björquist P
(1)
Bodin C
(1)
Carruthers AM
(1)
Compernolle G
(1)
Connor J
(1)
De Bondt HL
(1)
De Ranter CJ
(1)
Declerck P
(1)
Dufner P
(1)
Fjellstrom O
(1)
Fjellström O
(1)
Furie B
(1)
Furie BC
(1)
Gerard RD
(1)
Geschwindner S
(1)
Gettins PGW
(1)
Ginsburg D
(1)
Goldsmith EJ
(1)
Gong L
(1)
Gong LH
(1)
Gustafsson D
(1)
Han FQ
(1)
Han Q
(1)
Hu LH
(1)
Inghardt T
(1)
Jankun J
(1)
Jiang L
(1)
Johansson C
(1)
Johnson DJD
(1)
Lang D
(1)
Legnehed A
(1)
Lin Z
(1)
Linschoten M
(1)
Liu M
(1)
Lowe DC
(1)
Lundqvist T
(1)
Luo Z
(1)
Madsen JB
(1)
Mallinder PR
(1)
McPheat J
(1)
Mcpheat J
(1)
Min L
(1)
Mottonen J
(1)
Murray C
(1)
Murray LA
(1)
Musil D
(1)
Naiman B
(1)
Nar H
(1)
Nerme V
(1)
Newton P
(1)
Olsson K
(1)
 
More...
 
Homo / hetero assembly  (2)
homo
(18)
hetero
(12)
 
Assembly composition  (2)
protein structure
(18)
protein/protein complex
(12)
 
Assembly polymer count  (3)
monomer
(17)
dimer
(8)
trimer
(5)
 
Resolution distribution
1.5 - 2
(5)
2.0 - 2.5
(14)
2.5 - 3
(9)
3.0 - 3.5
(1)
3.5 - 4
(1)
 
Release year distribution
1995 - 2000
(7)
2000 - 2005
(4)
2005 - 2010
(4)
2010 - 2015
(11)
2015 - 2020
(7)
2020 - 2025
(6)
 
Journal  (13)
J Biol Chem
(5)
Int J Mol Sci
(3)
J Thromb Haemost
(3)
Nat Struct Biol
(3)
To be published
(3)
Biochemistry
(2)
J Struct Biol
(2)
Proc Natl Acad Sci U S A
(2)
Structure
(2)
Int J Mol Med
(1)
J Mol Biol
(1)
Protein Sci
(1)
Sci Rep
(1)
 
Macromolecules
Organism superkingdom  (1)
Eukaryota
(30)
 
Organism name  (2)
Homo sapiens
(29)
Mus musculus
(1)
 
Molecule name  (5)
Endothelial plasminogen activator inhibitor
(30)
PAI
(30)
PAI-1
(30)
Plasminogen activator inhibitor 1
(30)
Serpin E1
(30)
 
Molecule type  (1)
Protein
(30)
 
Gene names  (7)
PAI1
(29)
PLANH1
(29)
SERPINE1
(29)
Mr1
(1)
Pai1
(1)
Planh1
(1)
Serpine1
(1)
 
Interacting Molecules  (12)
VHH-2g-42
(3)
Tissue-type plasminogen activator chain B
(2)
VHH-2w-64
(2)
HEAVY CHAIN OF FAB FRAGMENT FROM AN PAI-1 ANTIBODY
(1)
LIGHT CHAIN OF FAB FRAGMENT FROM AN PAI-1 ANTIBODY
(1)
PENTAPEPTIDE
(1)
Plasminogen activator inhibitor 1
(1)
Somatomedin-B
(1)
Urokinase-type plasminogen activator chain B
(1)
VHH-2g-42 (Nb42)
(1)
VHH-2w-64 (Nb64)
(1)
VHH-s-a93 (Nb93)
(1)
 
