Gianfranco Caselli

CURRICULUM VITAE

Dr. Caselli holds a degree in Chemistry and Pharmaceutical Technology (1981) at the University of Milan (UniMI). He completed his post-doctoral training in Pharmacognosy at the Institute of Pharmacology, School of Pharmacy UNIMI . He has specialized in Toxicology at UniMI (1986) .

 

After leaving the University he directed the Nutritional Biochemistry Laboratory of Pierrel S.p.A. (Milan, 1983-1985). In 1985 he moved to Dompé S.p.A. initially directing the Laboratory of Biochemistry (Milan) and then assuming the responsibility of the Pharmacology Laboratories in the new headquarters of L’Aquila (1993-1998) and, subsequently, the management of the Section of Pharmacology and Toxicology always at the laboratories of L’Aquila (1999 -2001). Since 2001 he has been working in Rottapharm S.p.A., Monza, first as Head of Toxicology and then as Director of the Department of Pharmacology and Toxicology (2004-2014). Since 2014 he has directed the Pharmacology and Toxicology of Rottapharm Biotech S.r.l.

RESEARCH INTERESTS

Specific areas of expertise are:

  • Pharmacology: new drugs (small molecules or biologicals) for the therapy of rheumatological diseases and for pain therapy; drugs active on the gastrointestinal system by interacting with cholecystokinin (CCK) receptors; drugs active in the therapy of viral pathologies (hepatitis C, HIV); drugs active on the central nervous system (Parkinson’s disease, schizophrenia); drugs active on the respiratory system (asthma, COPD); study of natural active ingredients. Active drugs in tumors (colorectal carcinoma, glioblastoma).
  • Toxicology: early toxicological and regulatory development of new drugs (synthetic, biological or vaccines) up to the first administration in humans (mutagenesis, safety pharmacology and subacute toxicity); chronic toxicology and reproductive function, carcinogenesis.

RESEARCH SUMMARY

Our main activity in neuroscience is focused on preclinical research of new experimental drugs (NCE) with pain relieving action in inflammatory, neuropathic and postoperative pain models. In particular, our current biological target is the type 2 imidazoline receptor (I2R). I2 receptors are proteins not yet well characterized from a molecular point of view that were initially mistakenly associated with the alpha-adrenergic receptor family before reconsidering their role as modulators of a selective population of MAO enzymes. Furthermore, recent research suggests that compounds of this class, capable of efficiently crossing the cerebroematic barrier, are also able to directly control the descending pathway of pain and block the development of tolerance and dependence on opiates.
Still in the field of neuroscience, Rottapharm research is active in the study of new molecules active on degenerative diseases of the central nervous system (Alzheimer, Parkinson and Huntington).
In recent years, we have paid a lot of attention to new kinase inhibitors capable of inhibiting the growth and invasiveness of the most widespread and most serious primary brain tumor, glioblastoma. For this tumor, in fact, adequate therapy is not yet available that can significantly improve the evolution of the disease.

PUBLICATIONS

  1. M Paolino, A Reale, V Razzano, G Giuliani, A Donati, G Giorgi, C Bonechi, G Caselli, M Visintin, F Makovec, C Scialabba, M Licciardi, E Paccagnini, M Gentile, L Salvini,  F Tavanti, MC Menziani, A Cappelli  NANOREACTORS FOR THE MULTI-FUNCTIONALIZATION OF POLYHISTIDINE FRAGMENTS  New J Chem 43:6834 (2019)
  2. M Paolino, M Visintin, E Margotti, M Visentini, L Salvini, A Reale, V Razzano, G Giuliani, G Caselli, F Tavanti, MC Menziani, A Cappelli. FUNCTIONALIZATION OF PROTEIN HEXAHISTIDINE TAGS BY FUNCTIONAL NANOREACTORS. New J Chem 43: 17946 (2019)
  3. V Vellani, C Sabatini, C Milia, G Caselli, M Lanza, O Letari, LC Rovati, C Giacomoni.  CR4056, A POWERFUL ANALGESIC IMIDAZOLINE-2 RECEPTOR LIGAND, INHIBITS THE INFLAMMATION-INDUCED PKCε PHOSPHORYLATION AND MEMBRANE TRANSLOCATION IN SENSORY NEURONS. Br J Pharmacol 177:48–64 (2020)
  4. E Sala, F Ferrari, M Lanza, C Milia, C Sabatini, A Bonazzi1, E Comi, M Borsi Franchini, G Caselli, LC Rovati. IMPROVED EFFICACY, TOLERANCE, SAFETY AND ABUSE LIABILITY PROFILE OF THE COMBINATION CR4056-MORPHINE OVER MORPHINE ALONE IN RODENT MODELS Br J Pharmacol 2020 Jul; 177(14):3291-3308 
  5. C Galimberti, T Piepoli, O Letari, R Artusi, S Persiani, G Caselli, LC Rovati. CR13626: A NOVEL ORAL BRAIN PENETRANT TYROSINE KINASE INHIBITOR THAT REDUCES TUMOR GROWTH AND PROLONGS SURVIVAL IN A MOUSE MODEL OF GLIOBLASTOMA. Am J Canc Res 2021 in press