Results 41 to 50 of about 24,350 (247)

Enhancer Activation by Pharmacologic Displacement of LSD1 from GFI1 Induces Differentiation in Acute Myeloid Leukemia

open access: yesCell Reports, 2018
Summary: Pharmacologic inhibition of LSD1 promotes blast cell differentiation in acute myeloid leukemia (AML) with MLL translocations. The assumption has been that differentiation is induced through blockade of LSD1’s histone demethylase activity ...
Alba Maiques-Diaz   +16 more
doaj   +1 more source

Application of Small Epigenetic Modulators in Pediatric Medulloblastoma [PDF]

open access: yes, 2018
Medulloblastoma is one of the most frequent among pediatric brain tumors, and it has been classified in various subgroups. Some of them already benefit from quite good therapeutic options, whereas others urgently need novel therapeutic approaches ...
Annalisa Romanelli   +8 more
core   +2 more sources

The histone H3K4 demethylase JARID1A directly interacts with haematopoietic transcription factor GATA1 in erythroid cells through its second PHD domain [PDF]

open access: yes, 2020
Chromatin remodelling and transcription factors play important roles in lineage commitment and development through control of gene expression. Activation of selected lineage-specific genes and repression of alternative lineage-affiliated genes results in
Biasutto, Antonio J   +4 more
core   +1 more source

Defective heart development in hypomorphic LSD1 mice [PDF]

open access: yesCell Research, 2011
Lysine-specific demethylase 1 (LSD1/AOF2/KDM1A), the first enzyme with specific lysine demethylase activity to be described, demethylates histone and non-histone proteins and is essential for mouse embryogenesis. LSD1 interacts with numerous proteins through several different domains, most notably the tower domain, an extended helical structure that ...
Thomas B, Nicholson   +12 more
openaire   +2 more sources

The genetic equidistance result of molecular evolution is independent of mutation rates [PDF]

open access: yes, 2008
The well-established genetic equidistance result shows that sister species are approximately equidistant to a simpler outgroup as measured by DNA or protein dissimilarity.
Shi Huang
core   +3 more sources

Epigenetic regulation of LSD1 during mammary carcinogenesis [PDF]

open access: yesMolecular & Cellular Oncology, 2014
Inheritable epigenetic regulation is integral to the dynamic control of gene expression under different stimuli for cellular homeostasis and disease progression. Histone methylation is a common and important type of chromatin modification. LSD1, the first known histone lysine-specific demethylase, operates as a key component of several corepressor ...
Wu, Yadi, Zhou, Binhua P
openaire   +2 more sources

Tertiary sulphonamide derivatives as dual acting small molecules that inhibit LSD1 and suppress tubulin polymerisation against liver cancer

open access: yesJournal of Enzyme Inhibition and Medicinal Chemistry, 2021
A series of tertiary sulphonamide derivatives were synthesised and evaluated for their antiproliferative activity against liver cancer cell lines (SNU-475, HepG-2, and Bel-7402).
Lijuan Ding   +7 more
doaj   +1 more source

Discovery of an LSD1 PROTAC degrader. [PDF]

open access: yesProc Natl Acad Sci U S A
Aberrant expression of lysine-specific demethylase 1 (LSD1) has been implicated in various cancers, including acute myeloid leukemia (AML). Recent studies have revealed both catalytic and noncatalytic oncogenic functions of LSD1, which cannot be effectively addressed by traditional small-molecule inhibitors.
Hosseini A   +9 more
europepmc   +3 more sources

The long non-coding RNA Kcnq1ot1 controls maternal p57 expression in muscle cells by promoting H3K27me3 accumulation to an intragenic MyoD-binding region [PDF]

open access: yes, 2019
BACKGROUND: The cell-cycle inhibitor p57kip2 plays a critical role in mammalian development by coordinating cell proliferation and differentiation in many cell types.
Andresini, Oriella   +5 more
core   +4 more sources

Dual inhibitors of LSD1 and spermine oxidase [PDF]

open access: yesMedChemComm, 2019
Dual inhibitors of LSD1 and SMOX, with no activity against N1-acetylpolyamine oxidase (PAOX).
Steven Holshouser   +8 more
openaire   +2 more sources

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