Inhibition of 2-oxoglutarate dependent oxygenases

Development of homogeneous luminescence assays for histone demethylase catalysis and binding

(2010) Akane Kawamura et al.   ANALYTICAL BIOCHEMISTRY

The AlkB Domain of Mammalian ABH8 Catalyzes Hydroxylation of 5-Methoxycarbonylmethyluridine at the Wobble Position of tRNA

(2010) Ye Fu et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Mildronate exerts acute anticonvulsant and antihypnotic effects

(2010) Liga Zvejniece et al.   BEHAVIOURAL PHARMACOLOGY

Crystal structure of human gamma-butyrobetaine hydroxylase

(2010) Kaspars Tars et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Investigating the dependence of the hypoxia-inducible factor hydroxylases (factor inhibiting HIF and prolyl hydroxylase domain 2) on ascorbate and other reducing agents

(2010) Emily Flashman et al.   BIOCHEMICAL JOURNAL

Structural basis for binding of cyclic 2-oxoglutarate analogues to factor-inhibiting hypoxia-inducible factor

(2010) Ana Conejo-Garcia et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Hypoxia-dependent sequestration of an oxygen sensor by a widespread structural motif can shape the hypoxic response - a predictive kinetic model

(2010) Bernhard Schmierer et al.   BMC Systems Biology

The Common Feature of Leukemia-Associated IDH1 and IDH2 Mutations Is a Neomorphic Enzyme Activity Converting α-Ketoglutarate to 2-Hydroxyglutarate

(2010) Patrick S. Ward et al.   CANCER CELL

Monitoring the Activity of 2-Oxoglutarate Dependent Histone Demethylases by NMR Spectroscopy: Direct Observation of Formaldehyde

(2010) Richard J. Hopkinson et al.   CHEMBIOCHEM

Utilization of an In Vivo Reporter for High Throughput Identification of Branched Small Molecule Regulators of Hypoxic Adaptation

(2010) Natalya A. Smirnova et al.   CHEMISTRY & BIOLOGY

Structural and Mechanistic Studies on γ-Butyrobetaine Hydroxylase

(2010) Ivanhoe K.H. Leung et al.   CHEMISTRY & BIOLOGY

Structural studies on human 2-oxoglutarate dependent oxygenases

(2010) Michael A McDonough et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Prolyl hydroxylase domain-containing protein inhibitors as stabilizers of hypoxia-inducible factor: small molecule-based therapeutics for anemia

(2010) Lin Yan et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Evidence for the slow reaction of hypoxia-inducible factor prolyl hydroxylase 2 with oxygen

(2010) Emily Flashman et al.   FEBS Journal

Crystal structure of the PHF8 Jumonji domain, anNε-methyl lysine demethylase

(2010) Wyatt W. Yue et al.   FEBS LETTERS

Consequences of IkappaB alpha hydroxylation by the factor inhibiting HIF (FIH)

(2010) Ingrid L. Devries et al.   FEBS LETTERS

Expanding Role of the Jumonji C Domain as an RNA Hydroxylase

(2010) Akiko Noma et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Cancer-associated metabolite 2-hydroxyglutarate accumulates in acute myelogenous leukemia with isocitrate dehydrogenase 1 and 2 mutations

(2010) Stefan Gross et al.   JOURNAL OF EXPERIMENTAL MEDICINE

RIPENING OF CLIMACTERIC FRUITS AND THEIR CONTROL

(2010) A. PAYASI et al.   JOURNAL OF FOOD BIOCHEMISTRY

Selective Inhibitors of the JMJD2 Histone Demethylases: Combined Nondenaturing Mass Spectrometric Screening and Crystallographic Approaches

(2010) Nathan R. Rose et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, Enzyme-Inhibitory Activity, and Effect on Human Cancer Cells of a Novel Series of Jumonji Domain-Containing Protein 2 Histone Demethylase Inhibitors

(2010) Shohei Hamada et al.   JOURNAL OF MEDICINAL CHEMISTRY

Small-Molecule-Based Inhibition of Histone Demethylation in Cells Assessed by Quantitative Mass Spectrometry

(2010) Mukram M. Mackeen et al.   JOURNAL OF PROTEOME RESEARCH

2-Oxoglutarate oxygenases are inhibited by a range of transition metals

(2010) Rok Sekirnik et al.   Metallomics

Human AlkB Homolog ABH8 Is a tRNA Methyltransferase Required for Wobble Uridine Modification and DNA Damage Survival

(2010) D. Fu et al.   MOLECULAR AND CELLULAR BIOLOGY

Crystal structures of human FIH-1 in complex with quinol family inhibitors

(2010) Hyunjin Moon et al.   MOLECULES AND CELLS

Systematic sequencing of renal carcinoma reveals inactivation of histone modifying genes

