Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway
暂无分享,去创建一个
S. Estrem | C. Slapak | A. Cleverly | J. S. Sawyer | D. Desaiah | I. Gueorguieva | Kyla E. Driscoll | K. Benhadji | M. Lahn | S. Guba | A. Stauber | S. Herbertz | Sawyer | J. Scott | T. Shawn | estrem | C. Susan | Guba | J. Scott Sawyer | Christopher A Slapak
[1] G. De Velasco,et al. Brain perfusion and permeability in patients with advanced, refractory glioblastoma treated with lomustine and the transforming growth factor-β receptor I kinase inhibitor LY2157299 monohydrate. , 2015, Oncology letters.
[2] A. Maier,et al. Anti-tumor activity of the TGF-β receptor kinase inhibitor galunisertib (LY2157299 monohydrate) in patient-derived tumor xenografts , 2015, Cellular Oncology.
[3] J. Baselga,et al. Pharmacokinetic, pharmacodynamic and biomarker evaluation of transforming growth factor-β receptor I kinase inhibitor, galunisertib, in phase 1 study in patients with advanced cancer , 2014, Investigational New Drugs.
[4] J. Baselga,et al. Cardiac Safety of TGF-β Receptor I Kinase Inhibitor LY2157299 Monohydrate in Cancer Patients in a First-in-Human Dose Study , 2014, Cardiovascular Toxicology.
[5] J. Baselga,et al. First-in-Human Dose Study of the Novel Transforming Growth Factor-β Receptor I Kinase Inhibitor LY2157299 Monohydrate in Patients with Advanced Cancer and Glioma , 2014, Clinical Cancer Research.
[6] M. Carducci,et al. Case Series of Cancer Patients Treated With Galunisertib, a Transforming Growth Factor-Beta Receptor I Kinase Inhibitor in a First-in-Human Dose Study , 2014 .
[7] M. Farmen,et al. A phase I dose-escalation study to a predefined dose of a transforming growth factor-β1 monoclonal antibody (TβM1) in patients with metastatic cancer , 2014, International journal of oncology.
[8] Xiaohong Xu,et al. Neutralizing murine TGFβR2 promotes a differentiated tumor cell phenotype and inhibits pancreatic cancer metastasis. , 2014, Cancer research.
[9] Hiroshi I. Suzuki,et al. Differential knockdown of TGF-β ligands in a three-dimensional co-culture tumor- stromal interaction model of lung cancer , 2014, BMC Cancer.
[10] K. Credille,et al. Nonclinical Safety Evaluation of a Transforming Growth Factor β Receptor I Kinase Inhibitor in Fischer 344 Rats and Beagle Dogs , 2014 .
[11] G. Blobe,et al. Combinatorial TGF-β signaling blockade and anti-CTLA-4 antibody immunotherapy in a murine BRAFV600E-PTEN-/- transgenic model of melanoma. , 2014 .
[12] K. S. Rao,et al. Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. , 2014, Journal of medicinal chemistry.
[13] Jeong-Seok Nam,et al. EW-7197, a Novel ALK-5 Kinase Inhibitor, Potently Inhibits Breast to Lung Metastasis , 2014, Molecular Cancer Therapeutics.
[14] Ivelina Gueorguieva,et al. Defining a therapeutic window for the novel TGF-β inhibitor LY2157299 monohydrate based on a pharmacokinetic/pharmacodynamic model. , 2014, British journal of clinical pharmacology.
[15] G. Giannelli,et al. Transforming growth factor-β as a therapeutic target in hepatocellular carcinoma. , 2014, Cancer research.
[16] R. Bernards,et al. Reversible and adaptive resistance to BRAF(V600E) inhibition in melanoma , 2014, Nature.
[17] J. Berzofsky,et al. Phase I Study of GC1008 (Fresolimumab): A Human Anti-Transforming Growth Factor-Beta (TGFβ) Monoclonal Antibody in Patients with Advanced Malignant Melanoma or Renal Cell Carcinoma , 2014, PloS one.
[18] Samy Lamouille,et al. Molecular mechanisms of epithelial–mesenchymal transition , 2014, Nature Reviews Molecular Cell Biology.
