Bone morphogenetic protein receptor type 1A and Bone morphogenetic protein receptor type 2 (BMPR1A and BMPR2)

Bone morphogenetic protein receptor type 1A (BMPR1A) and type 2 (BMPR2) are transmembrane serine/threonine kinase receptors that function as heteromeric complexes to mediate signaling of bone morphogenetic proteins (BMPs), which are part of the TGF-β superfamily. These receptors are crucial in regulating cell fate, proliferation, differentiation, and apoptosis during development and tissue maintenance. Mutations in BMPR1A are linked to conditions such as juvenile polyposis syndrome, while BMPR2 mutations are causally associated with pulmonary arterial hypertension. The receptor-ligand interaction activates intracellular SMAD proteins, which translocate to the nucleus to regulate gene transcription. Both BMPR1A and BMPR2 are established drug targets, with clinical and investigational therapies aiming to modulate their activity in various diseases including cancer and cardiovascular conditions.

Other names

CD292ALK3BMPR-IIBone morphogenetic receptors, type IBone morphogenetic receptors, type II

Ligands (e.g., BMP2, BMP4, GDF5, GDF6) bind to and activate the receptors, inducing phosphorylation cascades and activation of SMAD transcription factors. Inhibitors (e.g., kinase inhibitors) block serine/threonine kinase activity, modulating downstream signaling.