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It shares with other type I receptors a high degree of similarity in serine-threonine kinase subdomains, a glycine- and serine-rich region (called the GS domain) preceding the kinase domain, and a short C-terminal tail. The encoded protein, sometimes termed ALK1, shares similar domain structures with other closely related ALK or activin receptor-like kinase.
P7170, a novel inhibitor of mTORC1/mTORC2 and Activin receptor-like Kinase.
Keywords: RepSox, supplier, potent, inhibitors, TGF-βRI, TGF-β, TGF-betaRI, TGFbRI, TGFbR1, tgf-b1ALK5, ALK, Receptors, Activin, Receptor-like, Kinase.
Inman GJ, Nicolás FJ, Callahan JF, Harling JD, Gaster LM, Reith AD, Laping NJ, Hill CS (2002). "SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7". Mol. Pharmacol. 62 (1): 65–74. doi:10. 1124/mol.
– February 5, 2013 – Acceleron Pharma, Inc. , a biopharmaceutical company developing protein therapeutics for cancer and orphan diseases, announced the initiation of a phase 2 study of dalantercept, a novel angiogenesis inhibitor that targets the activin receptor-like kinase 1 (ALK1) pathway. The phase 2 study is a two-part, randomized study of dalantercept in combination with axitinib (Inlyta®, Pfizer), a vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitor, to treat patients with metastatic renal cell carcinoma (RCC).
Ligand binding leads to formation of the receptor heterocomplex, in which TßRII phosphorylates threonine and serine residues in the TTSGSGSG motif of TßRI and thus activates TßRI [2,4]. The activated TßRI recruits and phosphorylates the R-Smad proteins, Smad2/3 for TGF-ß and activin signaling while Smad1/5/8 for BMP signaling, which then form a heterocomplex with the Co-Smad Smad4 [5,6]. The Smad complexes are then translocated into the nucleus to regulate transcription of the target genes in cooperation with other co-factors [5,7,8]. For each member of the TGF-ß family, they have their own type I and type II receptors. Among the seven type I receptors, which are also called as activin receptor-like kinases.
g. , TGF-βs, activins, and bone morphogenetic proteins (BMPs)) signal via heteromeric serine/threonine kinase transmembrane receptor complexes [10–13]. The effects of TGF-β are mediated by three TGF-β ligands, TGF-β1, 2, and 3 via TGF-β type I and II receptors [9, 14, 15]. The binding of the ligand to its primary (type II) receptor, a constitutively active kinase, allows the recruitment, trans-phosphorylation, and activation of the signaling (type I) receptor. The receptor, also known as activin receptor-like kinase.