ar antagonist enz  (MedKoo Inc)

Journal: PLoS ONE

Article Title: Castration-resistant prostate cancer: Androgen receptor inactivation induces telomere DNA damage, and damage response inhibition leads to cell death

doi: 10.1371/journal.pone.0211090

Figure Lengend Snippet: (A-C) ENZ induces telomere damage in CRPC cells. Based on the dose-response data shown in , CRPC cells were treated for 24 hr with 5 μM ENZ (22Rv1) or 10 μM ENZ (C4-2B and LNCaP/AR), then labeled with antibodies to DNA damage marker γ-H2AX and the telomere marker TIN2. Colocalization of γ-H2AX and TIN2 indicate DNA damage at telomeres. Cells with a TIF response to ENZ (>5 dual-labeled foci) were counted in enlarged (1000X) photomicrographs of representative fields. Data are expressed as mean ± SD of 3 independent experiments. (D-E) Combining ENZ with ATMi KU60019 leads to cell death. 22Rv1 (D) , C4-2B (E) , and LNCaP/AR (F) cells were treated with 5 μM ENZ in the presence or absence of 10 μM KU60019 for 24 hr, then washed to remove drugs and allowed to grow for 14 days (colony formation assay). The survival fraction is plotted relative to vehicle-treated controls; mean ± SD of 3 independent experiments.

Article Snippet: In order to test the effect of AR antagonist ENZ and ATM inhibitor KU59403 (Medkoo Bioscience, NC) on 22Rv1 tumors, athymic nude mice (Charles River) were inoculated subcutaneously with 4 X 10 6 22Rv1 cells as described by Wu et al.[ ], and when tumor size reached about 200 mm 3 , tumor-bearing mice were randomly assigned to the following 4 treatment groups: vehicle (control, 6 mice), ENZ (enzalutamide, Selleckchem, TX) alone (7 mice); ATMi KU59403 alone (7 mice); ENZ + KU59403 (6 mice).

Techniques: Labeling, Marker, Colony Assay

Journal: PLoS ONE

Article Title: Castration-resistant prostate cancer: Androgen receptor inactivation induces telomere DNA damage, and damage response inhibition leads to cell death

doi: 10.1371/journal.pone.0211090

Figure Lengend Snippet: 22Rv1 tumor-bearing athymic nude mice were randomly assigned to vehicle control (Cont), ENZ, ATMi KU59403 (KU), or combined ENZ+KU treatment for 4 weeks. A) Tumor size over time is presented as mean tumor volume (mm 3 ) of each treatment group (n = 6 or 7 mice/group). Error bars represent standard deviation. Statistical analysis was performed for comparison between ENZ alone or KU alone and KU+ENZ treatments: *, p<0.05; **, p<0.001; ***, p<0.0001. B) The doubling time of each tumor was calculated from a plot of log tumor volume vs. time. Doubling times of each treatment group are presented as Box-Whisker plots; horizontal lines represent mean, first and third quartiles, and whiskers represent the minimum and maximum doubling time of each group. The doubling time (days, mean ± SEM) of each group was: Control, 4.94 ± 1.0; KU, 5.50 ± 1.36; ENZ, 5.46 ± 1.36; ENZ+KU, 12.71 ± 4.38. P values are shown in the chart. C) Body weight of mice during the treatment period, relative to day 0 of treatment of each group. D) ENZ induces ATM activation in 22Rv1 xenograft tumors. Immunostaining of pATM is shown in a representative 22Rv1 xenograft tumor section from each treatment group. E) Evaluation of cell death in serial sections of 22Rv1 tumors. TUNEL assay to detect cell death was performed as described in the manufacturer’s protocol (InVitrogen). Images show ~1, 000 cells (blue) in a representative tumor tissue section from each treatment group. Cell death was analyzed by counting the percentage of cells that were dead (red) in each image.

Article Snippet: In order to test the effect of AR antagonist ENZ and ATM inhibitor KU59403 (Medkoo Bioscience, NC) on 22Rv1 tumors, athymic nude mice (Charles River) were inoculated subcutaneously with 4 X 10 6 22Rv1 cells as described by Wu et al.[ ], and when tumor size reached about 200 mm 3 , tumor-bearing mice were randomly assigned to the following 4 treatment groups: vehicle (control, 6 mice), ENZ (enzalutamide, Selleckchem, TX) alone (7 mice); ATMi KU59403 alone (7 mice); ENZ + KU59403 (6 mice).

Techniques: Control, Standard Deviation, Comparison, Whisker Assay, Activation Assay, Immunostaining, TUNEL Assay

Journal: Cell reports

Article Title: Polycomb- and Methylation-Independent Roles of EZH2 as a Transcription Activator

doi: 10.1016/j.celrep.2018.11.035

Figure Lengend Snippet: KEY RESOURCES TABLE

Article Snippet: Enz (MDV3100) AR antagonist , Selleck Chemicals , Cat# S1250.

Techniques: Recombinant, Western Blot, Isolation, cDNA Synthesis, Reporter Assay, Imaging, Control, Software