SB-431542 is a potent and specific inhibitor of transforming growth factor-β superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7

GJ Inman, FJ Nicolás, JF Callahan, JD Harling… - Molecular …, 2002 - ASPET
Small molecule inhibitors have proven extremely useful for investigating signal transduction
pathways and have the potential for development into therapeutics for inhibiting signal …

SB-505124 is a selective inhibitor of transforming growth factor-β type I receptors ALK4, ALK5, and ALK7

SDC Byfield, C Major, NJ Laping, AB Roberts - Molecular pharmacology, 2004 - ASPET
Clinically, there is a great need for small molecule inhibitors that could control pathogenic
effects of transforming growth factor (TGF-β) and/or modulate effects of TGF-β in normal …

The ALK‐5 inhibitor A‐83‐01 inhibits Smad signaling and epithelial‐to‐mesenchymal transition by transforming growth factor‐β

M Tojo, Y Hamashima, A Hanyu, T Kajimoto… - Cancer …, 2005 - Wiley Online Library
Transforming growth factor (TGF)‐β signaling facilitates tumor growth and metastasis in
advanced cancer. Use of inhibitors of TGF‐β signaling may thus be a novel strategy for the …

Identification of 1, 5-naphthyridine derivatives as a novel series of potent and selective TGF-β type I receptor inhibitors

F Gellibert, J Woolven, MH Fouchet… - Journal of medicinal …, 2004 - ACS Publications
Optimization of the screening hit 1 led to the identification of novel 1, 5-naphthyridine
aminothiazole and pyrazole derivatives, which are potent and selective inhibitors of the …

Identification of novel inhibitors of the transforming growth factor β1 (TGF-β1) type 1 receptor (ALK5)

JF Callahan, JL Burgess, JA Fornwald… - Journal of medicinal …, 2002 - ACS Publications
Screening of our internal compound collection for inhibitors of the transforming growth factor
β1 (TGF-β1) type I receptor (ALK5) identified several hits. Optimization of the …

[HTML][HTML] Specificity and structure of a high affinity activin receptor-like kinase 1 (ALK1) signaling complex

SA Townson, E Martinez-Hackert, C Greppi… - Journal of Biological …, 2012 - ASBMB
Activin receptor-like kinase 1 (ALK1), an endothelial cell-specific type I receptor of the TGF-β
superfamily, is an important regulator of normal blood vessel development as well as …

Development of an ALK2-biased BMP type I receptor kinase inhibitor

AH Mohedas, X Xing, KA Armstrong… - ACS chemical …, 2013 - ACS Publications
The bone morphogenetic protein (BMP) signaling pathway has essential functions in
development, homeostasis, and the normal and pathophysiologic remodeling of tissues …

ALK1-Fc inhibits multiple mediators of angiogenesis and suppresses tumor growth

D Mitchell, EG Pobre, AW Mulivor, AV Grinberg… - Molecular cancer …, 2010 - AACR
Abstract Activin receptor–like kinase-1 (ALK1) is a type I, endothelial cell–specific member of
the transforming growth factor-β superfamily of receptors known to play an essential role in …

Activin receptor-like kinases: a novel subclass of cell-surface receptors with predicted serine/threonine kinase activity.

P Ten Dijke, H Ichijo, P Franzen, P Schulz, J Saras… - Oncogene, 1993 - europepmc.org
Human cDNA clones encoding four novel putative transmembrane protein serine/threonine
kinases, denoted activin receptor-like kinase (ALK)-1,-2,-3 and-4, were obtained using a …

[HTML][HTML] Anti-human activin receptor-like kinase 1 (ALK1) antibody attenuates bone morphogenetic protein 9 (BMP9)-induced ALK1 signaling and interferes with …

LA van Meeteren, M Thorikay, S Bergqvist… - Journal of Biological …, 2012 - ASBMB
Genetic and molecular studies suggest that activin receptor-like kinase 1 (ALK1), a
transforming growth factor β (TGF-β) type I receptor, and endoglin, a TGF-β co-receptor, play …