Journal: Journal of Medicinal Chemistry

Article Title: First-in-Class Inhibitors of the Ribosomal Oxygenase MINA53

doi: 10.1021/acs.jmedchem.1c00605

Figure Lengend Snippet: Proapoptotic effects of 9 and 10 in combination with doxorubicin on U-87MG cells. (A) Representative images of flow cytometric analysis of cell cycle distribution and the Sub-G1 peak by PI staining, in U-87MG cells untreated or treated with the negative control 1 , 9 , or 10 (10 μM), alone or in combination with doxorubicin (Doxo, 0.5 μM) for 24 h. Each panel is representative of three independent experiments with comparable results. Percentage of cells in different phases of the cell cycle (B) and at Sub-G1 peak (C) in U-87MG untreated or treated with the negative control 1 , 9 , or 10 (10 μM), alone or in combination with doxorubicin (Doxo, 0.5 μM) for 24 h. The statistical analysis compares MINA53 inhibitors vs DMSO control (# p < 0.05, t -test), and MINA53 inhibitor single treatment vs MINA53 inhibitors in combination with Doxo (* p < 0.05, t -test).

Article Snippet: Cell pellets from a 1 L scale were resuspended in 50 mL of buffer containing 50 mM 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES) (pH 8.0), 500 mM NaCl, 10 mM imidazole, 0.5 mM tris(2-carboxyethyl)phosphine (TCEP), and 5% (v/v) aqueous glycerol, supplemented with 1 μL of benzonase nuclease (Sigma-Aldrich) and 50 μL of protease inhibitors cocktail III (Merck).

Techniques: Staining, Negative Control