[19] G. Giannelli,et al. A phase 2 study of a novel transforming growth factor-beta (TGF-{beta}1) receptor I kinase inhibitor, LY2157299 monohydrate (LY), in patients with advanced hepatocellular carcinoma (HCC). , 2014 .
[20] C. Hill,et al. Controlling Long-Term Signaling: Receptor Dynamics Determine Attenuation and Refractory Behavior of the TGF-β Pathway , 2013, Science Signaling.
[21] M. Farmen,et al. A Canonical Transforming Growth Factor Beta-Dependent Signaling Pathway is Present in Peripheral Blood Cells of Cancer Patients with Skeletal Metastasis , 2013 .
[22] Andreas Schlicker,et al. Colorectal cancer intrinsic subtypes predict chemotherapy benefit, deficient mismatch repair and epithelial-to-mesenchymal transition , 2013, International journal of cancer.
[23] T. Walshe,et al. The Role of Shear-Induced Transforming Growth Factor-&bgr; Signaling in the Endothelium , 2013, Arteriosclerosis, thrombosis, and vascular biology.
[24] P. ten Dijke,et al. Activin receptor-like kinase 1 as a target for anti-angiogenesis therapy , 2013, Expert opinion on investigational drugs.
[25] D. Heitjan,et al. Immunological effects of the TGFβ-blocking antibody GC1008 in malignant pleural mesothelioma patients , 2013, Oncoimmunology.
[26] E. D. Bal de Kier Joffé,et al. TGF-beta specifically enhances the metastatic attributes of murine lung adenocarcinoma: implications for human non-small cell lung cancer , 2013, Clinical & Experimental Metastasis.
[27] J. Tabernero,et al. Phase Ib study evaluating safety and pharmacokinetics (PK) of the oral transforming growth factor-beta (TGF-ß) receptor I kinase inhibitor LY2157299 monohydrate (LY) when combined with gemcitabine in patients with advanced cancer. , 2013 .
[28] A. Brandes,et al. Safety interim data from a three-arm phase II study evaluating safety and pharmacokinetics of the oral transforming growth factor-beta (TGF-ß) receptor I kinase inhibitor LY2157299 monohydrate in patients with glioblastoma at first progression. , 2013 .
[29] J. Baselga,et al. Integrated data review of the first-in-human dose (FHD) study evaluating safety, pharmacokinetics (PK), and pharmacodynamics (PD) of the oral transforming growth factor-beta (TGF-ß) receptor I kinase inhibitor, LY2157299 monohydrate (LY). , 2013 .
[30] V. Paradis,et al. Abstract 2094: Effects of TGF-beta signaling inhibition with LY2157299 in hepatocarcinoma models and in ex vivo whole tumor tissue samples from patient specimen. , 2013 .
[31] Tong-fu Yu,et al. Sorafenib reduces hepatic infiltrated regulatory T cells in hepatocellular carcinoma patients by suppressing TGF‐beta signal , 2013, Journal of surgical oncology.
[32] S. Rafii,et al. TGFβ restores hematopoietic homeostasis after myelosuppressive chemotherapy , 2013, The Journal of experimental medicine.
[33] Y. Koh,et al. Combined Treatment with Erlotinib and a Transforming Growth Factor-&bgr; Type I Receptor Inhibitor Effectively Suppresses the Enhanced Motility of Erlotinib-Resistant Non–Small-Cell Lung Cancer Cells , 2013, Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer.
[34] D. K. Wood,et al. Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c3lc41300d Click here for additional data file. , 2013, Lab on a chip.
[35] J. Balko,et al. TGF-β inhibition enhances chemotherapy action against triple-negative breast cancer. , 2013, The Journal of clinical investigation.
[36] S. Howng,et al. Plasma levels of transforming growth factor-beta 1 before and after removal of low- and high-grade astrocytomas. , 2013, Cytokine.
[37] R. Bernards,et al. MED12 Controls the Response to Multiple Cancer Drugs through Regulation of TGF-β Receptor Signaling , 2012, Cell.
[38] P. Jung,et al. Dependency of colorectal cancer on a TGF-β-driven program in stromal cells for metastasis initiation. , 2012, Cancer cell.
