Pierfrancesco Orlando


PhD Student


HCI G-322




Pierfrancesco Orlando



Study of Chemistry and Pharmaceutical Technology at the Urbino University (Italy).


Master Thesis with Prof. G. Zappia (Urbino University, Italy).


Medicinal Chemistry fellowship with Prof. G. Tarzia (Urbino University, Italy).

since 11.2007:

Ph.D. in Medicinal Chemistry with Prof. G. Spadoni (Urbino University, Italy).


Structure-Based Design and Synthesis of tRNA-Guanine Transglycosylase (TGT) Inhibitors

The goal of this research is the synthesis of drug-like inhibitors of Z. mobilis tRNA-guanine transglycosylase (TGT). A structural closely related TGT is found in Shigella bacteria, which causes bacillary dysentery or shigellosis - a disease affecting more than 160 million people and claiming 1.1 million deaths per year. It has been shown that the virulence of Shigella is closely linked to TGT. Although, TGT enzymes are present in bacteria and humans, different substrate specificity makes the selective inhibition of the bacterial enzyme possible. Hence, TGT represents an attractive target for the treatment of shigellosis.


M. Formica, V. Fusi, E. Macedi, P. Paoli, G. Piersanti, P. Rossi, G. Zappia, P. Orlando, New J. Chem. 2008, 32, 1204-1214. New branched macrocyclic ligand and its side-arm, two urea-based receptors for anions: synthesis, binding studies and crystal structure.

S. Rivara, F. Vacondio, A. Fioni, C. Silva, C. Carmi, M. Mor, V. Lucini, M. Pannacci, A. Caronno, F. Scaglione, G. Gobbi, G. Spadoni, A. Bedini, P. Orlando, S. Lucarini, G. Tarzia, ChemMedChem 2009, 4,1746-1755. Design and Synthesis of Metabolically Stable, Selective Melatonin Receptor Ligands.

Last update: July 2010