Inicio | Investigación e innovación | Programas Científicos | Programa de Terapias Experimentales | Sección de Biología
Investigadores Científicos
- Pablo Aparicio
- Marta San Martín
Técnicos de Laboratorio
- Mª Isabel Albarrán
- Antonio Cebriá
- Claudia Díaz
- Elena Gómez-Casero
The Biology Section works in early drug discovery projects with the final aim of achieving in vivo proof of concept (PoC) with the lead molecules developed by the Programme. There is a long road before we can select the best or even the first candidate to perform PoC experiments in mice. These molecules have to be novel, potent at both the biochemical and cellular levels, selective, and with good ADME (absorption, distribution, metabolism, and excretion) properties to predict good plasma/tumour levels in mice.
Pharmacokinetic studies allow us to determine if the compounds have achieved plasma levels after intravenous, intraperitoneal, or oral administration, the oral being the preferred route. In vitro and cellular ADME studies help us to identify the liabilities behind the poor oral bioavailability of compounds (i.e., solubility, permeability/efflux or metabolic stability).
Publicaciones
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- González-Muñoz T, Di Giannatale A, García-Silva S, Santos V, Sánchez-Redondo S, Savini C, Graña-Castro O, Blanco-Aparicio C, Fischer S, De Wever O, Creus-Bachiller E, Ortega-Bertran S, Pisapia DJ, Rodríguez-Peralto JL, Fernández-Rodríguez J, Pérez-Portabella CR, Alaggio R, Benassi MS, Pazzaglia L, Scotlandi K, Ratner N, Yohay K, Theuer CP, Peinado H. (2023). Endoglin, a Novel Biomarker and Therapeutical Target to Prevent Malignant Peripheral Nerve Sheath Tumor Growth and Metastasis. Clin Cancer Res 29, 3744-3758. Publicación CNIO.
- Jimenez L, Amenabar C, Mayoral-Varo V, Mackenzie TA, Ramos MC, Silva A, Calissi G, Grenho I, Blanco-Aparicio C, Pastor J, Megías D, Ferreira BI, Link W (2022). mTORC2 Is the Major Second Layer Kinase Negatively Regulating FOXO3 Activity. Molecules 27, 5414. Publicación CNIO.
Open Access - 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. Publicación CNIO.
- Jimenez L, Silva A, Calissi G, Grenho I, Monteiro R, Mayoral-Varo V, Blanco-Aparicio C, Pastor J, Bustos V, Bracher F, Megías D, Ferreira BI, Link W (2021). Screening health-promoting compounds for their capacity to induce the activity of FOXO3. J Gerontol A-Biol (in press). Publicación CNIO.
- Moore G, Lightner C, Elbai S, Brady L, Nicholson S, Ryan R, O'Sullivan KE, O'Byrne KJ, Blanco-Aparicio C, Cuffe S, O'Neill M, Heavey S, Finn SP, Gately K (2021). Co-Targeting PIM Kinase and PI3K/mTOR in NSCLC.. Cancers 13, 2139. Publicación CNIO.
- 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. Publicación CNIO.
- 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. Publicación CNIO.
- Ferrara-Romeo I, Martinez P, Saraswati S, Whittemore K, Graña-Castro O, Thelma Poluha L, Serrano R, Hernandez-Encinas E, Blanco-Aparicio C, Maria Flores J, Blasco MA (2020). The mTOR pathway is necessary for survival of mice with short telomeres.. Nat Commun 11, 1168. Publicación CNIO. Open Access
- Mohlin S, Hansson K, Radke K, Martinez S, Blanco-Apiricio C, Garcia-Ruiz C, Welinder C, Esfandyari J, O'Neill M, Pastor J, von Stedingk K, Bexell D (2020). Anti?tumor effects of PIM/PI3K/mTOR triple kinase inhibitor IBL?302 in neuroblastoma. EMBO Mol Med 12, e11749. Publicación CNIO.