(2010) Gillian L. Dalgliesh et al.   NATURE

Role of Tet proteins in 5mC to 5hmC conversion, ES-cell self-renewal and inner cell mass specification

(2010) Shinsuke Ito et al.   NATURE

Crystal structure of the FTO protein reveals basis for its substrate specificity

(2010) Zhifu Han et al.   NATURE

Overexpression of Fto leads to increased food intake and results in obesity

(2010) Chris Church et al.   NATURE GENETICS

Quantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase Inhibitors

(2010) Oliver N. F. King et al.   PLoS One

KDM8, a H3K36me2 histone demethylase that acts in the cyclin A1 coding region to regulate cancer cell proliferation

(2010) D. A. Hsia et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Physiological and biochemical aspects of hydroxylations and demethylations catalyzed by human 2-oxoglutarate oxygenases

(2010) Christoph Loenarz et al.   TRENDS IN BIOCHEMICAL SCIENCES

IDH mutations in glioma and acute myeloid leukemia

(2010) Lenny Dang et al.   TRENDS IN MOLECULAR MEDICINE

Direct Analysis of Enzyme-Catalyzed DNA Demethylation

(2009) Anna A. Karkhanina et al.   ANALYTICAL CHEMISTRY

FIH-Dependent Asparaginyl Hydroxylation of Ankyrin Repeat Domain-Containing Proteins

(2009) Matthew E. Cockman et al.   Annals of the New York Academy of Sciences

2-Oxoglutarate analogue inhibitors of prolyl hydroxylase domain 2

(2009) Jasmin Mecinović et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and activity of N-oxalylglycine and its derivatives as Jumonji C-domain-containing histone lysine demethylase inhibitors

(2009) Shohei Hamada et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

SDH5 Mutations and Familial Paraganglioma: Somewhere Warburg is Smiling

(2009) William G. Kaelin   CANCER CELL

Inhibition of the histone lysine demethylase JMJD2A by ejection of structural Zn(ii)

(2009) Rok Sekirnik et al.   CHEMICAL COMMUNICATIONS

Autism-associated familial microdeletion of Xp11.22

(2009) Y Qiao et al.   CLINICAL GENETICS

Regulation of the osteoblast-specific transcription factor Osterix by NO66, a Jumonji family histone demethylase

(2009) Krishna M Sinha et al.   EMBO JOURNAL

The Histone Demethylase RBP2 Is Overexpressed in Gastric Cancer and Its Inhibition Triggers Senescence of Cancer Cells

(2009) Jiping Zeng et al.   GASTROENTEROLOGY

PHF8, a gene associated with cleft lip/palate and mental retardation, encodes for an Nε-dimethyl lysine demethylase

(2009) Christoph Loenarz et al.   HUMAN MOLECULAR GENETICS

Nickel Ions Inhibit Histone Demethylase JMJD1A and DNA Repair Enzyme ABH2 by Replacing the Ferrous Iron in the Catalytic Centers

(2009) Haobin Chen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Mint3 Enhances the Activity of Hypoxia-inducible Factor-1 (HIF-1) in Macrophages by Suppressing the Activity of Factor Inhibiting HIF-1

(2009) Takeharu Sakamoto et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The Crystal Structure of an Algal Prolyl 4-Hydroxylase Complexed with a Proline-rich Peptide Reveals a Novel Buried Tripeptide Binding Motif

(2009) M. Kristian Koski et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Application of a Proteolysis/Mass Spectrometry Method for Investigating the Effects of Inhibitors on Hydroxylase Structure

(2009) Christopher J. Stubbs et al.   JOURNAL OF MEDICINAL CHEMISTRY

Asparaginyl β-Hydroxylation of Proteins Containing Ankyrin Repeat Domains Influences Their Stability and Function

(2009) Adam P. Hardy et al.   JOURNAL OF MOLECULAR BIOLOGY

Practical Applications of Manipulating Plant Architecture by Regulating Gibberellin Metabolism

(2009) Anjanabha Bhattacharya et al.   JOURNAL OF PLANT GROWTH REGULATION

Epigenetics in metal carcinogenesis: nickel, arsenic, chromium and cadmium

(2009) Adriana Arita et al.   Metallomics

A miniaturized screen for inhibitors of Jumonji histone demethylases

(2009) Masaaki Sakurai et al.   Molecular BioSystems

Cancer-associated IDH1 mutations produce 2-hydroxyglutarate

(2009) Lenny Dang et al.   NATURE

Inactivation of the Fto gene protects from obesity

(2009) Julia Fischer et al.   NATURE

Inhibition of oxygen sensors as a therapeutic strategy for ischaemic and inflammatory disease

(2009) Peter Fraisl et al.   NATURE REVIEWS DRUG DISCOVERY

Enzymatic and structural insights for substrate specificity of a family of jumonji histone lysine demethylases

