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Epigenetic Med Chem Lab
University of Salerno - Dept. of Pharmacy, via Giovanni Paolo II 132 84084 Fisciano (SA)

epigenetic writers, epigenetic erasers, epigenetic readers; chemical biology, biophysics



microwave assisted synthesis; flow-chemistry; ALPHAscreen; Surface Plasmon Resonance; thermal shift (Differential Scanning Fluorimetry); microscale thermophoresis; isothermal titration calorimetry; microfluidic mobility shift assay

Collaborations outside COST

EMCL collaborates with biologists on fundamental functional chromatin biology and on various other pathophysiological pathways (diabetes, synaptic plasticity, wound healing; Duchenne cardiomyopathy), with medical doctors (oncology, parasitology, neuropsychiatry, cardiology) and pharmacologists for animal models, with microbiologists (phenotypic studies), with biochemists (MS proteomics), with molecular biologists (ligand-protein complex structure) and biophysicists (studies of binding interactions): Mark T. Bedford - University of Texas, M.D. Anderson Cancer Center, TX, USA Vidya Gopalakrishnan - University of Texas, M.D. Anderson Cancer Center, TX, USA Wei Xu – University of Wisconsin Madison, McArdle Laboratory for Cancer Research, WI, USA Ronen Marmorstein - University of Pennsylvania, Department of Biochemistry and Biophysics, PA, USA Garland R. Marshall - Washington University, Biochemistry & Molecular Biophysics, MO, USA Li Gan - University of California, San Francisco (UCSF), Gladstone Institute of Neurological Diseases, CA, USA Georges Mer - Mayo Clinic, MN, USA Boyer Winters - Guelph University, Ontario, Canada Jose L. Medina-Franco - Universidad Nacional Autónoma de México, Department of Pharmacy, Mexico Minoru Yoshida - Chemical Genomics Research Group, RIKEN, Wako, Japan Haitao Li - Tsinghua University, School of Medicine, P.R.China Timothy Bredy - Queensland Brain Institute, The University of Queensland, Australia Ryszard Maleszka - Australian National University, College of Medicine, Biology and Environment, Canberra, Australia Danny Rangasamy - Australian National University, Epigenetics and Genome Stability lab, John Curtin School of Medical Research, Canberra, Australia Gerald Brosch – Biocenter-Innsbruck Medical University, Austria Oliver Kappe – University of Graz, Austria Frank Lyko – Division of Epigenetics, German Cancer Research Center, Heidelberg, Germany Rolf W. Hartmann – Saarland University, Saarbruecken, Germany. Axel Imhof - Adolf-Butenandt Institute Ludwig-Maximilians-Universität, Munich, Germany Carlo Gaetano - Goethe-Universität Frankfurt am Main, Germany Albert Jeltsch - Universität Stuttgart, Germany Pier Vincenzo Piazza – Fluofarma, Pessac, France. Jean Cavarelli - IGBMC - CNRS UMR 7104 - Inserm U 964, Strasbourg, France. Federico Da Settimo – Università di Pisa, Italy Giampiero Spalluto – Università di Trieste, Italy Stefano Moro – Università di Padova, Italy Corrado Spadafora- Institute of Translational Pharmacology, CNR, Roma, Italy Dr. Patrizia Lavia – Istitute of Molecular Biology and Pathology – CNR, Roma, Italy Patrizia Filetici – Sapienza Università di Roma, Italy

Short description of ongoing research projects

Development of small-molecule chemical probes for KATs, PRMTs, KMTs, KDMs, DNMTs, acetyl lysine readers (bromodomain), methyl lysine readers (Tudor, Chromo, MBT)

  1. Ciro Milite, Alessandra Feoli, Kazuki Sasaki, Valeria La Pietra, Amodio Luca Balzano, Luciana Marinelli, Antonello Mai, Ettore Novellino, Sabrina Castellano, Alessandra Tosco, Gianluca Sbardella (2015) A Novel Cell-Permeable, Selective, and Noncompetitive Inhibitor of KAT3 Histone Acetyltransferases from a Combined Molecular Pruning/Classical Isosterism Approach. J Med Chem 58: 6. 2779-2798.
  2. Matteo Vecellio, Francesco Spallotta, Simona Nanni, Claudia Colussi, Chiara Cencioni, Anja Derlet, Beatrice Bassetti, Manuela Tilenni, Maria Cristina Carena, Antonella Farsetti, Gianluca Sbardella, Sabrina Castellano, Antonello Mai, Fabio Martelli, Giulio Pompilio, Maurizio C Capogrossi, Alessandra Rossini, Stefanie Dimmeler, Andreas Zeiher, Carlo Gaetano (2014) The histone acetylase activator pentadecylidenemalonate 1b rescues proliferation and differentiation in the human cardiac mesenchymal cells of type 2 diabetic patients. Diabetes 63: 6. 2132-2147
  3. Hao Zeng, Jiacai Wu, Mark T Bedford, Gianluca Sbardella, F Michael Hoffmann, Kun Bi, Wei Xu (2013) A TR-FRET-based functional assay for screening activators of CARM1. ChemBioChem 14: 7. 827-835
  4. Sabrina Castellano, Astrid Spannhoff, Ciro Milite, Fabrizio Dal Piaz, Donghang Cheng, Alessandra Tosco, Monica Viviano, Abdellah Yamani, Agostino Cianciulli, Marina Sala, Vincent Cura, Jean Cavarelli, Ettore Novellino, Antonello Mai, Mark T Bedford, Gianluca Sbardella (2012) Identification of small-molecule enhancers of arginine methylation catalyzed by coactivator-associated arginine methyltransferase 1. J Med Chem 55: 22. 9875-9890 Nov.
  5. Sabrina Castellano, Dirk Kuck, Monica Viviano, Jakyung Yoo, Fabian López-Vallejo, Paola Conti, Lucia Tamborini, Andrea Pinto, José L Medina-Franco, Gianluca Sbardella (2011) Synthesis and biochemical evaluation of δ(2)-isoxazoline derivatives as DNA methyltransferase 1 inhibitors. J Med Chem 54: 21. 7663-7677 Nov.
Other activities of potential interest to others

Member of the Board of the European School of Medicinal Chemistry (ESMEC)

Cost UE