- Esteban-Burgos L, Wang H, Nieto P, Zheng J, Blanco-Aparicio C, Varela C, Gómez-López G, Fernández-García F, Sanclemente M, Guerra C, Drosten M, Galán J, Caleiras E, Martínez-Torrecuadrada J, Fajas L, Peng SB, Santamaría D, Musteanu M, Barbacid M (2020). Tumor regression and resistance mechanisms upon CDK4 and RAF1 inactivation in KRAS/P53 mutant lung adenocarcinomas. Proc Natl Acad Sci USA 117, 24415-24426. Publicación CNIO. Open Access
- Kennedy SP, O'Neill M, Cunningham D, Morris PG, Toomey S, Blanco-Aparicio C, Martinez S, Pastor J, Eustace AJ, Hennessy BT (2020). Preclinical evaluation of a novel triple-acting PIM/PI3K/mTOR inhibitor, IBL-302, in breast cancer.. Oncogene 39, 3028-3040. Publicación CNIO.
- Cash TP, Alcalá S, Rico-Ferreira MDR, Hernández-Encinas E, García J, Albarrán MI, Valle S, Muñoz J, Martínez-González S, Blanco-Aparicio C, Pastor J, Serrano M, Sainz B Jr (2020). Induction of Lysosome Membrane Permeabilization as a Therapeutic Strategy to Target Pancreatic Cancer Stem Cells. Cancers 12, 1790. Publicación CNIO. Open Access
- Martínez-González S, García AB, Albarrán MI, Cebriá A, Amezquita-Alves A, García-Campos FJ, Martínez-Gago J, Martínez-Torrecuadrada J, Muñoz IG, Blanco-Aparicio C, Pastor J (2020). Pyrido[2,3-b][1,5]benzoxazepin-5(6H)-one derivatives as CDK8 inhibitors.. Eur J Med Chem 201, 112443. Publicación CNIO.
- Klett J, Gómez-Casero E, Méndez-Pertuz M, Urbano-Cuadrado M, Megias D, Blasco MA, Martínez S, Pastor J, Blanco-Aparicio C (2020). Screening protocol for the identification of modulators by immunofluorescent cell-based assay. Chem Biol Drug Des 95, 66-78. Publicación CNIO.
- Trigg RM, Lee LC, Prokoph N, Jahangiri L, Reynolds CP, Amos Burke GA, Probst NA, Han M, Matthews JD, Kai Lim H, Manners E, Martinez S, Pastor J, Blanco-Aparicio C, Merkel O, de Los Fayos Alonso IG, Kodajova P, Tangermann S, Högler S, Luo J, Kenner L, Turner SD. (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
- Bejarano L, Bosso G, Louzame J, Serrano R, Gómez-Casero E, Martínez-Torrecuadrada J, Martínez S, Blanco-Aparicio C, Pastor J, Blasco MA (2019). Multiple cancer pathways regulate telomere protection.. EMBO Mol Med 11, e10292. Publicación CNIO. Open Access
- Mohlin S, Hansson K, Radke K, Martinez S, Blanco-Aparicio C, Garcia-Ruiz C, Welinder C, Esfandyari J, O'Neill M, Pastor J, von Stedingk K, Bexell D (2019). Anti-tumor effects of PIM/PI3K/mTOR triple kinase inhibitor IBL-302 in neuroblastoma.. EMBO Mol Med 11, e10058. Publicación CNIO. Open Access
- Llanos S, Megias D, Blanco-Aparicio C, Hernández-Encinas E, Rovira M, Pietrocola F, Serrano M (2019). Lysosomal trapping of palbociclib and its functional implications. Oncogene 38, 3886-3902. Publicación CNIO.
- 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. Publicación CNIO.
- Godoy CA, Klett J, Di Geronimo B, Hermoso JA, Guisán JM, Carrasco-López C (2019). Disulfide Engineered Lipase to Enhance the Catalytic Activity: A Structure-Based Approach on BTL2.. Int J Mol Sci 20, E5245. Publicación CNIO. Open Access