[39] Joshua M. Korn,et al. Isocitrate Dehydrogenase (IDH) Mutations Promote a Reversible ZEB1/MicroRNA (miR)-200-dependent Epithelial-Mesenchymal Transition (EMT)* , 2012, The Journal of Biological Chemistry.
[40] M. Barcellos-Hoff,et al. Resistance of glioblastoma-initiating cells to radiation mediated by the tumor microenvironment can be abolished by inhibiting transforming growth factor-β. , 2012, Cancer research.
[41] E. Fishman,et al. Loss-of-function mutations in TGFB2 cause a syndromic presentation of thoracic aortic aneurysm , 2012, Nature Genetics.
[42] J. Baselga,et al. The oral transforming growth factor-beta (TGF-ß) receptor I kinase inhibitor LY2157299 plus lomustine in patients with treatment-refractory malignant glioma: The first human dose study. , 2012 .
[43] I. Davis,et al. Role of cytokine-induced plasticity in melanoma on invasive, therapy-resistant cells that express EMT-related genes and pathways. , 2012 .
[44] U. Wirkner,et al. LY2109761 Attenuates Radiation-Induced Pulmonary Murine Fibrosis via Reversal of TGF-β and BMP-Associated Proinflammatory and Proangiogenic Signals , 2012, Clinical Cancer Research.
[45] E. Vazquez,et al. Effect of transforming growth factor beta (TGF-β) receptor I kinase inhibitor on prostate cancer bone growth. , 2012, Bone.
[46] J. McPherson,et al. Antibody targeting of TGF-β in cancer patients. , 2011, Current pharmaceutical biotechnology.
[47] J. Graff,et al. Abstract C201: The combination of the small molecule TGFβR1 inhibitor LY2157299 monohydrate with CCNU substantially blocks SMAD phosphorylation and significantly suppresses human glioblastoma xenograft growth. , 2011 .
[48] I. Bièche,et al. Abstract B175: TGF-β-RI kinase inhibitors LY2157299 and LY364947 decrease motility and invasion in hepatocarcinoma (HCC) cells developing resistance to VEGFR/PDGFR kinase inhibitors. , 2011 .
[49] Manuel Hidalgo,et al. Nodal/Activin signaling drives self-renewal and tumorigenicity of pancreatic cancer stem cells and provides a target for combined drug therapy. , 2011, Cell stem cell.
[50] Shobha N. Bhattachar,et al. Effect of gastric pH on the pharmacokinetics of a BCS class II compound in dogs: utilization of an artificial stomach and duodenum dissolution model and GastroPlus,™ simulations to predict absorption. , 2011, Journal of pharmaceutical sciences.
[51] J. Debus,et al. Blockade of TGF-beta signaling by the TGF β RI kinase Inhibitor LY 2109761 enhances radiation response and prolongs survival in glioblastoma , 2011 .
[52] M. Anderton,et al. Induction of Heart Valve Lesions by Small-Molecule ALK5 Inhibitors , 2011, Toxicologic pathology.
[53] B. Coomber,et al. VEGFR2 Expression and TGF-β Signaling in Initial and Recurrent High-Grade Human Glioma , 2011, Oncology.
[54] T. He,et al. BMP9 inhibits the proliferation and invasiveness of breast cancer cells MDA-MB-231 , 2011, Journal of Cancer Research and Clinical Oncology.
[55] G. Giannelli,et al. Kinase activation profile associated with TGF-β-dependent migration of HCC cells: a preclinical study , 2011, Cancer Chemotherapy and Pharmacology.
[56] Ute Wirkner,et al. Trimodal glioblastoma treatment consisting of concurrent radiotherapy, temozolomide, and the novel TGF-β receptor I kinase inhibitor LY2109761. , 2011, Neoplasia.
[57] A. Vickers,et al. Tumor markers in prostate cancer I: Blood-based markers , 2011, Acta oncologica.
[58] J. Baselga,et al. First human dose (FHD) study of the oral transforming growth factor-beta receptor I kinase inhibitor LY2157299 in patients with treatment-refractory malignant glioma. , 2011, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[59] Samarjit Patnaik,et al. Noncanonical TGFβ Signaling Contributes to Aortic Aneurysm Progression in Marfan Syndrome Mice , 2011, Science.
