Gloaguen, Celine; Voisin-Chiret, Anne Sophie; Sopkova-de Oliveira Santos, Jana; Fogha, Jade; Gautier, Fabien; De Giorgi, Marcella; Burzicki, Gregory; Perato, Serge; Petigny-Lechartier, Cecile; Simonin-Le Jeune, Karin; Brotin, Emilie; Goux, Didier; N’Diaye, Monique; Lambert, Bernard; Louis, Marie-Helene; Ligat, Laetitia; Lopez, Frederic; Juin, Philippe; Bureau, Ronan; Rault, Sylvain; Poulain, Laurent published the artcile< First Evidence That Oligopyridines, α-Helix Foldamers, Inhibit Mcl-1 and Sensitize Ovarian Carcinoma Cells to Bcl-xL-Targeting Strategies>, Related Products of 112-63-0, the main research area is oligopyridine preparation Mcl1 ovary cancer sensitization BclxL siRNA.
Apoptosis control defects such as the deregulation of Bcl-2 family member expression are frequently involved in chemoresistance. In ovarian carcinoma, we previously demonstrated that Bcl-xL and Mcl-1 cooperate to protect cancer cells against apoptosis and their concomitant inhibition leads to massive apoptosis even in the absence of chemotherapy. Whereas Bcl-xL inhibitors are now available, Mcl-1 inhibition, required to sensitize cells to Bcl-xL-targeting strategies, remains problematic. In this context, we designed and synthesized oligopyridines potentially targeting the Mcl-1 hydrophobic pocket, evaluated their capacity to inhibit Mcl-1 in live cells, and implemented a functional screening assay to evaluate their ability to sensitize ovarian carcinoma cells to Bcl-xL-targeting strategies. We established structure-activity relationships and focused our attention on MR29072, named Pyridoclax. Surface plasmon resonance assay demonstrated that pyridoclax directly binds to Mcl-1. Without cytotoxic activity when administered as a single agent, pyridoclax induced apoptosis in combination with Bcl-xL-targeting siRNA or with ABT-737 in ovarian, lung, and mesothelioma cancer cells.
Journal of Medicinal Chemistry published new progress about Antitumor agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Related Products of 112-63-0.
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