The angiopoietin receptors are receptors that bind angiopoietin. TIE-1 and TIE-2 comprise the cell-surface receptors that bind and are activated by the angiopoietins, (Ang1, Ang2, Ang3, Ang4). The angiopoietins are protein growth factors required for the formation of blood vessels (angiogenesis).
Angiopoietins
The angiopoietins are protein growth factors that regulate angiogenesis, the formation of blood vessels. In humans, three angiopoietins have been identified: Ang1, Ang2, and Ang4 (Ang 3 is the mouse ortholog of human Ang4).[1] Ang1 and Ang4 function as agonistic or activating ligands for Tie2, whereas Ang2 and Ang3 behave as competitive antagonists. They function by binding their physiologic receptors, Tie-1 and Tie-2. These are receptor tyrosine kinases, so named because they mediate cell signals by inducing the phosphorylation of key tyrosines, thus initiating cell signalling.
It is somewhat controversial which of the Tie receptors mediate functional signals downstream of Ang stimulation. But it is clear that at least Tie-2 is capable of physiologic activation as a result of binding the angiopoietins.
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- Kinase inhibitors: Altiratinib
- CE-245677
- Rebastinib
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CNTF | |
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EGF (ErbB) | |
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FGF | FGFR1 | |
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FGFR2 |
- Agonists: Ersofermin
- FGF (1, 2 (bFGF), 3, 4, 5, 6, 7 (KGF), 8, 9, 10 (KGF2), 17, 18, 22)
- Palifermin
- Repifermin
- Selpercatinib
- Sprifermin
- Trafermin
- Antibodies: Aprutumab
- Aprutumab ixadotin
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FGFR3 | |
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FGFR4 | |
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Unsorted | |
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HGF (c-Met) | |
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IGF | IGF-1 |
- Kinase inhibitors: BMS-754807
- Linsitinib
- NVP-ADW742
- NVP-AEW541
- OSl-906
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IGF-2 |
- Antibodies: Dusigitumab
- Xentuzumab (against IGF-1 and IGF-2)
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Others |
- Cleavage products/derivatives with unknown target: Glypromate (GPE, (1-3)IGF-1)
- Trofinetide
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LNGF (p75NTR) |
- Aptamers: Against NGF: RBM-004
- Decoy receptors: LEVI-04 (p75NTR-Fc)
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PDGF | |
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RET (GFL) | |
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SCF (c-Kit) | |
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TGFβ | |
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Trk | TrkA |
- Negative allosteric modulators: VM-902A
- Aptamers: Against NGF: RBM-004
- Decoy receptors: ReN-1820 (TrkAd5)
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TrkB |
- Agonists: 3,7-DHF
- 3,7,8,2'-THF
- 4'-DMA-7,8-DHF
- 7,3'-DHF
- 7,8-DHF
- 7,8,2'-THF
- 7,8,3'-THF
- Amitriptyline
- BDNF
- BNN-20
- Deoxygedunin
- Deprenyl
- Diosmetin
- DMAQ-B1
- HIOC
- LM22A-4
- N-Acetylserotonin
- NT-3
- NT-4
- Norwogonin (5,7,8-THF)
- R7
- R13
- TDP6
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TrkC | |
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VEGF | |
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Others |
- Additional growth factors: Adrenomedullin
- Colony-stimulating factors (see here instead)
- Connective tissue growth factor (CTGF)
- Ephrins (A1, A2, A3, A4, A5, B1, B2, B3)
- Erythropoietin (see here instead)
- Glucose-6-phosphate isomerase (GPI; PGI, PHI, AMF)
- Glia maturation factor (GMF)
- Hepatoma-derived growth factor (HDGF)
- Interleukins/T-cell growth factors (see here instead)
- Leukemia inhibitory factor (LIF)
- Macrophage-stimulating protein (MSP; HLP, HGFLP)
- Midkine (NEGF2)
- Migration-stimulating factor (MSF; PRG4)
- Oncomodulin
- Pituitary adenylate cyclase-activating peptide (PACAP)
- Pleiotrophin
- Renalase
- Thrombopoietin (see here instead)
- Wnt signaling proteins
- Additional growth factor receptor modulators: Cerebrolysin (neurotrophin mixture)
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