Journal: Oncogene
Article Title: EZH2 PROTACs outperform catalytic inhibitors in prostate cancer by targeting a methylation-independent function of PRC2
doi: 10.1038/s41388-025-03662-z
Figure Lengend Snippet: A A panel of PCa cell lines (LNCaP, C4-2B, LNCaP95, 22Rv1, and VCaP) and a normal prostate epithelial cell line (RWPE) were treated with PROTAC-6272 and EPZ-6438 with increasing doses from nM to µM for 48 h, and half inhibitory concentrations (IC 50 ) of proliferation rates were assayed by cell Titer Glo ( n = 6). B A panel of PCa cell lines was treated with DMSO, PROTAC-6272 (1 µM), and EPZ-6438 (1 µM) and incubated in an IncuCyte live imager chamber; images were taken every 2 h up to 9 days. Cell proliferation rates were analyzed by IncuCyte live imager software ( n = 6). C 22Rv1 cells were subjected to triplicate RNA-seq analysis upon 6 days of treatment with DMSO, PROTAC-6286, PROTAC-6272, and EPZ-6438 (1 µM). Heatmap shows combined differentially expressed genes identified ( | Log2FC | ≥0.585, adjusted p < 0.05) from treatment of PROTAC-6286, EPZ-6438, or PROTAC-6272 relative to DMSO. D VCaP cells were subjected to triplicate RNA-seq analysis upon 6 days of treatment with DMSO, PROTAC-6286, PROTAC-6272, and EPZ-6438. Heatmap shows combined differentially expressed genes identified ( | Log2FC | ≥0.585, adjusted p < 0.05) from treatment of PROTAC-6286, EPZ-6438, or PROTAC-6272 relative to DMSO.
Article Snippet: For the Incucyte assay, cells were seeded in 96-well plates and allowed to stabilize for 24 h. Cells were then treated with 1 μM of DMSO, PROTAC-6272, and EPZ-6438 and incubated in the Incucyte live imaging chamber (Sartorius).
Techniques: Incubation, Software, RNA Sequencing