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Discovery of MDV6058 (PF-06952229), a selective and potent TGFβR1 inhibitor: Design, synthesis and optimization

Bioorganic & medicinal chemistry letters, 2022-11, Vol.75, p.128979-128979, Article 128979

2022

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TNF‐α enhances TGF‐β‐induced endothelial‐to‐mesenchymal transition via TGF‐β signal augmentation

Cancer science, 2020-07, Vol.111 (7), p.2385-2399

2020

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The effects of ALK5 inhibition and simultaneous inhibition or activation of HIF-1α in melanoma tumor growth and angiogenesis

Tumor biology, 2023-10, Vol.45 (1), p.111-126

2023

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Design and synthesis of novel thiazole-derivatives as potent ALK5 inhibitors

Bioorganic & medicinal chemistry letters, 2024-08, Vol.108, p.129797-129797, Article 129797

2024

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Separating friend from foe: Inhibition of TGF-β-induced detrimental SMAD1/5/9 phosphorylation while maintaining protective SMAD2/3 signaling in OA chondrocytes

Osteoarthritis and cartilage, 2023-11, Vol.31 (11), p.1481-1490

2023

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Synthesis and biological evaluation of N-(3-fluorobenzyl)-4-(1-(methyl-d3)-1H-indazol-5-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-amine as a novel, potent ALK5 receptor inhibitor

Bioorganic & medicinal chemistry letters, 2023-04, Vol.85, p.129205-129205, Article 129205

2023

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Exploring anti-TGF-β therapies in cancer and fibrosis

Growth factors (Chur, Switzerland), 2011-08, Vol.29 (4), p.140-152

2011

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Targeting the TGF-β signaling pathway for resolution of pulmonary arterial hypertension

Trends in pharmacological sciences (Regular ed.), 2021-07, Vol.42 (7), p.510-513

2021

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Advances in the discovery of activin receptor-like kinase 5 (ALK5) inhibitors

Bioorganic chemistry, 2024-06, Vol.147, p.107332-107332, Article 107332

2024

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Cartilage-specific deletion of Alk5 gene results in a progressive osteoarthritis-like phenotype in mice

Osteoarthritis and cartilage, 2017-11, Vol.25 (11), p.1868-1879

2017

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Design, synthesis, and antifibrosis evaluation of 4-(benzo-[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methyl- pyridin-2-yl)pyrazole and 3(5)-(6-methylpyridin- 2-yl)-4-(thieno-[3,2,-c]pyridin-2-yl)pyrazole derivatives

European journal of medicinal chemistry, 2019-10, Vol.180, p.15-27

2019

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Interactions between TGF-β type I receptor and hypoxia-inducible factor-α mediates a synergistic crosstalk leading to poor prognosis for patients with clear cell renal cell carcinoma

Cell cycle (Georgetown, Tex.), 2019-09, Vol.18 (17), p.2141-2156

2019

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Cpd-0225 attenuates renal fibrosis via inhibiting ALK5

Biochemical pharmacology, 2022-10, Vol.204, p.115240-115240, Article 115240

2022

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Acetate controls endothelial-to-mesenchymal transition

Cell metabolism, 2023-07, Vol.35 (7), p.1163-1178.e10

2023

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Specialized endothelial tip cells guide neuroretina vascularization and blood-retina-barrier formation

Developmental cell, 2021-08, Vol.56 (15), p.2237-2251.e6

2021

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The function of CD146 in human annulus fibrosus cells and mechanism of the regulation by TGF‐β

Journal of orthopaedic research, 2022-07, Vol.40 (7), p.1661-1671

2022

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The TGF-β superfamily cytokine Activin-A is induced during autoimmune neuroinflammation and drives pathogenic Th17 cell differentiation

Immunity (Cambridge, Mass.), 2021-02, Vol.54 (2), p.308-323.e6

2021

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Bioreactor-Controlled Physoxia Regulates TGF-β Signaling to Alter Extracellular Matrix Synthesis by Human Chondrocytes

International journal of molecular sciences, 2019-04, Vol.20 (7), p.1715

2019

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Synthesis and biological evaluation of novel benzo[c][1,2,5]thiadiazol-5-yl and thieno[3,2-c]- pyridin-2-yl imidazole derivatives as ALK5 inhibitors

Bioorganic & medicinal chemistry letters, 2019-08, Vol.29 (16), p.2070-2075

2019

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Design, synthesis and biological activity evaluation of novel 4-((1-cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl) oxy) pyridine-2-yl) amino derivatives as potent transforming growth factor-β (TGF-β) type I receptor inhibitors

