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MODULATORI SMALL-MOLECULE DELL'ATTIVITÀ  BIOLOGICA DI P53: NUOVI TOOL PER LA CHIMICA FARMACEUTICA MITOCONDRIALE

Lo scopo di questo progetto è la modulazione della via apoptotica intrinseca attraverso la regolazione dell'attività di p53.1) C. Colussi, J. Rosati, S. Straino, F. Spallotta, R. Berni, D. Stilli, S. Rossi, E. Musso, E. Macchi, A. Mai, G. SBARDELLA, S. CASTELLANO, C. Chimenti, A. Frustaci, A. Nebbioso, L. Altucci, M.C. Capogrossi, C. GaetanoNε-lysine acetylation determines dissociation from GAP junctions and lateralization of connexin 43 in normal and dystrophic heartProc Natl Acad Sci U S A. 2011, 108, 2795–2800. (IF 9,737; PS 1,000; TOT 9,737)2) G. SBARDELLA*, A. Mai, S. Bartolini, S. CASTELLANO, R. Cirilli, D. Rotili, C. Milite, M. Santoriello, S. Orlando, I. Sciamanna, A. Serafino, P. Lavia, and C. SpadaforaModulation of Cell Differentiation, Proliferation and Tumor Growth by Dihydrobenzyloxopyrimidine Non Nucleoside Reverse Transcriptase InhibitorsJ. Med. Chem. 2011, 54, 5927–5936. (IF 5,614; PS 1,500; TOT 8,421)3) S. CASTELLANO, D. Kuck, M. Viviano, J. Yoo, F. López-Vallejo, P. Conti, L. Tamborini, A. Pinto, J.L. Medina-Franco, and G. SBARDELLA*Synthesis and Biochemical Evaluation of delta2-Isoxazoline Derivatives as DNA Methyltransferase 1 InhibitorsJ. Med. Chem. 2011, 54, 7663–7677. (IF 5,614;PS 1,500; TOT 8,421)4) S. CASTELLANO, S. Taliani, C. Milite, I. Pugliesi, E. Da Pozzo, E. Rizzetto, S. Bendinelli, B. Costa, S. Cosconati, G. Greco, E. Novellino, G. SBARDELLA, G. Stefancich, C. Martini, and F. Da SettimoSynthesis and Biological Evaluation of 4-Phenylquinazoline-2-carboxamides Designed as a Novel Class of Potent Ligands of the Translocator Protein J. Med. Chem. 2012, 55, 4506–4510. (IF 5,614;PS 1,500; TOT 8,421)5) S. CASTELLANO, A. Spannhoff, C. Milite, F. Dal Piaz, D. Cheng, A. Tosco, M. Viviano, A. Yamani, A. Cianciulli, M. Sala, V. Cura, J. Cavarelli, E. Novellino, A. Mai, M.T. Bedford, and G. SBARDELLA*Identification of Small-Molecule Enhancers of Arginine Methylation Catalyzed by Coactivator-Associated Arginine Methyltransferase 1J. Med. Chem. 2012, 55, 9875–9890. (IF 5,614;PS 1,500; TOT 8,421)6) A. Spannhoff, Y.K. Kim, N.J-M Raynal, V. Gharibyan, M.-B. Su, Y.-Y. Zhou, J. Li, S. CASTELLANO, G. SBARDELLA, J.-P.J. Issa, M.T. BedfordHistone deacetylase inhibitor activity in royal jelly might facilitate caste switching in beesEMBO rep. 2011, 12, 238–243. (IF 7,189; PS 1,000; TOT 7,189)7) W. Wei, C. Coelho, X. Li, R. Marek, S. Yan, S. Anderson, D. Meyers, C. Mukherjee, J. Hopkins, G. SBARDELLA, S. CASTELLANO, C. Milite, D. Rotili, A. Mai, P. Cole, P. Sah, T. Bredyp300/CBP-Associated Factor Selectively Regulates the Extinction of Conditioned FearJournal of Neuroscience 2012, 35, 11930–11941. (IF 6,908; PS 1,000; TOT 6,908)8) S. CASTELLANO, L. Tamborini, M. Viviano, A. Pinto, G. SBARDELLA, and P. ContiSynthesis of 3-Aryl/benzyl-4,5,6,6a-tetrahydro-3aHpyrrolo[3,4-d ]isoxazole Derivatives: A Comparison between Conventional, Microwave-Assisted and Flow-Based MethodologiesJ. Org. Chem. 2010, 57, 7439–7442. (IF 4,564; PS 1,500; TOT 6,846)9) C. Colussi, A. Scopece, S. Vitale, F. Spallotta, S. Mattiussi, J.D. Rosati, B. Illi, A. Mai, S. CASTELLANO, G. SBARDELLA, A. Farsetti, M.C. Capogrossi, and C. GaetanoP300/CBP Associated Factor Regulates Nitroglycerin-dependent Arterial Relaxation by N-Lysine Acetylation of Contractile ProteinsArterioscler. Thromb. Vasc. Biol. 2012, 32, 2435–2443. (IF 6,338; PS 1,000; TOT 6,338)10) I. Gomez-Monterrey, P. CAMPIGLIA, C. Aquino, A. BERTAMINO, I. Granata, A. Carotenuto, D. Brancaccio, P. Stiuso, I. Scognamiglio, M.R. Rusciano, A.S. Maione, M. Illario, P. Grieco, B. Maresca, and E. NovellinoDesign, Synthesis, and Cytotoxic Evaluation of Acyl Derivatives of 3-Aminonaphtho[2,3-b]thiophene-4,9-dione, a Quinone-Based SystemJ. Med. Chem., 2011, 54 (12), 4077–4091. (IF 5,614; PS 1,000; TOT 5,614)