Results 61 to 70 of about 24,350 (247)

LSD1 inhibition suppresses the growth of clear cell renal cell carcinoma via upregulating P21 signaling

open access: yesActa Pharmaceutica Sinica B, 2019
Histone lysine-specific demethylase 1 (LSD1) has been implicated in the disease progression of several types of solid tumors. This study provides the first evidence showing that LSD1 overexpression occurred in 62.6% (224/358) of clear cell renal cell ...
Liangsong Zhu   +7 more
doaj   +1 more source

Targeting class I histone deacetylases by the novel small molecule inhibitor 4SC-202 blocks oncogenic hedgehog-GLI signaling and overcomes smoothened inhibitor resistance [PDF]

open access: yes, 2017
Aberrant activation of Hedgehog (HH)/GLI signaling is causally involved in numerous human malignancies, including basal cell carcinoma (BCC) and medulloblastoma. HH pathway antagonists targeting smoothened (SMO), an essential effector of canonical HH/GLI
Aberger, Fritz   +12 more
core   +1 more source

Allelic Variation in Maize Malate Dehydrogenase 7 Shapes Promoter Methylation and Banded Leaf and Sheath Blight Resistance

open access: yesAdvanced Science, EarlyView.
In this study maize chloroplastic malate dehydrogenase7 (ZmMDH7), is identified as a Rhizoctonia solani resistance gene in maize. ZmMDH7 is regulated by transcription factor ZmWRKY44 via pathogens challenge to elevate mitochondrial ROS and SA signaling pathway.
Luyang Wei   +9 more
wiley   +1 more source

The kinase NEK6 positively regulates LSD1 activity and accumulation in local chromatin sub-compartments

open access: yesCommunications Biology
LSD1 plays a crucial role in mammalian biology, regulated through interactions with coregulators and post-translational modifications. Here we show that the kinase NEK6 stimulates LSD1 activity in cells and observe a strong colocalization of NEK6 and ...
Franziska Knodel   +5 more
doaj   +1 more source

Analysis of the levels of lysine-specific demethylase 1 (LSD1) mRNA in human ovarian tumors and the effects of chemical LSD1 inhibitors in ovarian cancer cell lines [PDF]

open access: yes, 2013
BACKGROUND: Lysine-specific demethylase 1 (LSD1, also known as KDM1A and AOF2) is a chromatin-modifying activity that catalyzes the removal of methyl groups from lysine residues in histone and non-histone proteins, regulating gene transcription.
Ivan Garcia-Bassets, Sergiy Konovalov
core   +2 more sources

Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors

open access: yesACS Medicinal Chemistry Letters, 2020
Leveraging the catalytic machinery of LSD1 (KDM1A), a series of covalent styrenylcyclopropane LSD1 inhibitors were identified. These inhibitors represent a new class of mechanism-based inhibitors that target and covalently label the FAD cofactor of LSD1.
Victor S. Gehling   +19 more
openaire   +3 more sources

LSD1 demethylates histone and non-histone proteins [PDF]

open access: yesEpigenetics, 2009
One of the key breakthroughs in the epigenetics/chromatin field in the last several years was the identification of enzymes capable of removing the methyl group from methylated lysines in histone proteins. Lysine-specific demethylase 1 (LSD1) was the first such enzyme identified, which has been shown to demethylate histone H3 on lysine 4 (H3K4) and ...
Thomas B, Nicholson, Taiping, Chen
openaire   +2 more sources

Nap1L4a Cooperates with Scl/Klf1 to Recruit H2A.Z in Mediating Interactions Among Cis‐Regulatory Elements and Transcription Required for Primitive Erythropoiesis in Zebrafish

open access: yesAdvanced Science, EarlyView.
Nap1l4a is required in erythropoiesis and hypoxia responses via physical interaction with Klf1 and Scl to recruit the histone variant H2A.Z. This facilitates its associated cis‐regulatory element (CRE) remodeling and the consequent chromatin assembly, and activates the transcription of erythroid lineage‐specific genes.
JiaHao Shi   +10 more
wiley   +1 more source

Fluorinated tranylcypromine analogues as inhibitors of lysine-specific demethylase 1 (LSD1, KDM1A) [PDF]

open access: yes, 2017
We report a series of tranylcypromine analogues containing a fluorine in the cyclopropyl ring. A number of compounds with additional m- or p- substitution of the aryl ring were micromolar inhibitors of the LSD1 enzyme.
Al-Jamal, Wafa T.   +10 more
core   +2 more sources

LSD1 protects against hippocampal and cortical neurodegeneration [PDF]

open access: yesNature Communications, 2017
AbstractTo investigate the mechanisms that maintain differentiated cells, here we inducibly delete the histone demethylase LSD1/KDM1A in adult mice. Loss of LSD1 leads to paralysis, along with widespread hippocampus and cortex neurodegeneration, and learning and memory defects.
Michael A. Christopher   +8 more
openaire   +3 more sources

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