Activin type 1 receptors
The Activin type I receptors transduce signals for a variety of members of the Transforming growth factor beta superfamily of ligands. This family of cytokines and hormones include activin, Anti-müllerian hormone (AMH), bone morphogenetic proteins (BMPs), and Nodal. They are involved in a host of physiological processes including, growth, cell differentiation, homeostasis, osteogenesis, apoptosis and many other functions. There are three type I Activin receptors: ACVR1, ACVR1B, and ACVR1C. Each bind to a specific type II receptor-ligand complex.
Despite the large amount of processes that these ligands regulate, they all operate through essentially the same pathway: A ligand binds to a Type two receptor, which recruits and trans-phosphorylate a type I receptor. The type I receptor recruits a receptor regulated SMAD (R-SMAD) which it phosphorylates. The RSMAD then translocates to the nucleus where it functions as a transcription factor.
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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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