Development of TGF-β signalling inhibitors for cancer therapy

New Guidelines to Evaluate the Response to Treatment in Solid Tumors

2000 • 15,583 citations

Activating Mutations in the Epidermal Growth Factor Receptor Underlying Responsiveness of Non–Small-Cell Lung Cancer to Gefitinib

2004 • 11,185 citations

Use of Chemotherapy plus a Monoclonal Antibody against HER2 for Metastatic Breast Cancer That Overexpresses HER2

2001 • 11,070 citations

EGFR Mutations in Lung Cancer: Correlation with Clinical Response to Gefitinib Therapy

2004 • 9,201 citations

Untangling the ErbB signalling network

2001 • 6,623 citations

Epithelial–mesenchymal transitions in tumour progression

2002 • 6,431 citations

Mechanisms of TGF-β Signaling from Cell Membrane to the Nucleus

2003 • 5,611 citations

Smad-dependent and Smad-independent pathways in TGF-β family signalling

2003 • 5,052 citations

Twist, a Master Regulator of Morphogenesis, Plays an Essential Role in Tumor Metastasis

2004 • 3,727 citations

Targeted disruption of the mouse transforming growth factor-β1 gene results in multifocal inflammatory disease

1992 • 2,969 citations

Efficacy and Safety of Trastuzumab as a Single Agent in First-Line Treatment of HER2-Overexpressing Metastatic Breast Cancer

2002 • 2,968 citations

Putting tumours in context

2001 • 2,145 citations

Transforming growth factor beta 1 null mutation in mice causes excessive inflammatory response and early death.

1993 • 1,941 citations

In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship.

2003 • 1,939 citations

REGULATION OF IMMUNE RESPONSES BY TGF-β

1998 • 1,908 citations

Efficacy and Safety of Trastuzumab as a Single Agent in First-Line Treatment of HER2-Overexpressing Metastatic Breast Cancer

2002 • 1,771 citations

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

2002 • 1,572 citations

Cytostatic and apoptotic actions of TGF-β in homeostasis and cancer

2003 • 1,572 citations

TGF-ß Signaling in Fibroblasts Modulates the Oncogenic Potential of Adjacent Epithelia

2004 • 1,346 citations

BMP-7 counteracts TGF-β1–induced epithelial-to-mesenchymal transition and reverses chronic renal injury

2003 • 1,308 citations

Integration of Smad and Forkhead Pathways in the Control of Neuroepithelial and Glioblastoma Cell Proliferation

2004 • 1,008 citations

Abrogation of TGFβ Signaling in T Cells Leads to Spontaneous T Cell Differentiation and Autoimmune Disease

2000 • 970 citations

TGF-β signaling blockade inhibits PTHrP secretion by breast cancer cells and bone metastases development

1999 • 969 citations

Phosphatidylinositol 3-Kinase Function Is Required for Transforming Growth Factor β-mediated Epithelial to Mesenchymal Transition and Cell Migration

2000 • 956 citations

SARA, a FYVE Domain Protein that Recruits Smad2 to the TGFβ Receptor

1998 • 952 citations

Snail blocks the cell cycle and confers resistance to cell death

2004 • 835 citations

TGF-β signaling: positive and negative effects on tumorigenesis

2002 • 830 citations

Genetic Analysis of the Mammalian Transforming Growth Factor-β Superfamily

2002 • 770 citations

Immune-mediated eradication of tumors through the blockade of transforming growth factor-β signaling in T cells

2001 • 759 citations

Integration of TGF-β/Smad and Jagged1/Notch signalling in epithelial-to-mesenchymal transition

2004 • 710 citations

TGF-beta receptor-activated p38 MAP kinase mediates Smad-independent TGF-beta responses

2002 • 703 citations

TGFβ1 Inhibits the Formation of Benign Skin Tumors, but Enhances Progression to Invasive Spindle Carcinomas in Transgenic Mice

1996 • 619 citations

Transforming Growth Factor β-1 Induces Snail Transcription Factor in Epithelial Cell Lines

