Novel therapies emerging in oncology to target the TGF-β pathway

Luspatercept in Patients with Lower-Risk Myelodysplastic Syndromes

(2020) Pierre Fenaux et al.   NEW ENGLAND JOURNAL OF MEDICINE

Bintrafusp Alfa, a Bifunctional Fusion Protein Targeting TGF-β and PD-L1, in Second-Line Treatment of Patients With NSCLC: Results From an Expansion Cohort of a Phase 1 Trial

(2020) Luis Paz-Ares et al.   Journal of Thoracic Oncology

Selective inhibition of TGFβ1 activation overcomes primary resistance to checkpoint blockade therapy by altering tumor immune landscape

(2020) Constance J. Martin et al.   Science Translational Medicine

TGF-β Signaling

(2020) Kalliopi Tzavlaki et al.   Biomolecules

Clinical development of therapies targeting TGFβ: current knowledge and future perspectives.

(2020) D. Ciardiello et al.   ANNALS OF ONCOLOGY

879TiP Phase II study of bintrafusp alfa, a bifunctional fusion protein targeting TGF-β and PD-L1, in platinum-experienced advanced cervical cancer

(2020) M.J. Birrer et al.   ANNALS OF ONCOLOGY

The role of TGFβ in hematopoiesis and myeloid disorders

(2019) Alex Bataller et al.   LEUKEMIA

Transforming Growth Factor-β Signaling in Immunity and Cancer

(2019) Eduard Batlle et al.   IMMUNITY

Pharmacokinetic characteristics of vactosertib, a new activin receptor-like kinase 5 inhibitor, in patients with advanced solid tumors in a first-in-human phase 1 study

(2019) Su Young Jung et al.   INVESTIGATIONAL NEW DRUGS

Preclinical Studies and Phase I Trial of Vactosertib in Combination with Pomalidomide in Relapsed Multiple Myeloma: A Corticosteroid-Free Approach By Targeting TGF-β Signaling Pathway

(2019) Ehsan Malek et al.   BLOOD

Clinical ALK5 Inhibitor, Vactosertib, Reverses TGFβ-1 Stimulated Smad-2 Driven Ineffective Hematopoiesis in MDS

(2019) Srinivas Aluri et al.   BLOOD

Population pharmacokinetics of vactosertib, a new TGF-β receptor type Ι inhibitor, in patients with advanced solid tumors

(2019) Su Young Jung et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Blocking TGF-β Signaling To Enhance The Efficacy Of Immune Checkpoint Inhibitor

(2019) Xianguang Bai et al.   OncoTargets and Therapy

c-Met activation leads to the establishment of a TGFβ-receptor regulatory network in bladder cancer progression

(2019) Wen Jing Sim et al.   Nature Communications

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

(2019) Huynh et al.   Biomolecules

Phase I Trial of M7824 (MSB0011359C), a Bifunctional Fusion Protein Targeting PD-L1 and TGFβ, in Advanced Solid Tumors

(2018) Julius Strauss et al.   CLINICAL CANCER RESEARCH

The Balance of Th17 versus Treg Cells in Autoimmunity

(2018) Gap Lee   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Dominant-Negative TGF-β Receptor Enhances PSMA-Targeted Human CAR T Cell Proliferation And Augments Prostate Cancer Eradication

(2018) Christopher C. Kloss et al.   MOLECULAR THERAPY

A Unidirectional Transition from Migratory to Perivascular Macrophage Is Required for Tumor Cell Intravasation

(2018) Esther N. Arwert et al.   Cell Reports

Deregulation of Negative Controls on TGF-β1 Signaling in Tumor Progression

(2018) Jiaqi Tang et al.   Cancers

TGF-β in T Cell Biology: Implications for Cancer Immunotherapy

(2018) Amina Dahmani et al.   Cancers

TGF-β1 programmed myeloid-derived suppressor cells (MDSC) acquire immune-stimulating and tumor killing activity capable of rejecting established tumors in combination with radiotherapy

(2018) Padmini Jayaraman et al.   OncoImmunology

Human monocytes and macrophages regulate immune tolerance via integrin αvβ8–mediated TGFβ activation

(2018) Aoife Kelly et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Crosstalk between the Tumor Microenvironment and Immune System in Pancreatic Ductal Adenocarcinoma: Potential Targets for New Therapeutic Approaches

(2018) Paola Parente et al.   Gastroenterology Research and Practice

TGF-β in pancreatic cancer initiation and progression: two sides of the same coin

