The emerging role of KDM5A in human cancer

Extended Recognition of the Histone H3 Tail by Histone Demethylase KDM5A

(2020) Nektaria Petronikolou et al.   BIOCHEMISTRY

Discovery of pyrazole derivatives as cellular active inhibitors of histone lysine specific demethylase 5B (KDM5B/JARID1B)

(2020) Bing Zhao et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Increased HDAC Activity and c-MYC Expression Mediate Acquired Resistance to WEE1 Inhibition in Acute Leukemia

(2020) Tamara B. Garcia et al.   Frontiers in Oncology

Alternative splicing of LSD1+8a in neuroendocrine prostate cancer is mediated by SRRM4

(2020) Daniel J. Coleman et al.   NEOPLASIA

X chromosome dosage of histone demethylase KDM5C determines sex differences in adiposity

(2020) Jenny C. Link et al.   JOURNAL OF CLINICAL INVESTIGATION

Activation of the KDM5A/miRNA-495/YTHDF2/m6A-MOB3B axis facilitates prostate cancer progression

(2020) Chen Du et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

Chromatin binding of FOXA1 is promoted by LSD1-mediated demethylation in prostate cancer

(2020) Shuai Gao et al.   NATURE GENETICS

Enhancing KDM5A and TLR activity improves the response to immune checkpoint blockade

(2020) Liangliang Wang et al.   Science Translational Medicine

Targeting of KDM5A by miR-421 in Human Ovarian Cancer Suppresses the Progression of Ovarian Cancer Cells

(2020) Fang Ren et al.   OncoTargets and Therapy

Histone H3 binding to the PHD1 domain of histone demethylase KDM5A enables active site remodeling

(2019) James E. Longbotham et al.   Nature Communications

CVID-Associated Tumors: Czech Nationwide Study Focused on Epidemiology, Immunology, and Genetic Background in a Cohort of Patients With CVID

(2019) Pavlina Kralickova et al.   Frontiers in Immunology

Structure-Based Discovery of a Selective KDM5A Inhibitor that Exhibits Anti-Cancer Activity via Inducing Cell Cycle Arrest and Senescence in Breast Cancer Cell Lines

(2019) Guan-Jun Yang et al.   Cancers

HDAC1 negatively regulates selective mitotic chromatin binding of the Notch effector RBPJ in a KDM5A-dependent manner

(2019) Kostiantyn Dreval et al.   NUCLEIC ACIDS RESEARCH

Drosophila Histone Demethylase KDM5 Regulates Social Behavior through Immune Control and Gut Microbiota Maintenance

(2019) Kun Chen et al.   Cell Host & Microbe

Identification of ortho-hydroxy anilide as a novel scaffold for lysine demethylase 5 inhibitors

(2019) Pattaporn Jaikhan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Cellular therapy for acute myeloid Leukemia – Current status and future prospects

(2019) Panupong Hansrivijit et al.   BLOOD REVIEWS

Histone demethylase KDM5A is transactivated by the transcription factor C/EBPβ and promotes preadipocyte differentiation by inhibiting Wnt/β-catenin signaling

(2019) Liang Guo et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Identification of ryuvidine as a KDM5A inhibitor

(2019) Eishin Mitsui et al.   Scientific Reports

Reduction in H3K4me patterns due to aberrant expression of methyltransferases and demethylases in renal cell carcinoma: prognostic and therapeutic implications

(2019) Aman Kumar et al.   Scientific Reports

Targeting of Histone Demethylases KDM5A and KDM6B Inhibits the Proliferation of Temozolomide-Resistant Glioblastoma Cells

(2019) Massimo Romani et al.   Cancers

Patients aged less than 3 years with acute myeloid leukaemia characterize a molecularly and clinically distinct subgroup

(2019) Yusuke Hara et al.   BRITISH JOURNAL OF HAEMATOLOGY

The KDM5A/RBP2 histone demethylase represses NOTCH signaling to sustain neuroendocrine differentiation and promote small cell lung cancer tumorigenesis

(2019) Matthew G. Oser et al.   GENES & DEVELOPMENT

A novel KDM5A/MPC-1 signaling pathway promotes pancreatic cancer progression via redirecting mitochondrial pyruvate metabolism

(2019) Jiujie Cui et al.   ONCOGENE

The therapeutic effect of dexmedetomidine on protection from renal failure via inhibiting KDM5A in lipopolysaccharide-induced sepsis of mice

(2019) Yan Liu et al.   LIFE SCIENCES

Selective Inhibition of Lysine-Specific Demethylase 5A (KDM5A) Using a Rhodium(III) Complex for Triple-Negative Breast Cancer Therapy

(2018) Guan-Jun Yang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Histone demethylase KDM5A inhibits glioma cells migration and invasion by down regulating ZEB1

