Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.

Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.

In prostate cancer, two different types of histone lysine demethylases (KDM), LSD1/KDM1 and JMJD2/KDM4, are coexpressed and colocalize with the androgen receptor. We designed and synthesized hybrid LSD1/JmjC or "pan-KDM" inhibitors 1-6 by coupling the skeleton of tranylcypromine 7, a known...

Volledige beschrijving

Bibliografische gegevens
Hoofdauteurs:	Rotili, D, Tomassi, S, Conte, M, Benedetti, R, Tortorici, M, Ciossani, G, Valente, S, Marrocco, B, Labella, D, Novellino, E, Mattevi, A, Altucci, L, Tumber, A, Yapp, C, King, O, Hopkinson, R, Kawamura, A, Schofield, C, Mai, A
Formaat:	Journal article
Taal:	English
Gepubliceerd in:	2014

Gelijkaardige items

Crystal structure of the PHF8 Jumonji domain, an Nepsilon-methyl lysine demethylase
door: Yue, W, et al.
Gepubliceerd in: (2010)

Crystal structure of the PHF8 Jumonji domain, an Nepsilon-methyl lysine demethylase.
door: Yue, W, et al.
Gepubliceerd in: (2010)

Targeting histone lysine demethylases - Progress, challenges, and the future.
door: Thinnes, C, et al.
Gepubliceerd in: (2014)

A miniaturized screen for inhibitors of Jumonji histone demethylases.
door: Sakurai, M, et al.
Gepubliceerd in: (2010)

A miniaturized screen for inhibitors of Jumonji histone demethylases.
door: Sakurai, M, et al.
Gepubliceerd in: (2010)

Structure-activity studies of a macrocyclic peptide inhibitor of histone lysine demethylase 4A
door: Passioura, T, et al.
Gepubliceerd in: (2018)

Arginine demethylation is catalysed by a subset of JmjC histone lysine demethylases.
door: Walport, L, et al.
Gepubliceerd in: (2016)

Chemical probes for histone lysine demethylases
door: Gerken, P
Gepubliceerd in: (2016)

In vitro enzyme assays for JmjC-domain-containing lysine histone demethylases (JmjC-KDMs)
door: Tarhonskaya, H, et al.
Gepubliceerd in: (2018)

The oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylases.
door: Chowdhury, R, et al.
Gepubliceerd in: (2011)

The oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylases
door: Chowdhury, R, et al.
Gepubliceerd in: (2011)

The oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylases
door: Chowdhury, R, et al.
Gepubliceerd in: (2011)

A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases.
door: Luo, X, et al.
Gepubliceerd in: (2011)

Recent progress in histone demethylase inhibitors
door: McAllister, T, et al.
Gepubliceerd in: (2016)

Analysis of JmjC Demethylase-Catalyzed Demethylation Using Geometrically-Constrained Lysine Analogues
door: Langley, G, et al.
Gepubliceerd in: (2015)

Discovery of a highly selective cell-active inhibitor of the histone lysine demethylases KDM2/7
door: Gerken, PA, et al.
Gepubliceerd in: (2017)

The clinically used iron chelator deferasirox is an inhibitor of epigenetic jumonjiC domain-containing histone demethylases
door: Roatsch, M, et al.
Gepubliceerd in: (2019)

Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity.
door: Suzuki, T, et al.
Gepubliceerd in: (2013)

Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.
door: Rose, N, et al.
Gepubliceerd in: (2008)

Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.
door: Rose, N, et al.
Gepubliceerd in: (2008)

Regulation of Jumonji-domain-containing histone demethylases by hypoxia-inducible factor (HIF)-1alpha.
door: Pollard, P, et al.
Gepubliceerd in: (2008)

Discovery of a highly selective cell‐active inhibitor of the histone lysine demethylases KDM2/7
door: Gerken, P, et al.
Gepubliceerd in: (2017)

Investigating the role of lysine demethylase UTX-1 in lifespan regulation of C. elegans
door: Guillermo, A
Gepubliceerd in: (2018)

The activity of JmjC histone lysine demethylase KDM4A is highly sensitive to oxygen concentrations
door: Hancock, R, et al.
Gepubliceerd in: (2017)

A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.
door: Kruidenier, L, et al.
Gepubliceerd in: (2012)

A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.
door: Kruidenier, L, et al.
Gepubliceerd in: (2012)

Highly selective inhibition of histone demethylases by de novo macrocyclic peptides
door: Kawamura, A, et al.
Gepubliceerd in: (2017)

Mechanistic Studies on Histone Demethylases and Related Enzymes
door: Hopkinson, R
Gepubliceerd in: (2013)

Mechanistic studies on histone demethylases and related enzymes
door: Hopkinson, RJ
Gepubliceerd in: (2013)

The role of the lysine demethylases KDM5 and KDM6 in bone malignancies
door: Hookway, E
Gepubliceerd in: (2016)

Development of homogeneous luminescence assays for histone demethylase catalysis and binding.
door: Kawamura, A, et al.
Gepubliceerd in: (2010)

Development of homogeneous luminescence assays for histone demethylase catalysis and binding.
door: Kawamura, A, et al.
Gepubliceerd in: (2010)

Inhibitors of both the N-methyl lysyl- and arginyl- demethylase activities of the JmjC oxygenases
door: Bonnici, J, et al.
Gepubliceerd in: (2018)

Inhibitors of JmjC-containing histone demethylases
door: Wright, M, et al.
Gepubliceerd in: (2020)

Contrasting roles of histone 3 lysine 27 demethylases in acute lymphoblastic leukaemia
door: Ntziachristos, Panagiotis, et al.
Gepubliceerd in: (2015)

Mechanisms of human histone and nucleic acid demethylases
door: Walport, L, et al.
Gepubliceerd in: (2012)

Mechanisms of human histone and nucleic acid demethylases.
door: Walport, L, et al.
Gepubliceerd in: (2012)

In vitro and in vivo investigation into the role of lysine specific demethylases in the molecular circadian oscillator
door: Shepherd, H
Gepubliceerd in: (2015)

Lysine demethylase 5A is required for MYC-driven transcription in multiple myeloma
door: Ohguchi, H, et al.
Gepubliceerd in: (2021)

Inhibition of the histone lysine demethylase JMJD2A by ejection of structural Zn(II).
door: Sekirnik, R, et al.
Gepubliceerd in: (2009)