Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTBPCU2O)

DOT Name Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A)
Synonyms Death receptor 4; TNF-related apoptosis-inducing ligand receptor 1; TRAIL receptor 1; TRAIL-R1; CD antigen CD261
Gene Name TNFRSF10A
UniProt ID
TR10A_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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PDB ID
5CIR
Pfam ID
PF00531 ; PF00020
Sequence
MAPPPARVHLGAFLAVTPNPGSAASGTEAAAATPSKVWGSSAGRIEPRGGGRGALPTSMG
QHGPSARARAGRAPGPRPAREASPRLRVHKTFKFVVVGVLLQVVPSSAATIKLHDQSIGT
QQWEHSPLGELCPPGSHRSEHPGACNRCTEGVGYTNASNNLFACLPCTACKSDEEERSPC
TTTRNTACQCKPGTFRNDNSAEMCRKCSRGCPRGMVKVKDCTPWSDIECVHKESGNGHNI
WVILVVTLVVPLLLVAVLIVCCCIGSGCGGDPKCMDRVCFWRLGLLRGPGAEDNAHNEIL
SNADSLSTFVSEQQMESQEPADLTGVTVQSPGEAQCLLGPAEAEGSQRRRLLVPANGADP
TETLMLFFDKFANIVPFDSWDQLMRQLDLTKNEIDVVRAGTAGPGDALYAMLMKWVNKTG
RNASIHTLLDALERMEERHAREKIQDLLVDSGKFIYLEDGTGSAVSLE
Function
Receptor for the cytotoxic ligand TNFSF10/TRAIL. The adapter molecule FADD recruits caspase-8 to the activated receptor. The resulting death-inducing signaling complex (DISC) performs caspase-8 proteolytic activation which initiates the subsequent cascade of caspases (aspartate-specific cysteine proteases) mediating apoptosis. Promotes the activation of NF-kappa-B.
Tissue Specificity Widely expressed. High levels are found in spleen, peripheral blood leukocytes, small intestine and thymus, but also in K-562 erythroleukemia cells, MCF-7 breast carcinoma cells and activated T-cells.
KEGG Pathway
Cytokine-cytokine receptor interaction (hsa04060 )
Viral protein interaction with cytokine and cytokine receptor (hsa04061 )
p53 sig.ling pathway (hsa04115 )
Apoptosis (hsa04210 )
Necroptosis (hsa04217 )
.tural killer cell mediated cytotoxicity (hsa04650 )
Pathogenic Escherichia coli infection (hsa05130 )
Salmonella infection (hsa05132 )
Influenza A (hsa05164 )
Lipid and atherosclerosis (hsa05417 )
Reactome Pathway
Cell surface interactions at the vascular wall (R-HSA-202733 )
Regulation by c-FLIP (R-HSA-3371378 )
RIPK1-mediated regulated necrosis (R-HSA-5213460 )
CASP8 activity is inhibited (R-HSA-5218900 )
TP53 Regulates Transcription of Death Receptors and Ligands (R-HSA-6803211 )
Dimerization of procaspase-8 (R-HSA-69416 )
TRAIL signaling (R-HSA-75158 )
Caspase activation via Death Receptors in the presence of ligand (R-HSA-140534 )

