Assessing histone demethylase inhibitors in cells: lessons learned

Interrogating the Druggability of the 2-Oxoglutarate-Dependent Dioxygenase Target Class by Chemical Proteomics

(2016) Gérard Joberty et al.   ACS Chemical Biology

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

8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors

(2016) Vassilios Bavetsias et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives

(2016) Susan M. Westaway et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives

(2016) Susan M. Westaway et al.   JOURNAL OF MEDICINAL CHEMISTRY

Recent Progress in Histone Demethylase Inhibitors

(2016) Tom E. McAllister et al.   JOURNAL OF MEDICINAL CHEMISTRY

HDAC inhibitors induce global changes in histone lysine and arginine methylation and alter expression of lysine demethylases

(2016) Ryan Lillico et al.   Journal of Proteomics

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

Lateral Thinking: How Histone Modifications Regulate Gene Expression

(2016) Moyra Lawrence et al.   TRENDS IN GENETICS

Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases

(2015) C. C. Thinnes et al.   CHEMICAL COMMUNICATIONS

Advances in the development of histone lysine demethylase inhibitors

(2015) Tamara Maes et al.   CURRENT OPINION IN PHARMACOLOGY

Histone demethylases in chromatin biology and beyond

(2015) E. Dimitrova et al.   EMBO REPORTS

The interplay of histone modifications - writers that read

(2015) T. Zhang et al.   EMBO REPORTS

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

Targeting histone lysine methylation in cancer

(2015) John McGrath et al.   PHARMACOLOGY & THERAPEUTICS

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

A Cell-Permeable Ester Derivative of the JmjC Histone Demethylase Inhibitor IOX1

(2014) Rachel Schiller et al.   ChemMedChem

Incorporating DNA shearing in standard affinity purification allows simultaneous identification of both soluble and chromatin-bound interaction partners

(2014) Jean-Philippe Lambert et al.   Journal of Proteomics

Inhibition of demethylases by GSK-J1/J4

(2014) Bo Heinemann et al.   NATURE

Histone core modifications regulating nucleosome structure and dynamics

(2014) Peter Tessarz et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Epigenetic Regulation of Memory by Acetylation and Methylation of Chromatin: Implications in Neurological Disorders, Aging, and Addiction

(2014) Nilkantha Sen   NEUROMOLECULAR MEDICINE

The roles of Jumonji-type oxygenases in human disease

(2014) Catrine Johansson et al.   Epigenomics

Loss of Histone H3 Methylation at Lysine 4 Triggers Apoptosis in Saccharomyces cerevisiae

(2014) David Walter et al.   PLoS Genetics

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

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

Drug-induced histone eviction from open chromatin contributes to the chemotherapeutic effects of doxorubicin

(2013) Baoxu Pang et al.   Nature Communications

Epigenetic Chemical Probes

(2012) S Müller et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response

(2012) Laurens Kruidenier et al.   NATURE

Bromodomains as therapeutic targets

(2011) Susanne Muller et al.   EXPERT REVIEWS IN MOLECULAR MEDICINE

A Selective Inhibitor and Probe of the Cellular Functions of Jumonji C Domain-Containing Histone Demethylases

(2011) Xuelai Luo et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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