(2017) Wei Shen et al.   Cell and Bioscience

Phase II study of Vigil® DNA engineered immunotherapy as maintenance in advanced stage ovarian cancer

(2016) Jonathan Oh et al.   GYNECOLOGIC ONCOLOGY

Emerging Frontiers in Drug Delivery

(2016) Mark W. Tibbitt et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The Discovery and Early Days of TGF-β: A Historical Perspective

(2016) Harold L. Moses et al.   Cold Spring Harbor Perspectives in Biology

Transforming Growth Factor-β1 as a Predictor for the Development of Hepatocellular Carcinoma: A Nested Case–Controlled Study

(2016) Yuko Watanabe et al.   EBioMedicine

Phase 1 study of galunisertib, a TGF-beta receptor I kinase inhibitor, in Japanese patients with advanced solid tumors

(2015) Yutaka Fujiwara et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

High Serum Transforming Growth Factor- 1 Levels Predict Outcome in Hepatocellular Carcinoma Patients Treated with Sorafenib

(2015) T.-H. Lin et al.   CLINICAL CANCER RESEARCH

A phase III study of belagenpumatucel-L, an allogeneic tumour cell vaccine, as maintenance therapy for non-small cell lung cancer

(2015) G. Giaccone et al.   EUROPEAN JOURNAL OF CANCER

Id1 suppresses anti-tumour immune responses and promotes tumour progression by impairing myeloid cell maturation

(2015) Marianna Papaspyridonos et al.   Nature Communications

Abstract B046: Therapeutic targeting of integrin αvβ6 in high-risk breast cancer

(2015) Kate M. Moore et al.   MOLECULAR CANCER RESEARCH

Tumor-Derived Transforming Growth Factor-β is Critical for Tumor Progression and Evasion from Immune Surveillance

(2014) Zheng Li et al.   Asian Pacific Journal of Cancer Prevention

An novel inhibitor of TGF-β type I receptor, IN-1130, blocks breast cancer lung metastasis through inhibition of epithelial–mesenchymal transition

(2014) Chul-Yong Park et al.   CANCER LETTERS

Cardiac Safety of TGF-β Receptor I Kinase Inhibitor LY2157299 Monohydrate in Cancer Patients in a First-in-Human Dose Study

(2014) Richard J. Kovacs et al.   Cardiovascular Toxicology

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) Jordi Rodón et al.   INVESTIGATIONAL NEW DRUGS

Cutting Edge: Autocrine TGF-  Sustains Default Tolerogenesis by IDO-Competent Dendritic Cells

(2014) M. L. Belladonna et al.   JOURNAL OF IMMUNOLOGY

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) Cheng Hua Jin et al.   JOURNAL OF MEDICINAL CHEMISTRY

EW-7197, a Novel ALK-5 Kinase Inhibitor, Potently Inhibits Breast to Lung Metastasis

(2014) J. Y. Son et al.   MOLECULAR CANCER THERAPEUTICS

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) John C. Morris et al.   PLoS One

Defining a therapeutic window for the novel TGF-β inhibitor LY2157299 monohydrate based on a pharmacokinetic/pharmacodynamic model

(2013) Ivelina Gueorguieva et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Activin receptor-like kinase5 inhibition suppresses mouse melanoma by ubiquitin degradation of Smad4, thereby derepressing eomesodermin in cytotoxic T lymphocytes

(2013) Jeong-Hwan Yoon et al.   EMBO Molecular Medicine

Low-dose paclitaxel modulates tumour fibrosis in gastric cancer

(2013) TOMOYA TSUKADA et al.   INTERNATIONAL JOURNAL OF ONCOLOGY

TGF-  Signaling in Myeloid Cells Is Required for Tumor Metastasis

(2013) Y. Pang et al.   Cancer Discovery

TGF-β Signalling Is Required for CD4+ T Cell Homeostasis But Dispensable for Regulatory T Cell Function

(2013) Anna Śledzińska et al.   PLOS BIOLOGY

A phase I study of tasisulam sodium (LY573636 sodium), a novel anticancer compound, administered as a 24-h continuous infusion in patients with advanced solid tumors

(2012) Michael S. Gordon et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Molecular Pathways: Targeting the TGF-  Pathway for Cancer Therapy

(2012) A. L. Smith et al.   CLINICAL CANCER RESEARCH

Gr-1+CD11b+ cells are responsible for tumor promoting effect of TGF-β in breast cancer progression

