Journal: Oncotarget

Article Title: Therapeutic opportunities in Ewing sarcoma: EWS-FLI inhibition via LSD1 targeting

doi: 10.18632/oncotarget.7124

Figure Lengend Snippet: Current LSD1 inhibitor trials

Article Snippet: Recently, our laboratory investigated the therapeutic potential of a novel reversible and non-competitive LSD1 inhibitor (HCI-2509, Salarius Pharmaceuticals) for the treatment of Ewing sarcoma.

Techniques: Drug discovery

Journal: Oncotarget

Article Title: Therapeutic opportunities in Ewing sarcoma: EWS-FLI inhibition via LSD1 targeting

doi: 10.18632/oncotarget.7124

Figure Lengend Snippet: Chemical structure of HCI-2509 and GSK-2879552, reversible and irreversible inhibitors of LSD1 respectively

Article Snippet: Recently, our laboratory investigated the therapeutic potential of a novel reversible and non-competitive LSD1 inhibitor (HCI-2509, Salarius Pharmaceuticals) for the treatment of Ewing sarcoma.

Techniques:

Journal: Oncotarget

Article Title: Therapeutic opportunities in Ewing sarcoma: EWS-FLI inhibition via LSD1 targeting

doi: 10.18632/oncotarget.7124

Figure Lengend Snippet: Frequency of LSD1 mutation in Ewing sarcoma

Article Snippet: Recently, our laboratory investigated the therapeutic potential of a novel reversible and non-competitive LSD1 inhibitor (HCI-2509, Salarius Pharmaceuticals) for the treatment of Ewing sarcoma.

Techniques: Mutagenesis, Sequencing

Journal: Oncotarget

Article Title: Therapeutic opportunities in Ewing sarcoma: EWS-FLI inhibition via LSD1 targeting

doi: 10.18632/oncotarget.7124

Figure Lengend Snippet: LSD1 inhibition (LSDi) negatively impacts direct transcriptional targets of EWS-FLI, in a manner distinct from HDAC inhibition (HDACi). Moreover, there is data to suggest additional roles for both LSD1 and HDACs in the downstream effects leading to oncogenesis, and these remain an area of active study.

Article Snippet: Recently, our laboratory investigated the therapeutic potential of a novel reversible and non-competitive LSD1 inhibitor (HCI-2509, Salarius Pharmaceuticals) for the treatment of Ewing sarcoma.

Techniques: Inhibition

Journal: PLoS ONE

Article Title: LSD1 mediated changes in the local redox environment during the DNA damage response

doi: 10.1371/journal.pone.0201907

Figure Lengend Snippet: A. U2OS cells were irradiated with 800 nm laser light, fixed at different time points post irradiation then immunostained for LSD1. Quantification of LSD1 was determined by dividing pixel intensity of fluorescence along laser by background (uncut region). B. U2OS cells were treated with ROS sensing dye and irradiated with 800 nm light from a femtosecond near infrared (NIR) laser and either mock treated or treated with 3.4 μM of the LSD1 inhibitor GSK2879552. The pixel intensity along the laser track was quantified and divided by the background nuclear signal. The 95% confidence interval are shown above and below the best fit line for each data set. C. U2OS stained with antibody against LSD1 in either control siRNA treated cells or siLSD1 treated cells 36 hours post transfection. LSD1 expression as determined by IF was reduced approximately 39% in siLSD1 treated cells. D. Accumulation of ROS as sensed by ROS sensing dye in sicontrol treated cells vs siLSD1 treated cells. Pixel intensity of dye fluorescence (higher intensity indicates presence of ROS) along laser track divided by background was calculated to determine the kinetics of dye reaction following laser irradiation.

Article Snippet: Cells treated with LSD1 inhibitor GSK2879552 (Chemietek, Indianapolis, IN) were incubated in HBSS containing 3.4μM GSK inhibitor for 1 hour at 37°C prior to irradiation.

Techniques: Irradiation, Fluorescence, Staining, Control, Transfection, Expressing

Journal: PLoS ONE

Article Title: LSD1 mediated changes in the local redox environment during the DNA damage response

doi: 10.1371/journal.pone.0201907

Figure Lengend Snippet: LSD1 is recruited to double strand breaks. Its histone demethylase activity results in H 2 O 2 as a byproduct. H 2 O 2 reduces DNA end binding activity of Ku80 favoring Nbs1 and HR.

Article Snippet: Cells treated with LSD1 inhibitor GSK2879552 (Chemietek, Indianapolis, IN) were incubated in HBSS containing 3.4μM GSK inhibitor for 1 hour at 37°C prior to irradiation.

Techniques: Activity Assay, Binding Assay