Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTT0MPQ3)

DOT Name Plasminogen activator inhibitor 1 (SERPINE1)
Synonyms PAI; PAI-1; Endothelial plasminogen activator inhibitor; Serpin E1
Gene Name SERPINE1
Related Disease
Congenital plasminogen activator inhibitor type 1 deficiency ( )
UniProt ID
PAI1_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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PDB ID
1A7C; 1B3K; 1C5G; 1DB2; 1DVM; 1DVN; 1LJ5; 1OC0; 3CVM; 3EOX; 3PB1; 3Q02; 3Q03; 3R4L; 3UT3; 4AQH; 4G8O; 4G8R; 4IC0; 5BRR; 5ZLZ; 6GWN; 6GWP; 6GWQ; 6I8S; 6ZRV; 7AQF; 7AQG; 9PAI
Pfam ID
PF00079
Sequence
MQMSPALTCLVLGLALVFGEGSAVHHPPSYVAHLASDFGVRVFQQVAQASKDRNVVFSPY
GVASVLAMLQLTTGGETQQQIQAAMGFKIDDKGMAPALRHLYKELMGPWNKDEISTTDAI
FVQRDLKLVQGFMPHFFRLFRSTVKQVDFSEVERARFIINDWVKTHTKGMISNLLGKGAV
DQLTRLVLVNALYFNGQWKTPFPDSSTHRRLFHKSDGSTVSVPMMAQTNKFNYTEFTTPD
GHYYDILELPYHGDTLSMFIAAPYEKEVPLSALTNILSAQLISHWKGNMTRLPRLLVLPK
FSLETEVDLRKPLENLGMTDMFRQFQADFTSLSDQEPLHVAQALQKVKIEVNESGTVASS
STAVIVSARMAPEEIIMDRPFLFVVRHNPTGTVLFMGQVMEP
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.
Tissue Specificity Expressed in endothelial cells . Found in plasma, platelets, and hepatoma and fibrosarcoma cells.
KEGG Pathway
HIF-1 sig.ling pathway (hsa04066 )
p53 sig.ling pathway (hsa04115 )
Cellular senescence (hsa04218 )
Apelin sig.ling pathway (hsa04371 )
Hippo sig.ling pathway (hsa04390 )
Complement and coagulation cascades (hsa04610 )
AGE-RAGE sig.ling pathway in diabetic complications (hsa04933 )
Chagas disease (hsa05142 )
Reactome Pathway
BMAL1 (R-HSA-1368108 )
SMAD2/SMAD3 (R-HSA-2173796 )
ECM proteoglycans (R-HSA-3000178 )
Dissolution of Fibrin Clot (R-HSA-75205 )
Platelet degranulation (R-HSA-114608 )

