Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2)

L Tan, T Nomanbhoy, D Gurbani… - Journal of medicinal …, 2015 - ACS Publications
We developed a pharmacophore model for type II inhibitors that was used to guide the
construction of a library of kinase inhibitors. Kinome-wide selectivity profiling of the library …

A specific inhibitor of TGF-β receptor kinase, SB-431542, as a potent antitumor agent for human cancers

SK Halder, RD Beauchamp, PK Datta - Neoplasia, 2005 - Elsevier
Small molecule inhibitors of signaling pathways have proven to be extremely useful for the
development of therapeutic strategies for human cancers. Blocking the tumor-promoting …

Structural characterization of an activin class ternary receptor complex reveals a third paradigm for receptor specificity

EJ Goebel, RA Corpina, CS Hinck… - Proceedings of the …, 2019 - National Acad Sciences
TGFβ family ligands, which include the TGFβs, BMPs, and activins, signal by forming a
ternary complex with type I and type II receptors. For TGFβs and BMPs, structures of ternary …

[HTML][HTML] Specific activation of Smad1 signaling pathways by the BMP7 type I receptor, ALK2

M Macı́as-Silva, PA Hoodless, SJ Tang… - Journal of Biological …, 1998 - ASBMB
BMP7 and activin are members of the transforming growth factor β superfamily. Here we
characterize endogenous activin and BMP7 signaling pathways in P19 embryonic …

Targeting activin receptor-like kinase 1 inhibits angiogenesis and tumorigenesis through a mechanism of action complementary to anti-VEGF therapies

DD Hu-Lowe, E Chen, L Zhang, KD Watson… - Cancer research, 2011 - AACR
Genetic and molecular studies suggest that activin receptor-like kinase 1 (ALK1) plays an
important role in vascular development, remodeling, and pathologic angiogenesis. Here we …

[HTML][HTML] Assignment of transforming growth factor β1 and β3 and a third new ligand to the type I receptor ALK-1

A Lux, L Attisano, DA Marchuk - Journal of Biological Chemistry, 1999 - ASBMB
Germ line mutations in one of two distinct genes, endoglin or ALK-1, cause hereditary
hemorrhagic telangiectasia (HHT), an autosomal dominant disorder of localized …

[HTML][HTML] Bone morphogenetic protein receptors: Structure, function and targeting by selective small molecule kinase inhibitors

G Sanchez-Duffhues, E Williams, MJ Goumans… - Bone, 2020 - Elsevier
Bone morphogenetic proteins (BMPs) are secreted cytokines that control the fate and
function of many different cell types. They exert their cellular responses via heteromeric …

Targeting the transforming growth factor-β signaling pathway in human cancer

NS Nagaraj, PK Datta - Expert opinion on investigational drugs, 2010 - Taylor & Francis
The transforming growth factor-ß (TGF-β) signaling pathway plays a pivotal role in diverse
cellular processes. TGF-β switches its role from a tumor suppressor in normal or dysplastic …

[HTML][HTML] A Perspective on the Development of TGF-β Inhibitors for Cancer Treatment

LK Huynh, CJ Hipolito, P Ten Dijke - Biomolecules, 2019 - mdpi.com
Transforming growth factor (TGF)-β is a secreted multifunctional cytokine that signals via
plasma membrane TGF-β type I and type II receptors and intercellular SMAD transcriptional …

Signal transduction pathway through activin receptors as a therapeutic target of musculoskeletal diseases and cancer

K Tsuchida, M Nakatani, A Uezumi, T Murakami… - Endocrine …, 2008 - jstage.jst.go.jp
Activin, myostatin and other members of the TGF-β superfamily signal through a combination
of type II and type I receptors, both of which are transmembrane serine/threonine kinases …