[60] A. Hinck,et al. TGF‐β signalling is mediated by two autonomously functioning TβRI:TβRII pairs , 2011, The EMBO journal.
[61] B. Hann,et al. Outgrowth of drug-resistant carcinomas expressing markers of tumor aggression after long-term TβRI/II kinase inhibition with LY2109761. , 2011, Cancer research.
[62] D. Hanahan,et al. Hallmarks of Cancer: The Next Generation , 2011, Cell.
[63] G. Remuzzi,et al. A phase 1, single-dose study of fresolimumab, an anti-TGF-β antibody, in treatment-resistant primary focal segmental glomerulosclerosis , 2011, Kidney international.
[64] M. Bitzer,et al. Reduced SMAD7 leads to overactivation of TGF-beta signaling in MDS that can be reversed by a specific inhibitor of TGF-beta receptor I kinase. , 2011, Cancer research.
[65] J. Baselga,et al. TGF-β Receptor Inhibitors Target the CD44(high)/Id1(high) Glioma-Initiating Cell Population in Human Glioblastoma. , 2010, Cancer cell.
[66] I. Bièche,et al. 217 Specific TGF-beta receptor-I inhibition using LY364947 impairs signaling, motility, and invasion in parental and multikinase inhibitor-resistant hepatocarcinoma cells , 2010 .
[67] L. Feagins. Role of transforming growth factor‐&bgr; in inflammatory bowel disease and colitis‐associated colon cancer , 2010, Inflammatory bowel diseases.
[68] M. Zaaroor,et al. Targeted therapy for high-grade glioma with the TGF-β2 inhibitor trabedersen: results of a randomized and controlled phase IIb study , 2010, Neuro-oncology.
[69] Richard A. Flavell,et al. The polarization of immune cells in the tumour environment by TGFβ , 2010, Nature Reviews Immunology.
[70] M. Reiss,et al. Targeting the Transforming Growth Factor-β pathway inhibits human basal-like breast cancer metastasis , 2010, Molecular Cancer.
[71] K. Hahm,et al. Connection between inflammation and carcinogenesis in gastrointestinal tract: focus on TGF-beta signaling. , 2010, World journal of gastroenterology.
[72] C. Arteaga,et al. Oncogenic Mutations Regulate Tumor Microenvironment through Induction of Growth Factors and Angiogenic Mediators , 2010, Oncogene.
[73] Thomas Zander,et al. Application of T cell-based transcriptomics to identify three candidate biomarkers for monitoring anti-TGFβR therapy , 2010, Pharmacogenetics and genomics.
[74] Zhen-ping Zhu,et al. Anti–Transforming Growth Factor β Receptor II Antibody Has Therapeutic Efficacy against Primary Tumor Growth and Metastasis through Multieffects on Cancer, Stroma, and Immune Cells , 2010, Clinical Cancer Research.
[75] G. Giannelli,et al. Down‐regulation of connective tissue growth factor by inhibition of transforming growth factor β blocks the tumor–stroma cross‐talk and tumor progression in hepatocellular carcinoma , 2010, Hepatology.
[76] S. Gabriel,et al. Integrated genomic analysis identifies clinically relevant subtypes of glioblastoma characterized by abnormalities in PDGFRA, IDH1, EGFR, and NF1. , 2010, Cancer cell.
[77] N. Nagaraj,et al. Targeting the transforming growth factor-β signaling pathway in human cancer , 2010, Expert opinion on investigational drugs.
[78] K. Garber. Companies waver in efforts to target transforming growth factor beta in cancer. , 2009, Journal of the National Cancer Institute.
[79] Douglas B. Evans,et al. TrkBT1 induces liver metastasis of pancreatic cancer cells by sequestering Rho GDP dissociation inhibitor and promoting RhoA activation. , 2009, Cancer research.
[80] G. Giannelli,et al. Inhibition of transforming growth factor β receptor I kinase blocks hepatocellular carcinoma growth through neo‐angiogenesis regulation , 2009, Hepatology.
[81] R. Brierley. International Liver Cancer Association Annual Conference. , 2009, The Lancet. Oncology.