Interacting ligands  (16)
CL : CHLORIDE ION
(3)
96P : (2S)-3-({[3-(trifluoromethyl)phenoxy]carbonyl}amino)propane-1,2-diyl bis(3,4,5-trihydroxybenzoate)
(2)
EDO : 1,2-ETHANEDIOL
(2)
NAG : 2-acetamido-2-deoxy-beta-D-glucopyranose
(2)
RV2 : 5-Chloro-2-[[2-[3-(furan-3-yl)anilino]-2-oxoacetyl]amino]benzoic acid
(2)
SO4 : SULFATE ION
(2)
ZN : ZINC ION
(2)
ACY : ACETIC ACID
(1)
BMA : beta-D-mannopyranose
(1)
DMS : DIMETHYL SULFOXIDE
(1)
EMJ : 2,5-dihydroxy-3-undecylcyclohexa-2,5-diene-1,4-dione
(1)
FUC : alpha-L-fucopyranose
(1)
GDE : 3,4,5-trihydroxybenzoic acid
(1)
GOL : GLYCEROL
(1)
RIP : beta-D-ribopyranose
(1)
TB7 : TERT-BUTYL 3-[(4-OXO-3H-PYRIDO[2,3-D]PYRIMIDIN-2-YL)AMINO]AZETIDINE-1-CARBOXYLATE
(1)
 
Function and Biology
Biological function  (6)
serine-type endopeptidase inhibitor activity
(30)
peptidase inhibitor activity
(28)
protein binding
(28)
endopeptidase inhibitor activity
(27)
protease binding
(27)
signaling receptor binding
(27)
 
Biological process  (33)
angiogenesis
(28)
defense response to Gram-negative bacterium
(28)
negative regulation of fibrinolysis
(28)
negative regulation of plasminogen activation
(28)
negative regulation of vascular wound healing
(28)
positive regulation of angiogenesis
(28)
cellular response to lipopolysaccharide
(27)
dentinogenesis
(27)
fibrinolysis
(27)
negative regulation of blood coagulation
(27)
negative regulation of cell adhesion mediated by integrin
(27)
negative regulation of cell migration
(27)
negative regulation of endothelial cell apoptotic process
(27)
negative regulation of extrinsic apoptotic signaling pathway via death domain receptors
(27)
negative regulation of integrin-mediated signaling pathway
(27)
negative regulation of proteolysis
(27)
negative regulation of smooth muscle cell migration
(27)
negative regulation of smooth muscle cell-matrix adhesion
(27)
negative regulation of thrombin-activated receptor signaling pathway
(27)
negative regulation of wound healing
(27)
positive regulation of blood coagulation
(27)
positive regulation of coagulation
(27)
positive regulation of inflammatory response
(27)
positive regulation of interleukin-8 production
(27)
positive regulation of leukotriene production involved in inflammatory response
(27)
positive regulation of monocyte chemotaxis
(27)
positive regulation of odontoblast differentiation
(27)
positive regulation of receptor-mediated endocytosis
(27)
replicative senescence
(27)
cellular response to transforming growth factor beta stimulus
(1)
placenta development
(1)
regulation of angiogenesis
(1)
regulation of cell population proliferation
(1)
 
Biological cell component  (8)
extracellular space
(30)
extracellular region
(28)
peptidase inhibitor complex
(28)
serine protease inhibitor complex
(28)
collagen-containing extracellular matrix
(27)
extracellular exosome
(27)
plasma membrane
(27)
platelet alpha granule lumen
(27)
 
Sequence and Structure classification
SCOP fold  (1)
Serpins
(9)
 
SCOP family  (1)
Serpins
(9)
 
CATH class  (2)
Alpha Beta
(24)
Mainly Beta
(24)
 
CATH topology  (2)
Alpha-1-antitrypsin; domain 1
(24)
Antithrombin; Chain I, domain 2
(24)
 
Pfam accession / name  (1)
PF00079 : Serpin
(30)
 
Experimental Information
Diffraction protocol  (1)
Single wavelength
(29)
 
Diffraction radiation source type  (2)
Synchrotron
(25)
Rotating anode
(5)
 