2003 • 617 citations

TGF-β/Smad3 Signals Repress Chondrocyte Hypertrophic Differentiation and Are Required for Maintaining Articular Cartilage

2001 • 614 citations

Molecular mechanisms underlying ErbB2/HER2 action in breast cancer

2000 • 580 citations

Interdependent SMAD and JNK Signaling in Transforming Growth Factor-β-mediated Transcription

1999 • 534 citations

Blockade of TGF-β inhibits mammary tumor cell viability, migration, and metastases

2002 • 490 citations

Cyclin-dependent kinases regulate the antiproliferative function of Smads

2004 • 485 citations

Transforming growth factor β signaling impairs Neu-induced mammary tumorigenesis while promoting pulmonary metastasis

2003 • 433 citations

Disruption of TGF-β signaling in T cells accelerates atherosclerosis

2003 • 426 citations

SD-208, a Novel Transforming Growth Factor β Receptor I Kinase Inhibitor, Inhibits Growth and Invasiveness and Enhances Immunogenicity of Murine and Human Glioma CellsIn vitroandIn vivo

2004 • 407 citations

Blockade of TGF-β inhibits mammary tumor cell viability, migration, and metastases

2002 • 406 citations

Nucleocytoplasmic Shuttling of Smads 2, 3, and 4 Permits Sensing of TGF-β Receptor Activity

2002 • 397 citations

SB-505124 Is a Selective Inhibitor of Transforming Growth Factor-β Type I Receptors ALK4, ALK5, and ALK7

2004 • 393 citations

Akt interacts directly with Smad3 to regulate the sensitivity to TGF-β-induced apoptosis

2004 • 384 citations

Requirement of Type III TGF-β Receptor for Endocardial Cell Transformation in the Heart

1999 • 376 citations

Lifetime exposure to a soluble TGF-β antagonist protects mice against metastasis without adverse side effects

2002 • 375 citations

PKB/Akt modulates TGF-β signalling through a direct interaction with Smad3

2004 • 369 citations

Metastasis is driven by sequential elevation of H-ras and Smad2 levels

2002 • 365 citations

The TGFβ Receptor Activation Process

2001 • 360 citations

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 • 356 citations

TGF-β switches from tumor suppressor to prometastatic factor in a model of breast cancer progression

2003 • 352 citations

Eradication of established intracranial rat gliomas by transforming growth factor beta antisense gene therapy.

1996 • 341 citations

Endogenous TGF-β signaling suppresses maturation of osteoblastic mesenchymal cells

2004 • 327 citations

Lifetime exposure to a soluble TGF-β antagonist protects mice against metastasis without adverse side effects

2002 • 326 citations

Development of anticancer drugs targeting the MAP kinase pathway

2000 • 322 citations

Direct signaling by the BMP type II receptor via the cytoskeletal regulator LIMK1

2003 • 319 citations

AEE788

2004 • 315 citations

TGF-β switches from tumor suppressor to prometastatic factor in a model of breast cancer progression

2003 • 314 citations

Transforming growth factor β1 is associated with angiogenesis, metastasis, and poor clinical outcome in prostate cancer

1998 • 311 citations

Identification of Novel Inhibitors of the Transforming Growth Factor β1 (TGF-β1) Type 1 Receptor (ALK5)

2002 • 306 citations

Double-Outlet Right Ventricle and Overriding Tricuspid Valve Reflect Disturbances of Looping, Myocardialization, Endocardial Cushion Differentiation, and Apoptosis in TGF-β ₂ –Knockout Mice

2001 • 302 citations

Conditional inactivation of the TGF‐β type II receptor using Cre:Lox

2002 • 265 citations

Disruption of Transforming Growth Factor-β Signaling in ELF β-Spectrin-Deficient Mice

2003 • 258 citations

Targeting the TGFβ signaling network in human neoplasia

2003 • 245 citations

Induced disruption of the transforming growth factor beta type II receptor gene in mice causes a lethal inflammatory disorder that is transplantable