[82] M. Goumans,et al. VEGF and inhibitors of TGFβ type-I receptor kinase synergistically promote blood-vessel formation by inducing α5-integrin expression , 2009, Journal of Cell Science.
[83] Xin Lu,et al. Imaging transforming growth factor-β signaling dynamics and therapeutic response in breast cancer bone metastasis , 2009, Nature Medicine.
[84] G. Alexe,et al. Transforming growth factor-β signaling: emerging stem cell target in metastatic breast cancer? , 2009, Breast Cancer Research and Treatment.
[85] David García-Dorado,et al. TGF-beta increases glioma-initiating cell self-renewal through the induction of LIF in human glioblastoma. , 2009, Cancer cell.
[86] G. Giannelli,et al. Targeting transforming growth factor (TGF)‐βRI inhibits activation of β1 integrin and blocks vascular invasion in hepatocellular carcinoma , 2009, Hepatology.
[87] C. Chung,et al. Transforming growth factor beta engages TACE/ADAM17 and ErbB3 to activate PI3K/Akt in HER2-overexpressing breast cancer and desensitizes cells to trastuzumab. , 2009 .
[88] M. Bitzer,et al. Inhibition of the TGF-beta receptor I kinase promotes hematopoiesis in MDS. , 2008, Blood.
[89] J. Baselga,et al. Analysis and variability of TGFβ measurements in cancer patients with skeletal metastases , 2008, Biologics : targets & therapy.
[90] M. Konopleva,et al. TGF‐β receptor kinase inhibitor LY2109761 reverses the anti‐apoptotic effects of TGF‐β1 in myelo‐monocytic leukaemic cells co‐cultured with stromal cells , 2008, British journal of haematology.
[91] J. Baselga,et al. First human dose escalation study in patients with metastatic malignancies to determine safety and pharmacokinetics of LY2157299, a small molecule inhibitor of the transforming growth factor-beta receptor I kinase , 2008 .
[92] G. Giannelli,et al. Blocking transforming growth factor–beta up‐regulates E‐cadherin and reduces migration and invasion of hepatocellular carcinoma cells , 2008, Hepatology.
[93] Gerard C Blobe,et al. Role of transforming growth factor-beta superfamily signaling pathways in human disease. , 2008, Biochimica et biophysica acta.
[94] G. Tortora,et al. LY2109761, a novel transforming growth factor β receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis , 2008, Molecular Cancer Therapeutics.
[95] M. Reiss,et al. Cancer-associated transforming growth factor beta type II receptor gene mutant causes activation of bone morphogenic protein-Smads and invasive phenotype. , 2008, Cancer research.
[96] R. Campbell,et al. Optimization of a dihydropyrrolopyrazole series of transforming growth factor-beta type I receptor kinase domain inhibitors: discovery of an orally bioavailable transforming growth factor-beta receptor type I inhibitor as antitumor agent. , 2008, Journal of medicinal chemistry.
[97] J. Seoane. The TGFß pathway as a therapeutic target in cancer , 2008 .
[98] J. Baselga,et al. TGF-β signalling-related markers in cancer patients with bone metastasis , 2008 .
[99] J. Yingling,et al. Genomic analysis of TGFβ treated cell lines with phenotypically distinct outcomes to identify transcriptional signatures for assessment in stratification of cancers , 2007 .
[100] R. Urrutia,et al. Basics of TGF-β and Pancreatic Cancer , 2007, Pancreatology.
[101] H. Moses,et al. Inhibition of TGF-beta with neutralizing antibodies prevents radiation-induced acceleration of metastatic cancer progression. , 2007, The Journal of clinical investigation.
[102] M. Reiss,et al. Transforming Growth Factor β pathway antagonists inhibit human breast cancer metastases to lung and bone , 2007 .
[103] Kazunori Kataoka,et al. Improvement of cancer-targeting therapy, using nanocarriers for intractable solid tumors by inhibition of TGF-β signaling , 2007, Proceedings of the National Academy of Sciences.
[104] Alejandra Bruna,et al. High TGFbeta-Smad activity confers poor prognosis in glioma patients and promotes cell proliferation depending on the methylation of the PDGF-B gene. , 2007, Cancer cell.
