Medicinal Chemistry (MedChem) is a scientific discipline concerned with the design and synthesis of bioactive molecules to address unmet medical needs or to improve existing drugs. The discipline combines expertise in organic chemistry with knowledge of ligand-receptor interactions and pharmacology to design and modify the structure and properties of molecules, to improve potency and drug-like properties.
The Medicinal Chemistry Section is part of the multidisciplinary Experimental Therapeutics Programme (ETP), which focuses on early drug discovery activities. The ETP is integrated into the CNIO’s structure, and acts as a bridge between basic research groups in cancer biology, which identify innovative targets that play a relevant role in cancer, and the pharmaceutical industry. Our goal is to generate molecules against these cancer targets and to demonstrate their efficacy and mechanism of action in animal models (in vivo proof of concept). This allows us to translate the results obtained in basic research laboratories into potential drugs that contribute to the understanding of cancer biology, as well as to increase the interest of the pharmaceutical industry to develop new therapies.
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.
Open Access