Details of Drug Off-Target (DOT)

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

DOT Name Endoplasmic reticulum chaperone BiP (HSPA5)
Synonyms
EC 3.6.4.10; 78 kDa glucose-regulated protein; GRP-78; Binding-immunoglobulin protein; BiP; Heat shock protein 70 family protein 5; HSP70 family protein 5; Heat shock protein family A member 5; Immunoglobulin heavy chain-binding protein
Gene Name HSPA5
UniProt ID
BIP_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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PDB ID
3IUC; 3LDL; 3LDN; 3LDO; 3LDP; 5E84; 5E85; 5E86; 5EVZ; 5EX5; 5EXW; 5EY4; 5F0X; 5F1X; 5F2R; 6ASY; 6CZ1; 6DFM; 6DFO; 6DO2; 6DWS; 6ZMD; 7N1R
EC Number
3.6.4.10
Pfam ID
PF00012
Sequence
MKLSLVAAMLLLLSAARAEEEDKKEDVGTVVGIDLGTTYSCVGVFKNGRVEIIANDQGNR
ITPSYVAFTPEGERLIGDAAKNQLTSNPENTVFDAKRLIGRTWNDPSVQQDIKFLPFKVV
EKKTKPYIQVDIGGGQTKTFAPEEISAMVLTKMKETAEAYLGKKVTHAVVTVPAYFNDAQ
RQATKDAGTIAGLNVMRIINEPTAAAIAYGLDKREGEKNILVFDLGGGTFDVSLLTIDNG
VFEVVATNGDTHLGGEDFDQRVMEHFIKLYKKKTGKDVRKDNRAVQKLRREVEKAKRALS
SQHQARIEIESFYEGEDFSETLTRAKFEELNMDLFRSTMKPVQKVLEDSDLKKSDIDEIV
LVGGSTRIPKIQQLVKEFFNGKEPSRGINPDEAVAYGAAVQAGVLSGDQDTGDLVLLDVC
PLTLGIETVGGVMTKLIPRNTVVPTKKSQIFSTASDNQPTVTIKVYEGERPLTKDNHLLG
TFDLTGIPPAPRGVPQIEVTFEIDVNGILRVTAEDKGTGNKNKITITNDQNRLTPEEIER
MVNDAEKFAEEDKKLKERIDTRNELESYAYSLKNQIGDKEKLGGKLSSEDKETMEKAVEE
KIEWLESHQDADIEDFKAKKKELEEIVQPIISKLYGSAGPPPTGEEDTAEKDEL
Function
Endoplasmic reticulum chaperone that plays a key role in protein folding and quality control in the endoplasmic reticulum lumen. Involved in the correct folding of proteins and degradation of misfolded proteins via its interaction with DNAJC10/ERdj5, probably to facilitate the release of DNAJC10/ERdj5 from its substrate. Acts as a key repressor of the ERN1/IRE1-mediated unfolded protein response (UPR). In the unstressed endoplasmic reticulum, recruited by DNAJB9/ERdj4 to the luminal region of ERN1/IRE1, leading to disrupt the dimerization of ERN1/IRE1, thereby inactivating ERN1/IRE1. Accumulation of misfolded protein in the endoplasmic reticulum causes release of HSPA5/BiP from ERN1/IRE1, allowing homodimerization and subsequent activation of ERN1/IRE1. Plays an auxiliary role in post-translational transport of small presecretory proteins across endoplasmic reticulum (ER). May function as an allosteric modulator for SEC61 channel-forming translocon complex, likely cooperating with SEC62 to enable the productive insertion of these precursors into SEC61 channel. Appears to specifically regulate translocation of precursors having inhibitory residues in their mature region that weaken channel gating. May also play a role in apoptosis and cell proliferation ; (Microbial infection) Plays an important role in viral binding to the host cell membrane and entry for several flaviruses such as Dengue virus, Zika virus and Japanese encephalitis virus. Acts as a component of the cellular receptor for Dengue virus serotype 2/DENV-2 on human liver cells ; (Microbial infection) Acts as a receptor for CotH proteins expressed by fungi of the order mucorales, the causative agent of mucormycosis, which plays an important role in epithelial cell invasion by the fungi. Acts as a receptor for R.delemar CotH3 in nasal epithelial cells, which may be an early step in rhinoorbital/cerebral mucormycosis (RCM) disease progression.