(2018) Bin Dai et al.   BIOMEDICINE & PHARMACOTHERAPY

The histone demethylase KDM5A is required for the repression of astrocytogenesis and regulated by the translational machinery in neural progenitor cells

(2018) Sun-Young Kong et al.   FASEB JOURNAL

NUP98-BPTF gene fusion identified in primary refractory acute megakaryoblastic leukemia of infancy

(2018) Mathieu Roussy et al.   GENES CHROMOSOMES & CANCER

Prominent role of histone lysine demethylases in cancer epigenetics and therapy

(2018) Avilala Janardhan et al.   Oncotarget

Lysine-Specific Demethylase 1A as a Promising Target in Acute Myeloid Leukemia

(2018) Daniela Magliulo et al.   Frontiers in Oncology

Genome-Wide Methylation Analysis Identifies NOX4 and KDM5A as Key Regulators in Inhibiting Breast Cancer Cell Proliferation by Ginsenoside Rg3

(2018) Juyeon Ham et al.   AMERICAN JOURNAL OF CHINESE MEDICINE

KDM5 demethylases and their role in cancer cell chemoresistance

(2018) J. Plch et al.   INTERNATIONAL JOURNAL OF CANCER

KDM5 Histone Demethylase Activity Links Cellular Transcriptomic Heterogeneity to Therapeutic Resistance

(2018) Kunihiko Hinohara et al.   CANCER CELL

Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A

(2018) John R. Horton et al.   JOURNAL OF MEDICINAL CHEMISTRY

HER2-positive breast-cancer cell lines are sensitive to KDM5 inhibition: definition of a gene-expression model for the selection of sensitive cases

(2018) Gabriela Paroni et al.   ONCOGENE

The Kdm/Kmt gene families in the self-fertilizing mangrove rivulus fish, Kryptolebias marmoratus, suggest involvement of histone methylation machinery in development and reproduction

(2018) Alexandre Fellous et al.   GENE

Prognostic impact of specific molecular profiles in pediatric acute megakaryoblastic leukemia in non-Down syndrome

(2017) Yusuke Hara et al.   GENES CHROMOSOMES & CANCER

Histone demethylase KDM5A regulates the ZMYND8–NuRD chromatin remodeler to promote DNA repair

(2017) Fade Gong et al.   JOURNAL OF CELL BIOLOGY

Antiviral activity of GS-5801, a liver-targeted prodrug of a lysine demethylase 5 inhibitor, in a hepatitis B virus primary human hepatocyte infection model

(2017) S. Gilmore et al.   JOURNAL OF HEPATOLOGY

Role of RBP2-Induced ER and IGF1R-ErbB Signaling in Tamoxifen Resistance in Breast Cancer

(2017) Hee-Joo Choi et al.   JNCI-Journal of the National Cancer Institute

KDM5A promotes proliferation and EMT in ovarian cancer and closely correlates with PTX resistance

(2017) Tongfu Feng et al.   Molecular Medicine Reports

Pediatric non–Down syndrome acute megakaryoblastic leukemia is characterized by distinct genomic subsets with varying outcomes

(2017) Jasmijn D E de Rooij et al.   NATURE GENETICS

Dynamic site-specific recruitment of RBP2 by pocket protein p130 modulates H3K4 methylation on E2F-responsive promoters

(2017) Zaffer Ullah Zargar et al.   NUCLEIC ACIDS RESEARCH

Toxoplasma gondii Infection Is Associated with Mitochondrial Dysfunction in-Vitro

(2017) Genevieve Syn et al.   Frontiers in Cellular and Infection Microbiology

Role of RBP2-Induced ER and IGF1R-ErbB Signaling in Tamoxifen Resistance in Breast Cancer

(2017) Hee-Joo Choi et al.   JNCI-Journal of the National Cancer Institute

High Expression of Retinoblastoma-Binding Protein 2 (RBP2) in Patients with Hepatocellular Carcinoma and Its Prognostic Significance

(2017) Zhen-Yu Wang et al.   MEDICAL SCIENCE MONITOR

Vitamin C promotes pluripotency of human induced pluripotent stem cells via the histone demethylase JARID1A

(2016) Wassim Eid et al.   BIOLOGICAL CHEMISTRY

Identification of potent, selective KDM5 inhibitors

(2016) Victor S. Gehling et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies

(2016) Jun Liang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

JARID1D Is a Suppressor and Prognostic Marker of Prostate Cancer Invasion and Metastasis

(2016) N. Li et al.   CANCER RESEARCH

Recruitment of the Mammalian Histone-modifying EMSY Complex to Target Genes Is Regulated by ZNF131

(2016) Radhika A. Varier et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structural analysis of human KDM5B guides histone demethylase inhibitor development

