Target Information
| Target General Information | Top | |||||
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| Target ID |
T21960
(Former ID: TTDC00210)
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| Target Name |
Angiopoietin-2 (ANGPT2)
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| Synonyms |
ANG-2
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| Gene Name |
ANGPT2
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 4 Target-related Diseases | + | ||||
| 1 | Breast cancer [ICD-11: 2C60-2C6Y] | |||||
| 2 | General pain disorder [ICD-11: 8E43] | |||||
| 3 | Ovarian cancer [ICD-11: 2C73] | |||||
| 4 | Retinopathy [ICD-11: 9B71] | |||||
| Function |
Can induce tyrosine phosphorylation of TEK/TIE2 in the absence of ANGPT1. In the absence of angiogenic inducers, such as VEGF, ANGPT2-mediated loosening of cell-matrix contacts may induce endothelial cell apoptosis with consequent vascular regression. In concert with VEGF, it may facilitate endothelial cell migration and proliferation, thus serving as a permissive angiogenic signal. Binds to TEK/TIE2, competing for the ANGPT1 binding site, and modulating ANGPT1 signaling.
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| BioChemical Class |
Fibrinogen protein
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| UniProt ID | ||||||
| Sequence |
MWQIVFFTLSCDLVLAAAYNNFRKSMDSIGKKQYQVQHGSCSYTFLLPEMDNCRSSSSPY
VSNAVQRDAPLEYDDSVQRLQVLENIMENNTQWLMKLENYIQDNMKKEMVEIQQNAVQNQ TAVMIEIGTNLLNQTAEQTRKLTDVEAQVLNQTTRLELQLLEHSLSTNKLEKQILDQTSE INKLQDKNSFLEKKVLAMEDKHIIQLQSIKEEKDQLQVLVSKQNSIIEELEKKIVTATVN NSVLQKQQHDLMETVNNLLTMMSTSNSAKDPTVAKEEQISFRDCAEVFKSGHTTNGIYTL TFPNSTEEIKAYCDMEAGGGGWTIIQRREDGSVDFQRTWKEYKVGFGNPSGEYWLGNEFV SQLTNQQRYVLKIHLKDWEGNEAYSLYEHFYLSSEELNYRIHLKGLTGTAGKISSISQPG NDFSTKDGDNDKCICKCSQMLTGGWWFDACGPSNLNGMYYPQRQNTNKFNGIKWYYWKGS GYSLKATTMMIRPADF Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T29PJS | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 13 Clinical Trial Drugs | + | ||||
| 1 | AMG 386 | Drug Info | Phase 3 | Neuropathic pain | [2] | |
| 2 | Faricimab | Drug Info | Phase 3 | Diabetic macular edema | [3] | |
| 3 | Trebananib | Drug Info | Phase 3 | Ovarian cancer | [4] | |
| 4 | REGN910-3 | Drug Info | Phase 2 | Neovascular age-related macular degeneration | [5] | |
| 5 | RG7221 | Drug Info | Phase 2 | Colorectal cancer | [6] | |
| 6 | RO5520985 | Drug Info | Phase 2 | Colorectal cancer | [7] | |
| 7 | CVX-060 | Drug Info | Phase 1/2 | Solid tumour/cancer | [8] | |
| 8 | BI 836880 | Drug Info | Phase 1 | Neoplasm | [9] | |
| 9 | CVX-241 | Drug Info | Phase 1 | Solid tumour/cancer | [10] | |
| 10 | LY3127804 | Drug Info | Phase 1 | Solid tumour/cancer | [11] | |
| 11 | MEDI3617 | Drug Info | Phase 1 | Solid tumour/cancer | [12] | |
| 12 | Nesvacumab | Drug Info | Phase 1 | Solid tumour/cancer | [13] | |
| 13 | REGN-910 | Drug Info | Phase 1 | Solid tumour/cancer | [14], [15], [16] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Modulator | [+] 4 Modulator drugs | + | ||||
| 1 | AMG 386 | Drug Info | [1] | |||
| 2 | RG7221 | Drug Info | [19] | |||
| 3 | RO5520985 | Drug Info | [20] | |||
| 4 | CVX-241 | Drug Info | [10], [22] | |||
| Inhibitor | [+] 4 Inhibitor drugs | + | ||||
| 1 | Trebananib | Drug Info | [18] | |||
| 2 | REGN910-3 | Drug Info | [5] | |||
| 3 | MEDI3617 | Drug Info | [23] | |||
| 4 | Nesvacumab | Drug Info | [24] | |||
| Blocker | [+] 1 Blocker drugs | + | ||||
| 1 | BI 836880 | Drug Info | [21] | |||
| Binder | [+] 1 Binder drugs | + | ||||
| 1 | ABTAA | Drug Info | [26] | |||
| 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 Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 4 KEGG Pathways | + | ||||
| 1 | Ras signaling pathway | |||||
| 2 | Rap1 signaling pathway | |||||
| 3 | HIF-1 signaling pathway | |||||
| 4 | PI3K-Akt signaling pathway | |||||
| NetPath Pathway | [+] 1 NetPath Pathways | + | ||||
| 1 | TGF_beta_Receptor Signaling Pathway | |||||
| Panther Pathway | [+] 1 Panther Pathways | + | ||||
| 1 | Angiogenesis | |||||
| PID Pathway | [+] 1 PID Pathways | + | ||||
