Giuseppe Zagotto

 

Department of Pharmaceutical and Pharmacological Sciences, University of Padova
via F. Marzolo 5, 35131 Padova - Italy

Current Position
Associate Professor of Medicinal Chemistry (SSD: CHIM/08)

Contacts
Phone: +39-049-827-5686
Fax:  +39-049-827-5366
e-mail: giuseppe.zagotto@unipd.it

  Short CV

Giuseppe Zagotto received his degree in Padua in 1982. In the same year he started his first job at "FIS - Fabbrica Italiana Sintetici", a FDA-inspected and totally GMP-compliant pharmaceutical company where he worked for seven years reaching the research position of project leader. He then worked for one year in an Official Food Control Laboratory in Vicenza (Italy) mainly as food and drinkable water analyst. Since 1990 he is Professor, assistant and then associate (2000), of medicinal chemistry at the University of Padova. He spent one year in UK working with Prof. Michael North synthesizing conformationally constrained peptides. He is now teaching two medicinal chemistry courses and a course on advance analytical techniques of a pharmaceutical interest. He is member of the board in charge for the libraries of the University of Padova.

Teaching

  Office hours

Monday: 10:00 - 12:00
Thursday: 10:00 - 12:00

  Availability for Thesis Projects

Tesi sperimentali:

Synthesis and characterization of chemical probes for the investigation of non-canonical DNA and RNA structures

Extraction, synthesis and characterization of novel potential PDE5 inhibitors

Synthesis of novel non-immunosuppressive Fingolimod analogues as innovative anticancer agents

Synthesis and characterization of naphthoquinone derivatives as potential anticancer agents

Synthesis and biophysical studies of novel organochalcogen species

Research 

  Scientific Activities

The research activity of our group has always been connected with the design, the synthesis, the purification and the characterization of organic compounds. Currently our research interests are focused towards two main streams: anticancer and cardiovascular systems. For what concerns the first topic, we are pursuing multiple strategies to develop novel potential anticancer agents. Besides targeting some of the traditional proteins known to play a role in the development and progression of the disease, such as topoisomerase, telomerase and CK2, we recently started to investigate the field of new generation potential anticancer agents such as protein phospatase 2A (PP2A) activators. To better understand how some of the compounds exploit their action at a molecular level, we are also developing small molecules to be used as chemical probes for the investigation of non-canonical arrangements of nucleic acids and macromolecules in general. Besides anticancer, we are also interested in the search for novel phosphodiesterase (PDE) inhibitors that may have a number of potential application, from the treatment of erectile dysfunction to pulmonary hypertension. Concerning this topic, we design and develop the synthetic schemes with a particular eye to the world of the compounds of a natural origin

  Technical expertise

Design and synthesis of organic compounds; extraction of organic compounds from natural sources; characterization of organic compounds by advanced Nuclear Magnetic Resonance (NMR) spectroscopy such as homo- and heteronuclear 2D experiments; use of advanced mass spectrometry for the characterization of the compounds, for structural investigation and for biophysical studies; purification techniques such as preparative flash chromatography and preparative HPLC; purity assessment by HPLC-UV and HPLC-DAD.

  Publications

Sosic, A., Sinigaglia, L., Cappellini, M., Carli, I., Parolin, C., Zagotto, G., Sabatino, G., Rovero, P., Fabris, D., Gatto, B.
 Mechanisms of HIV-1 Nucleocapsid Protein Inhibition by Lysyl-Peptidyl-Anthraquinone Conjugates
(2016) Bioconjugate Chemistry, 27 (1), pp. 247-256. Impact factor (2014): 4.401

Cozza, G., Zanin, S., Sarno, S., Costa, E., Girardi, C., Ribaudo, G., Salvi, M., Zagotto, G., Ruzzene, M., Pinna, L.A.
Design, validation and efficacy of bisubstrate inhibitors specifically affecting ecto-CK2 kinase activity
(2015) Biochemical Journal, 471 (3), pp. 415-430. Impact factor (2014): 4.166

Ribaudo, G., Pagano, M.A., Pavan, V., Redaelli, M., Zorzan, M., Pezzani, R., Mucignat-Caretta, C., Vendrame, T., Bova, S., Zagotto, G.
Semi-synthetic derivatives of natural isoflavones from Maclura pomifera as a novel class of PDE-5A inhibitors
(2015) Fitoterapia, 105, art. no. 3215, pp. 132-138. Impact factor (2014): 2.611

Zonta, F., Pagano, M.A., Trentin, L., Tibaldi, E., Frezzato, F., Trimarco, V., Facco, M., Zagotto, G., Pavan, V., Ribaudo, G., Bordin, L., Semenzato, G., Brunati, A.M.
Lyn sustains oncogenic signaling in chronic lymphocytic leukemia by strengthening SET-mediated inhibition of PP2A
(2015) Blood, 125 (24), pp. 3747-3755. Impact factor (2014): 8.496

Redaelli, M., Mucignat-Caretta, C., Isse, A.A., Gennaro, A., Pezzani, R., Pasquale, R., Pavan, V., Crisma, M., Ribaudo, G., Zagotto, G.
New naphthoquinone derivatives against glioma cells
(2015) European Journal of Medicinal Chemistry, 96, pp. 458-466. Impact factor (2014): 3.781

  Patents

IT1213519, 1986-10-30, Creatinol phosphate prepn. 

IT1215357, 1987-02-17, Chloro-acetamido-methyl chloro-benzophenone synthesis 

US4900859, 1987-12-03, Process for 4-dimethylamino-3,5-dimethoxybenzaldehyde 

ES2353203, 2001-05-10, Aloe-emodin derivatives and their use in the treatment of neoplasias