2002 • 235 citations

Synthesis and Activity of New Aryl- and Heteroaryl-Substituted Pyrazole Inhibitors of the Transforming Growth Factor-β Type I Receptor Kinase Domain

2003 • 231 citations

Phase I Clinical Trial Design in Cancer Drug Development

2000 • 228 citations

Direct Interaction of c-Myc with Smad2 and Smad3 to Inhibit TGF-β-Mediated Induction of the CDK Inhibitor p15Ink4B

2002 • 224 citations

Cooperation of the ErbB2 receptor and transforming growth factor β in induction of migration and invasion in mammary epithelial cells

2004 • 224 citations

Evaluation of Anti-TGF-β2 Antibody as a New Postoperative Anti-scarring Agent in Glaucoma Surgery

2003 • 222 citations

Alterations of Smad signaling in human breast carcinoma are associated with poor outcome: a tissue microarray study.

2002 • 219 citations

Preoperative Plasma Levels of Transforming Growth Factor Beta₁ (TGF-β₁) Strongly Predict Progression in Patients Undergoing Radical Prostatectomy

2001 • 211 citations

Identification of 1,5-Naphthyridine Derivatives as a Novel Series of Potent and Selective TGF-β Type I Receptor Inhibitors

2004 • 198 citations

Transgenic mice overexpressing a dominant-negative mutant type II transforming growth factor beta receptor show enhanced tumorigenesis in the mammary gland and lung in response to the carcinogen 7,12-dimethylbenz-[a]-anthracene.

1997 • 195 citations

SB-431542, a small molecule transforming growth factor-beta-receptor antagonist, inhibits human glioma cell line proliferation and motility.

2004 • 194 citations

Increased Malignancy of Neu-Induced Mammary Tumors Overexpressing Active Transforming Growth Factor β1

2003 • 192 citations

Induction by transforming growth factor-β1 of epithelial to mesenchymal transition is a rare event in vitro

2004 • 186 citations

Add-On Anti–TGF-β Antibody to ACE Inhibitor Arrests Progressive Diabetic Nephropathy in the Rat

2003 • 184 citations

Reduction in Smad2/3 signaling enhances tumorigenesis but suppresses metastasis of breast cancer cell lines.

2003 • 181 citations

MEKK-1, a Component of the Stress (Stress-activated Protein Kinase/c-Jun N-terminal Kinase) Pathway, Can Selectively Activate Smad2-mediated Transcriptional Activation in Endothelial Cells

1999 • 171 citations

SB-431542, a small molecule transforming growth factor-β-receptor antagonist, inhibits human glioma cell line proliferation and motility

2004 • 168 citations

Successful shape-Based virtual screening: The discovery of a potent inhibitor of the type I TGFβ receptor kinase (TβRI)

2003 • 161 citations

Overexpression of HER2 (erbB2) in Human Breast Epithelial Cells Unmasks Transforming Growth Factor β-induced Cell Motility

2004 • 159 citations

Transforming Growth Factor β Receptor Type II Inactivation Promotes the Establishment and Progression of Colon Cancer

2004 • 152 citations

Biomarkers in Drug Discovery and Development: From Target Identification through Drug Marketing

2003 • 150 citations

Synthesis and activity of new aryl- and heteroaryl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole inhibitors of the transforming growth factor-β type I receptor kinase domain

2004 • 146 citations

Antitumor activity of a recombinant soluble betaglycan in human breast cancer xenograft.

