Recent Advances of m6A Demethylases Inhibitors and Their Biological Functions in Human Diseases

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

(2021) Sarah Huff et al.   ACS Chemical Biology

FTO modifies the m6A level of MALAT and promotes bladder cancer progression

(2021) Le Tao et al.   Clinical and Translational Medicine

Small-Molecule Inhibitors of the RNA M6A Demethylases FTO Potently Support the Survival of Dopamine Neurons

(2021) Simona Selberg et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Rational Design of Novel Anticancer Small-Molecule RNA m6A Demethylase ALKBH5 Inhibitors

(2021) Simona Selberg et al.   ACS Omega

M6A Demethylase ALKBH5 Regulates PD-L1 Expression and Tumor Immunoenvironment in Intrahepatic Cholangiocarcinoma

(2021) Xinyao Qiu et al.   CANCER RESEARCH

ALKBH5-HOXA10 loop-mediated JAK2 m6A demethylation and cisplatin resistance in epithelial ovarian cancer

(2021) Sipei Nie et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

RNA m6A demethylase FTO-mediated epigenetic up-regulation of LINC00022 promotes tumorigenesis in esophageal squamous cell carcinoma

(2021) Yuanbo Cui et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

ALKBH5 Facilitates Hypoxia-Induced Paraspeckle Assembly and IL8 Secretion to Generate an Immunosuppressive Tumor Microenvironment

(2021) Feng Dong et al.   CANCER RESEARCH

Hallmarks of response, resistance, and toxicity to immune checkpoint blockade

(2021) Golnaz Morad et al.   CELL

Identification of Potent and Selective Inhibitors of Fat Mass Obesity-Associated Protein Using a Fragment-Merging Approach

(2021) Muthuraj Prakash et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2021) Shifali Shishodia et al.   JOURNAL OF MEDICINAL CHEMISTRY

FTO promotes multiple myeloma progression by posttranscriptional activation of HSF1 in an m6A-YTHDF2-dependent manner

(2021) Aoshuang Xu et al.   MOLECULAR THERAPY

FTO promotes tumour proliferation in bladder cancer via the FTO/miR-576/CDK6 axis in an m6A-dependent manner

(2021) Guanwen Zhou et al.   Cell Death Discovery

DDX3 modulates cisplatin resistance in OSCC through ALKBH5-mediated m6A-demethylation of FOXM1 and NANOG

(2020) Omprakash Shriwas et al.   APOPTOSIS

BMP2 Modified by the m6A Demethylation Enzyme ALKBH5 in the Ossification of the Ligamentum Flavum Through the AKT Signaling Pathway

(2020) Hai-Feng Wang et al.   CALCIFIED TISSUE INTERNATIONAL

ALKBH5-mediated m6A demethylation of lncRNA PVT1 plays an oncogenic role in osteosarcoma

(2020) Shuo Chen et al.   Cancer Cell International

N6-methyladenosine ALKBH5 promotes non-small cell lung cancer progress by regulating TIMP3 stability

(2020) Zhiyuan Zhu et al.   GENE

m6A demethylase ALKBH5 inhibits pancreatic cancer tumorigenesis by decreasing WIF-1 RNA methylation and mediating Wnt signaling

(2020) Bo Tang et al.   Molecular Cancer

m6A demethylase ALKBH5 inhibits tumor growth and metastasis by reducing YTHDFs-mediated YAP expression and inhibiting miR-107/LATS2–mediated YAP activity in NSCLC

(2020) Dan Jin et al.   Molecular Cancer

Interferon gamma inhibits CXCL8–CXCR2 axis mediated tumor-associated macrophages tumor trafficking and enhances anti-PD1 efficacy in pancreatic cancer

(2020) Mingjie Zhang et al.   Journal for ImmunoTherapy of Cancer

RNA Demethylase ALKBH5 Selectively Promotes Tumorigenesis and Cancer Stem Cell Self-Renewal in Acute Myeloid Leukemia

(2020) Chao Shen et al.   Cell Stem Cell

RNA demethylase ALKBH5 prevents pancreatic cancer progression by posttranscriptional activation of PER1 in an m6A-YTHDF2-dependent manner

(2020) Xingya Guo et al.   Molecular Cancer

Targeting FTO Suppresses Cancer Stem Cell Maintenance and Immune Evasion

(2020) Rui Su et al.   CANCER CELL

HDAC3-dependent transcriptional repression of FOXA2 regulates FTO/m6A/MYC signaling to contribute to the development of gastric cancer

(2020) Zhi Yang et al.   CANCER GENE THERAPY

ALKBH5 suppresses malignancy of hepatocellular carcinoma via m6A-guided epigenetic inhibition of LYPD1

(2020) Yunhao Chen et al.   Molecular Cancer

ALKBH5 regulates anti–PD-1 therapy response by modulating lactate and suppressive immune cell accumulation in tumor microenvironment

