What is the catalytic mechanism of enzymatic histone N‐methyl arginine demethylation and can it be influenced by an external electric field?
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 …
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
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 …
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 …
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 …
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 …
Schistosomiasis endangers the lives of greater than 200 million people every year and is
predominantly controlled by a single class chemotherapy, praziquantel (PZQ). Development …
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 …
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 …
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 …
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 …
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 …
hematological malignancies. Here, we report the design, synthesis, and profiling of new …