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 …
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 …
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 …
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
BMP7 and activin are members of the transforming growth factor β superfamily. Here we
characterize endogenous activin and BMP7 signaling pathways in P19 embryonic …
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 …
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 …
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 …
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 …
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
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 …
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
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 …
of type II and type I receptors, both of which are transmembrane serine/threonine kinases …