Target Information

Target General Infomation
Target ID
T77645
Former ID
TTDC00267
Target Name
Tumor necrosis factor receptor superfamily member 10A
Gene Name
TNFRSF10A
Synonyms
CD261; Death receptor 4; TNF-related apoptosis-inducing ligand receptor 1; TRAIL receptor 1; TRAIL-R1; TNFRSF10A
Target Type
Clinical Trial
Disease Advanced hepatocellular carcinoma; Non-small cell lung cancer [ICD9:155; ICD10: C22.0, C33-C34]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Function
Receptor for thecytotoxic 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 activationwhich initiates the subsequent cascade of caspases (aspartate-specific cysteine proteases) mediating apoptosis. Promotes the activation of NF- kappa-B.
BioChemical Class
Cytokine receptor
Target Validation
T77645
UniProt ID
O00220
Sequence
MAPPPARVHLGAFLAVTPNPGSAASGTEAAAATPSKVWGSSAGRIEPRGGGRGALPTSMG
QHGPSARARAGRAPGPRPAREASPRLRVHKTFKFVVVGVLLQVVPSSAATIKLHDQSIGT
QQWEHSPLGELCPPGSHRSEHPGACNRCTEGVGYTNASNNLFACLPCTACKSDEEERSPC
TTTRNTACQCKPGTFRNDNSAEMCRKCSRGCPRGMVKVKDCTPWSDIECVHKESGNGHNI
WVILVVTLVVPLLLVAVLIVCCCIGSGCGGDPKCMDRVCFWRLGLLRGPGAEDNAHNEIL
SNADSLSTFVSEQQMESQEPADLTGVTVQSPGEAQCLLGPAEAEGSQRRRLLVPANGADP
TETLMLFFDKFANIVPFDSWDQLMRQLDLTKNEIDVVRAGTAGPGDALYAMLMKWVNKTG
RNASIHTLLDALERMEERHAREKIQDLLVDSGKFIYLEDGTGSAVSLE
Drugs and Mode of Action
Drug(s) Mapatumumab Drug Info Phase 2 Advanced hepatocellular carcinoma; Non-small cell lung cancer [521614]
RhApo2L/TRAIL Drug Info Discontinued in Phase 1/2 Cancer [546989]
Modulator Mapatumumab Drug Info [550408]
Agonist RhApo2L/TRAIL Drug Info [525341], [550250]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Cytokine-cytokine receptor interaction
Apoptosis
Natural killer cell mediated cytotoxicity
Measles
Influenza A
NetPath Pathway TCR Signaling Pathway
PANTHER Pathway Apoptosis signaling pathway
p53 pathway
Pathway Interaction Database TRAIL signaling pathway
Direct p53 effectors
Caspase Cascade in Apoptosis
Reactome Ligand-dependent caspase activation
Regulation by c-FLIP
RIPK1-mediated regulated necrosis
CASP8 activity is inhibited
Dimerization of procaspase-8
TRAIL signaling
WikiPathways miR-targeted genes in lymphocytes - TarBase
Apoptosis Modulation and Signaling
References
Ref 521614ClinicalTrials.gov (NCT00094848) Study of TRM-1 (TRAIL-R1 Monoclonal Antibody) in Subjects With Relapsed or Refractory Non-Hodgkin's Lymphoma (NHL). U.S. National Institutes of Health.
Ref 546989Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011860)
Ref 525341ClinicalTrials.gov (NCT00508625) Amgen. Report of Amgen. July 2007.
Ref 543518(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).
Ref 550250Clinical pipeline report, company report or official report of Amgen (2009).
Ref 550408National Cancer Institute Drug Dictionary (drug id 486626).

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