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
1744 A 77-01 TGF-βR 1 inhibitor; ALK 5 inhibitor €80.00
1421 A 83-01 TGF-βR 1 inhibitor; ALK 5 inhibitor €75.00
1708 Dorsomorphin Inhibitor of BMP signaling. Inhibits ALK2, 3 and 6 €65.00
2150 Dorsomorphin dihydrochloride Inhibitor of BMP signaling. Inhibits ALK2, 3 and 6 €65.00
1832 GW 788388 TGF-βR 1 inhibitor €60.00
2236 IN 1130 TGF-βR 1 inhibitor €125.00
2323 ITD 1 Selective inhibitor of TGFβ/Smad signaling that promotes cardiogenesis €105.00
2467 ITD-1, (+)- Selective inhibitor of TGFβ/Smad signaling that promotes cardiogenesis €165.00
2189 K 02288 Inhibitor of BMP signaling. Inhibits ALK1, 2, and 6 €90.00
1509 LDN 193189 hydrochloride Highly potent small molecule inhibitor of BMP type I receptors ALK2, ALK3, and ALK6 €70.00
2201 LDN 212854 trihydrochloride Potent ALK2-biased BMP type I receptor kinase inhibitor €105.00
1491 LY 2157299 TGF-βR2 inhibitor €70.00
1661 SB 431542 TGF-βR1 inhibitor; ALK inhibitor €70.00
2197 SB 505124 Selective inhibitor of TGF-β type I receptors ALK4 and ALK5 €95.00
2285 SB 525334 Potent and selective inhibitor of the TGF-βR1 (ALK5) receptor €105.00

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