Target General Infomation
Target ID
T70067 (Former ID: TTDC00266)
Target Name
TRAIL receptor 2 (TRAIL-R2)
Synonyms
ZTNFR9; UNQ160/PRO186; Tumor necrosis factor receptor superfamily member 10B; TRICK2; TRAILR2; TNF-related apoptosis-inducing ligand receptor 2; KILLER; Death receptor 5; DR5; CD262
Gene Name
TNFRSF10B
Target Type
Clinical trial target
[1]
Disease [+] 3 Target-related Diseases +
1 Colorectal cancer [ICD-11: 2B91]
2 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
3 Liver cancer [ICD-11: 2C12]
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. Essential for ER stress-induced apoptosis. Receptor for the cytotoxic ligand TNFSF10/TRAIL.
BioChemical Class
Cytokine receptor
UniProt ID
TR10B_HUMAN
Sequence
MEQRGQNAPAASGARKRHGPGPREARGARPGPRVPKTLVLVVAAVLLLVSAESALITQQD
LAPQQRAAPQQKRSSPSEGLCPPGHHISEDGRDCISCKYGQDYSTHWNDLLFCLRCTRCD
SGEVELSPCTTTRNTVCQCEEGTFREEDSPEMCRKCRTGCPRGMVKVGDCTPWSDIECVH
KESGTKHSGEVPAVEETVTSSPGTPASPCSLSGIIIGVTVAAVVLIVAVFVCKSLLWKKV
LPYLKGICSGGGGDPERVDRSSQRPGAEDNVLNEIVSILQPTQVPEQEMEVQEPAEPTGV
NMLSPGESEHLLEPAEAERSQRRRLLVPANEGDPTETLRQCFDDFADLVPFDSWEPLMRK
LGLMDNEIKVAKAEAAGHRDTLYTMLIKWVNKTGRDASVHTLLDALETLGERLAKQKIED
HLLSSGKFMYLEGNADSAMS
Drugs and Modes of Action
Clinical Trial Drug(s) [+] 3 Clinical Trial Drugs +
1 Conatumumab Drug Info Phase 2 Colorectal cancer [2]
2 Lexatumumab Drug Info Phase 2 Solid tumour/cancer [3]
3 Anti-DR5 cells Drug Info Phase 1/2 Hepatocellular carcinoma [4]
Discontinued Drug(s) [+] 3 Discontinued Drugs +
1 RhApo2L/TRAIL Drug Info Discontinued in Phase 1/2 Solid tumour/cancer [5]
2 HGS-TR2J Drug Info Discontinued in Phase 1 Solid tumour/cancer [6]
3 LBY-135 Drug Info Discontinued in Phase 1 Solid tumour/cancer [7]
Mode of Action [+] 2 Modes of Action +
Agonist [+] 2 Agonist drugs +
1 Conatumumab Drug Info [1], [8]
2 RhApo2L/TRAIL Drug Info [1], [10]
CAR-T-Cell-Therapy [+] 1 CAR-T-Cell-Therapy drugs +
1 Anti-DR5 cells Drug Info [4]
Target Regulators
Target-regulating microRNAs
Target-interacting Proteins
Target Profiles in Patients
Target Expression
 Profile (TEP)
Target Affiliated Biological Pathways
KEGG Pathway [+] 6 KEGG Pathways +
1 Cytokine-cytokine receptor interaction
2 p53 signaling pathway
3 Apoptosis
4 Natural killer cell mediated cytotoxicity
5 Measles
6 Influenza A
NetPath Pathway [+] 2 NetPath Pathways +
1 TCR Signaling Pathway
2 TNFalpha Signaling Pathway
Panther Pathway [+] 2 Panther Pathways +
1 Apoptosis signaling pathway
2 p53 pathway
PID Pathway [+] 3 PID Pathways +
1 TRAIL signaling pathway
2 Direct p53 effectors
3 Caspase Cascade in Apoptosis
Reactome [+] 6 Reactome Pathways +
1 Ligand-dependent caspase activation
2 Regulation by c-FLIP
3 RIPK1-mediated regulated necrosis
4 CASP8 activity is inhibited
5 Dimerization of procaspase-8
6 TRAIL signaling
WikiPathways [+] 10 WikiPathways +
1 DNA Damage Response
2 Apoptosis-related network due to altered Notch3 in ovarian cancer
3 Apoptosis
4 miR-targeted genes in squamous cell - TarBase
5 miR-targeted genes in muscle cell - TarBase
6 miR-targeted genes in lymphocytes - TarBase
7 miR-targeted genes in epithelium - TarBase
8 Extrinsic Pathway for Apoptosis
9 Apoptosis Modulation and Signaling
10 miRNA Regulation of DNA Damage Response
Target-Related Models and Studies
Target Validation
References
REF 1 Clinical pipeline report, company report or official report of Amgen (2009).
REF 2 ClinicalTrials.gov (NCT01327612) Open Label Extension Study of Conatumumab and AMG 479. U.S. National Institutes of Health.
REF 3 Drug evaluation: lexatumumab, an intravenous human agonistic mAb targeting TRAIL receptor 2. Curr Opin Mol Ther. 2006 Dec;8(6):539-46.
REF 4 ClinicalTrials.gov (NCT03638206) Autologous CAR-T/TCR-T Cell Immunotherapy for Malignancies
REF 5 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011860)
REF 6 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021611)
REF 7 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026275)
REF 8 ClinicalTrials.gov (NCT00534027) Amgen. Report of Amgen. January 22, 2009.
REF 9 National Cancer Institute Drug Dictionary (drug id 528015).
REF 10 ClinicalTrials.gov (NCT00508625) Amgen. Report of Amgen. July 2007.
REF 11 Enhancement 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 12 Safety, 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 13 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: 1880).

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