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Receptor Serine/Threonine Kinases (RSTKs) as Drug Target

Receptor Serine/Threonine Kinases (RSTKs) as Drug Target Background

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.

Receptor Serine/Threonine Kinases as Drug Target List

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

References

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.

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