(2009) John R Horton et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Conversion of 5-Methylcytosine to 5-Hydroxymethylcytosine in Mammalian DNA by MLL Partner TET1

(2009) M. Tahiliani et al.   SCIENCE

The Nuclear DNA Base 5-Hydroxymethylcytosine Is Present in Purkinje Neurons and the Brain

(2009) S. Kriaucionis et al.   SCIENCE

Structural Basis for Binding of Hypoxia-Inducible Factor to the Oxygen-Sensing Prolyl Hydroxylases

(2009) Rasheduzzaman Chowdhury et al.   STRUCTURE

A Mouse Model for the Metabolic Effects of the Human Fat Mass and Obesity Associated FTO Gene

(2009) Chris Church et al.   PLoS Genetics

Kinetic characterization and identification of a novel inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 using a time-resolved fluorescence resonance energy transfer-based assay technology

(2008) Jennifer H. Dao et al.   ANALYTICAL BIOCHEMISTRY

Prolyl 4-hydroxylases, key enzymes in the synthesis of collagens and regulation of the response to hypoxia, and their roles as treatment targets

(2008) Johanna Myllyharju   ANNALS OF MEDICINE

Gibberellin Metabolism and its Regulation

(2008) Shinjiro Yamaguchi   Annual Review of Plant Biology

Iron- and 2-oxoglutarate-dependent Dioxygenases: an emerging group of molecular targets for nickel toxicity and carcinogenicity

(2008) Haobin Chen et al.   BIOMETALS

Discovery of novel hydroxy-thiazoles as HIF-α prolyl hydroxylase inhibitors: SAR, synthesis, and modeling evaluation

(2008) Christopher M. Tegley et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Evaluation of aspirin metabolites as inhibitors of hypoxia-inducible factor hydroxylases

(2008) Benoit M. Lienard et al.   CHEMICAL COMMUNICATIONS

The human oxygen sensing machinery and its manipulation

(2008) Rasheduzzaman Chowdhury et al.   CHEMICAL SOCIETY REVIEWS

Hypoxia Inducible Factor-1α, Endothelial Progenitor Cells, Monocytes,Cardiovascular Risk, Wound Healing, Cobalt and Hydralazine:A Unifying Hypothesis

(2008) Michel Hoenig et al.   CURRENT DRUG TARGETS

The emerging functions of histone demethylases

(2008) Karl Agger et al.   CURRENT OPINION IN GENETICS & DEVELOPMENT

Dynamic states of the DNA repair enzyme AlkB regulate product release

(2008) Boris Bleijlevens et al.   EMBO REPORTS

Erasing the methyl mark: histone demethylases at the center of cellular differentiation and disease

(2008) P. A.C. Cloos et al.   GENES & DEVELOPMENT

Evidence That Two Enzyme-derived Histidine Ligands Are Sufficient for Iron Binding and Catalysis by Factor Inhibiting HIF (FIH)

(2008) Kirsty S. Hewitson et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Recessive osteogenesis imperfecta caused by LEPRE1 mutations: clinical documentation and identification of the splice form responsible for prolyl 3-hydroxylation

(2008) A Willaert et al.   JOURNAL OF MEDICAL GENETICS

Inhibitor Scaffolds for 2-Oxoglutarate-Dependent Histone Lysine Demethylases⊥

(2008) Nathan R. Rose et al.   JOURNAL OF MEDICINAL CHEMISTRY

18O Kinetic Isotope Effects in Non-Heme Iron Enzymes: Probing the Nature of Fe/O2Intermediates

(2008) Liviu M. Mirica et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Asparagine β-hydroxylation stabilizes the ankyrin repeat domain fold

(2008) Leanne Kelly et al.   Molecular BioSystems

Baicalein Induces Functional Hypoxia-Inducible Factor-1  and Angiogenesis

(2008) H. Cho et al.   MOLECULAR PHARMACOLOGY

Crystal structures of DNA/RNA repair enzymes AlkB and ABH2 bound to dsDNA

(2008) Cai-Guang Yang et al.   NATURE

Expanding chemical biology of 2-oxoglutarate oxygenases

(2008) Christoph Loenarz et al.   Nature Chemical Biology

The Histone H3 Lysine 27-Specific Demethylase Jmjd3 Is Required for Neural Commitment

(2008) Thomas Burgold et al.   PLoS One

ESI-MS Studies on Prolyl Hydroxylase Domain 2 Reveal a New Metal Binding Site

(2007) Jasmin Mecinović et al.   ChemMedChem

Flavonoids-induced accumulation of hypoxia-inducible factor (HIF)-1α/2α is mediated through chelation of iron

(2007) Sung-Soo Park et al.   JOURNAL OF CELLULAR BIOCHEMISTRY