Receptor Serine/Threonine Kinases (RSTKs), respond to specific cytokines, including the transforming growth factor β (TGFβ) and bone morphogenetic protein (BMP) families. With the recent clinical success of drugs targeting protein kinase activity, drug discovery efforts are focusing on the role of reversible protein phosphorylation in disease states.
Activins signal through a combination of type I and II transmembrane serine/threonine kinase receptors. Activin receptors are shared by multiple transforming growth factor-β (TGF-β) ligands such as myostatin, growth and differentiation factor-11 and nodal.
| Category | Drug Target | Nomenclature |
|---|---|---|
| Type I receptor serine/threonine kinases | ACVRL1 ACVR1 BMPR1A ACVR1B TGFBR1 BMPR1B ACVR1C |
activin A receptor type IL activin A receptor type 1 bone morphogenetic protein receptor type IA activin A receptor type 1B transforming growth factor beta receptor 1 bone morphogenetic protein receptor type IB activin A receptor type 1C |
| Type II receptor serine/threonine kinases | ACVR2A ACVR2B AMHR2 BMPR2 TGFBR2 |
activin A receptor type 2A activin A receptor type 2B anti-Mullerian hormone receptor type 2 bone morphogenetic protein receptor type 2 transforming growth factor beta receptor 2 |
| Type III receptor serine/threonine kinases | TGFBR3 | transforming growth factor beta receptor 3 |
1. ten Dijke P, et al. Serine/threonine kinase receptors[J]. Progress in growth factor research, 1994, 5(1): 55-72.
2. Tsuchida K, et al. Activin signaling as an emerging target for therapeutic interventions[J]. Cell Communication and Signaling, 2009, 7(1): 15.
