Our group conducts targeted early drug discovery projects to identify and develop small molecules as potential therapeutics against oncogenic targets. After target validation, the starting point of these projects is a screening campaign using scalable and robust assays that reflect target interaction and biological relevance; these can be either biochemical or cellular assays. Biochemical assays are simpler, with fast turnarounds but lack context. Conversely, cellular assays are more physiologically relevant, more complex to interpret, and have a slower turnaround. In a project flowchart, typically we run a biochemical HTS screen followed by validation in a target-dependent cellular assay. However, this sometimes fails to identify potential hits, at which point we move to a more complex cellular assay that measures the target activity in cells. In the latter case, the identification of a hit then requires a target deconvolution task to determine whether its mechanism of action is direct, or through modulation of another pathway.
Research Scientists
- Pablo Aparicio
- Marta San Martín
Technicians
- Antonio Cebriá
- Claudia Díaz
- Elena Gómez-Casero
Recent publications
- (2023). Endoglin, a Novel Biomarker and Therapeutical Target to Prevent Malignant Peripheral Nerve Sheath Tumor Growth and Metastasis. Clin Cancer Res 29, 3744-3758. CNIO Publication.
- (2022). mTORC2 Is the Major Second Layer Kinase Negatively Regulating FOXO3 Activity. Molecules 27, 5414. CNIO Publication.
Open Access - (2021). Omipalisib inspired macrocycles as dual PI3K/mTOR inhibitors.. Eur J Med Chem 211, 113109. CNIO Publication.
- (2021). Screening health-promoting compounds for their capacity to induce the activity of FOXO3. J Gerontol A-Biol (in press). CNIO Publication.
- (2021). Co-Targeting PIM Kinase and PI3K/mTOR in NSCLC.. Cancers 13, 2139. CNIO Publication.
- (2021). Macrocyclization as a source of desired polypharmacology. Discovery of triple PI3K/mTOR/PIM inhibitors.. ACS Med Chem Lett 12, 1794-1801. CNIO Publication.