Target Information

Target General Infomation
Target ID
T70067
Former ID
TTDC00266
Target Name
Tumor necrosis factor receptor superfamily member 10B
Gene Name
TNFRSF10B
Synonyms
CD262; Death receptor 5; TNF-related apoptosis-inducing ligand receptor 2; TRAIL receptor 2; TRAIL-R2; TNFRSF10B
Target Type
Clinical Trial
Disease Cancer [ICD9: 140-229; ICD10: C00-C96]
Colorectal cancer [ICD9: 153, 154; ICD10: C18-C21]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Function
Receptorfor 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. Essential for ER stress-induced apoptosis.
BioChemical Class
Cytokine receptor
Target Validation
T70067
UniProt ID
O14763
Sequence
MEQRGQNAPAASGARKRHGPGPREARGARPGPRVPKTLVLVVAAVLLLVSAESALITQQD
LAPQQRAAPQQKRSSPSEGLCPPGHHISEDGRDCISCKYGQDYSTHWNDLLFCLRCTRCD
SGEVELSPCTTTRNTVCQCEEGTFREEDSPEMCRKCRTGCPRGMVKVGDCTPWSDIECVH
KESGTKHSGEVPAVEETVTSSPGTPASPCSLSGIIIGVTVAAVVLIVAVFVCKSLLWKKV
LPYLKGICSGGGGDPERVDRSSQRPGAEDNVLNEIVSILQPTQVPEQEMEVQEPAEPTGV
NMLSPGESEHLLEPAEAERSQRRRLLVPANEGDPTETLRQCFDDFADLVPFDSWEPLMRK
LGLMDNEIKVAKAEAAGHRDTLYTMLIKWVNKTGRDASVHTLLDALETLGERLAKQKIED
HLLSSGKFMYLEGNADSAMS
Drugs and Mode of Action
Drug(s) Conatumumab Drug Info Phase 2 Colorectal cancer [523418]
Lexatumumab Drug Info Phase 2 Cancer [528631]
RhApo2L/TRAIL Drug Info Discontinued in Phase 1/2 Cancer [546989]
HGS-TR2J Drug Info Discontinued in Phase 1 Cancer [548059]
LBY-135 Drug Info Discontinued in Phase 1 Solid tumours [548517]
Agonist Conatumumab Drug Info [525342], [550250]
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
p53 signaling pathway
Apoptosis
Natural killer cell mediated cytotoxicity
Measles
Influenza A
NetPath Pathway TCR Signaling Pathway
TNFalpha 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 DNA Damage Response
Apoptosis-related network due to altered Notch3 in ovarian cancer
Apoptosis
miR-targeted genes in squamous cell - TarBase
miR-targeted genes in muscle cell - TarBase
miR-targeted genes in lymphocytes - TarBase
miR-targeted genes in epithelium - TarBase
Extrinsic Pathway for Apoptosis
Apoptosis Modulation and Signaling
miRNA Regulation of DNA Damage Response
References
Ref 523418ClinicalTrials.gov (NCT01327612) Open Label Extension Study of Conatumumab and AMG 479. U.S. National Institutes of Health.
Ref 528631Drug evaluation: lexatumumab, an intravenous human agonistic mAb targeting TRAIL receptor 2. Curr Opin Mol Ther. 2006 Dec;8(6):539-46.
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 548059Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021611)
Ref 548517Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026275)
Ref 525341ClinicalTrials.gov (NCT00508625) Amgen. Report of Amgen. July 2007.
Ref 525342ClinicalTrials.gov (NCT00534027) Amgen. Report of Amgen. January 22, 2009.
Ref 532312Safety, pharmacokinetics, and pharmacodynamics of the DR5 antibody LBY135 alone and in combination with capecitabine in patients with advanced solid tumors. Invest New Drugs. 2014 Feb;32(1):135-44.
Ref 543519(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: 1880).
Ref 544097Enhancement of Glioma Radiation Therapy and Chemotherapy Response with Targeted Antibody Therapy Against Death Receptor 5. Int J Radiat Oncol Biol Phys. 2008 June 1; 71(2): 507-516.
Ref 550250Clinical pipeline report, company report or official report of Amgen (2009).
Ref 550413National Cancer Institute Drug Dictionary (drug id 528015).

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