Transforming growth factor
Transforming growth factor (sometimes referred to as Tumor growth factor, or TGF) is used to describe two classes of polypeptide growth factors, TGFα and TGFβ.
The name "Transforming Growth Factor" is somewhat arbitrary, since the two classes of TGFs are not structurally or genetically related to one another, and they act through different receptor mechanisms. Furthermore, they do not always induce cellular transformation, and are not the only growth factors that induce cellular transformation.
Types
- TGFα is upregulated in some human cancers. It is produced in macrophages, brain cells, and keratinocytes, and induces epithelial development.
- TGFβ exists in three known subtypes in humans, TGFβ1, TGFβ2, and TGFβ3. These are upregulated in Marfan's syndrome[1][2] and some human cancers, and play crucial roles in tissue regeneration, cell differentiation, embryonic development, and regulation of the immune system. Isoforms of transforming growth factor-beta (TGF-β1) are also thought to be involved in the pathogenesis of pre-eclampsia. TGFβ receptors are single pass serine/threonine kinase receptors.
Function
These proteins were originally characterized by their capacity to induce oncogenic transformation in a specific cell culture system, rat kidney fibroblasts. Application of the transforming growth factors to normal rat kidney fibroblasts induces the cultured cells to proliferate and overgrow, no longer subject to the normal inhibition caused by contact between cells.
See also
References
- ↑ Matt, P; Schoenhoff, F; Habashi, J; Holm, T; Van Erp, C; Loch, D; Carlson, OD; Griswold, BF; Fu, Q; De Backer, J; Loeys, B; Huso, DL; McDonnell, NB; Van Eyk, JE; Dietz, HC (Aug 2009). "Circulating transforming growth factor-{beta} in Marfan syndrome". Circulation. 120 (6): 526–32. PMC 2779568 . PMID 19635970. doi:10.1161/CIRCULATIONAHA.108.841981.
- ↑ Inhibiting TGF to help Marfan
External links
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Angiopoietin |
- 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
- 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
- Diosmetin
- GZ-389988
- HIOC
- LM22A-4
- N-Acetylserotonin
- NT-3
- NT-4
- Norwogonin (5,7,8-THF)
- R7
- 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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- See also
- Receptor/signaling modulators
- Signaling peptide/protein receptor modulators
- Cytokine receptor modulators
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Type I | ALK1 (ACVRL1) |
- Kinase inhibitors: K-02288
- ML-347 (LDN-193719, VU0469381)
- Other inhibitors: Disitertide
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ALK2 (ACVR1A) |
- Kinase inhibitors: DMH-1
- DMH-2
- Dorsomorphin (BML-275)
- K-02288
- ML-347 (LDN-193719, VU0469381)
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ALK3 (BMPR1A) |
- Kinase inhibitors: DMH-2
- Dorsomorphin (BML-275)
- K-02288
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ALK4 (ACVR1B) |
- Kinase inhibitors: A 83-01
- SB-431542
- SB-505124
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ALK5 (TGFβR1) | |
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ALK6 (BMPR1B) |
- Agonists: BMP (2, 4, 5, 6, 7, 8A, 8B, 15 (GDF9B))
- Dibotermin alfa
- Eptotermin alfa
- GDF (5 (BMP14), 6 (BMP13), 7 (BMP12), 9, 15)
- Radotermin
- Kinase inhibitors: DMH-2
- Dorsomorphin (BML-275)
- K-02288
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ALK7 (ACVR1C) |
- Kinase inhibitors: A 83-01
- SB-431542
- SB-505124
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Type II | TGFβR2 |
- Kinase inhibitors: DMH-2
- LY-364947
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BMPR2 | |
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ACVR2A (ACVR2) |
- Agonists: Activin (A, B, AB)
- BMP (2, 4, 5, 6, 7, 8A, 8B, 15 (GDF9B))
- Dibotermin alfa
- Eptotermin alfa
- GDF (1, 3, 5 (BMP14), 6 (BMP13), 7 (BMP12), 9, 11 (BMP11), 15)
- Myostatin (GDF8)
- Nodal
- Radotermin
- Decoy receptors: Sotatercept
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ACVR2B |
- Agonists: Activin (A, B, AB)
- BMP (2, 4, 6, 7)
- Dibotermin alfa
- Eptotermin alfa
- GDF (1, 3, 5 (BMP14), 6 (BMP13), 7 (BMP12))
- Myostatin (GDF8)
- Nodal
- Osteogenin (BMP3, BMP3A)
- Radotermin
- Decoy receptors: Ramatercept
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AMHR2 (AMHR) | |
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Type III | |
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Unsorted | |
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- See also
- Receptor/signaling modulators
- Signaling peptide/protein receptor modulators
- Growth factor receptor modulators
- Cytokine receptor modulators
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