(2020) Na Li et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Identification of Specific N6-Methyladenosine RNA Demethylase FTO Inhibitors by Single-Quantum-Dot-Based FRET Nanosensors

(2020) Yan Zhang et al.   ANALYTICAL CHEMISTRY

FTO demethylates m6A modifications in HOXB13 mRNA and promotes endometrial cancer metastasis by activating the WNT signaling pathway

(2020) Lin zhang et al.   RNA Biology

The m6A RNA Demethylase ALKBH5 Promotes Radioresistance and Invasion Capability of Glioma Stem Cells

(2020) Aline Kowalski-Chauvel et al.   Cancers

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

(2019) Yi Niu et al.   Molecular Cancer

METTL3 and ALKBH5 oppositely regulate m6A modification of TFEB mRNA, which dictates the fate of hypoxia/reoxygenation-treated cardiomyocytes

(2019) Huiwen Song et al.   Autophagy

The Yin and Yang of RNA Methylation: An Imbalance of Erasers Enhances Sensitivity to FTO Demethylase Small-Molecule Targeting in Leukemia Stem Cells

(2019) Inge Van Der Werf et al.   CANCER CELL

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

(2019) Yue Huang et al.   CANCER CELL

ALKBH5 inhibited autophagy of epithelial ovarian cancer through miR-7 and BCL-2

(2019) Hongtao Zhu et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

Where, When, and How: Context-Dependent Functions of RNA Methylation Writers, Readers, and Erasers

(2019) Hailing Shi et al.   MOLECULAR CELL

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

(2019) Shiming Peng et al.   Science Translational Medicine

Identification of Clausine E as an inhibitor of fat mass and obesity‐associated protein (FTO) demethylase activity

(2019) Ying Wang et al.   JOURNAL OF MOLECULAR RECOGNITION

ALKBH5 promotes invasion and metastasis of gastric cancer by decreasing methylation of the lncRNA NEAT1

(2019) Jun Zhang et al.   JOURNAL OF PHYSIOLOGY AND BIOCHEMISTRY

m6A mRNA demethylase FTO regulates melanoma tumorigenicity and response to anti-PD-1 blockade

(2019) Seungwon Yang et al.   Nature Communications

Reduced m6A modification predicts malignant phenotypes and augmented Wnt/PI3K-Akt signaling in gastric cancer

(2019) Cheng Zhang et al.   Cancer Medicine

PVT1 Signaling Is a Mediator of Cancer Progression

(2019) Camille Derderian et al.   Frontiers in Oncology

In vivo modelling of chemo-resistant neuroblastoma provides new insights into chemo-refractory disease and metastasis.

(2019) Orli Yogev et al.   CANCER RESEARCH

Reading, writing and erasing mRNA methylation

(2019) Sara Zaccara et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

The interplay between m6A RNA methylation and noncoding RNA in cancer

(2019) Shuai Ma et al.   Journal of Hematology & Oncology

The m6A methyltransferase METTL3 cooperates with demethylase ALKBH5 to regulate osteogenic differentiation through NF-κB signaling

(2019) Jinjin Yu et al.   MOLECULAR AND CELLULAR BIOCHEMISTRY

m6A RNA Methylation Regulators Contribute to Malignant Progression and Have Clinical Prognostic Impact in Gastric Cancer

(2019) Yunshu Su et al.   Frontiers in Oncology

ALKBH5-m6A-FOXM1 signaling axis promotes proliferation and invasion of lung adenocarcinoma cells under intermittent hypoxia

(2019) Yinghui Chao et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

3D proteome-wide scale screening and activity evaluation of a new ALKBH5 inhibitor in U87 glioblastoma cell line

(2019) Alessio Malacrida et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Loss of Endothelial FTO Antagonizes Obesity-Induced Metabolic and Vascular Dysfunction

(2019) Nenja Krüger et al.   CIRCULATION RESEARCH

Changes in m6A RNA methylation contribute to heart failure progression by modulating translation

(2019) Tea Berulava et al.   EUROPEAN JOURNAL OF HEART FAILURE

Functions of N6-methyladenosine and its role in cancer

(2019) Liuer He et al.   Molecular Cancer

R-2HG Exhibits Anti-tumor Activity by Targeting FTO/m 6 A/MYC/CEBPA Signaling

(2018) Rui Su et al.   CELL

Dynamic transcriptomic m6A decoration: writers, erasers, readers and functions in RNA metabolism

(2018) Ying Yang et al.   CELL RESEARCH

Multi-Protein Dynamic Combinatorial Chemistry: A Novel Strategy that Leads to Simultaneous Discovery of Subfamily-Selective Inhibitors for Nucleic Acid Demethylases FTO and ALKBH3

