Activin receptor-like kinase 3 (ALK3)

Activin receptor-like kinase 3 (ALK3), also known as bone morphogenetic protein receptor type IA (BMPR1A), is a type I transmembrane serine/threonine kinase receptor in the TGF-β superfamily. ALK3 is a critical cell-surface receptor for bone morphogenetic proteins (BMPs), particularly BMP2 and BMP4, mediating both canonical (SMAD-dependent) and non-canonical signaling pathways that regulate gene transcription, cell fate, and morphogenesis. ALK3 signaling is essential for the development and regeneration of mineralized tissues (bone, teeth) and maintains tissue homeostasis by modulating cell differentiation, proliferation, and apoptosis. Dysfunction or mutation of ALK3 is linked to developmental abnormalities and diseases such as skeletal dysplasias, cancer, and fibrotic conditions. Therapeutically, ALK3 modulation is under investigation for tissue repair, fibrosis reversal, and potentially cancer, with both agonists and antagonists being studied for targeted interventions.

Other names

Bone morphogenetic protein receptor type IA (BMPR1A)BMP receptor type IABMPRI-ACD292

Agonists (e.g., THR-123, BMP2) activate ALK3 to promote BMP-mediated signaling and tissue regeneration, inhibit inflammation and fibrosis. Antagonists/inhibitors block ALK3 kinase activity, altering SMAD and non-SMAD signaling.