The Medicinal Chemistry 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 that are then characterised in the Biology Section of ETP, in order to evaluate their potency in biological targets in vitro and in vivo and ultimately to demonstrate their efficacy and mechanism of action in animal models (in vivo proof-of-concept). As a complementary strategy to the classic inhibitors, we also contemplate the degradation of particular targets using different chemical approaches such as the use of PROTACs. Additionally, we have entered the field of Chemical Biology in order to discover and identify novel drugs and targets from phenotypic screenings. In this regard, we contribute by synthesising high quality chemical tools needed for interrogating the observed phenotype.
Publications
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Álvarez RM, García AB, Riesco-Fagundo C, Martín JI, Varela C, Rodríguez Hergueta A, González Cantalapiedra E, Oyarzabal J, Di Geronimo B, Lorenzo M, Albarrán MI, Cebriá A, Cebrián D, Martínez-González S, Blanco-Aparicio C, Pastor J (2021).Omipalisib inspired macrocycles as dual PI3K/mTOR inhibitors.. Eur J Med Chem 211, 113109. CNIO Publication.
Martínez-González S, Alvarez RM, Martín JI, García AB, Riesco-Fagundo C, Varela C, Rodríguez Hergueta A, González Cantalapiedra E, Albarrán MI, Gómez-Casero E, Cebriá A, Aguirre A, Ajenjo N, Cebrián D, Geronimo B, Cunningham D, O'Neill M, Dave HPG, Blanco-Aparicio C, Pastor J (2021).Macrocyclization as a source of desired polypharmacology. Discovery of triple PI3K/mTOR/PIM inhibitors.. ACS Med Chem Lett 12, 1794-1801. CNIO Publication.
Lynch CJ, Bernad R, Martínez-Val A, Shahbazi MN, Nóbrega-Pereira S, Calvo I, Blanco-Aparicio C, Tarantino C, Garreta E, Richart-Ginés L, Alcazar N, Graña-Castro O, Gómez-Lopez G, Aksoy I, Muñoz-Martín M, Martinez S, Ortega S, Prieto S, Simboeck E, Camasses A, Stephan-Otto Attolini C, Fernandez AF, Sierra MI, Fraga MF, Pastor J, Fisher D, Montserrat N, Savatier P, Muñoz J, Zernicka-Goetz M, Serrano M (2020).Global hyperactivation of enhancers stabilizes human and mouse naive pluripotency through inhibition of CDK8/19 Mediator kinases. Nat Cell Biol 22, 1223-1238. CNIO Publication.
Martínez-González S, Rodríguez-Arístegui S, Gómez de la Oliva CA, Hernández AI, González Cantalapiedra E, Varela C, García AB, Rabal O, Oyarzabal J, Bischoff JR, Klett J, Albarrán MI, Cebriá A, Ajenjo N, García-Serelde B, Gómez-Casero E, Cuadrado-Urbano M, Cebrián D, Blanco-Aparicio C, Pastor J (2019).Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors. Eur J Med Chem 168, 87-109. CNIO Publication.
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