- Ana B. García
- Cristina Ana Gómez
- Esther González
- Sonsoles Rodríguez
- Carmen Varela
- Lucía De Andrés
- Francisco Javier García
The Medicinal Chemistry Section is part of the interdisciplinary Experimental Therapeutics Programme dedicated to early Drug Discovery. Our activities consist of the design and synthesis of potential drugs with a therapeutic use in the field of cancer. Other activities integrated in our Section include the synthesis of high-quality chemical probes – potent, selective and cell-permeable compounds that are essential for target validation activities and the early stages of the drug discovery process. Additionally, we help CNIO’s basic research groups to decipher the mechanism of action that mediates an observed phenotype in cancer cells after screening for small organic molecules. Identifying the molecular target is essential to increase our knowledge about cancer and is a great aid to start drug discovery activities. To do this, we synthesise affinity chemical probes that enable cellular localisation of the target through imaging techniques and target identification through pull-down experiments coupled with proteomics.
- (2020). Screening protocol for the identification of modulators by immunofluorescent cell-based assay. Chem Biol Drug Des 95, 66-78. CNIO Publication.
- (2020). Induction of Lysosome Membrane Permeabilization as a Therapeutic Strategy to Target Pancreatic Cancer Stem Cells. Cancers (in press). CNIO Publication. Open Access
- (2019). The targetable kinase PIM1 drives ALK inhibitor resistance in high-risk neuroblastoma independent of MYCN status.. Nat Commun 10, 5428. CNIO Publication. Open Access
- (2016). PI3K inhibition reduces obesity in mice.. Aging (Albany NY) 8, 2747-2753. CNIO Publication.
- (2016). ETP-46321, a dual p110a/d class IA phosphoinositide 3-kinase inhibitor modulates T lymphocyte activation and collagen-induced arthritis. Biochem Pharmacol 106, 56-59. CNIO Publication.
- (2015). Pharmacological inhibition of PI3K reduces adiposity and metabolic syndrome in obese mice and rhesus monkeys.. Cell Metab 21, 558-570. CNIO Publication.
- (2015). Therapeutic inhibition of TRF1 impairs the growth of p53-deficient K-RasG12V-induced lung cancer by induction of telomeric DNA damage. EMBO Mol Med 7, 930-949. CNIO Publication. Open Access
- (2015). RAB7 counteracts PI3K-driven macropinocytosis activated at early stages of melanoma development. Oncotarget 6, 11848-11862. CNIO Publication. Open Access