RSTK

Transforming growth factor-β (TGF-β) family, including TGF-β, activin, Nodal, bone morphogenetic proteins (BMPs) and others, play vital roles in diverse cellular processes, including cell proliferation, differentiation, apoptosis, cell plasticity and migration. The type I receptor serine/threonine kinases (RSTKs) are also known as activin receptor-like kinases (ALKs) for which a systematic nomenclature has been proposed (ALK1-7) Its dysfunctions can result in various kinds of diseases, such as cancer and tissue fibrosis. Ligand binding leads to formation of the receptor heterocomplex, in which TGF-βRII phosphorylates threonine and serine residues  of TGF-βRI and thus activates TGF-βRI. The activated TGF-βRI recruits and phosphorylates a subset of SMAD proteins (SMAD 2/3) which are then translocated to the nucleus where they form transcription complexes with DNA binding factors and co-activators/co-repressors to regulate transcription of the target genes[1]. In normal cells, TGF-β, acting through its signaling pathway, stops the cell cycle at the G1 stage to stop proliferation, induce differentiation, or promote apoptosis. When a cell is transformed into a cancer cell, parts of the TGF-β signaling pathway are mutated, and TGF-β no longer controls the cell. These cancer cells proliferate[2].
Activins are dimeric growth and differentiation factors which belong to the transforming growth factor-beta (TGF-beta) superfamily of structurally related signaling proteins. Activins signal through a heteromeric complex of receptor serine kinases which include type I and type II receptors, and transduce signals through Smad-dependent and independent mechanisms. Type I receptors are essential for signaling; and type II receptors are required for binding ligands and for expression of type I receptors. Type I and II receptors form a stable complex after ligand binding, resulting in phosphorylation of type I receptors by type II receptors. Type II receptors are considered to be constitutively active kinases[3],[4].

RSTKs listed: BMP-ALK, TGF-βR


[1] Regulation of TGF-β receptor activity. F. Huang Y.G. Chen. Cell Biosc. 2012, 2-9.
[2] Mechanisms of TGF-beta signaling from cell membrane to the nucleus. Shi Y, Massagué J. Cell. 2003, 113, 685-700.
[3] Activin receptor signaling: a potential therapeutic target for osteoporosis. S. Lotinun, R.S.Pearsall, W.C. Horne, R. Baron Curr. Mol. Pharmacol. 2012, 5, 195-204.
[4] Activin receptor antagonists for cancer-related anemia and bone disease. S.Z. Fields et al.  Exp. Opinion Invest. Drugs 2013, 22, 87-101. 

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Axon ID Name Description From price
1387 SD 208 TGF-βR 1 inhibitor €60.00
2903 SJ000291942 Activator of the canonical BMP signaling pathway €95.00
2943 SRI-011381 hydrochloride TGF-β signaling agonist €125.00
5009 Stem Cell 4i inhibitor Set Set of Thiazovivin, SB 431542, PD 0325901, and CHIR 99021 (inhibitors of ROCK, TGF-β, MEK, and GSK-3 resp.) €190.00
5007 Stem Cell 5i inhibitor Set Set of five inhibitors for neural differentiation of human pluripotent stem cells. €220.00
5004 Stem Cell LSB inhibitor Set Set of BMP inhibitor LDN 193189 (Axon 1509) and TGF-β inhibitor SB 431542 (Axon 1661) €105.00
5005 Stem Cell LSC inhibitor Set Set of LDN 193189 HCl, SB 431542 and CHIR 99021, inhibitors of BMP, TGF-β, and GSK-3 resp. €145.00

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