Bioorganic & medicinal chemistry letters, 2020-08, Vol.30 (16), p.127339, Article 127339

2020

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TGF-β3 enhances cell-to-cell communication in chondrocytes via the ALK5/p-Smad3 axis

Biochemical and biophysical research communications, 2022-12, Vol.636 (Pt 1), p.64-74

2022

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ADRM1/RPN13 attenuates cartilage extracellular matrix degradation via enhancing UCH37-mediated ALK5 deubiquitination

International journal of biological macromolecules, 2023-08, Vol.247, p.125670-125670, Article 125670

2023

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Albumin induces excitatory synaptogenesis through astrocytic TGF-β/ALK5 signaling in a model of acquired epilepsy following blood–brain barrier dysfunction

Neurobiology of disease, 2015-06, Vol.78, p.115-125

2015

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Enriched environment treatment promotes neurofunctional recovery by regulating the ALK5/Smad2/3/Gadd45β signaling pathway in rats with cerebral ischemia /reperfusion injury

Neurochemistry international, 2024-09, Vol.178, p.105806, Article 105806

2024

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Synthesis and anti-liver fibrosis activity of imidazole and thiazole compounds containing amino acids

European journal of medicinal chemistry, 2024-04, Vol.269, p.116311-116311, Article 116311

2024

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Discovery of MDV6058 (PF-06952229), a selective and potent TGFβR1 inhibitor: Design, synthesis and optimization

TNF‐α enhances TGF‐β‐induced endothelial‐to‐mesenchymal transition via TGF‐β signal augmentation

The effects of ALK5 inhibition and simultaneous inhibition or activation of HIF-1α in melanoma tumor growth and angiogenesis

Design and synthesis of novel thiazole-derivatives as potent ALK5 inhibitors

Separating friend from foe: Inhibition of TGF-β-induced detrimental SMAD1/5/9 phosphorylation while maintaining protective SMAD2/3 signaling in OA chondrocytes

Synthesis and biological evaluation of N-(3-fluorobenzyl)-4-(1-(methyl-d3)-1H-indazol-5-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-amine as a novel, potent ALK5 receptor inhibitor

Exploring anti-TGF-β therapies in cancer and fibrosis

Targeting the TGF-β signaling pathway for resolution of pulmonary arterial hypertension

Advances in the discovery of activin receptor-like kinase 5 (ALK5) inhibitors

Cartilage-specific deletion of Alk5 gene results in a progressive osteoarthritis-like phenotype in mice

Design, synthesis, and antifibrosis evaluation of 4-(benzo-[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methyl- pyridin-2-yl)pyrazole and 3(5)-(6-methylpyridin- 2-yl)-4-(thieno-[3,2,-c]pyridin-2-yl)pyrazole derivatives

Interactions between TGF-β type I receptor and hypoxia-inducible factor-α mediates a synergistic crosstalk leading to poor prognosis for patients with clear cell renal cell carcinoma

Cpd-0225 attenuates renal fibrosis via inhibiting ALK5

Acetate controls endothelial-to-mesenchymal transition

Specialized endothelial tip cells guide neuroretina vascularization and blood-retina-barrier formation

The function of CD146 in human annulus fibrosus cells and mechanism of the regulation by TGF‐β

The TGF-β superfamily cytokine Activin-A is induced during autoimmune neuroinflammation and drives pathogenic Th17 cell differentiation

Bioreactor-Controlled Physoxia Regulates TGF-β Signaling to Alter Extracellular Matrix Synthesis by Human Chondrocytes

Synthesis and biological evaluation of novel benzo[c][1,2,5]thiadiazol-5-yl and thieno[3,2-c]- pyridin-2-yl imidazole derivatives as ALK5 inhibitors

Design, synthesis and biological activity evaluation of novel 4-((1-cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl) oxy) pyridine-2-yl) amino derivatives as potent transforming growth factor-β (TGF-β) type I receptor inhibitors

TGF-β3 enhances cell-to-cell communication in chondrocytes via the ALK5/p-Smad3 axis

ADRM1/RPN13 attenuates cartilage extracellular matrix degradation via enhancing UCH37-mediated ALK5 deubiquitination

Albumin induces excitatory synaptogenesis through astrocytic TGF-β/ALK5 signaling in a model of acquired epilepsy following blood–brain barrier dysfunction

Enriched environment treatment promotes neurofunctional recovery by regulating the ALK5/Smad2/3/Gadd45β signaling pathway in rats with cerebral ischemia /reperfusion injury

Synthesis and anti-liver fibrosis activity of imidazole and thiazole compounds containing amino acids

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