2002 • 144 citations

Bone Morphogenetic Protein-7 Signals Opposing Transforming Growth Factor β in Mesangial Cells

2004 • 136 citations

Targeting Endogenous Transforming Growth Factor β Receptor Signaling in SMAD4-Deficient Human Pancreatic Carcinoma Cells Inhibits Their Invasive Phenotype

2004 • 133 citations

Transgenic Mice Expressing a Dominant-Negative Mutant Type II Transforming Growth Factor-β Receptor Exhibit Impaired Mammary Development and Enhanced Mammary Tumor Formation

2003 • 129 citations

Itch E3 Ligase-Mediated Regulation of TGF-β Signaling by Modulating Smad2 Phosphorylation

2004 • 116 citations

Kinetic Characterization of Novel Pyrazole TGF-β Receptor I Kinase Inhibitors and Their Blockade of the Epithelial−Mesenchymal Transition

2005 • 101 citations

Proteins associated with type II bone morphogenetic protein receptor (BMPR‐II) and identified by two‐dimensional gel electrophoresis and mass spectrometry

2004 • 100 citations

Phase I and II trials of novel anti-cancer agents: Endpoints, efficacy and existentialism

1998 • 100 citations

JNK Regulates Autocrine Expression of TGF-β1

2004 • 91 citations

A Central Role for the JNK Pathway in Mediating the Antagonistic Activity of Pro-inflammatory Cytokines against Transforming Growth Factor-β-driven SMAD3/4-specific Gene Expression

2003 • 90 citations

Tyrosine kinase inhibitors

2004 • 89 citations

c-Jun Inhibits Transforming Growth Factor β-mediated Transcription by Repressing Smad3 Transcriptional Activity

2000 • 86 citations

Smad-Binding Defective Mutant of Transforming Growth Factor β Type I Receptor Enhances Tumorigenesis but Suppresses Metastasis of Breast Cancer Cell Lines

2004 • 84 citations

TLP, a novel modulator of TGF- signaling, has opposite effects on Smad2- and Smad3-dependent signaling

2003 • 78 citations

The role of transforming growth factor-beta in primary brain tumors

2003 • 75 citations

Prolonged survival of rats with intracranial C6 gliomas by treatment wit~ TGF-β antisense gene

1998 • 70 citations

Hepatocellular expression of a dominant-negative mutant TGF-β type II receptor accelerates chemically induced hepatocarcinogenesis

2001 • 67 citations

Heterozygous mice for the transforming growth factor-beta type II receptor gene have increased susceptibility to hepatocellular carcinogenesis.

2001 • 55 citations

Minimal Effects on Immune Parameters Following Chronic Anti-TGF-β Monoclonal Antibody Administration to Normal Mice

2003 • 53 citations

Gene expression profiling of human colon xenograft tumors following treatment with SU11248, a multitargeted tyrosine kinase inhibitor

2004 • 46 citations

Transforming the TGFbeta pathway: convergence of distinct lead generation strategies on a novel kinase pharmacophore for TbetaRI (ALK5).

2004 • 40 citations

Selective inhibitors of type I receptor kinase block cellular transforming growth factor-β signaling

2004 • 38 citations

Clinical development of anticancer agents--a National Cancer Institute perspective.

1984 • 33 citations

The TGF-beta1 antisense oligonucleotide AP 11014 for the treatment of non-small cell lung, colorectal and prostate cancer: Preclinical studies

2004 • 31 citations

ALK5 inhibition in renal disease

2003 • 29 citations

Attenuated type II TGF‐β receptor signalling in human malignant oral keratinocytes induces a less differentiated and more aggressive phenotype that is associated with metastatic dissemination

2004 • 29 citations

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 • 23 citations

Specific therapy for high-grade glioma by convection-enhanced delivery of the TGF-β2 specific antisense oligonucleotide AP 12009

2004 • 20 citations

The TGF-beta1 antisense oligonucleotide AP 11014 for the treatment of non-small cell lung, colorectal and prostate cancer: Preclinical studies

2004 • 15 citations

Lerdelimumab

2003 • 5 citations

Specific therapy for high-grade glioma by convection-enhanced delivery of the TGF-β2 specific antisense oligonucleotide AP 12009

2004 • 4 citations

318 Dihydropyrrolopyrazoles as TGF-beta receptor kinase inhibitors for cancer therapy

2004 • 1 citations

Deleted Work

1955 • 0 citations