Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT5WLRX)

DTT Name	TRAIL receptor 1 (TRAIL-R1)
Synonyms	Tumor necrosis factor receptor superfamily member 10A; TRAILR1; TNF-related apoptosis-inducing ligand receptor 1; Death receptor 4; DR4; CD261; APO2
Gene Name	TNFRSF10A
DTT Type	Clinical trial target	[1]
BioChemical Class	Cytokine receptor
UniProt ID	TR10A_HUMAN
TTD ID	T77645
3D Structure	Download 2D Sequence (FASTA) Download 3D Structure (PDB) Download
Sequence	MAPPPARVHLGAFLAVTPNPGSAASGTEAAAATPSKVWGSSAGRIEPRGGGRGALPTSMG QHGPSARARAGRAPGPRPAREASPRLRVHKTFKFVVVGVLLQVVPSSAATIKLHDQSIGT QQWEHSPLGELCPPGSHRSEHPGACNRCTEGVGYTNASNNLFACLPCTACKSDEEERSPC TTTRNTACQCKPGTFRNDNSAEMCRKCSRGCPRGMVKVKDCTPWSDIECVHKESGNGHNI WVILVVTLVVPLLLVAVLIVCCCIGSGCGGDPKCMDRVCFWRLGLLRGPGAEDNAHNEIL SNADSLSTFVSEQQMESQEPADLTGVTVQSPGEAQCLLGPAEAEGSQRRRLLVPANGADP TETLMLFFDKFANIVPFDSWDQLMRQLDLTKNEIDVVRAGTAGPGDALYAMLMKWVNKTG RNASIHTLLDALERMEERHAREKIQDLLVDSGKFIYLEDGTGSAVSLE
Function	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. Receptor for the cytotoxic ligand TNFSF10/TRAIL.
KEGG Pathway	Cytokine-cytokine receptor interaction (hsa04060 ) Apoptosis (hsa04210 ) Natural killer cell mediated cytotoxicity (hsa04650 ) Measles (hsa05162 ) Influenza A (hsa05164 )
Reactome Pathway	Regulation by c-FLIP (R-HSA-3371378 ) RIPK1-mediated regulated necrosis (R-HSA-5213460 ) CASP8 activity is inhibited (R-HSA-5218900 ) Dimerization of procaspase-8 (R-HSA-69416 ) TRAIL signaling (R-HSA-75158 ) Ligand-dependent caspase activation (R-HSA-140534 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA)

MIA Detail

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1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Mapatumumab	DMGQ175	Non-small-cell lung cancer	2C25.Y	Phase 2	[1]
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1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
RhApo2L/TRAIL	DMIAZJ9	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1/2	[2]
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1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
DR-5/DR-4 cross reactive mabs	DMX2TZD	Solid tumour/cancer	2A00-2F9Z	Investigative	[3]
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Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA)

MEA Detail

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Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Rectal cancer	2C82	Rectal colon tissue	4.44E-01	0.13	0.31
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References

1	National Cancer Institute Drug Dictionary (drug id 486626).
2	Clinical pipeline report, company report or official report of Amgen (2009).
3	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1879).