[105] K. Miyazono,et al. Ki26894, a novel transforming growth factor‐β type I receptor kinase inhibitor, inhibits in vitro invasion and in vivo bone metastasis of a human breast cancer cell line , 2007, Cancer science.
[106] Y. Qian,et al. Development and validation of a phosphorylated SMAD ex vivo stimulation assay , 2007, Biomarkers : biochemical indicators of exposure, response, and susceptibility to chemicals.
[107] P. Byers,et al. Aneurysm syndromes caused by mutations in the TGF-beta receptor. , 2006, The New England journal of medicine.
[108] George H. Thomas,et al. Aneurysm Syndromes Caused by Mutations in the TGF-β Receptor , 2006 .
[109] C. Arteaga,et al. Inhibition of Transforming Growth Factor-β Signaling in Human Cancer: Targeting a Tumor Suppressor Network as a Therapeutic Strategy , 2006, Clinical Cancer Research.
[110] M. Loeffler,et al. Targeting tumor-associated fibroblasts improves cancer chemotherapy by increasing intratumoral drug uptake. , 2006, The Journal of clinical investigation.
[111] Xiu-fen Lei,et al. Inhibition of pulmonary and skeletal metastasis by a transforming growth factor-beta type I receptor kinase inhibitor. , 2006, Cancer research.
[112] M. Barcellos-Hoff,et al. Activated type I TGFβ receptor kinase enhances the survival of mammary epithelial cells and accelerates tumor progression , 2006, Oncogene.
[113] J. Yingling,et al. A small molecule inhibitor of TGFβ RI kinase potentiates VEGF dependent angiogenesis in vitro , 2006 .
[114] C. Hill,et al. Alterations in components of the TGF-beta superfamily signaling pathways in human cancer. , 2006, Cytokine & growth factor reviews.
[115] A. Balmain,et al. Transforming Growth Factor-β Receptor Inhibition Enhances Adenoviral Infectability of Carcinoma Cells via Up-Regulation of Coxsackie and Adenovirus Receptor in Conjunction with Reversal of Epithelial-Mesenchymal Transition , 2006 .
[116] G. Giannelli,et al. Laminin-5 with transforming growth factor-beta1 induces epithelial to mesenchymal transition in hepatocellular carcinoma. , 2005, Gastroenterology.
[117] Chris Sander,et al. Signal Processing in the TGF-β Superfamily Ligand-Receptor Network , 2005, PLoS Comput. Biol..
[118] S. Kloeker,et al. TGF-β inhibitors for the treatment of cancer , 2005 .
[119] J. Yingling. Targeting the TGF-β RI kinase with LY2157299: A PK/PD-driven drug discovery and clinical development program , 2005 .
[120] C. June,et al. Regulatory T cells and cytokines in malignant pleural effusions secondary to mesothelioma and carcinoma , 2005, Cancer biology & therapy.
[121] G. De Nicolao,et al. A pharmacokinetic-pharmacodynamic model for predicting tumour growth inhibition in mice: a useful tool in oncology drug development. , 2005, Basic & clinical pharmacology & toxicology.
[122] S. A. Watkins,et al. Kinetic characterization of novel pyrazole TGF-beta receptor I kinase inhibitors and their blockade of the epithelial-mesenchymal transition. , 2005, Biochemistry.
[123] Jonathan M. Yingling,et al. Development of TGF-β signalling inhibitors for cancer therapy , 2004, Nature Reviews Drug Discovery.
[124] R. Campbell,et al. Novel and Potent Transforming Growth Factor Beta Type I Receptor Kinase Domain Inhibitor: 7‐Amino 4‐(2‐Pyridin‐2‐yl‐5,6‐dihydro‐4H‐pyrrolo [1,2‐b]pyrazol‐3‐yl)‐quinolines. , 2004 .
[125] R. Campbell,et al. Synthesis and activity of new aryl- and heteroaryl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain. , 2004, Bioorganic & medicinal chemistry letters.
[126] R. Campbell,et al. Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor: 7-amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)-quinolines. , 2004, Bioorganic & medicinal chemistry letters.
