Technical Articles
ActRIIA
Novel 7-Azaindole Small Molecule Inhibitors Targeting ActRIIB: A New Strategy to Tackle Cancer Cachexia
ActRIIB (Activin Type IIB Receptor) and ACTRIIA (Activin Type IIA Receptor) are structurally similar transmembrane receptors belonging to the TGF-β receptor superfamily. They collectively function to receive extracellular "growth regulatory signals," yet exhibit key distinctions in their physiological roles and their value as drug targets.
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- Drug Research
- ActRIIB
- ACTRIIA
- TGF-β receptor
- UA BIOSCIENCE
- UA Protein
ALK4:ActRIIB heterodimer signaling axis, its cooperative inhibition mechanism, and its application in ligand-selective trapping.
ALK4 and ActRIIB are a functionally coupled pair of type I and type II transmembrane serine/threonine kinase receptors within the transforming growth factor-beta (TGF-β) superfamily signaling pathway. ActRIIB, as the type II receptor, features an extracellular domain that binds with high affinity to various ligands, including activin, GDF8 (myostatin), and GDF11, and possesses constitutive kinase activity. In contrast, ALK4, as the type I receptor, is strictly dependent on the type II receptor for its activation. Together, in the presence of ligand, they form a stable heterotetrameric signal transduction complex.
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- Signaling Pathway
- ALK4
- ActRIIB
- ActRIIA
- kinase
- and TGF-β.
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