KEGG Pathway
Protein export (hsa03060 )
Protein processing in endoplasmic reticulum (hsa04141 )
Antigen processing and presentation (hsa04612 )
Thyroid hormone synthesis (hsa04918 )
Parkinson disease (hsa05012 )
Amyotrophic lateral sclerosis (hsa05014 )
Prion disease (hsa05020 )
Pathways of neurodegeneration - multiple diseases (hsa05022 )
Lipid and atherosclerosis (hsa05417 )
Reactome Pathway
Regulation of HSF1-mediated heat shock response (R-HSA-3371453 )
ATF6 (ATF6-alpha) activates chaperones (R-HSA-381033 )
PERK regulates gene expression (R-HSA-381042 )
IRE1alpha activates chaperones (R-HSA-381070 )
ATF6 (ATF6-alpha) activates chaperone genes (R-HSA-381183 )
ATF6B (ATF6-beta) activates chaperones (R-HSA-8874177 )
Antigen Presentation (R-HSA-983170 )
Platelet degranulation (R-HSA-114608 )

Molecular Interaction Atlas (MIA) of This DOT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
This DOT Affected the Drug Response of 4 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Deoxycholic acid DM3GYAL Approved Endoplasmic reticulum chaperone BiP (HSPA5) decreases the response to substance of Deoxycholic acid. [90]
Lidocaine DML4ZOT Approved Endoplasmic reticulum chaperone BiP (HSPA5) increases the Gastrointestinal disorders ADR of Lidocaine. [91]
Zalcitabine DMH7MUV Approved Endoplasmic reticulum chaperone BiP (HSPA5) increases the Cardiotoxicity ADR of Zalcitabine. [91]
Forskolin DM6ITNG Investigative Endoplasmic reticulum chaperone BiP (HSPA5) increases the response to substance of Forskolin. [92]
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100 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [1]
Ciclosporin DMAZJFX Approved Ciclosporin increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [2]
Tretinoin DM49DUI Approved Tretinoin decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [3]
Acetaminophen DMUIE76 Approved Acetaminophen increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [4]
Doxorubicin DMVP5YE Approved Doxorubicin increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [5]
Cupric Sulfate DMP0NFQ Approved Cupric Sulfate decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [6]
Cisplatin DMRHGI9 Approved Cisplatin decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [7]
Estradiol DMUNTE3 Approved Estradiol decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [8]
Ivermectin DMDBX5F Approved Ivermectin decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [9]
Arsenic DMTL2Y1 Approved Arsenic increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [10]
Quercetin DM3NC4M Approved Quercetin decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [11]
Arsenic trioxide DM61TA4 Approved Arsenic trioxide decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [12]
Hydrogen peroxide DM1NG5W Approved Hydrogen peroxide increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [13]
Triclosan DMZUR4N Approved Triclosan decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [14]
Marinol DM70IK5 Approved Marinol decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [15]
Zoledronate DMIXC7G Approved Zoledronate decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [16]
Menadione DMSJDTY Approved Menadione increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [17]
Fluorouracil DMUM7HZ Approved Fluorouracil decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [18]
Folic acid DMEMBJC Approved Folic acid decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [19]
Cannabidiol DM0659E Approved Cannabidiol increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [20]
Bortezomib DMNO38U Approved Bortezomib increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [21]
Troglitazone DM3VFPD Approved Troglitazone increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [22]
Hydroquinone DM6AVR4 Approved Hydroquinone increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [23]
Rosiglitazone DMILWZR Approved Rosiglitazone increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [22]
Ethanol DMDRQZU Approved Ethanol increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [24]
Aspirin DM672AH Approved Aspirin decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [25]
Diclofenac DMPIHLS Approved Diclofenac increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [26]
Nicotine DMWX5CO Approved Nicotine increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [27]
Indomethacin DMSC4A7 Approved Indomethacin increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [18]
Menthol DMG2KW7 Approved Menthol increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [28]
Cidofovir DMA13GD Approved Cidofovir decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [29]
Cocaine DMSOX7I Approved Cocaine increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [30]
Simvastatin DM30SGU Approved Simvastatin increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [31]
Gemcitabine DMSE3I7 Approved Gemcitabine increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [32]
Rifampicin DM5DSFZ Approved Rifampicin increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [33]
Cyclophosphamide DM4O2Z7 Approved Cyclophosphamide increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [12]
Capsaicin DMGMF6V Approved Capsaicin increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [34]
Ibuprofen DM8VCBE Approved Ibuprofen decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [29]
Methamphetamine DMPM4SK Approved Methamphetamine increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [35]
Acocantherin DM7JT24 Approved Acocantherin increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [36]
Colchicine DM2POTE Approved Colchicine increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [37]
Vitamin C DMXJ7O8 Approved Vitamin C decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [38]
Ursodeoxycholic acid DMCUT21 Approved Ursodeoxycholic acid decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [39]
Sodium phenylbutyrate DMXLBCQ Approved Sodium phenylbutyrate decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [40]
