On July 31, 2020, Arribas, Raquel L.; Bordas, Anna; Domenech Omella, Judit; Cedillo, Jose Luis; Janssens, Veerle; Montiel, Carmen; de los Rios, Cristobal published an article.Formula: C12H16O7 The title of the article was An okadaic acid fragment analogue prevents nicotine-induced resistance to cisplatin by recovering PP2A activity in non-small cell lung cancer cells. And the article contained the following:
We herein report the design, synthesis, and functional impact of an okadaic acid (OA) small analog, ITH12680, which restores the activity of phosphoprotein phosphatase 2A (PP2A), whose deficient activity has been implicated in nicotine-mediated tumor progression and chemoresistance in non-small cell lung cancer (NSCLC). For its design, we paid attention to the structure of the PP2A-OA complex, where the C16-C38 OA fragment confers PP2A affinity and selectivity, but it is not involved in the inhibitory effect. Confirming this hypothesis, PP2A activity was not inhibited by ITH12680. By contrast, the compound partially restored OA-exerted PP2A inhibition in vitro. Moreover, flow cytometry and immunoblotting experiments revealed that ITH12680 reversed nicotine-induced cisplatin resistance in NSCLC cells, as it prevented nicotine-induced reduction of Bax expression and inhibited nicotine-mediated activation of cell survival and proliferation kinases, Akt and ERK1/2. Our findings suggest that the rescue of nicotine-inhibited PP2A activity could diminish the resistance to cisplatin treatment observed in NSCLC patients who continue smoking. The experimental process involved the reaction of (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate(cas: 2873-29-2).Formula: C12H16O7
The Article related to drug design nsclc pp2a chemoresistance cisplatin okadaic acid, chemoresistance, cisplatin, computer-aided drug design, non-small cell lung cancer, okadaic acid, phosphoprotein phosphatase 2a and other aspects.Formula: C12H16O7
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