Structure-Based Design of Selective Fat Mass and Obesity Associated Protein (FTO) Inhibitors

m6A-RNA Demethylase FTO Inhibitors Impair Self-Renewal in Glioblastoma Stem Cells

(2021) Sarah Huff et al.   ACS Chemical Biology

Long‐term efficacy and safety of hypoxia‐inducible factor prolyl hydroxylase inhibitors in anaemia of chronic kidney disease: A meta‐analysis including 13,146 patients

(2021) Huanhuan Chen et al.   JOURNAL OF CLINICAL PHARMACY AND THERAPEUTICS

Structural Basis of Prolyl Hydroxylase Domain Inhibition by Molidustat

(2021) William D. Figg et al.   ChemMedChem

Distinct RNAN-demethylation pathways catalyzed by nonheme iron ALKBH5 and FTO enzymes enable regulation of formaldehyde release rates

(2020) Joel D. W. Toh et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Improved Synthesis of Phosphoramidite-Protected N6-Methyladenosine via BOP-Mediated SNAr Reaction

(2020) Shifali Shishodia et al.   MOLECULES

Structural insights into FTO’s catalytic mechanism for the demethylation of multiple RNA substrates

(2019) Xiao Zhang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

FTO controls reversible m6Am RNA methylation during snRNA biogenesis

(2019) Jan Mauer et al.   Nature Chemical Biology

RNA N6-methyladenosine demethylase FTO promotes breast tumor progression through inhibiting BNIP3

(2019) Yi Niu et al.   Molecular Cancer

Small-Molecule Targeting of Oncogenic FTO Demethylase in Acute Myeloid Leukemia

(2019) Yue Huang et al.   CANCER CELL

Targeting the RNA m6A Reader YTHDF2 Selectively Compromises Cancer Stem Cells in Acute Myeloid Leukemia

(2019) Jasmin Paris et al.   Cell Stem Cell

Identification of entacapone as a chemical inhibitor of FTO mediating metabolic regulation through FOXO1

(2019) Shiming Peng et al.   Science Translational Medicine

Macromolecular structure determination using X-rays, neutrons and electrons: recent developments in Phenix

(2019) Dorothee Liebschner et al.   Acta Crystallographica Section D-Structural Biology

Structure‐Activity Relationship and Crystallographic Studies on 4‐Hydroxypyrimidine HIF Prolyl Hydroxylase Domain Inhibitors

(2019) James P. Holt‐Martyn et al.   ChemMedChem

2-Oxoglutarate-Dependent Oxygenases

(2018) Md. Saiful Islam et al.   Annual Review of Biochemistry

NMR analyses on N-hydroxymethylated nucleobases – implications for formaldehyde toxicity and nucleic acid demethylases

(2018) S. Shishodia et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Effects of Molidustat in the Treatment of Anemia in CKD

(2018) Iain C. Macdougall et al.   Clinical Journal of the American Society of Nephrology

Lysine demethylase�2A promotes the progression of ovarian cancer by regulating the PI3K pathway and reversing epithelial‑mesenchymal transition

(2018) Dan‑Hua Lu et al.   ONCOLOGY REPORTS

Molecular and cellular mechanisms of HIF prolyl hydroxylase inhibitors in clinical trials

(2017) Tzu-Lan Yeh et al.   Chemical Science

m 6 A RNA Methylation Regulates the Self-Renewal and Tumorigenesis of Glioblastoma Stem Cells

(2017) Qi Cui et al.   Cell Reports

A Novel Inhibitor of the Obesity-Related Protein FTO

(2016) Yan Qiao et al.   BIOCHEMISTRY

Structural basis for oxygen degradation domain selectivity of the HIF prolyl hydroxylases

(2016) Rasheduzzaman Chowdhury et al.   Nature Communications

Fluorescein Derivatives as Bifunctional Molecules for the Simultaneous Inhibiting and Labeling of FTO Protein

(2015) Tianlu Wang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Pharmacological Inhibition of FTO

(2015) Fiona McMurray et al.   PLoS One

A strategy based on nucleotide specificity leads to a subfamily-selective and cell-active inhibitor of N6-methyladenosine demethylase FTO

(2015) Joel D. W. Toh et al.   Chemical Science

Synthesis of a FTO Inhibitor with Anticonvulsant Activity

(2014) Guanqun Zheng et al.   ACS Chemical Neuroscience

Meclofenamic acid selectively inhibits FTO demethylation of m6A over ALKBH5

(2014) Yue Huang et al.   NUCLEIC ACIDS RESEARCH

Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor

(2014) Katherine S. England et al.   MedChemComm

Selective Small Molecule Probes for the Hypoxia Inducible Factor (HIF) Prolyl Hydroxylases

(2013) Rasheduzzaman Chowdhury et al.   ACS Chemical Biology

KDM2A promotes lung tumorigenesis by epigenetically enhancing ERK1/2 signaling

(2013) Klaus W. Wagner et al.   JOURNAL OF CLINICAL INVESTIGATION

Structural Basis for Inhibition of the Fat Mass and Obesity Associated Protein (FTO)

(2013) WeiShen Aik et al.   JOURNAL OF MEDICINAL CHEMISTRY

5-Carboxy-8-hydroxyquinoline is a broad spectrum 2-oxoglutarate oxygenase inhibitor which causes iron translocation

(2013) Richard J. Hopkinson et al.   Chemical Science

FTO-mediated formation of N6-hydroxymethyladenosine and N6-formyladenosine in mammalian RNA

(2013) Ye Fu et al.   Nature Communications

Linking of 2-Oxoglutarate and Substrate Binding Sites Enables Potent and Highly Selective Inhibition of JmjC Histone Demethylases

(2012) Esther C. Y. Woon et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Role of the jelly-roll fold in substrate binding by 2-oxoglutarate oxygenases

(2012) WeiShen Aik et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Dynamic Combinatorial Mass Spectrometry Leads to Inhibitors of a 2-Oxoglutarate-Dependent Nucleic Acid Demethylase

(2012) Esther C. Y. Woon et al.   JOURNAL OF MEDICINAL CHEMISTRY

Reporter Ligand NMR Screening Method for 2-Oxoglutarate Oxygenase Inhibitors

(2012) Ivanhoe K. H. Leung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of Cell-Active N6-Methyladenosine RNA Demethylase FTO Inhibitor

(2012) Baoen Chen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Spin echo NMR spectra without J modulation

(2011) Juan A. Aguilar et al.   CHEMICAL COMMUNICATIONS

Structural and Evolutionary Basis for the Dual Substrate Selectivity of Human KDM4 Histone Demethylase Family

(2011) Lars Hillringhaus et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

N6-Methyladenosine in nuclear RNA is a major substrate of the obesity-associated FTO

(2011) Guifang Jia et al.   Nature Chemical Biology

Features and development ofCoot

(2010) P. Emsley et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

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

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

(2010) Zhifu Han et al.   NATURE

xia2: an expert system for macromolecular crystallography data reduction

(2009) G. Winter   JOURNAL OF APPLIED CRYSTALLOGRAPHY

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

(2009) Rasheduzzaman Chowdhury et al.   STRUCTURE

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

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