The Medicinal Chemistry (MedChem) Section is part of the multidisciplinary Experimental Therapeutics Programme (ETP) focused on early drug discovery activities. ETP is integrated into the CNIO’s structure, and acts as a bridge between basic research groups in cancer biology and the pharmaceutical industry, with the aim of transferring the results obtained in basic research laboratories to products, potential drugs that help to understand the biology of cancer, or the development of new therapies. The Section deals with the design, synthesis, and optimisation of compounds, classical inhibitors, and degraders such as PROTACs, which are then characterised by ETP´s Biology Section, in order to evaluate their potency in biological targets in vitro and in vivo and ultimately to demonstrate their efficacy and mechanisms of action in animal models (in vivo proof-of-concept). The Section is also involved in the synthesis of high-quality chemical tools that help to decipher the mechanism of action of an observed phenotype in cellular assays, as well as in the synthesis of reference compounds that assist basic researchers in their investigations.
- Ana B. García
- Cristina Ana Gómez
- Esther González
- Sonsoles Rodríguez
- Terry Pascal Tomakinian
- Carmen Varela
- (2021). Omipalisib inspired macrocycles as dual PI3K/mTOR inhibitors.. Eur J Med Chem 211, 113109. Publicación CNIO.
- (2021). Macrocyclization as a source of desired polypharmacology. Discovery of triple PI3K/mTOR/PIM inhibitors.. ACS Med Chem Lett 12, 1794-1801. Publicación CNIO.
- (2020). Global hyperactivation of enhancers stabilizes human and mouse naive pluripotency through inhibition of CDK8/19 Mediator kinases. Nat Cell Biol 22, 1223-1238. Publicación CNIO.
- (2020). Anti?tumor effects of PIM/PI3K/mTOR triple kinase inhibitor IBL?302 in neuroblastoma. EMBO Mol Med 12, e11749. Publicación CNIO.
- (2020). Preclinical evaluation of a novel triple-acting PIM/PI3K/mTOR inhibitor, IBL-302, in breast cancer.. Oncogene 39, 3028-3040. Publicación CNIO.
- (2020). Induction of Lysosome Membrane Permeabilization as a Therapeutic Strategy to Target Pancreatic Cancer Stem Cells. Cancers 12, 1790. Publicación CNIO. Open Access
- (2020). Screening protocol for the identification of modulators by immunofluorescent cell-based assay. Chem Biol Drug Des 95, 66-78. Publicación CNIO.
- (2019). The targetable kinase PIM1 drives ALK inhibitor resistance in high-risk neuroblastoma independent of MYCN status.. Nat Commun 10, 5428. Publicación CNIO. Open Access
- (2019). Multiple cancer pathways regulate telomere protection.. EMBO Mol Med 11, e10292. Publicación CNIO. Open Access
- (2019). Anti-tumor effects of PIM/PI3K/mTOR triple kinase inhibitor IBL-302 in neuroblastoma.. EMBO Mol Med 11, e10058. Publicación CNIO. Open Access
- (2019). Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors. Eur J Med Chem 168, 87-109. Publicación CNIO.