What is the catalytic mechanism of enzymatic histone N‐methyl arginine demethylation and can it be influenced by an external electric field?

R Ramanan, SO Waheed, CJ Schofield… - … –A European Journal, 2021 - Wiley Online Library
Arginine methylation is an important mechanism of epigenetic regulation. Some Fe (II) and 2‐
oxoglutarate dependent Jumonji‐C (JmjC) Nϵ‐methyl lysine histone demethylases also …

[HTML][HTML] Catalysis by the JmjC histone demethylase KDM4A integrates substrate dynamics, correlated motions and molecular orbital control

R Ramanan, SS Chaturvedi, N Lehnert… - Chemical …, 2020 - pubs.rsc.org
The Nε-methyl lysine status of histones is important in the regulation of eukaryotic
transcription. The Fe (II) and 2-oxoglutarate (2OG)-dependent JmjC domain enzymes are …

Design, synthesis, and biological evaluation of lysine demethylase 5 C degraders

T Iida, Y Itoh, Y Takahashi, Y Yamashita… - …, 2021 - Wiley Online Library
Abstract Lysine demethylase 5 C (KDM5C) controls epigenetic gene expression and is
attracting great interest in the field of chemical epigenetics. KDM5C has emerged as a …

[HTML][HTML] Probiotics and trained immunity

NG Cortes-Perez, A de Moreno de LeBlanc… - Biomolecules, 2021 - mdpi.com
The characteristics of innate immunity have recently been investigated in depth in several
research articles, and original findings suggest that innate immunity also has a memory …

[HTML][HTML] Combining bioinformatics, cheminformatics, functional genomics and whole organism approaches for identifying epigenetic drug targets in Schistosoma …

G Padalino, S Ferla, A Brancale, IW Chalmers… - International Journal for …, 2018 - Elsevier
Schistosomiasis endangers the lives of greater than 200 million people every year and is
predominantly controlled by a single class chemotherapy, praziquantel (PZQ). Development …

Designing the next generation of vaccines: relevance for future pandemics

J Domínguez-Andrés, R van Crevel, M Divangahi… - MBio, 2020 - Am Soc Microbiol
The development of vaccines is one of the greatest medical interventions in the history of
global infectious diseases and has contributed to the annual saving of at least 2 to 3 million …

[HTML][HTML] The repositioning of epigenetic probes/inhibitors identifies new anti-schistosomal lead compounds and chemotherapeutic targets

KCL Whatley, G Padalino, H Whiteland… - PLoS Neglected …, 2019 - journals.plos.org
Background Praziquantel represents the frontline chemotherapy used to treat
schistosomiasis, a neglected tropical disease (NTD) caused by infection with macro …

BET inhibition therapy counteracts cancer cell survival, clonogenic potential and radioresistance mechanisms in rhabdomyosarcoma cells

S Camero, L Camicia, F Marampon, S Ceccarelli… - Cancer Letters, 2020 - Elsevier
The antitumour effects of OTX015, a first-in-class BET inhibitor (BETi), were investigated as a
single agent or in combination with ionizing radiation (IR) in preclinical in vitro models of …

Molecular manipulations and intestinal stem cell-derived organoids in inflammatory bowel disease

TL Boye, C Steenholdt, KB Jensen, OH Nielsen - Stem Cells, 2022 - academic.oup.com
The pathogenesis of inflammatory bowel diseases (IBD) involves genetic predisposition,
environmental factors, and a broadly dysregulated intestinal immune response to the …

Synthesis and Profiling of Highly Selective Inhibitors of Methyltransferase DOT1L Based on Carbocyclic C-Nucleosides

P Khirsariya, P Pospisil, L Maier… - Journal of Medicinal …, 2022 - ACS Publications
Histone methyltransferase DOT1L is an attractive therapeutic target for the treatment of
hematological malignancies. Here, we report the design, synthesis, and profiling of new …