Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T21960
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| Former ID |
TTDC00210
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| Target Name |
Angiopoietin-2
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| Gene Name |
ANGPT2
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| Synonyms |
ANG-2; ANGPT2
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| Target Type |
Clinical Trial
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| Disease | Breast cancer [ICD9: 174, 175; ICD10: C50] | ||||
| 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 |
Binds to TEK/TIE2, competing for the ANGPT1 bindingsite, and modulating ANGPT1 signaling. 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.
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| BioChemical Class |
Fibrinogen
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| Target Validation |
T21960
|
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| UniProt ID | |||||
| Sequence |
MWQIVFFTLSCDLVLAAAYNNFRKSMDSIGKKQYQVQHGSCSYTFLLPEMDNCRSSSSPY
VSNAVQRDAPLEYDDSVQRLQVLENIMENNTQWLMKLENYIQDNMKKEMVEIQQNAVQNQ TAVMIEIGTNLLNQTAEQTRKLTDVEAQVLNQTTRLELQLLEHSLSTNKLEKQILDQTSE INKLQDKNSFLEKKVLAMEDKHIIQLQSIKEEKDQLQVLVSKQNSIIEELEKKIVTATVN NSVLQKQQHDLMETVNNLLTMMSTSNSAKDPTVAKEEQISFRDCAEVFKSGHTTNGIYTL TFPNSTEEIKAYCDMEAGGGGWTIIQRREDGSVDFQRTWKEYKVGFGNPSGEYWLGNEFV SQLTNQQRYVLKIHLKDWEGNEAYSLYEHFYLSSEELNYRIHLKGLTGTAGKISSISQPG NDFSTKDGDNDKCICKCSQMLTGGWWFDACGPSNLNGMYYPQRQNTNKFNGIKWYYWKGS GYSLKATTMMIRPADF |
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| Drugs and Mode of Action | |||||
| Drug(s) | AMG 386 | Drug Info | Phase 3 | Breast cancer | [1], [2] |
| RG7221 | Drug Info | Phase 2 | Colorectal cancer | [3] | |
| RO5520985 | Drug Info | Phase 2 | Colorectal cancer | [4] | |
| CVX-060 | Drug Info | Phase 1/2 | Solid tumours | [5] | |
| CVX-241 | Drug Info | Phase 1 | Cancer | [6] | |
| MEDI-3617 | Drug Info | Phase 1 | Solid tumours | [7] | |
| REGN-910 | Drug Info | Phase 1 | Solid tumours | [8] | |
| Modulator | AMG 386 | Drug Info | [9] | ||
| CVX-241 | Drug Info | [6] | |||
| RG7221 | Drug Info | ||||
| RO5520985 | Drug Info | [10] | |||
| Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
| TEP | EXP Info | ||||
| Pathways | |||||
| KEGG Pathway | Ras signaling pathway | ||||
| Rap1 signaling pathway | |||||
| HIF-1 signaling pathway | |||||
| PI3K-Akt signaling pathway | |||||
| NetPath Pathway | TGF_beta_Receptor Signaling Pathway | ||||
| PANTHER Pathway | Angiogenesis | ||||
| Pathway Interaction Database | Angiopoietin receptor Tie2-mediated signaling | ||||
| Reactome | Tie2 Signaling | ||||
| WikiPathways | Cell surface interactions at the vascular wall | ||||
| References | |||||
| REF 1 | ClinicalTrials.gov (NCT01281254) TRINOVA-2: Trebananib in Ovarian Cancer-2. U.S. National Institutes of Health. | ||||
| REF 2 | (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: 8414). | ||||
| REF 3 | 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 4 | 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 5 | Clinical pipeline report, company report or official report of CovX (2011). | ||||
| REF 6 | Chemical generation of bispecific antibodies. Proc Natl Acad Sci U S A. 2010 December 28; 107(52): 22611-22616. | ||||
| 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 800030291) | ||||
| REF 8 | ClinicalTrials.gov (NCT01271972) Study of Nesvacumab (REGN910/ SAR307746). U.S. National Institutes of Health. | ||||
| REF 9 | Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41. | ||||
| REF 10 | Bispecific antibodies rise again. Nat Rev Drug Discov. 2014 Nov;13(11):799-801. doi: 10.1038/nrd4478. | ||||
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