| 靶标 | SKR1, Activin receptor type-1, Activin receptor-like kinase 2, TSR-I, ACVRLK2, ACTR-I, ALK-2, Serine/threonine-protein kinase receptor R1, TGF-B superfamily receptor type I, ACVR1, Activin receptor type I |
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| 背景 | Activin receptor type-1 (ACVR1/ALK-2) is a ~57 kDa protein. Bone morphogenetic protein (BMP) type I receptor that is involved in a wide variety of biological processes, including bone, heart, cartilage, nervous, and reproductive system development and regulation. As a type I receptor, forms heterotetrameric receptor complexes with the type II receptors AMHR2, ACVR2A or ACVR2B. Upon binding of ligands such as BMP7 or GDF2/BMP9 to the heteromeric complexes, type II receptors transphosphorylate ACVR1 intracellular domain. In turn, ACVR1 kinase domain is activated and subsequently phosphorylates SMAD1/5/8 proteins that transduce the signal. In addition to its role in mediating BMP pathway-specific signaling, suppresses TGFbeta/activin pathway signaling by interfering with the binding of activin to its type II receptor. 1. Luo, J. et al. (2010) The Journal of biological chemistry 285, 29588-98. PMID: 206280592. Chaikuad, A. et al. (2012) The Journal of biological chemistry 287, 36990-8. PMID: 229772373. Renlund, N. et al. (2007) The Journal of endocrinology 195, 95-103. PMID: 179114014. Fujimoto, M. et al. (2015) Molecular endocrinology (Baltimore, Md.) 29, 140-52. PMID: 253542965. Macías-Silva, M. et al. (1998) The Journal of biological chemistry 273, 25628-36. PMID: 9748228 |
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