Diffraction source  (22)
SSRF BEAMLINE BL17U
(4)
APS BEAMLINE 21-ID-D
(2)
RIGAKU RUH3R
(2)
SIEMENS
(2)
SLS BEAMLINE X06SA
(2)
SOLEIL BEAMLINE PROXIMA 1
(2)
ALS BEAMLINE 5.0.3
(1)
APS BEAMLINE 19-ID
(1)
APS BEAMLINE 22-ID
(1)
EMBL/DESY, HAMBURG BEAMLINE BW7B
(1)
EMBL/DESY, HAMBURG BEAMLINE X13
(1)
ESRF BEAMLINE ID23-1
(1)
ESRF BEAMLINE ID23-2
(1)
ESRF BEAMLINE ID29
(1)
ESRF BEAMLINE ID30B
(1)
ESRF BEAMLINE MASSIF-3
(1)
NSLS BEAMLINE X12C
(1)
RIGAKU RUH2R
(1)
SLS BEAMLINE X10SA
(1)
SOLEIL BEAMLINE PROXIMA 2
(1)
SRS BEAMLINE PX14.1
(1)
SSRF BEAMLINE BL17U1
(1)
 
Synchrotron site  (9)
ESRF
(5)
SSRF
(5)
APS
(4)
SLS
(3)
SOLEIL
(3)
EMBL/DESY, Hamburg
(2)
ALS
(1)
NSLS
(1)
SRS
(1)
 
Diffraction detector type  (5)
CCD
(13)
Pixel
(9)
Image plate
(4)
Area detector
(3)
Diffractometer
(1)
 
Refinement software  (6)
PHENIX
(10)
REFMAC
(10)
X-PLOR
(5)
BUSTER
(3)
BUSTER-TNT
(2)
CNS
(2)
 