[127] Juswinder Singh,et al. Transforming the TGFbeta pathway: convergence of distinct lead generation strategies on a novel kinase pharmacophore for TbetaRI (ALK5). , 2004, Current opinion in drug discovery & development.
[128] Andrew Leask,et al. TGF‐β signaling and the fibrotic response , 2004, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.
[129] M. Kattan,et al. Association of Pre- and Postoperative Plasma Levels of Transforming Growth Factor β1 and Interleukin 6 and Its Soluble Receptor with Prostate Cancer Progression , 2004, Clinical Cancer Research.
[130] Paolo Magni,et al. Predictive Pharmacokinetic-Pharmacodynamic Modeling of Tumor Growth Kinetics in Xenograft Models after Administration of Anticancer Agents , 2004, Cancer Research.
[131] M. Vieth,et al. Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain. , 2003, Journal of medicinal chemistry.
[132] L. Wakefield,et al. Lifetime exposure to a soluble TGF-beta antagonist protects mice against metastasis without adverse side effects. , 2002, The Journal of clinical investigation.
[133] M. Kattan,et al. Plasma levels of interleukin-6 and its soluble receptor are associated with prostate cancer progression and metastasis. , 2001, Urology.
[134] R. Derynck,et al. TGF-β signaling in cancer – a double-edged sword , 2001 .
[135] M. Kattan,et al. Preoperative plasma levels of transforming growth factor beta(1) (TGF-beta(1)) strongly predict progression in patients undergoing radical prostatectomy. , 2001, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[136] K. Matsuzaki,et al. Regulatory mechanisms for transforming growth factor β as an autocrine inhibitor in human hepatocellular carcinoma: Implications for roles of Smads in its growth , 2000, Hepatology.
[137] O. Schiraldi,et al. Transforming growth factor beta1 and soluble Fas serum levels in hepatocellular carcinoma. , 2000, Cytokine.
[138] C. Heldin,et al. Specificity, diversity, and regulation in TGF‐β superfamily signaling , 1999 .
[139] H. Friess,et al. Transforming growth factor betas and their signaling receptors in human hepatocellular carcinoma. , 1999, American journal of surgery.
[140] K. Kinzler,et al. Mutational inactivation of transforming growth factor beta receptor type II in microsatellite stable colon cancers. , 1999, Cancer research.
[141] M. Reiss,et al. Transforming growth factor-β in breast cancer: A working hypothesis , 1997, Breast Cancer Research and Treatment.
[142] T. Yaginuma,et al. Shear stress as an inhibitor of vascular smooth muscle cell proliferation. Role of transforming growth factor-beta 1 and tissue-type plasminogen activator. , 1997, Arteriosclerosis, thrombosis, and vascular biology.
[143] A. Mackensen,et al. Comparison of cytogenetics, cytokine secretion, and oncogene expression in primary cultures of renal carcinoma cells. , 1997, Oncology.
[144] Scott E. Kern,et al. DPC4, A Candidate Tumor Suppressor Gene at Human Chromosome 18q21.1 , 1996, Science.
[145] J. Massagué,et al. GS domain mutations that constitutively activate T beta R‐I, the downstream signaling component in the TGF‐beta receptor complex. , 1995, The EMBO journal.
[146] Mahlon D. Johnson,et al. Anti-transforming growth factor (TGF)-beta antibodies inhibit breast cancer cell tumorigenicity and increase mouse spleen natural killer cell activity. Implications for a possible role of tumor cell/host TGF-beta interactions in human breast cancer progression. , 1993, The Journal of clinical investigation.
[147] Jeffrey L. Wrana,et al. TGFβ signals through a heteromeric protein kinase receptor complex , 1992, Cell.
[148] C. Osborne,et al. Transforming growth factor β: potential autocrine growth inhibitor of estrogen receptor-negative human breast cancer cells , 1988 .
[149] J. Massagué,et al. The transforming growth factor-β system, a complex pattern of cross-reactive ligands and receptors , 1987, Cell.
[150] M. Sporn,et al. Production of transforming growth factor beta by human T lymphocytes and its potential role in the regulation of T cell growth , 1986, The Journal of experimental medicine.