(2016) Catrine Johansson et al.   Nature Chemical Biology

An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells

(2016) Maia Vinogradova et al.   Nature Chemical Biology

The KDM5 family is required for activation of pro-proliferative cell cycle genes during adipocyte differentiation

(2016) Ann-Sofie B. Brier et al.   NUCLEIC ACIDS RESEARCH

Resistance to docetaxel in prostate cancer is associated with androgen receptor activation and loss of KDM5D expression

(2016) Kazumasa Komura et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

KDM5A controls bone morphogenic protein 2-induced osteogenic differentiation of bone mesenchymal stem cells during osteoporosis

(2016) Chuandong Wang et al.   Cell Death & Disease

Arginine demethylation is catalysed by a subset of JmjC histone lysine demethylases

(2016) Louise J. Walport et al.   Nature Communications

Screen-identified selective inhibitor of lysine demethylase 5A blocks cancer cell growth and drug resistance

(2016) Molly Gale et al.   Oncotarget

SUMOylated ORC2 Recruits a Histone Demethylase to Regulate Centromeric Histone Modification and Genomic Stability

(2016) Chao Huang et al.   Cell Reports

H3K4me3 Demethylase Kdm5a Is Required for NK Cell Activation by Associating with p50 to Suppress SOCS1

(2016) Dezhi Zhao et al.   Cell Reports

KDM5 lysine demethylases are involved in maintenance of 3'UTR length

(2016) L. P. Blair et al.   Science Advances

Depletion of Histone Demethylase Jarid1A Resulting in Histone Hyperacetylation and Radiation Sensitivity Does Not Affect DNA Double-Strand Break Repair

(2016) Corina Penterling et al.   PLoS One

The histone demethylase KDM5A is a key factor for the resistance to temozolomide in glioblastoma

(2015) Barbara Banelli et al.   CELL CYCLE

Tetrazolylhydrazides as Selective Fragment-Like Inhibitors of the JumonjiC-Domain-Containing Histone Demethylase KDM4A

(2015) Nicole Rüger et al.   ChemMedChem

Molecular Pathways: At the Crossroads of Cancer Epigenetics and Immunotherapy

(2015) M. Maio et al.   CLINICAL CANCER RESEARCH

Characterization of a Linked Jumonji Domain of the KDM5/JARID1 Family of Histone H3 Lysine 4 Demethylases

(2015) John R. Horton et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors

(2015) Magdalena Korczynska et al.   JOURNAL OF MEDICINAL CHEMISTRY

Two Splice Variants of Y Chromosome-Located Lysine-Specific Demethylase 5D Have Distinct Function in Prostate Cancer Cell Line (DU-145)

(2015) Zohreh Jangravi et al.   JOURNAL OF PROTEOME RESEARCH

H3K4me3 demethylation by the histone demethylase KDM5C/JARID1C promotes DNA replication origin firing

(2015) Beatrice Rondinelli et al.   NUCLEIC ACIDS RESEARCH

Identification of Jumonji AT-Rich Interactive Domain 1A Inhibitors and Their Effect on Cancer Cells

(2015) Yukihiro Itoh et al.   ACS Medicinal Chemistry Letters

Histone demethylase KDM5A is regulated by its reader domain through a positive-feedback mechanism

(2015) Idelisse Ortiz Torres et al.   Nature Communications

Histone demethylase RBP2 promotes malignant progression of gastric cancer through TGF-β1-(p-Smad3)-RBP2-E-cadherin-Smad3 feedback circuit

(2015) Xiuming Liang et al.   Oncotarget

Histone demethylase RBP2 decreases miR-21 in blast crisis of chronic myeloid leukemia

(2015) Minran Zhou et al.   Oncotarget

Histone demethylase RBP2 induced by Helicobactor Pylori CagA participates in the malignant transformation of gastric epithelial cells

(2015) Xiuming Liang et al.   Oncotarget

Critical role of histone demethylase RBP2 in human gastric cancer angiogenesis

(2014) Lupeng Li et al.   Molecular Cancer

Dynamic Epigenetic Regulation by Menin During Pancreatic Islet Tumor Formation

(2014) Wenchu Lin et al.   MOLECULAR CANCER RESEARCH

Retinoblastoma Binding Protein 2 (RBP2) Promotes HIF-1α–VEGF-Induced Angiogenesis of Non-Small Cell Lung Cancer via the Akt Pathway

(2014) Lei Qi et al.   PLoS One

The KDM5 family of histone demethylases as targets in oncology drug discovery

(2014) Peter Birk Rasmussen et al.   Epigenomics

Histone Demethylase RBP2 Is Critical for Breast Cancer Progression and Metastasis

(2014) Jian Cao et al.   Cell Reports

Histone Demethylase RBP2 Promotes Lung Tumorigenesis and Cancer Metastasis

(2013) Y.-C. Teng et al.   CANCER RESEARCH

Structural insight into substrate recognition by histone demethylase LSD2/KDM1b

(2013) Fei Chen et al.   CELL RESEARCH

Deregulated expression of selected histone methylases and demethylases in prostate carcinoma

