Targeting the ATF4 pathway in cancer therapy

Autophagy inhibitor Lys05 has single-agent antitumor activity and reproduces the phenotype of a genetic autophagy deficiency

(2012) Q. McAfee et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Pyruvate kinase M2 promotes de novo serine synthesis to sustain mTORC1 activity and cell proliferation

(2012) J. Ye et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Identification of new inhibitors of protein kinase R guided by statistical modeling

(2011) Ruslana Bryk et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Stress-Regulated Transcription Factor ATF4 Promotes Neoplastic Transformation by Suppressing Expression of the INK4a/ARF Cell Senescence Factors

(2011) M. Horiguchi et al.   CANCER RESEARCH

Functional Interaction between Responses to Lactic Acidosis and Hypoxia Regulates Genomic Transcriptional Outputs

(2011) X. Tang et al.   CANCER RESEARCH

Targeting Tumor Hypoxia: Suppression of Breast Tumor Growth and Metastasis by Novel Carbonic Anhydrase IX Inhibitors

(2011) Y. Lou et al.   CANCER RESEARCH

Androgen Receptor and Nutrient Signaling Pathways Coordinate the Demand for Increased Amino Acid Transport during Prostate Cancer Progression

(2011) Q. Wang et al.   CANCER RESEARCH

Suppression of PKR Promotes Network Excitability and Enhanced Cognition by Interferon-γ-Mediated Disinhibition

(2011) Ping Jun Zhu et al.   CELL

The 2-Nitroimidazole EF5 Is a Biomarker for Oxidoreductases That Activate the Bioreductive Prodrug CEN-209 under Hypoxia

(2011) J. Wang et al.   CLINICAL CANCER RESEARCH

Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors

(2011) Aldo Andreani et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Ribosomal protein RPL41 induces rapid degradation of ATF4, a transcription factor critical for tumour cell survival in stress

(2011) Aiyuan Wang et al.   JOURNAL OF PATHOLOGY

Protein kinase A antagonist inhibits β-catenin nuclear translocation, c-Myc and COX-2 expression and tumor promotion in ApcMin/+ mice

(2011) Kristoffer W Brudvik et al.   Molecular Cancer

Chemical genetics identify eIF2α kinase heme-regulated inhibitor as an anticancer target

(2011) Ting Chen et al.   Nature Chemical Biology

Selective Inhibition of a Regulatory Subunit of Protein Phosphatase 1 Restores Proteostasis

(2011) P. Tsaytler et al.   SCIENCE

Protein quality control in the ER: balancing the ubiquitin checkbook

(2011) Jasper H.L. Claessen et al.   TRENDS IN CELL BIOLOGY

Identification of an Ire1alpha endonuclease specific inhibitor with cytotoxic activity against human multiple myeloma

(2010) I. Papandreou et al.   BLOOD

Structural Determinants of PERK Inhibitor Potency and Selectivity

(2010) Hong Wang et al.   Chemical Biology & Drug Design

Virtual Ligand Screening of the p300/CBP Histone Acetyltransferase: Identification of a Selective Small Molecule Inhibitor

(2010) Erin M. Bowers et al.   CHEMISTRY & BIOLOGY

The GCN2-ATF4 pathway is critical for tumour cell survival and proliferation in response to nutrient deprivation

(2010) Jiangbin Ye et al.   EMBO JOURNAL

Pyruvate kinase type M2: A key regulator of the metabolic budget system in tumor cells

(2010) Sybille Mazurek   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Hepatic Heme-Regulated Inhibitor (HRI) Eukaryotic Initiation Factor 2  Kinase: A Protagonist of Heme-Mediated Translational Control of CYP2B Enzymes and a Modulator of Basal Endoplasmic Reticulum Stress Tone

(2010) P. Acharya et al.   MOLECULAR PHARMACOLOGY

Regulation of autophagy by ATF4 in response to severe hypoxia

(2010) T Rzymski et al.   ONCOGENE

Shaping Development of Autophagy Inhibitors with the Structure of the Lipid Kinase Vps34

(2010) S. Miller et al.   SCIENCE

Autophagy and Metabolism

(2010) J. D. Rabinowitz et al.   SCIENCE

Discovery of the first known small-molecule inhibitors of heme-regulated eukaryotic initiation factor 2α (HRI) kinase

(2009) Mark D. Rosen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The Role of ATF4 Stabilization and Autophagy in Resistance of Breast Cancer Cells Treated with Bortezomib

(2009) M. Milani et al.   CANCER RESEARCH

Bidirectional Transport of Amino Acids Regulates mTOR and Autophagy

(2009) Paul Nicklin et al.   CELL

Blocking UV-Induced eIF2α Phosphorylation with Small Molecule Inhibitors of GCN2

(2009) Francis Robert et al.   Chemical Biology & Drug Design

Atf4 Regulates Obesity, Glucose Homeostasis, and Energy Expenditure

(2009) J. Seo et al.   DIABETES

Activating transcription factor 4 and CCAAT/enhancer-binding protein-β negatively regulate the mammalian target of rapamycin via Redd1 expression in response to oxidative and endoplasmic reticulum stress

(2009) Hyeon-Ok Jin et al.   FREE RADICAL BIOLOGY AND MEDICINE

The transcription factor ATF4 regulates glucose metabolism in mice through its expression in osteoblasts

(2009) Tatsuya Yoshizawa et al.   JOURNAL OF CLINICAL INVESTIGATION

Increased antitumor activity of bevacizumab in combination with hypoxia inducible factor-1 inhibition

(2009) A. Rapisarda et al.   MOLECULAR CANCER THERAPEUTICS

ATF4 is necessary and sufficient for ER stress-induced upregulation of REDD1 expression

(2008) Michael L. Whitney et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Preferential Cytotoxicity of Bortezomib toward Hypoxic Tumor Cells via Overactivation of Endoplasmic Reticulum Stress Pathways

(2008) D. R. Fels et al.   CANCER RESEARCH

SP600125 negatively regulates the mammalian target of rapamycin via ATF4-induced Redd1 expression

(2008) Hyeon-Ok Jin et al.   FEBS LETTERS

From endoplasmic-reticulum stress to the inflammatory response

(2008) Kezhong Zhang et al.   NATURE

Pharmacological PKA Inhibition: All May Not Be What It Seems

(2008) A. J. Murray   Science Signaling

Transfer-NMR and Docking Studies Identify the Binding of the Peptide Derived from Activating Transcription Factor 4 to Protein Ubiquitin Ligase β-TrCP. Competition STD-NMR with β-Catenin†

(2007) Julien Pons et al.   BIOCHEMISTRY