Giuseppe La Regina

Associate Professor in Medicinal Chemistry, Dipartimento di Chimica e Tecnologie del Farmaco

giuseppe.laregina@uniroma1.it

Academic Appointments:

Since September 2019: Associate Professor in Medicinal Chemistry, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma.

November 2008 – September 2020: Assistant Professor in Medicinal Chemistry, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma.

April 2007 – November 2008: Design, synthesis and development of new inhibitors of tubulin polymerization as anticancer agents, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma (three-year grant financed by Associazione Italiana per la Ricerca sul Cancro, Milan, Italy).

April 2005 – March 2007: Post-Doc Position, Welsh School of Pharmacy, Cardiff University, United Kingdom, Molecular modelling studies to design new inhibitors of tubulin polymerization as anticancer agents (two-year grant financed by Institute Pasteur Italy – Cenci Bolognetti Foundation, Rome, Italy).

November 2001 – October 2004: PhD course in Medicinal Chemistry, Dipartimento di Studi Farmaceutici (Medicinal Chemistry Department), Sapienza Università di Roma, Design, synthesis and development of new non-nucleoside reverse transcriptase inhibitors of HIV-1 as anti-AIDS agents.

Honors and Awards:

  • 2018: Publons Peer Review Award 2017.
  • 2007: Farmindustria Prize for Pharmaceutical Research – Outstanding for researching activity.

Scientific interests:

Design, synthesis and development of anti-infective, anti-cancer and central nervous system active agents; microwave-assisted synthesis and fully automated chromatography purification of heterocyclic compounds.

Contribution to Science

Prof. Giuseppe La Regina is co-Author of more than 100 scientific papers published in impacted professional journals and 5 patents about design, synthesis and development of anti-infective (human immunodeficiency virus, rhinovirus, hepatitis C virus, dengue virus, coronavirus, norovirus, zika virus, Mycobacterium tuberculosis and Candida albicans), anti-cancer (tubulin and microtubules, Wnt/beta-catenin signalling, histone demethylases, matrix metalloproteinases, B-cell lymphoma-2, carbonic anhydrase, indoleamine 2,3-dioxygenase 1, murine double minute 2 and 4 proteins, Na+/H+ exchanger 3 regulating factor 1, growth factor receptor bound protein 2, lactate dehydrogenase, PDZ domains, apoptosis and ferroptosis) and central nervous system active (monoamine oxidases, endocannabinoid system, glycogen synthase kinase 3 beta) agents.

5 Selected publications

  • Puxeddu, M.; Ling, L.; Ripa, S.; D’Ambrosio, M.; Nalli, M.; Parisi, A.; Sciò, P.; Coluccia, A.; Granese, A.; Santelli, M.; Masci, D.; Cuřínová, P.; Naro; C.; Sette, C.; Pastore, A.; Stornaiuolo, M.; Bigogno, C.; Dondio, G.; Di Magno, L.; Canettieri, G.; Liu, T.; Silvestri, R.; La Regina, G. Development of N-(4-(1H-Imidazol-1-yl)phenyl)-4-chlorobenzenesulfonamide, a Novel Potent Inhibitor of β-Catenin with Enhanced Antitumor Activity and Metabolic Stability. J. Med. Chem. 2024, 67, 20298‒20314.
  • Masci, D.; Puxeddu, M.; Di Magno, L.; D’Ambrosio, M.; Parisi, A.; Nalli, M.; Bai, R.; Coluccia, A.; Sciò, P.; Orlando, V.; D’Angelo, S.; Biagioni, S.; Urbani, A.; Hamel, E.; Nocentini, A.; Filiberti, S.; Turati, M.; Ronca, R.; Kopecka, J.; Riganti, C.; Fionda, C.; Bordone, R.; Della Rocca, G.; Canettieri; G.; Supuran, C. T.; Silvestri, R.; La Regina, G. 4-(3-Phenyl-4-(3,4,5-trimethoxybenzoyl)-1H-pyrrol-1-yl)benzenesulfonamide, a Novel Carbonic Anhydrase and Wnt/β-Catenin Signaling Pathway Dual-Targeting Inhibitor with Potent Activity against Multidrug Resistant Cancer Cells. J. Med. Chem. 2023, 66, 14824‒14842.
  • Sebastiani, S.; Puxeddu, M.; Nalli, M.; Bai, R.; Altieri, L.; Rovella P.; Gaudio, E.; Trisciuoglio, D.; Spriano, F.; Lavia, P.; Fionda, C.; Masci, D.; Urbani, A.; Bigogno, C.; Dondio, G.; Hamel, E.; Bertoni, F.; Silvestri, R.; La Regina, G. RS6077 induces mitotic arrest and selectively activates cell death in human cancer cell lines and in a lymphoma tumor in vivo. Eur. J. Med. Chem. 2023, 246, e114997.
  • Puxeddu, M.; Wu, J.; Bai, R.; D’Ambrosio, M.; Nalli, M.; Coluccia, A.; Manetto, S.; Ciogli, A.; Masci, D.; Urbani, A.; Fionda, C.; Coni, S.; Bordone R.; Canettieri, G.; Bigogno, C.; Dondio, G.; Hamel, E.; Liu, T.; Silvestri, R.; La Regina, G. Induction of Ferroptosis in Glioblastoma and Ovarian Cancers by a New Pyrrole Tubulin Assembly Inhibitor. J. Med. Chem. 2022, 65, 15805‒15818.
  • Puxeddu M.; Shen, H.; Bai, R.; Coluccia, A.; Bufano, M.; Nalli, M.; Sebastiani, J.; Brancaccio, D.; Da Pozzo, E.; Tremolanti, C.; Martini, C.; Orlando, V.; Biagioni, S.; Sinicropi, M. S.; Ceramella, J.; Iacopetta, D.; Coluccia, A. M. L.; Hamel, E.; Liu, T.; Silvestri, R.; La Regina, G. (corresponding Author). Discovery of pyrrole derivatives for the treatment of glioblastoma and chronic myeloid leukemia. Eur. J. Med. Chem. 2021, 221, e113532.

On-going Grants

Project Title Funding source Amount (Euros) Period Role of the PI
Targeting Wnt/beta-catenin pathway: identification and development of selective allosteric modulators of Dishevelled and Frizzled proteins as a promising approach to cancer therapy (INdWNT) - 2022TPPNTK Call PRIN 2022, Ministero dell’Università e della Ricerca 203.748 2023-2026 PI (20% of time)
Tubulin inhibitors as ferroptosis inducers in cancer treatment - RG123188B4D193AE Call Research Projects 2023, Sapienza Università di Roma 60.840 2023-2026 PI (20% of time)

Complete list of published work in MyBibliography:

https://pubmed.ncbi.nlm.nih.gov/?term=La+Regina+G&sort=date

 KEYWORDS:

Anti-cancer agents, anti-infective agents, central nervous system active agents, drug discovery, heterocyclic compounds.

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