Representative Structures
Representative Structures
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Entries 1 to 10 of 30
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Crystal Structure of Small Molecule Inhibitor TM5484 Bound to Stabilized Active Plasminogen Activator Inhibitor-1 (PAI-1-stab)
Sillen M, Strelkov SV, Declerck PJ
Int J Mol Sci (2021) [PMID: 33540702  ]
Source organism: Homo sapiens  
Assembly composition: protein only structure
Bound ligands: RV2   
Assembly name: Plasminogen activator inhibitor 1 (Preferred)   search this complex
PDBe complex ID: PDB-CPX-138523 (Preferred)   search this ID
PDBe-KB: P05121   
X-ray diffraction
1.77Å resolution
Released: 17 Feb 2021
Model geometry
Fit model/data
7aqf
7aqf
7aqf
Structure of tPA and PAI-1
Min L, Huang M
To be published
Source organism: Homo sapiens  
Assembly composition: protein/protein complex
Bound ligands: GOL   
Assembly name: tPA-PAI-1 complex (Preferred)   search this complex
PDBe complex ID: PDB-CPX-133301 (Preferred)   search this ID
PDBe-KB: P05121    P00750   
X-ray diffraction
3.581Å resolution
Released: 3 Apr 2019
Model geometry
Fit model/data
5zlz
5zlz
5zlz
Michaelis complex of tPA-S195A:PAI-1
Gong L
J Biol Chem (2015) [PMID: 26324706  ]
Source organism: Homo sapiens  
Assembly composition: protein/protein complex
Bound ligands: GOL    PGE    PGE   
Assembly name: tPA-PAI-1 complex (Preferred)   search this complex
PDBe complex ID: PDB-CPX-133301 (Preferred)   search this ID
PDBe-KB: P05121    P00750   
X-ray diffraction
3.16Å resolution
Released: 2 Sep 2015
Model geometry
Fit model/data
5brr
5brr
5brr
Crystal Structure of Small Molecule Inhibitor TM5484 Bound to Stabilized Active Plasminogen Activator Inhibitor-1 (PAI-1-W175F)
Sillen M, Strelkov SV, Declerck PJ
Int J Mol Sci (2021) [PMID: 33540702  ]
Assembly composition: protein/protein complex
Bound ligands: RV2   
Assembly name: Plasminogen activator inhibitor 1 and IG-heavy chain and IG-heavy chain (Preferred)   search this complex
PDBe complex ID: PDB-CPX-209239 (Preferred)   search this ID
PDBe-KB: P05121   
X-ray diffraction
2.27Å resolution
Released: 24 Feb 2021
Model geometry
Fit model/data
7aqg
7aqg
7aqg
CLEAVED SUBSTRATE VARIANT OF PLASMINOGEN ACTIVATOR INHIBITOR-1
Aertgeerts K, De Bondt HL, De Ranter CJ, Declerck PJ
Nat Struct Biol (1995) [PMID: 7552714  ]
Source organism: Homo sapiens  
Assembly composition: protein/protein complex
Assembly name: Plasminogen activator inhibitor 1 (Preferred)   search this complex
PDBe complex ID: PDB-CPX-272317 (Preferred)   search this ID
PDBe-KB: P05121   
X-ray diffraction
2.7Å resolution
Released: 19 Mar 1999
Model geometry
Fit model/data
9pai
9pai
9pai
Crystal Structure of Stabilized Active Plasminogen Activator Inhibitor-1 (PAI-1-W175F) in Complex with an Inhibitory Nanobody (VHH-s-a93, Nb93)
Sillen M, Weeks SD, Strelkov SV, Declerck PJ
Int J Mol Sci (2020) [PMID: 32824134  ]
Assembly composition: protein/protein complex
Assembly name: Plasminogen activator inhibitor 1 and IG-heavy chain (Preferred)   search this complex
PDBe complex ID: PDB-CPX-279527 (Preferred)   search this ID
PDBe-KB: P05121   
X-ray diffraction
1.88Å resolution
Released: 26 Aug 2020
Model geometry
Fit model/data
6zrv
6zrv
6zrv
Crystal Structure of Stabilized Active Plasminogen Activator Inhibitor-1 (PAI-1-stab) in Complex with Two Inhibitory Nanobodies (VHH-2g-42, VHH-2w-64)
Sillen M, Weeks SD, Strelkov SV, Declerck PJ
J Thromb Haemost (2020) [PMID: 31858714  ]
Assembly composition: protein/protein complex
Assembly name: Plasminogen activator inhibitor 1 and IG-heavy chain and IG-heavy chain (Preferred)   search this complex
PDBe complex ID: PDB-CPX-209235 (Preferred)   search this ID
PDBe-KB: P05121   
X-ray diffraction
2.28Å resolution
Released: 1 Jan 2020
Model geometry
Fit model/data
6gwp
6gwp
6gwp
Discovery and characterisation of an antibody that selectively modulates the inhibitory activity of plasminogen activator inhibitor-1
Vousden KA, Lundqvist T, Popovic B
Sci Rep (2019) [PMID: 30733557  ]
Source organism: Homo sapiens  
Assembly composition: protein/protein complex
Assembly name: Plasminogen activator inhibitor 1 and IG-heavy chain and IG-light kappa chain (Preferred)   search this complex
PDBe complex ID: PDB-CPX-209237 (Preferred)   search this ID
PDBe-KB: P05121   
X-ray diffraction
2.9Å resolution
Released: 13 Feb 2019
Model geometry
Fit model/data
6i8s
6i8s
6i8s
Crystal structure of plasminogen activator inhibitor-1 in a metastable active conformation.
Jensen JK, Morth JP
J Biol Chem (2011) [PMID: 21697084  ]
Source organism: Homo sapiens  
Assembly composition: protein only structure
Bound ligands: ZN    ZN    CL    EDO   
Assembly name: Plasminogen activator inhibitor 1 (Preferred)   search this complex
PDBe complex ID: PDB-CPX-138523 (Preferred)   search this ID
PDBe-KB: P05121   
X-ray diffraction
2.3Å resolution
Released: 22 Jun 2011
Model geometry
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3q02
3q02
3q02
Crystal Structure of a Michaelis Complex between Plasminogen Activator Inhibitor-1 and Urokinase-type Plasminogen Activator
Lin Z, Jiang L, Huang M, Structure 2 Function Project (S2F)
J Biol Chem (2011) [PMID: 21199867  ]
Source organism: Homo sapiens  
Assembly composition: protein/protein complex
Bound ligands: SO4   
Assembly name: uPA-PAI-1 complex (Preferred)   search this complex
PDBe complex ID: PDB-CPX-133255 (Preferred)   search this ID
PDBe-KB: P05121    P00749   
X-ray diffraction
2.3Å resolution
Released: 29 Dec 2010
Model geometry
Fit model/data
3pb1
3pb1
3pb1
Entries 1 to 10 of 30
Entries 1 to 10 of 30