Target Information
| Target General Information | Top | |||||
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| Target ID |
T70067
(Former ID: TTDC00266)
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| Target Name |
TRAIL receptor 2 (TRAIL-R2)
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| 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
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| Gene Name |
TNFRSF10B
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 4 Target-related Diseases | + | ||||
| 1 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
| 2 | Liver cancer [ICD-11: 2C12] | |||||
| 3 | Colorectal cancer [ICD-11: 2B91] | |||||
| 4 | Malignant haematopoietic neoplasm [ICD-11: 2B33] | |||||
| 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.
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| BioChemical Class |
Cytokine receptor
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| UniProt ID | ||||||
| Sequence |
MEQRGQNAPAASGARKRHGPGPREARGARPGPRVPKTLVLVVAAVLLLVSAESALITQQD
LAPQQRAAPQQKRSSPSEGLCPPGHHISEDGRDCISCKYGQDYSTHWNDLLFCLRCTRCD SGEVELSPCTTTRNTVCQCEEGTFREEDSPEMCRKCRTGCPRGMVKVGDCTPWSDIECVH KESGTKHSGEVPAVEETVTSSPGTPASPCSLSGIIIGVTVAAVVLIVAVFVCKSLLWKKV LPYLKGICSGGGGDPERVDRSSQRPGAEDNVLNEIVSILQPTQVPEQEMEVQEPAEPTGV NMLSPGESEHLLEPAEAERSQRRRLLVPANEGDPTETLRQCFDDFADLVPFDSWEPLMRK LGLMDNEIKVAKAEAAGHRDTLYTMLIKWVNKTGRDASVHTLLDALETLGERLAKQKIED HLLSSGKFMYLEGNADSAMS Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| ADReCS ID | BADD_A06535 | |||||
| HIT2.0 ID | T30L86 | |||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 8 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] | |
| 4 | BI 905711 | Drug Info | Phase 1 | Solid tumour/cancer | [5] | |
| 5 | DS-8273 | Drug Info | Phase 1 | Solid tumour/cancer | [6] | |
| 6 | GEN1029 | Drug Info | Phase 1 | Solid tumour/cancer | [7] | |
| 7 | IGM-8444 | Drug Info | Phase 1 | Solid tumour/cancer | [8] | |
| 8 | INBRX-109 | Drug Info | Phase 1 | Solid tumour/cancer | [9] | |
| Discontinued Drug(s) | [+] 3 Discontinued Drugs | + | ||||
| 1 | RhApo2L/TRAIL | Drug Info | Discontinued in Phase 1/2 | Solid tumour/cancer | [10] | |
| 2 | HGS-TR2J | Drug Info | Discontinued in Phase 1 | Solid tumour/cancer | [11] | |
| 3 | LBY-135 | Drug Info | Discontinued in Phase 1 | Solid tumour/cancer | [12] | |
| Mode of Action | [+] 3 Modes of Action | + | ||||
| Agonist | [+] 5 Agonist drugs | + | ||||
| 1 | Conatumumab | Drug Info | [1], [13] | |||
| 2 | DS-8273 | Drug Info | [16] | |||
| 3 | GEN1029 | Drug Info | [17] | |||
| 4 | IGM-8444 | Drug Info | [18] | |||
| 5 | RhApo2L/TRAIL | Drug Info | [1], [20] | |||
| CAR-T-Cell-Therapy | [+] 1 CAR-T-Cell-Therapy drugs | + | ||||
| 1 | Anti-DR5 cells | Drug Info | [4] | |||
| Activator | [+] 1 Activator drugs | + | ||||
| 1 | BI 905711 | Drug Info | [15] | |||
| Target Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| Target-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| 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 | ClinicalTrials.gov (NCT04137289) A Study to Find a Safe and Effective Dose of BI 905711 in Patients With Advanced Gastrointestinal Cancer. U.S. National Institutes of Health. | |||||
| REF 6 | ClinicalTrials.gov (NCT02076451) Open-label Study of DS-8273a to Assess Its Safety and Tolerability, and Assess Its Pharmacokinetic and Pharmacodynamic Properties in Subjects With Advanced Solid Tumors or Lymphomas. U.S. National Institutes of Health. | |||||
| REF 7 | ClinicalTrials.gov (NCT03576131) GEN1029 (HexaBody-DR5/DR5) Safety Trial in Patients With Malignant Solid Tumors. U.S. National Institutes of Health. | |||||
| REF 8 | ClinicalTrials.gov (NCT04553692) Study of IGM-8444 as a Single Agent and in Combination With Chemotherapy-based Regimens in Subjects With Solid Cancers. U.S. National Institutes of Health. | |||||
| REF 9 | ClinicalTrials.gov (NCT03715933) Phase 1 Study of INBRX-109 in Subjects With Locally Advanced or Metastatic Solid Tumors Including Sarcomas. U.S. National Institutes of Health. | |||||
| REF 10 | 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 11 | 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 12 | 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 13 | ClinicalTrials.gov (NCT00534027) Amgen. Report of Amgen. January 22, 2009. | |||||
| REF 14 | National Cancer Institute Drug Dictionary (drug id 528015). | |||||
| REF 15 | Selective Tumor Cell Apoptosis and Tumor Regression in CDH17-Positive Colorectal Cancer Models using BI 905711, a Novel Liver-Sparing TRAILR2 Agonist. Mol Cancer Ther. 2021 Jan;20(1):96-108. | |||||
| REF 16 | First-in-human study of the antibody DR5 agonist DS-8273a in patients with advanced solid tumors. Invest New Drugs. 2017 Jun;35(3):298-306. | |||||
| REF 17 | National Cancer Institute Drug Dictionary (drug name Tilogotamab). | |||||
| REF 18 | Clinical pipeline report, company report or official report of IGM Biosciences. | |||||
| REF 19 | Clinical pipeline report, company report or official report of Inhibrx. | |||||
| REF 20 | ClinicalTrials.gov (NCT00508625) Amgen. Report of Amgen. July 2007. | |||||
| REF 21 | 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 22 | 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 23 | 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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