| 1 | Angiopoietin receptor Tie2-mediated signaling | |||||
| Reactome | [+] 1 Reactome Pathways | + | ||||
| 1 | Tie2 Signaling | |||||
| WikiPathways | [+] 1 WikiPathways | + | ||||
| 1 | Cell surface interactions at the vascular wall | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41. | |||||
| REF 2 | Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26. | |||||
| REF 3 | ClinicalTrials.gov (NCT04432831) A Study to Evaluate the Long-Term Safety and Tolerability of Faricimab in Participants With Diabetic Macular Edema (Rhone-X). U.S. National Institutes of Health. | |||||
| REF 4 | ClinicalTrials.gov (NCT01281254) AMG 386 (Trebananib) in Ovarian Cancer (TRINOVA-2). U.S. National Institutes of Health. | |||||
| REF 5 | ClinicalTrials.gov (NCT02713204) Anti-angiOpoeitin 2 Plus Anti-vascular eNdothelial Growth Factor as a therapY for Neovascular Age Related Macular Degeneration: Evaluation of a fiXed Combination Intravitreal Injection (ONYX). U.S. National Institutes of Health. | |||||
| 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 800037469) | |||||
| REF 7 | ClinicalTrials.gov (NCT02141295) A Study Comparing the Efficacy and Safety of Vanucizumab and FOLFOX With Bevacizumab and FOLFOX in Participants With Untreated Metastatic Colorectal Cancer | |||||
| REF 8 | Clinical pipeline report, company report or official report of CovX (2011). | |||||
| REF 9 | ClinicalTrials.gov (NCT03972150) A Study to Find the Best Dose of BI 836880 Alone and in Combination With BI 754091 in Japanese Patients With Different Types of Advanced Cancer. U.S. National Institutes of Health. | |||||
| REF 10 | Chemical generation of bispecific antibodies. Proc Natl Acad Sci U S A. 2010 December 28; 107(52): 22611-22616. | |||||
| REF 11 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| 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 800030291) | |||||
| REF 13 | ClinicalTrials.gov (NCT01271972) Study of Nesvacumab (REGN910/ SAR307746). U.S. National Institutes of Health. | |||||
| REF 14 | ClinicalTrials.gov (NCT01271972) Study of Nesvacumab (REGN910/ SAR307746). U.S. National Institutes of Health. | |||||
| REF 15 | 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. (Ligand id: 8457). | |||||
| REF 16 | ClinicalTrials.gov (NCT01997164) Study of Intravitreal (IVT) REGN910-3 and IVT REGN910 in Patients With Either Neovascular ("Wet") Age Related Macular Degeneration (AMD) or Diabetic Macular Edema (DME). U.S. National Institutes of Health. | |||||
| REF 17 | Faricimab: an investigational agent targeting the Tie-2/angiopoietin pathway and VEGF-A for the treatment of retinal diseases. Expert Opin Investig Drugs. 2021 Mar;30(3):193-200. | |||||
| REF 18 | Pediatric Phase I Trial and Pharmacokinetic Study of Trebananib in Relapsed Solid Tumors, Including Primary Tumors of the Central Nervous System ADVL1115: A Children's Oncology Group Phase I Consortium Report. Clin Cancer Res. 2017 Oct 15;23(20):6062-6069. | |||||
| REF 19 | Company report (Roche pipeline: July 27, 2017) | |||||
| REF 20 | Bispecific antibodies rise again. Nat Rev Drug Discov. 2014 Nov;13(11):799-801. | |||||
| REF 21 | Clinical pipeline report, company report or official report of Boehringer Ingelheim. | |||||
| REF 22 | A Safety, Tolerability, And Pharmacokinetic Trial With CVX-241 In Patients With Advanced Solid Tumors | |||||
| REF 23 | Phase I Study of MEDI3617, a Selective Angiopoietin-2 Inhibitor Alone and Combined with Carboplatin/Paclitaxel, Paclitaxel, or Bevacizumab for Advanced Solid Tumors. Clin Cancer Res. 2018 Jun 15;24(12):2749-2757. | |||||
| REF 24 | Tie-2/Angiopoietin pathway modulation as a therapeutic strategy for retinal disease. Expert Opin Investig Drugs. 2019 Oct;28(10):861-869. | |||||
| REF 25 | Angiopoietin-2 functions as a Tie2 agonist in tumor models, where it limits the effects of VEGF inhibition. Cancer Res. 2013 Jan 1;73(1):108-18. | |||||
| REF 26 | Amelioration of sepsis by TIE2 activation-induced vascular protection. Sci Transl Med. 2016 Apr 20;8(335):335ra55. | |||||
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