Molecular Interaction Atlas (MIA) of This DOT

1 Disease(s) Related to This DOT
Disease Name Disease ID Evidence Level Mode of Inheritance REF
Congenital plasminogen activator inhibitor type 1 deficiency DISYEZ45 Definitive Autosomal recessive [1]
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Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
This DOT Affected the Drug Response of 3 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Paclitaxel DMLB81S Approved Plasminogen activator inhibitor 1 (SERPINE1) affects the response to substance of Paclitaxel. [78]
Topotecan DMP6G8T Approved Plasminogen activator inhibitor 1 (SERPINE1) affects the response to substance of Topotecan. [78]
Vinblastine DM5TVS3 Approved Plasminogen activator inhibitor 1 (SERPINE1) affects the response to substance of Vinblastine. [78]
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4 Drug(s) Affected the Post-Translational Modifications of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate decreases the methylation of Plasminogen activator inhibitor 1 (SERPINE1). [2]
Folic acid DMEMBJC Approved Folic acid increases the methylation of Plasminogen activator inhibitor 1 (SERPINE1). [21]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene increases the methylation of Plasminogen activator inhibitor 1 (SERPINE1). [54]
Choline DM5D9YK Investigative Choline increases the methylation of Plasminogen activator inhibitor 1 (SERPINE1). [21]
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78 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Ciclosporin DMAZJFX Approved Ciclosporin decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [3]
Acetaminophen DMUIE76 Approved Acetaminophen increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [4]
Doxorubicin DMVP5YE Approved Doxorubicin decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [5]
Cupric Sulfate DMP0NFQ Approved Cupric Sulfate increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [6]
Cisplatin DMRHGI9 Approved Cisplatin increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [7]
Estradiol DMUNTE3 Approved Estradiol increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [8]
Arsenic DMTL2Y1 Approved Arsenic decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [9]
Quercetin DM3NC4M Approved Quercetin decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [10]
Temozolomide DMKECZD Approved Temozolomide decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [11]
Arsenic trioxide DM61TA4 Approved Arsenic trioxide decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [12]
Hydrogen peroxide DM1NG5W Approved Hydrogen peroxide increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [13]
Triclosan DMZUR4N Approved Triclosan decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [14]
Carbamazepine DMZOLBI Approved Carbamazepine affects the expression of Plasminogen activator inhibitor 1 (SERPINE1). [15]
Methotrexate DM2TEOL Approved Methotrexate increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [16]
Decitabine DMQL8XJ Approved Decitabine increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [17]
Marinol DM70IK5 Approved Marinol decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [18]
Progesterone DMUY35B Approved Progesterone increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [19]
Dexamethasone DMMWZET Approved Dexamethasone increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [20]
Cannabidiol DM0659E Approved Cannabidiol decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [22]
Troglitazone DM3VFPD Approved Troglitazone decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [23]
Rosiglitazone DMILWZR Approved Rosiglitazone decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [24]
Azathioprine DMMZSXQ Approved Azathioprine increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [25]
Diclofenac DMPIHLS Approved Diclofenac affects the expression of Plasminogen activator inhibitor 1 (SERPINE1). [15]
Nicotine DMWX5CO Approved Nicotine increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [26]
Sodium lauryl sulfate DMLJ634 Approved Sodium lauryl sulfate increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [27]
Indomethacin DMSC4A7 Approved Indomethacin increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [28]
Mitomycin DMH0ZJE Approved Mitomycin increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [29]
Simvastatin DM30SGU Approved Simvastatin decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [30]
Obeticholic acid DM3Q1SM Approved Obeticholic acid decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [31]
Mifepristone DMGZQEF Approved Mifepristone decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [32]
Capsaicin DMGMF6V Approved Capsaicin decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [33]
Daunorubicin DMQUSBT Approved Daunorubicin decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [34]
Palbociclib DMD7L94 Approved Palbociclib increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [35]
Pioglitazone DMKJ485 Approved Pioglitazone increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [36]
Nefazodone DM4ZS8M Approved Nefazodone increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [37]
Bezafibrate DMZDCS0 Approved Bezafibrate increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [24]
Atazanavir DMSYRBX Approved Atazanavir increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [37]
Busulfan DMXYJ9C Approved Busulfan increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [38]
Aldosterone DM9S2JW Approved Aldosterone increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [40]
Spironolactone DM2AQ5N Approved Spironolactone decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [41]
Tibolone DM78XFG Approved Tibolone increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [42]
Gemfibrozil DMD8Q3J Approved Gemfibrozil decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [24]
Cenestin DMXQS7K Approved Cenestin decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [44]
Azelaic Acid DMHVL0J Approved Azelaic Acid increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [45]
SNDX-275 DMH7W9X Phase 3 SNDX-275 increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [46]
Resveratrol DM3RWXL Phase 3 Resveratrol decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [47]
Curcumin DMQPH29 Phase 3 Curcumin increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [48]
Genistein DM0JETC Phase 2/3 Genistein decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [49]
DNCB DMDTVYC Phase 2 DNCB affects the expression of Plasminogen activator inhibitor 1 (SERPINE1). [50]
GSK2110183 DMZHB37 Phase 2 GSK2110183 decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [51]
PEITC DMOMN31 Phase 2 PEITC increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [53]
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [55]
Leflunomide DMR8ONJ Phase 1 Trial Leflunomide increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [56]
PMID28460551-Compound-2 DM4DOUB Patented PMID28460551-Compound-2 decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [57]
Geldanamycin DMS7TC5 Discontinued in Phase 2 Geldanamycin increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [58]
Scriptaid DM9JZ21 Preclinical Scriptaid affects the expression of Plasminogen activator inhibitor 1 (SERPINE1). [59]
PIRINIXIC ACID DM82Y75 Preclinical PIRINIXIC ACID increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [24]
Bisphenol A DM2ZLD7 Investigative Bisphenol A decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [60]
Trichostatin A DM9C8NX Investigative Trichostatin A increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [58]
Formaldehyde DM7Q6M0 Investigative Formaldehyde increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [61]
Milchsaure DM462BT Investigative Milchsaure affects the expression of Plasminogen activator inhibitor 1 (SERPINE1). [62]
chloropicrin DMSGBQA Investigative chloropicrin decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [63]
methyl p-hydroxybenzoate DMO58UW Investigative methyl p-hydroxybenzoate decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [64]
Paraquat DMR8O3X Investigative Paraquat increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [65]
Nickel chloride DMI12Y8 Investigative Nickel chloride affects the expression of Plasminogen activator inhibitor 1 (SERPINE1). [50]
Hexadecanoic acid DMWUXDZ Investigative Hexadecanoic acid increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [66]
D-glucose DMMG2TO Investigative D-glucose decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [67]
OXYQUINOLINE DMZVS9Y Investigative OXYQUINOLINE decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [69]
cinnamaldehyde DMZDUXG Investigative cinnamaldehyde increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [70]
Bilirubin DMI0V4O Investigative Bilirubin increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [71]
Lead acetate DML0GZ2 Investigative Lead acetate increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [72]
CATECHIN DMY38SB Investigative CATECHIN decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [10]
Pyrrolidine dithiocarbamate DM5ZAS6 Investigative Pyrrolidine dithiocarbamate increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [73]
Fibrates DMFNTMY Investigative Fibrates increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [24]
ROSMARINIC ACID DMQ6SJT Investigative ROSMARINIC ACID decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [74]
GW-788388 DMIBUW5 Investigative GW-788388 decreases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [75]
CFTRinh-172 DM8TJW3 Investigative CFTRinh-172 increases the expression of Plasminogen activator inhibitor 1 (SERPINE1). [76]
waixenicin A DMB6H35 Investigative waixenicin A decreases the activity of Plasminogen activator inhibitor 1 (SERPINE1). [77]
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⏷ Show the Full List of 78 Drug(s)
5 Drug(s) Affected the Protein Interaction/Cellular Processes of This DOT
Drug Name Drug ID Highest Status Interaction REF
Efavirenz DMC0GSJ Approved Efavirenz increases the secretion of Plasminogen activator inhibitor 1 (SERPINE1). [39]
Magnesium DMU4ORS Approved Magnesium increases the stability of Plasminogen activator inhibitor 1 (SERPINE1). [43]
phorbol 12-myristate 13-acetate DMJWD62 Phase 2 phorbol 12-myristate 13-acetate increases the secretion of Plasminogen activator inhibitor 1 (SERPINE1). [52]
[3H]methyltrienolone DMTSGOW Investigative [3H]methyltrienolone increases the secretion of Plasminogen activator inhibitor 1 (SERPINE1). [68]
Manganese DMKT129 Investigative Manganese increases the stability of Plasminogen activator inhibitor 1 (SERPINE1). [43]
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