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A Novel Approach in Glioblastoma Multiforme Drug Discovery: Perturbation Studies in vitro

Luís Carlos Oliveira, Maria Paula Marques, Armando José Caseiro, Simona Rapposelli Rapposelli, Ana Lúcia Batista-de-Carvalho, Ana Paula Fonseca.

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Despite impressive advances in drug discovery methods, predicting cellular response to anticancer drugs remains challenging. In glioblastoma multiforme, this fact is even marked as many promising drugs were followed by disappointment. As a result, the aim of this study is to clarify the effects of inhibition of PDK1 in glioblastoma multiforme, while exploring how the focus on potency might ignore the potential impact of variation in other pharmacological parameters. The evaluation of the induced drug perturbation in glioblastoma cancer cells and a multiparametric characterization dose-response of two PDK1 inhibitors were performed. Singular analysis of potency would lead to the conclusion that FC100 compound would be the most promising to treat glioblastoma multiforme. However, exploring other pharmacological parameters shows the opposite giving more information about the cell response. In conclusion, the study shows that potency should not be the critical factor in developing new drugs as our most potent compound lack of growth inhibition effect. So, the evaluation of promising drugs during the drug discovery phase need to be re-evaluated and multiparametric dose-response analysis might be a useful approach to compare drugs and potentially better characterization of both drug and disease profiles.

Key words: Drug discovery & development, quantitative & systems pharmacology, perturbation studies, multiparametric dose-response analyses, glioblastoma multiforme, PDK1 inhibitors.

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