- Ana B. García
- Cristina Ana Gómez
- Esther González
- Sonsoles Rodríguez
- Carmen Varela
The Medicinal Chemistry Section is part of the interdisciplinary Experimental Therapeutics Programme that is dedicated to early Drug Discovery in the oncology field. Our aim is to discover new anticancer agents based on the hypotheses and targets generated by CNIO’s Basic Research Groups; this is done in close collaboration with these Groups. Medicinal Chemistry activities start with the identification of hits through High Throughput Screening (HTS) campaigns from targeted or phenotypic assay or hits generated in our Section by applying Rational Drug Design Strategies; these are then optimised to obtain novel lead compounds with in vivo activity in different animal models. For hits obtained from phenotypic screenings, we help to decipher the mechanism of action responsible for the observed phenotype, synthesising affinity probes that will be used for cellular localisation (imaging techniques) and extracting the target/s (pull down experiments). We are also developing PROTACs (proteolysis targeting chimeras) as promoters of cell protein degradation to establish their applicability across diverse drug discovery projects.
- (2016). PI3K inhibition reduces obesity in mice.. Aging (Albany NY) 8, 2747-2753.
- (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.
- (2015). Pharmacological inhibition of PI3K reduces adiposity and metabolic syndrome in obese mice and rhesus monkeys.. Cell Metab 21, 558-570.
- (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.
- (2015). RAB7 counteracts PI3K-driven macropinocytosis activated at early stages of melanoma development.. Oncotarget 6, 11848-11862.
- (2014). Non-genotoxic activation of p53 through the RPL11-dependent ribosomal stress pathway.. Carcinogenesis 35, 2822-2830.
- (2013). Biological characterization of ETP-46321 a selective and efficacious inhibitor of phosphoinositide-3-kinases.. Invest New Drug 31, 66-76.