(2018) Mohua Das et al.   Chemistry-An Asian Journal

FTO-Dependent m6A Regulates Cardiac Function During Remodeling and Repair

(2018) Prabhu Mathiyalagan et al.   CIRCULATION

Identification of the binding between three fluoronucleoside analogues and fat mass and obesity-associated protein by isothermal titration calorimetry and spectroscopic techniques

(2018) Zhigang Li et al.   JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS

FTO regulates the chemo-radiotherapy resistance of cervical squamous cell carcinoma (CSCC) by targeting β-catenin through mRNA demethylation

(2018) Shun Zhou et al.   MOLECULAR CARCINOGENESIS

The MiR-135b–BMAL1–YY1 loop disturbs pancreatic clockwork to promote tumourigenesis and chemoresistance

(2018) Weiliang Jiang et al.   Cell Death & Disease

Identification of Natural Compound Radicicol as a Potent FTO Inhibitor

(2018) Ruiyong Wang et al.   MOLECULAR PHARMACEUTICS

A dynamic N6-methyladenosine methylome regulates intrinsic and acquired resistance to tyrosine kinase inhibitors

(2018) Fei Yan et al.   CELL RESEARCH

Identification of nafamostat mesilate as an inhibitor of the fat mass and obesity-associated protein (FTO) demethylase activity

(2018) Xinxin Han et al.   CHEMICO-BIOLOGICAL INTERACTIONS

The role of chlorine atom on the binding between 2-phenyl-1H-benzimidazole analogues and fat mass and obesity-associated protein

(2018) Junya Li et al.   JOURNAL OF MOLECULAR RECOGNITION

Interaction of two flavonols with fat mass and obesity-associated protein investigated by fluorescence quenching and molecular docking

(2017) Zechun Wang et al.   JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS

Study of the Binding between Camptothecin Analogs and FTO by Spectroscopy and Molecular Docking

(2017) Ting Ren et al.   JOURNAL OF FLUORESCENCE

Binding of clenbuterol to HSA and FTO: a spectroscopic analysis and molecular docking

(2017) Zechun Wang et al.   MEDICINAL CHEMISTRY RESEARCH

Investigation of the interaction between FTO and 3-substituted 2-aminochromones by spectroscopy and molecular modeling

(2017) Lijiao Zhang et al.   MEDICINAL CHEMISTRY RESEARCH

MODOMICS: a database of RNA modification pathways. 2017 update

(2017) Pietro Boccaletto et al.   NUCLEIC ACIDS RESEARCH

FTO Gene Affects Obesity and Breast Cancer Through Similar Mechanisms: A New Insight into the Molecular Therapeutic Targets

(2017) M. E. Akbari et al.   NUTRITION AND CANCER-AN INTERNATIONAL JOURNAL

FTO expression is associated with the occurrence of gastric cancer and prognosis

(2017) Dong Xu et al.   ONCOLOGY REPORTS

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

Investigation of the Interaction between 1,3-Diazaheterocyclic Compounds and the Fat Mass and Obesity-Associated Protein by Fluorescence Spectroscopy and Molecular Modeling

(2016) Lijiao Zhang et al.   JOURNAL OF FLUORESCENCE

Comparative study of the binding between FTO protein and five pyrazole derivatives by spectrofluorimetry

(2016) Lingling Yang et al.   JOURNAL OF MOLECULAR LIQUIDS

Unique features of long non-coding RNA biogenesis and function

(2016) Jeffrey J. Quinn et al.   NATURE REVIEWS GENETICS

Post-transcriptional gene regulation by mRNA modifications

(2016) Boxuan Simen Zhao et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Estrogen promotes fat mass and obesity-associated protein nuclear localization and enhances endometrial cancer cell proliferation via the mTOR signaling pathway

(2016) YAPING ZHU et al.   ONCOLOGY REPORTS

Hypoxia induces the breast cancer stem cell phenotype by HIF-dependent and ALKBH5-mediated m6A-demethylation of NANOG mRNA

(2016) Chuanzhao Zhang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Important Role of FTO in the Survival of Rare Panresistant Triple-Negative Inflammatory Breast Cancer Cells Facing a Severe Metabolic Challenge

(2016) Balraj Singh et al.   PLoS One

Tumor suppressor functions of BNIP3 and mitophagy

(2015) Aparajita H Chourasia et al.   Autophagy

ATG16L1 phosphorylation is oppositely regulated by CSNK2/casein kinase 2 and PPP1/protein phosphatase 1 which determines the fate of cardiomyocytes during hypoxia/reoxygenation

(2015) Huiwen Song et al.   Autophagy

Novel Associations between Common Breast Cancer Susceptibility Variants and Risk-Predicting Mammographic Density Measures

(2015) J. Stone et al.   CANCER RESEARCH

FoxM1 Drives a Feed-Forward STAT3-Activation Signaling Loop That Promotes the Self-Renewal and Tumorigenicity of Glioblastoma Stem-like Cells

