4 documents found, page 1 of 1
Discovery of a Novel, Isothiazolonaphthoquinone-Based Small Molecule Activator ...
Cautain, Bastien; Castillo, Francisco; Musso, Loana; Ferreira, Bibiana; de Pedro, Nuria; Quesada, Lorena Rodriguez; Machado, Susana; Vicente, FranciscaFOXO factors are tumour suppressor proteins commonly inactivated in human tumours by posttranslational modifications. Furthermore, genetic variation within the FOXO3a gene is consistently associated with human longevity. Therefore, the pharmacological activation of FOXO proteins is considered as an attractive therapeutic approach to treat cancer and age-related diseases. In order to identify agents capable of a...
Components and regulation of nuclear transport processes
Cautain, Bastien; Hill, Richard; de Pedro, Nuria; Link, WolfgangThe spatial separation of DNA replication and gene transcription in the nucleus and protein translation in the cytoplasm is a uniform principle of eukaryotic cells. This compartmentalization imposes a requirement for a transport network of macromolecules to shuttle these components in and out of the nucleus. This nucleo-cytoplasmic transport of macromolecules is critical for both cell physiology and pathology. ...
High-content screening of natural products reveals novel nuclear export inhibitors
Cautain, Bastien; de Pedro, Nuria; Garzon, Virginia Murillo; de Escalona, Maria Munoz; Menendez, Victor Gonzalez; Tormo, Jose R.; Martin, JesusNatural products are considered an extremely valuable source for the discovery of new drugs against diverse pathologies. As yet, we have only explored a fraction of the diversity of bioactive compounds, and opportunities for discovering new natural products leading to new drugs are huge. In the present study, U2nesRELOC, a previously established cell-based imaging assay, was employed to screen a collection of e...
Targeting nucleocytoplasmic transport in cancer therapy
Hill, Richard; Cautain, Bastien; de Pedro, Nuria; Link, WolfgangThe intracellular location and regulation of proteins within each cell is critically important and is typically deregulated in disease especially cancer. The clinical hypothesis for inhibiting the nucleo-cytoplasmic transport is based on the dependence of certain key proteins within malignant cells. This includes a host of well-characterized tumor suppressor and oncoproteins that require specific localization f...