Molecular Interaction Atlas (MIA) of This DOT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
58 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate decreases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [1]
Ciclosporin DMAZJFX Approved Ciclosporin increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [2]
Tretinoin DM49DUI Approved Tretinoin decreases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [3]
Doxorubicin DMVP5YE Approved Doxorubicin increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [4]
Cupric Sulfate DMP0NFQ Approved Cupric Sulfate increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [5]
Cisplatin DMRHGI9 Approved Cisplatin increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [6]
Estradiol DMUNTE3 Approved Estradiol increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [2]
Quercetin DM3NC4M Approved Quercetin increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [7]
Temozolomide DMKECZD Approved Temozolomide increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [8]
Arsenic trioxide DM61TA4 Approved Arsenic trioxide increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [9]
Vorinostat DMWMPD4 Approved Vorinostat increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [10]
Triclosan DMZUR4N Approved Triclosan decreases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [11]
Carbamazepine DMZOLBI Approved Carbamazepine affects the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [12]
Methotrexate DM2TEOL Approved Methotrexate increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [13]
Zoledronate DMIXC7G Approved Zoledronate increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [15]
Fluorouracil DMUM7HZ Approved Fluorouracil increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [16]
Bortezomib DMNO38U Approved Bortezomib decreases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [17]
Troglitazone DM3VFPD Approved Troglitazone increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [18]
Paclitaxel DMLB81S Approved Paclitaxel increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [19]
Menthol DMG2KW7 Approved Menthol increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [20]
Capsaicin DMGMF6V Approved Capsaicin increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [21]
Alitretinoin DMME8LH Approved Alitretinoin increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [22]
Acocantherin DM7JT24 Approved Acocantherin increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [23]
Thalidomide DM70BU5 Approved Thalidomide decreases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [24]
Docetaxel DMDI269 Approved Docetaxel increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [19]
Cantharidin DMBP5N3 Approved Cantharidin increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [25]
Chlorambucil DMRKE63 Approved Chlorambucil affects the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [26]
Fludarabine DMVRLT7 Approved Fludarabine affects the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [26]
Bupropion DM5PCS7 Approved Bupropion increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [27]
Vismodegib DM5IXKQ Approved Vismodegib increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [28]
SNDX-275 DMH7W9X Phase 3 SNDX-275 increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [29]
Resveratrol DM3RWXL Phase 3 Resveratrol increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [30]
Epigallocatechin gallate DMCGWBJ Phase 3 Epigallocatechin gallate decreases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [31]
Curcumin DMQPH29 Phase 3 Curcumin increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [32]
Chloroquine DMSI5CB Phase 3 Trial Chloroquine increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [33]
Flavopiridol DMKSUOI Phase 2 Flavopiridol increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [34]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [2]
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 decreases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [35]
LY294002 DMY1AFS Phase 1 LY294002 increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [36]
PMID28460551-Compound-2 DM4DOUB Patented PMID28460551-Compound-2 increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [37]
PMID28870136-Compound-52 DMFDERP Patented PMID28870136-Compound-52 decreases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [31]
PMID26394986-Compound-22 DM43Z1G Patented PMID26394986-Compound-22 increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [38]
PMID28870136-Compound-49 DMTUC9E Patented PMID28870136-Compound-49 increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [39]
DUP 697 DMUMAHC Discontinued in Phase 1 DUP 697 increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [38]
MG-132 DMKA2YS Preclinical MG-132 increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [40]
Celastrol DMWQIJX Preclinical Celastrol increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [41]
CKI-7 DMV0RFU Preclinical CKI-7 increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [42]
NS398 DMINUWH Terminated NS398 increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [38]
EMBELIN DMFZO4Y Terminated EMBELIN increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [43]
SC-58125 DM874YU Terminated SC-58125 increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [38]
Bisphenol A DM2ZLD7 Investigative Bisphenol A decreases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [44]
Trichostatin A DM9C8NX Investigative Trichostatin A increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [45]
Formaldehyde DM7Q6M0 Investigative Formaldehyde increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [46]
Sulforaphane DMQY3L0 Investigative Sulforaphane increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [47]
Paraquat DMR8O3X Investigative Paraquat decreases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [48]
Phencyclidine DMQBEYX Investigative Phencyclidine decreases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [49]
AHPN DM8G6O4 Investigative AHPN increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [50]
SC-560 DMT1GJL Investigative SC-560 increases the expression of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [38]
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⏷ Show the Full List of 58 Drug(s)
1 Drug(s) Affected the Post-Translational Modifications of This DOT
Drug Name Drug ID Highest Status Interaction REF
Decitabine DMQL8XJ Approved Decitabine affects the methylation of Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A). [14]
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References

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