(2015) Ai-hua Gong et al.   CANCER RESEARCH

Identification of A Novel Small-Molecule Binding Site of the Fat Mass and Obesity Associated Protein (FTO)

(2015) Wu He et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

FBXW7 modulates cellular stress response and metastatic potential through HSF1 post-translational modification

(2015) Nikos Kourtis et al.   NATURE CELL BIOLOGY

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

Association study of susceptibility loci with specific breast cancer subtypes in Chinese women

(2014) Bo Zhang et al.   BREAST CANCER RESEARCH AND TREATMENT

FTO-dependent demethylation of N6-methyladenosine regulates mRNA splicing and is required for adipogenesis

(2014) Xu Zhao et al.   CELL RESEARCH

Crystal structure of the RNA demethylase ALKBH5 from zebrafish

(2014) Weizhong Chen et al.   FEBS LETTERS

Structures of Human ALKBH5 Demethylase Reveal a Unique Binding Mode for Specific Single-strandedN6-Methyladenosine RNA Demethylation

(2014) Chao Xu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Crystal Structures of the Human RNA Demethylase Alkbh5 Reveal Basis for Substrate Recognition

(2014) Chong Feng et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure of human RNA N6-methyladenine demethylase ALKBH5 provides insights into its mechanisms of nucleic acid recognition and demethylation

(2014) WeiShen Aik et al.   NUCLEIC ACIDS RESEARCH

Meclofenamic acid selectively inhibits FTO demethylation of m6A over ALKBH5

(2014) Yue Huang et al.   NUCLEIC ACIDS RESEARCH

Obesity-related genetic variants, human pigmentation, and risk of melanoma

(2013) Xin Li et al.   HUMAN GENETICS

Emerging role of nanog in tumorigenesis and cancer stem cells

(2013) Luis E. IV Santaliz-Ruiz et al.   INTERNATIONAL JOURNAL OF CANCER

A link between FTO, ghrelin, and impaired brain food-cue responsivity

(2013) Efthimia Karra 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

A variant in FTO shows association with melanoma risk not due to BMI

(2013) Mark M Iles et al.   NATURE GENETICS

MELK-Dependent FOXM1 Phosphorylation is Essential for Proliferation of Glioma Stem Cells

(2013) Kaushal Joshi et al.   STEM CELLS

Increased incidence of non-Hodgkin lymphoma, leukemia, and myeloma in patients with diabetes mellitus type 2: a meta-analysis of observational studies

(2012) J. J. Castillo et al.   BLOOD

Estrogen induces endometrial cancer cell proliferation and invasion by regulating the fat mass and obesity-associated gene via PI3K/AKT and MAPK signaling pathways

(2012) Zhenbo Zhang et al.   CANCER LETTERS

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

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

ALKBH5 Is a Mammalian RNA Demethylase that Impacts RNA Metabolism and Mouse Fertility

(2012) Guanqun Zheng et al.   MOLECULAR CELL

N6-methyl-adenosine (m6A) in RNA: An Old Modification with A Novel Epigenetic Function

(2012) Yamei Niu et al.   GENOMICS PROTEOMICS & BIOINFORMATICS

Association of Obesity-related Genetic Variants With Endometrial Cancer Risk: A Report From the Shanghai Endometrial Cancer Genetics Study

(2011) R. J. Delahanty et al.   AMERICAN JOURNAL OF EPIDEMIOLOGY

The role of the fat mass and obesity associated gene (FTO) in breast cancer risk

(2011) Virginia Kaklamani et al.   BMC Medical Genetics

Oncometabolite 2-Hydroxyglutarate Is a Competitive Inhibitor of α-Ketoglutarate-Dependent Dioxygenases

(2011) Wei Xu et al.   CANCER CELL

Impaired Insulin Signaling in Endothelial Cells Reduces Insulin-Induced Glucose Uptake by Skeletal Muscle

(2011) Tetsuya Kubota et al.   Cell Metabolism

Inhibition of 2-oxoglutarate dependent oxygenases

(2011) Nathan R. Rose et al.   CHEMICAL SOCIETY REVIEWS

Association of variations in the FTO, SCG3 and MTMR9 genes with metabolic syndrome in a Japanese population

(2011) Kikuko Hotta et al.   JOURNAL OF HUMAN GENETICS

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

(2011) Guifang Jia et al.   Nature Chemical Biology

Human AlkB Homologue 5 Is a Nuclear 2-Oxoglutarate Dependent Oxygenase and a Direct Target of Hypoxia-Inducible Factor 1α (HIF-1α)

(2011) Armin Thalhammer et al.   PLoS One

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

(2010) Zhifu Han et al.   NATURE

Inactivation of the Fto gene protects from obesity

(2009) Julia Fischer et al.   NATURE