[151] H. Moses,et al. Induction of c-sis mRNA and activity similar to platelet-derived growth factor by transforming growth factor beta: a proposed model for indirect mitogenesis involving autocrine activity. , 1986, Proceedings of the National Academy of Sciences of the United States of America.
[152] M. Sporn,et al. Synergistic interaction of two classes of transforming growth factors from murine sarcoma cells. , 1982, Cancer research.
[153] M. Sporn,et al. New class of transforming growth factors potentiated by epidermal growth factor: isolation from non-neoplastic tissues. , 1981, Proceedings of the National Academy of Sciences of the United States of America.
[154] M. Sporn,et al. Transforming growth factors: isolation of polypeptides from virally and chemically transformed cells by acid/ethanol extraction. , 1980, Proceedings of the National Academy of Sciences of the United States of America.
[155] T. S. P. S.,et al. GROWTH , 1924, Nature.
[156] Susan P. Mattern. The Prince of Medicine: Galen in the Roman Empire , 2013 .
[157] J. Stockman,et al. Noncanonical TGFβ Signaling Contributes to Aortic Aneurysm Progression in Marfan Syndrome Mice , 2012 .
[158] Zhaohui J. Cai,et al. Pretreatment data is highly predictive of liver chemistry signals in clinical trials , 2012, Drug design, development and therapy.
[159] Helen Diller Family. Targeting the TGFβ signalling pathway in disease , 2012 .
[160] Marie-José Goumans,et al. TGF-β signaling in vascular biology and dysfunction , 2009, Cell Research.
[161] J. Seoane. The TGFBeta pathway as a therapeutic target in cancer. , 2008, Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico.
[162] Iñaki F Trocóniz,et al. Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-beta kinase antagonist, in mice. , 2008, European journal of cancer.
[163] R. Urrutia,et al. Basics of TGF-beta and pancreatic cancer. , 2007, Pancreatology : official journal of the International Association of Pancreatology (IAP) ... [et al.].
[164] A. Balmain,et al. Transforming growth factor-beta receptor inhibition enhances adenoviral infectability of carcinoma cells via up-regulation of Coxsackie and Adenovirus Receptor in conjunction with reversal of epithelial-mesenchymal transition. , 2006, Cancer research.
[165] N. Laping,et al. TGF-β Receptor Kinase Inhibitors for Treatment of Fibrosis , 2006 .
[166] S. Kloeker,et al. TGF-beta inhibitors for the treatment of cancer. , 2005, Expert opinion on investigational drugs.
[167] J. Yingling,et al. Development of TGF-beta signalling inhibitors for cancer therapy. , 2004, Nature reviews. Drug discovery.
[168] J. Massagué,et al. Cytostatic and apoptotic actions of TGF-beta in homeostasis and cancer. , 2003, Nature reviews. Cancer.
[169] A. Balmain,et al. TGF-beta signaling in tumor suppression and cancer progression. , 2001, Nature genetics.
[170] R. Derynck,et al. TGF-beta signaling in cancer--a double-edged sword. , 2001, Trends in cell biology.
[171] J. Massagué,et al. TGFbeta signaling in growth control, cancer, and heritable disorders. , 2000, Cell.
[172] C. Heldin,et al. Specificity, diversity, and regulation in TGF-beta superfamily signaling. , 1999, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.
[173] Y. Shim,et al. Reduced transforming growth factor-beta type II receptor (TGF-beta RII) expression in adenocarcinoma of the lung. , 1999, Anticancer research.
[174] Keunchil Park,et al. Reduced transforming growth factor-β type II receptor (TGF-β RII) expression in adenocarcinoma of the lung , 1999 .
[175] R. Clough,et al. Plasma transforming growth factor β1 as a predictor of radiation pneumonitis , 1997 .
[176] M. Reiss,et al. Transforming growth factor-beta in breast cancer: a working hypothesis. , 1997, Breast cancer research and treatment.
[177] J. Massagué,et al. TGF beta signals through a heteromeric protein kinase receptor complex. , 1992, Cell.
[178] D. V. Von Hoff,et al. Transforming growth factor beta: potential autocrine growth inhibitor of estrogen receptor-negative human breast cancer cells. , 1988, Cancer research.