Journal: bioRxiv

Article Title: A Novel Drug Candidate that Selectively Targets the Critical Androgen Receptor-ELK1 Growth Axis in Advanced and Drug-Resistant Prostate Cancer

doi: 10.64898/2026.05.26.727474

Figure Lengend Snippet: Panels A-I: Viability of VCaP cells, LNCaP cells or CWR22Rv1-AR-EK cells was determined at the indicated time points of treatment with vehicle or three concentrations of the enzalutamide, KCI807 or KCI838, as indicated, using a standard MTT assay conducted as described under Methods and values were plotted as percent of the Day 0 values. For statistical analysis, the treatment curves were compared in each case with the corresponding vehicle control as described under Methods. Panels J-M: Viability of the AR-negative DU145 cells, MDA-MB-231 cells, HeLa cells and MDA-MB-231 cells was determined at the end of four days of treatment with vehicle and two concentrations of KCI838, as indicated, using a standard MTT assay conducted as described under Methods and values were plotted as percent of the Day 0 values, considering the Day 0 values to be 100 percent. Statistical analysis of the histograms, conducted as described under Methods, did not show significant effects of the compounds.

Article Snippet: 22Rv1 cells, LNCaP cells, VCaP cells, DU145 cells, A549 cells, MDA-231 cells and HeLa cells were purchased from ATCC and frozen after less than 5 passages.

Techniques: MTT Assay, Control

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Targeting ALDH7A1 with covalent inhibitors reveals new chemical space for prostate cancer therapy

doi: 10.1080/14756366.2026.2664708

Figure Lengend Snippet: Effects of compound 3b and 4b in migration, cell cycle progression, and MDA accumulation in PCa cells. (a) Representative images of DU145 cells migration upon scratch generation in a confluent monolayer. Time point 0 h (T = 0 h) or 60 h (T = 60 h) points post-incubation in presence of DMSO, compound 3b or compound 4b at 20 µM final concentration, are shown. Scale bar = 100 µm. (b) Quantification of scratch area reduction over time normalised to the scratch area at T = 0 h. Wound healing was monitored at 12, 24, 36, 48 and 60 h post-incubation with the indicated compounds. (c) Quantification of cell cycle distribution in DU145 cells treated with DMSO, compound 3b or compound 4b at 20 µM final concentration for 24 h prior to cytofluorimetric analysis. The percentage of cells in each population is shown. (d) Total intracellular ALDH activity measured in DU145 cell lysates following pre-incubation with 20 µM 3b or 4b for 24 h at 37 °C. Cells were extensively washed prior to lysis to eliminate any non-covalently bound material. (e) Quantification of malondialdehyde (MDA) levels in the same cell lysates. MDA concentration was measured and normalised to the total protein content of each sample, as determined by the Bradford assay. In all plots, error bars represent the standard deviation, and asterisks indicate statistical significance levels: p ≤ 0.05 (*), p ≤ 0.01 (**), and p ≤ 0.001 (***).

Article Snippet: To validate the in vitro and in silico findings in a cellular context, the DU145 PCa cell line was selected as a suitable model due to its high expression of ALDH7A1, as reported in the Human Protein Atlas ( www.proteinatlas.org ).

Techniques: Migration, Incubation, Concentration Assay, Activity Assay, Lysis, Bradford Assay, Standard Deviation

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Targeting ALDH7A1 with covalent inhibitors reveals new chemical space for prostate cancer therapy

doi: 10.1080/14756366.2026.2664708

Figure Lengend Snippet: Effects of compound 3b and 4b in migration, cell cycle progression, and MDA accumulation in PCa cells. (a) Representative images of DU145 cells migration upon scratch generation in a confluent monolayer. Time point 0 h (T = 0 h) or 60 h (T = 60 h) points post-incubation in presence of DMSO, compound 3b or compound 4b at 20 µM final concentration, are shown. Scale bar = 100 µm. (b) Quantification of scratch area reduction over time normalised to the scratch area at T = 0 h. Wound healing was monitored at 12, 24, 36, 48 and 60 h post-incubation with the indicated compounds. (c) Quantification of cell cycle distribution in DU145 cells treated with DMSO, compound 3b or compound 4b at 20 µM final concentration for 24 h prior to cytofluorimetric analysis. The percentage of cells in each population is shown. (d) Total intracellular ALDH activity measured in DU145 cell lysates following pre-incubation with 20 µM 3b or 4b for 24 h at 37 °C. Cells were extensively washed prior to lysis to eliminate any non-covalently bound material. (e) Quantification of malondialdehyde (MDA) levels in the same cell lysates. MDA concentration was measured and normalised to the total protein content of each sample, as determined by the Bradford assay. In all plots, error bars represent the standard deviation, and asterisks indicate statistical significance levels: p ≤ 0.05 (*), p ≤ 0.01 (**), and p ≤ 0.001 (***).

Article Snippet: The PCa cells DU145 (#HTB-81, ATCC) and LNCaP (#CRL1740, ATCC) were cultured in an RPMI-1640 culture medium, supplemented with 10% foetal bovine serum (yourSIAL-FBS-SA, S.I.A.L.

Techniques: Migration, Incubation, Concentration Assay, Activity Assay, Lysis, Bradford Assay, Standard Deviation