Crystal Structure of the LSD1/CoREST Histone Demethylase Bound to Its Nucleosome Substrate.
Molecules and Cells, 2020 LSD1 (lysine specific demethylase; also known as KDM1A), the first histone demethylase discovered, regulates cell-fate determination and is overexpressed in multiple cancers.
Sang-Ah Kim +4 more
semanticscholar +1 more source
ATF4‐mediated stress response as a therapeutic vulnerability in chordoma
Molecular Oncology, EarlyView.We screened 5 chordoma cell lines against 100+ inhibitors of epigenetic and metabolic pathways and kinases and identified halofuginone, a tRNA synthetase inhibitor. Mechanistically halofuginone induces an integrated stress response, with eIF2alpha phosphorylation, activation of ATF4 and its target genes CHOP, ASNS, INHBE leading to cell death ...
Lucia Cottone +11 more
wiley +1 more source
Identification and characterization of PKF118-310 as a KDM4A inhibitor
Epigenetics, 2017 Epigenetic modifications are functionally involved in gene expression regulation. In particular, histone posttranslational modifications play a crucial role in functional chromatin organization. Several drugs able to inhibit or stimulate some families of
Gianluigi Franci +3 more
doaj +1 more source
Does litomosoides sigmodontis synthesize dimethylethanolamine from choline? [PDF]
, 2008 Juvenile female Litomosoides sigmodontis secrete a protein (Juv-p120) highly modified with dimethylethanolamine (DMAE). In an attempt to establish the source of this decoration worms were pulsed with [3H]-choline and [3H]-ethanolamine and the radio ...
Allen, J E +4 more
core +2 more sources
Histone demethylase KDM6A directly senses oxygen to control chromatin and cell fate
Science, 2019 Oxygen sensing revisited The cellular response to hypoxia (oxygen deficiency) is a contributing factor in many human diseases. Previous studies examining the way in which hypoxia alters gene expression have focused on oxygen-sensing enzymes that regulate
A. Chakraborty +18 more
semanticscholar +1 more source
Targeting p38α in cancer: challenges, opportunities, and emerging strategies
Molecular Oncology, EarlyView.p38α normally regulates cellular stress responses and homeostasis and suppresses malignant transformation. In cancer, however, p38α is co‐opted to drive context‐dependent proliferation and dissemination. p38α also supports key functions in cells of the tumor microenvironment, including fibroblasts, myeloid cells, and T lymphocytes.
Angel R. Nebreda
wiley +1 more source
Epigenomic Regulation of Androgen Receptor Signaling: Potential Role in Prostate Cancer Therapy. [PDF]
, 2017 Androgen receptor (AR) signaling remains the major oncogenic pathway in prostate cancer (PCa). Androgen-deprivation therapy (ADT) is the principle treatment for locally advanced and metastatic disease.
Cucchiara, Vito +5 more
core +2 more sources
Transfer RNA demethylase ALKBH3 promotes cancer progression via induction of tRNA-derived small RNAs
Nucleic Acids Research, 2018 Transfer RNA is heavily modified and plays a central role in protein synthesis and cellular functions. Here we demonstrate that ALKBH3 is a 1-methyladenosine (m1A) and 3-methylcytidine (m3C) demethylase of tRNA.
Zhuojia Chen +9 more
semanticscholar +1 more source
Histone demethylase KDM3B protects against ferroptosis by upregulating SLC7A11
FEBS Open Bio, 2020 Ferroptosis is a type of adaptive cell death driven by cellular metabolism and iron‐dependent lipid peroxidation. Though multiple genes (including SLC7A11 and GPX4) have been demonstrated to play key roles in ferroptosis, little is known about the ...
Yishu Wang +7 more
semanticscholar +1 more source
Histone demethylases regulate adipocyte thermogenesis [PDF]
Diabetology International, 2018 Adipocytes play a pivotal role in the regulation of energy metabolism. While white adipocyte stores energy, brown adipocyte dissipates energy by producing heat. In addition, another type of heat-producing adipocyte, beige adipocyte, emerges in white adipose tissue in response to chronic coldness.
openaire +2 more sources