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Receptor serine/threonine kinase receptors

Receptor serine/threonine kinases (RSTKs) are a group of related catalytic receptors that includes TGF-β receptors (TGF-βRI-III) and activin receptors (ALK1-7).  RSTKs exist as heterodimers of type I and type II receptors and the ligand binding domain is located in the type II receptor.  Upon ligand-receptor binding, the type I receptors are recruited to the complex and are phosphorylated by the type II receptor.  Many human diseases are caused by dysregulation of RSTK signaling, including gastrointestinal, pancreatic and pituitary malignancies.

Peptides
Cat No. Product Name Activity
EI-030 BMP-2 derived peptide Inhibits BMP-2 binding to BMP receptors type IA and type II
RK-010 BMP2pp BMP-2 mimetic
Small molecules
Cat No. Product Name Activity
RK-030 SB 431542 Potent, selective inhibitor of TGF-βRI, ALK4 and ALK7
RK-020 A 83-01 TGF-βRI, ALK4 and ALK7 inhibitor
KS-300 Dorsomorphin AMPK inhibitor

Further reading

Josso and di Clemente (1997) Serine/threonine kinase receptors and ligands. Curr. Opin. Genet. Dev. 1997 7(3) 371 PMID: 9229113

Botello-Smith et al (2017) Polymodal allosteric regulation of Type 1 Serine/Threonine Kinase Receptors via a conserved electrostatic lock. PLoS Comput. Biol. 13(8) e1005711 PMID: 28827795

Chaplin et al (2017) Insights into cellular signalling by G protein coupled receptor transactivation of cell surface protein kinase receptors. J. Cell Commun. Signal. 11 117 PMID: 28168348

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