Details of the Target

General Information of Target

Target ID LDTP02085
Target Name Plasminogen activator inhibitor 1 (SERPINE1)
Gene Name SERPINE1
Gene ID 5054
Synonyms
PAI1; PLANH1; Plasminogen activator inhibitor 1; PAI; PAI-1; Endothelial plasminogen activator inhibitor; Serpin E1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MQMSPALTCLVLGLALVFGEGSAVHHPPSYVAHLASDFGVRVFQQVAQASKDRNVVFSPY
GVASVLAMLQLTTGGETQQQIQAAMGFKIDDKGMAPALRHLYKELMGPWNKDEISTTDAI
FVQRDLKLVQGFMPHFFRLFRSTVKQVDFSEVERARFIINDWVKTHTKGMISNLLGKGAV
DQLTRLVLVNALYFNGQWKTPFPDSSTHRRLFHKSDGSTVSVPMMAQTNKFNYTEFTTPD
GHYYDILELPYHGDTLSMFIAAPYEKEVPLSALTNILSAQLISHWKGNMTRLPRLLVLPK
FSLETEVDLRKPLENLGMTDMFRQFQADFTSLSDQEPLHVAQALQKVKIEVNESGTVASS
STAVIVSARMAPEEIIMDRPFLFVVRHNPTGTVLFMGQVMEP
Target Type
Clinical trial
Target Bioclass
Other
Family
Serpin family
Subcellular location
Secreted
Function
Serine protease inhibitor. Inhibits TMPRSS7. Is a primary inhibitor of tissue-type plasminogen activator (PLAT) and urokinase-type plasminogen activator (PLAU). As PLAT inhibitor, it is required for fibrinolysis down-regulation and is responsible for the controlled degradation of blood clots. As PLAU inhibitor, it is involved in the regulation of cell adhesion and spreading. Acts as a regulator of cell migration, independently of its role as protease inhibitor. It is required for stimulation of keratinocyte migration during cutaneous injury repair. It is involved in cellular and replicative senescence. Plays a role in alveolar type 2 cells senescence in the lung. Is involved in the regulation of cementogenic differentiation of periodontal ligament stem cells, and regulates odontoblast differentiation and dentin formation during odontogenesis.
TTD ID
T15556
Uniprot ID
P05121
DrugMap ID
TTHW8O3
Ensemble ID
ENST00000223095.5
HGNC ID
HGNC:8583
ChEMBL ID
CHEMBL3475

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
ABC1 SNV: p.M1? .
BT549 SNV: p.I282T .
LNCaP clone FGC SNV: p.A119T .
NCIH23 SNV: p.R323T .
SW620 SNV: p.I282T .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 6 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		5.43  LDD0402  [1]
Alkylaryl probe 1
 Probe Info  		17.00  LDD0387  [2]
Alkylaryl probe 2
 Probe Info  		20.00  LDD0391  [2]
YN-1
 Probe Info  		100.00  LDD0444  [3]
STPyne
 Probe Info  		K145(2.26); K164(4.79); K92(7.86)  LDD0277  [4]
Jackson_14
 Probe Info  		2.50  LDD0123  [5]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0099  Phenelzine MDA-MB-231 3.00  LDD0388  [2]
 LDCM0016  Ranjitkar_cp1 MDA-MB-231 2.50  LDD0123  [5]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Estradiol 17-beta-dehydrogenase 11 (HSD17B11) Short-chain dehydrogenases/reductases (SDR) family Q8NBQ5
Transcription factor
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Pituitary homeobox 1 (PITX1) Paired homeobox family P78337
T-cell leukemia homeobox protein 3 (TLX3) . O43711
Other
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Alpha-1-acid glycoprotein 1 (ORM1) Lipocalin family P02763
Small glutamine-rich tetratricopeptide repeat-containing protein alpha (SGTA) SGT family O43765
Small glutamine-rich tetratricopeptide repeat-containing protein beta (SGTB) SGT family Q96EQ0
Ubiquilin-1 (UBQLN1) . Q9UMX0
Ubiquilin-2 (UBQLN2) . Q9UHD9

The Drug(s) Related To This Target

Approved
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Alteplase BiotechDrug DB00009
Anistreplase BiotechDrug DB00029
Drotrecogin Alfa BiotechDrug DB00055
Reteplase BiotechDrug DB00015
Tenecteplase BiotechDrug DB00031
Urokinase BiotechDrug DB00013
Troglitazone Small molecular drug DB00197
Copper . DB09130
Investigative
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Colforsin Small molecular drug DB02587
Bucladesine . DB13242
Fibrinolysin . DB05254

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
2 Hydrazines as versatile chemical biology probes and drug-discovery tools for cofactor-dependent enzymes. bioRxiv, 2020-06.
3 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
4 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
5 Appendage and Scaffold Diverse Fully Functionalized Small-Molecule Probes via a Minimalist Terminal Alkyne-Aliphatic Diazirine Isocyanide. J Org Chem. 2018 Sep 21;83(18):11245-11253. doi: 10.1021/acs.joc.8b01831. Epub 2018 Aug 31.