Nefazodone DM4ZS8M Approved Nefazodone increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [41]
Dactinomycin DM2YGNW Approved Dactinomycin decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [42]
Dopamine DMPGUCF Approved Dopamine increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [43]
Isoproterenol DMK7MEY Approved Isoproterenol decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [44]
Etretinate DM2CZFA Approved Etretinate increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [45]
Glucosamine DM4ZLFD Approved Glucosamine increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [46]
Orlistat DMRJSP8 Approved Orlistat increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [47]
2-deoxyglucose DMIAHVU Approved 2-deoxyglucose increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [48]
Atazanavir DMSYRBX Approved Atazanavir decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [41]
Penicillamine DM40EF6 Approved Penicillamine increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [49]
Cantharidin DMBP5N3 Approved Cantharidin increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [50]
Hesperetin DMKER83 Approved Hesperetin increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [51]
Nilotinib DM7HXWT Approved Nilotinib increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [52]
Nelfinavir mesylate DMFX6G8 Approved Nelfinavir mesylate increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [53]
Allopurinol DMLPAOB Approved Allopurinol increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [18]
Gallium nitrate DMF9O6B Approved Gallium nitrate decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [54]
Ketamine DMT5HA4 Approved Ketamine increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [55]
Bupropion DM5PCS7 Approved Bupropion increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [56]
Indinavir DM0T3YH Approved Indinavir increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [18]
Furazolidone DM3P6V7 Approved Furazolidone increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [57]
Riluzole DMECBWN Approved Riluzole increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [58]
Naloxone DM3FXMA Approved Naloxone increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [59]
Pyrazinamide DM4IF32 Approved Pyrazinamide increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [60]
Saquinavir DMG814N Approved Saquinavir increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [61]
Oxycodone DMXLKHV Approved Oxycodone increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [59]
Dihydrotestosterone DM3S8XC Phase 4 Dihydrotestosterone increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [62]
Resveratrol DM3RWXL Phase 3 Resveratrol decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [63]
Curcumin DMQPH29 Phase 3 Curcumin increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [64]
Fenretinide DMRD5SP Phase 3 Fenretinide increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [65]
Bardoxolone methyl DMODA2X Phase 3 Bardoxolone methyl increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [66]
Psoralen DMIZJ8M Phase 3 Psoralen increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [67]
Amiodarone DMUTEX3 Phase 2/3 Trial Amiodarone increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [68]
Thymoquinone DMVDTR2 Phase 2/3 Thymoquinone increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [69]
Tanespimycin DMNLQHK Phase 2 Tanespimycin increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [70]
URSOLIC ACID DM4SOAW Phase 2 URSOLIC ACID increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [71]
CERC-801 DM3SZ7P Phase 2 CERC-801 increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [72]
ME-344 DM6JN19 Phase 1/2 ME-344 increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [73]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [12]
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [74]
Tetrandrine DMAOJBX Phase 1 Tetrandrine increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [75]
PMID28460551-Compound-2 DM4DOUB Patented PMID28460551-Compound-2 increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [76]
PMID26394986-Compound-22 DM43Z1G Patented PMID26394986-Compound-22 increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [77]
PMID26560530-Compound-35 DMO36RL Patented PMID26560530-Compound-35 increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [78]
Clioquinol DM746BZ Withdrawn from market Clioquinol decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [79]
Geldanamycin DMS7TC5 Discontinued in Phase 2 Geldanamycin increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [80]
THAPSIGARGIN DMDMQIE Preclinical THAPSIGARGIN increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [81]
MG-132 DMKA2YS Preclinical MG-132 increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [34]
Celastrol DMWQIJX Preclinical Celastrol increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [82]
UNC0379 DMD1E4J Preclinical UNC0379 decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [83]
5-(N,N-hexamethylene)-amiloride DMC4IUQ Preclinical 5-(N,N-hexamethylene)-amiloride affects the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [84]
Bisphenol A DM2ZLD7 Investigative Bisphenol A increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [85]
Trichostatin A DM9C8NX Investigative Trichostatin A decreases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [86]
chloropicrin DMSGBQA Investigative chloropicrin increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [87]
3R14S-OCHRATOXIN A DM2KEW6 Investigative 3R14S-OCHRATOXIN A increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [12]
methyl p-hydroxybenzoate DMO58UW Investigative methyl p-hydroxybenzoate increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [88]
Paraquat DMR8O3X Investigative Paraquat increases the expression of Endoplasmic reticulum chaperone BiP (HSPA5). [89]
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⏷ Show the Full List of 100 Drug(s)

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