(2012) Zhaoyang Li et al.   INTERNATIONAL JOURNAL OF CANCER

Dendritic Cell-Specific Disruption of TGF-  Receptor II Leads to Altered Regulatory T Cell Phenotype and Spontaneous Multiorgan Autoimmunity

(2012) R. Ramalingam et al.   JOURNAL OF IMMUNOLOGY

TGFβ signalling in context

(2012) Joan Massagué   NATURE REVIEWS MOLECULAR CELL BIOLOGY

A human monoclonal antibody 264RAD targeting αvβ6 integrin reduces tumour growth and metastasis and modulates key biomarkers in vivo

(2012) C Eberlein et al.   ONCOGENE

TGF-beta signalling in colon carcinogenesis

(2011) Pavlos Lampropoulos et al.   CANCER LETTERS

Outgrowth of Drug-Resistant Carcinomas Expressing Markers of Tumor Aggression after Long-term T RI/II Kinase Inhibition with LY2109761

(2011) E. C. Connolly et al.   CANCER RESEARCH

The Antisense Oligonucleotide Trabedersen (AP 12009) for the Targeted Inhibition of TGF-β2

(2011) Frank Jaschinski et al.   CURRENT PHARMACEUTICAL BIOTECHNOLOGY

T Cell Surveillance of Oncogene-Induced Prostate Cancer Is Impeded by T Cell-Derived TGF-β1 Cytokine

(2011) Moses K. Donkor et al.   IMMUNITY

Indoleamine 2,3-dioxygenase is a signaling protein in long-term tolerance by dendritic cells

(2011) Maria T Pallotta et al.   NATURE IMMUNOLOGY

TGF-  downregulates the activating receptor NKG2D on NK cells and CD8+ T cells in glioma patients

(2011) C. A. Crane et al.   NEURO-ONCOLOGY

Smad6-specific recruitment of Smurf E3 ligases mediates TGF-β1-induced degradation of MyD88 in TLR4 signalling

(2011) Youn Sook Lee et al.   Nature Communications

Molecular characterization of TGFβ-induced epithelial-mesenchymal transition in normal finite lifespan human mammary epithelial cells

(2010) Linsey E. Lindley et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Inhibitory effect of a TGFβ receptor type-I inhibitor, Ki26894, on invasiveness of scirrhous gastric cancer cells

(2010) O Shinto et al.   BRITISH JOURNAL OF CANCER

Intravital Imaging Illuminates Transforming Growth Factor β Signaling Switches during Metastasis

(2010) Silvia Giampieri et al.   CANCER RESEARCH

TGF- -RI Kinase Inhibitor SD-208 Reduces the Development and Progression of Melanoma Bone Metastases

(2010) K. S. Mohammad et al.   CANCER RESEARCH

Smad2 and Smad3 Are Redundantly Essential for the TGF- -Mediated Regulation of Regulatory T Plasticity and Th1 Development

(2010) T. Takimoto et al.   JOURNAL OF IMMUNOLOGY

TGF-β Inhibition Restores Terminal Osteoblast Differentiation to Suppress Myeloma Growth

(2010) Kyoko Takeuchi et al.   PLoS One

TGF-β and immune cells: an important regulatory axis in the tumor microenvironment and progression

(2010) Li Yang et al.   TRENDS IN IMMUNOLOGY

The regulation of TGF  signal transduction

(2009) A. Moustakas et al.   DEVELOPMENT

Treatment of malignant gliomas with TGF-β2 antisense oligonucleotides

(2009) Peter Hau et al.   Expert Review of Anticancer Therapy

Human Dendritic Cells Produce TGF- 1 under the Influence of Lung Carcinoma Cells and Prime the Differentiation of CD4+CD25+Foxp3+ Regulatory T Cells

(2009) I. E. Dumitriu et al.   JOURNAL OF IMMUNOLOGY

An Anti-Transforming Growth Factor   Antibody Suppresses Metastasis via Cooperative Effects on Multiple Cell Compartments

(2008) J.-S. Nam et al.   CANCER RESEARCH

TGFβ in Cancer

(2008) Joan Massagué   CELL

Effect of IN-1130, a Small Molecule Inhibitor of Transforming Growth Factor-β Type I Receptor/Activin Receptor-Like Kinase-5, on Prostate Cancer Cells

(2008) Geun Taek Lee et al.   JOURNAL OF UROLOGY

LY2109761, a novel transforming growth factor   receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis

(2008) D. Melisi et al.   MOLECULAR CANCER THERAPEUTICS