info@epichembio.eu + 34 986 812 316

Mai's Group

dante.rotili@uniroma1.it
dctf.uniroma1.it/dipartimento/persone/docenti/ricercatori/rotili-dante
Address
University of Rome “La Sapienza”, Aldo Moro Square n5, 00185 Rome
Italy
Keywords

Epigenetics, Medicinal Chemistry, Chemical Biology, Chemoproteomics Probes, Cancer

Models

Solid-phase and solution-phase parallel organic synthesis, flow chemistry, microwave-assisted synthesis, “click” chemistry.

Techniques

NMR, IR, UV and MS spectroscopy, flash chromatography and HPLC purifications.

Collaborations outside COST

Prof. Clemens Steegborn, University of Bayreuth (Germany) Prof. Benedikt Kessler, University of Oxford (UK) Prof. Aleksey G. Kazantsev, University of Harvard (USA) Prof. Xiaodong Cheng, Emory University, (Atlanta, USA)

Short description of ongoing research projects

Dr. Rotili is involved in the design, synthesis and biological validation of chemical probes for different epigenetic targets (histone deacetylase/acetyltransferase, demethylase/methyltransferase, DNA methyltransferase, PARP, reader domains of different histone modifications) involved in cancer, neurological and inflammatory diseases.

Publications
  1. 1) Rotili D, Tomassi S, Conte M, Benedetti R, Tortorici M, Ciossani G, Valente S, Marrocco B, Labella D, Novellino E, Mattevi A, Altucci L, Tumber A, Yapp C, King ON, Hopkinson RJ, Kawamura A, Schofield CJ, Mai A. Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities. J Med Chem. 2014 Jan 9;57(1):42-55. doi: 10.1021/jm4012802.
  2. 2) Rotili D, Tarantino D, Marrocco B, Gros C, Masson V, Poughon V, Ausseil F, Chang Y, Labella D, Cosconati S, Di Maro S, Novellino E, Schnekenburger M, Grandjenette C, Bouvy C, Diederich M, Cheng X, Arimondo PB, Mai A. Properly substituted analogues of BIX-01294 lose inhibition of G9a histone methyltransferase and gain selective anti-DNA methyltransferase 3A activity. PLoS One. 2014 May 8;9(5):e96941. doi: 10.1371/journal.pone.0096941. eCollection 2014.
  3. 3) Rotili D, Tarantino D, Nebbioso A, Paolini C, Huidobro C, Lara E, Mellini P, Lenoci A, Pezzi R, Botta G, Lahtela-Kakkonen M, Poso A, Steinkühler C, Gallinari P, De Maria R, Fraga M, Esteller M, Altucci L, Mai A. Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. J Med Chem. 2012 Dec 27;55(24):10937-47. doi: 10.1021/jm3011614.
  4. 4) Rotili D, Tarantino D, Carafa V, Paolini C, Schemies J, Jung M, Botta G, Di Maro S, Novellino E, Steinkühler C, De Maria R, Gallinari P, Altucci L, Mai A. Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells. J Med Chem. 2012 Sep 27;55(18):8193-7.
  5. 5) Rotili D, Altun M, Kawamura A, Wolf A, Fischer R, Leung IK, Mackeen MM, Tian YM, Ratcliffe PJ, Mai A, Kessler BM, Schofield CJ. A photoreactive small-molecule probe for 2-oxoglutarate oxygenases. Chem Biol. 2011 May 27;18(5):642-54. doi: 10.1016/j.chembiol.2011.03.007.
Other activities of potential interest to others

Dr. Rotili is also involved in the design, synthesis and biological validation of inhibitors of glutatione-S-transferase (GST) and of HIV-1 Non Nucleoside Reverse Transcriptase.


Cost UE