(2013) Filipa Quintela Vieira et al.   ENDOCRINE-RELATED CANCER

Glioblastoma and Other Malignant Gliomas

(2013) Antonio Omuro   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

NUP98/JARID1A is a novel recurrent abnormality in pediatric acute megakaryoblastic leukemia with a distinct HOX gene expression pattern

(2013) J D E de Rooij et al.   LEUKEMIA

Histone Demethylase Retinoblastoma Binding Protein 2 is Overexpressed in Hepatocellular Carcinoma and Negatively Regulated by hsa-miR-212

(2013) Xiuming Liang et al.   PLoS One

RBP2 Induces Epithelial-Mesenchymal Transition in Non-Small Cell Lung Cancer

(2013) Shikun Wang et al.   PLoS One

Identification and Characterization of Small Molecule Inhibitors of a Plant Homeodomain Finger

(2012) Elise K. Wagner et al.   BIOCHEMISTRY

Structure-function analysis reveals a novel mechanism for regulation of histone demethylase LSD2/AOF1/KDM1b

(2012) Qi Zhang et al.   CELL RESEARCH

Histone lysine demethylases in breast cancer

(2012) Elisa Paolicchi et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Mechanisms of human histone and nucleic acid demethylases

(2012) Louise J Walport et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Inhibition of the LSD1 (KDM1A) demethylase reactivates the all-trans-retinoic acid differentiation pathway in acute myeloid leukemia

(2012) Tino Schenk et al.   NATURE MEDICINE

The EP300, KDM5A, KDM6A and KDM6B Chromatin Regulators Cooperate with KLF4 in the Transcriptional Activation of POU5F1

(2012) Wan-Ping Wang et al.   PLoS One

Coordinated repression of cell cycle genes by KDM5A and E2F4 during differentiation

(2012) M. L. Beshiri et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

H3K4 demethylation by Jarid1a and Jarid1b contributes to retinoblastoma-mediated gene silencing during cellular senescence

(2012) A. Chicas et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

NUP98 gene fusions and hematopoietic malignancies: common themes and new biologic insights

(2011) S. M. Gough et al.   BLOOD

Inhibitors of histone demethylation and histone deacetylation cooperate in regulating gene expression and inhibiting growth in human breast cancer cells

(2011) Yi Huang et al.   BREAST CANCER RESEARCH AND TREATMENT

Handpicking epigenetic marks with PHD fingers

(2011) C. A. Musselman et al.   NUCLEIC ACIDS RESEARCH

Drug-Tolerant Cancer Cells Show Reduced Tumor-Initiating Capacity: Depletion of CD44+ Cells and Evidence for Epigenetic Mechanisms

(2011) Hong Yan et al.   PLoS One

Histone Lysine Demethylase JARID1a Activates CLOCK-BMAL1 and Influences the Circadian Clock

(2011) L. DiTacchio et al.   SCIENCE

Epigenetic Regulation by Lysine Demethylase 5 (KDM5) Enzymes in Cancer

(2011) Lauren P. Blair et al.   Cancers

A Chromatin-Mediated Reversible Drug-Tolerant State in Cancer Cell Subpopulations

(2010) Sreenath V. Sharma et al.   CELL

The JmjN Domain of Jhd2 Is Important for Its Protein Stability, and the Plant Homeodomain (PHD) Finger Mediates Its Chromatin Association Independent of H3K4 Methylation

(2010) Fu Huang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Recognition of Histone H3K4 Trimethylation by the Plant Homeodomain of PHF2 Modulates Histone Demethylation

(2010) Hong Wen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Histone Deacetylase Inhibitors Stimulate Histone H3 Lysine 4 Methylation in Part Via Transcriptional Repression of Histone H3 Lysine 4 Demethylases

(2010) P.-H. Huang et al.   MOLECULAR PHARMACOLOGY

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

(2009) Jiping Zeng et al.   GASTROENTEROLOGY

Haematopoietic malignancies caused by dysregulation of a chromatin-binding PHD finger

(2009) Gang G. Wang et al.   NATURE

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

Coordinated regulation of transcriptional repression by the RBP2 H3K4 demethylase and Polycomb-Repressive Complex 2

(2008) D. Pasini et al.   GENES & DEVELOPMENT

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

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

Genome-wide Analysis of the H3K4 Histone Demethylase RBP2 Reveals a Transcriptional Program Controlling Differentiation

(2008) Nuria Lopez-Bigas et al.   MOLECULAR CELL

The ARID domain of the H3K4 demethylase RBP2 binds to a DNA CCGCCC motif

(2008) Shengjiang Tu et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY