Target Information

Target General Infomation
Target ID
T21960
Former ID
TTDC00210
Target Name
Angiopoietin-2
Gene Name
ANGPT2
Synonyms
ANG-2; ANGPT2
Target Type
Clinical Trial
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.
BioChemical Class
Fibrinogen
Target Validation
T21960
UniProt ID
O15123
Sequence
MWQIVFFTLSCDLVLAAAYNNFRKSMDSIGKKQYQVQHGSCSYTFLLPEMDNCRSSSSPY
VSNAVQRDAPLEYDDSVQRLQVLENIMENNTQWLMKLENYIQDNMKKEMVEIQQNAVQNQ
TAVMIEIGTNLLNQTAEQTRKLTDVEAQVLNQTTRLELQLLEHSLSTNKLEKQILDQTSE
INKLQDKNSFLEKKVLAMEDKHIIQLQSIKEEKDQLQVLVSKQNSIIEELEKKIVTATVN
NSVLQKQQHDLMETVNNLLTMMSTSNSAKDPTVAKEEQISFRDCAEVFKSGHTTNGIYTL
TFPNSTEEIKAYCDMEAGGGGWTIIQRREDGSVDFQRTWKEYKVGFGNPSGEYWLGNEFV
SQLTNQQRYVLKIHLKDWEGNEAYSLYEHFYLSSEELNYRIHLKGLTGTAGKISSISQPG
NDFSTKDGDNDKCICKCSQMLTGGWWFDACGPSNLNGMYYPQRQNTNKFNGIKWYYWKGS
GYSLKATTMMIRPADF
Drugs and Mode of Action
Drug(s) AMG 386 Drug Info Phase 3 Breast cancer [523327], [543118]
RG7221 Drug Info Phase 2 Colorectal cancer [549449]
RO5520985 Drug Info Phase 2 Colorectal cancer [889398]
CVX-060 Drug Info Phase 1/2 Solid tumours [550567]
CVX-241 Drug Info Phase 1 Cancer [544157]
MEDI-3617 Drug Info Phase 1 Solid tumours [548917]
REGN-910 Drug Info Phase 1 Solid tumours [523314]
Modulator AMG 386 Drug Info [1572591]
CVX-241 Drug Info [544157]
RG7221 Drug Info
RO5520985 Drug Info [889442]
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 523314ClinicalTrials.gov (NCT01271972) Study of Nesvacumab (REGN910/ SAR307746). U.S. National Institutes of Health.
Ref 523327ClinicalTrials.gov (NCT01281254) TRINOVA-2: Trebananib in Ovarian Cancer-2. U.S. National Institutes of Health.
Ref 543118(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 544157Chemical generation of bispecific antibodies. Proc Natl Acad Sci U S A. 2010 December 28; 107(52): 22611-22616.
Ref 548917Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030291)
Ref 549449Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800037469)
Ref 550567Clinical pipeline report, company report or official report of CovX (2011).
Ref 889398ClinicalTrials.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
Ref 531798MEDI3617, a human anti-angiopoietin 2 monoclonal antibody, inhibits angiogenesis and tumor growth in human tumor xenograft models. Int J Oncol. 2012 May;40(5):1321-30.
Ref 532117Angiopoietin-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 544157Chemical generation of bispecific antibodies. Proc Natl Acad Sci U S A. 2010 December 28; 107(52): 22611-22616.
Ref 550567Clinical pipeline report, company report or official report of CovX (2011).
Ref 889442Bispecific antibodies rise again. Nat Rev Drug Discov. 2014 Nov;13(11):799-801. doi: 10.1038/nrd4478.
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

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