Università della Svizzera italiana

Multi-targeting bioactive compounds extracted from essential oils as kinase inhibitors

Maruca, Annalisa ; Lanzillotta, Delia ; Rocca, Roberta ; Lupia, Antonio ; Costa, Giosuè ; Catalano, Raffaella ; Moraca, Federica ; Gaudio, Eugenio ; Ortuso, Francesco ; Artese, Anna ; Trapasso, Francesco ; Alcaro, Stefano

In: Molecules, 2020, vol. 25, no. 9, p. 14 p

Essential oils (EOs) are popular in aromatherapy, a branch of alternative medicine that claims their curative effects. Moreover, several studies reported EOs as potential anti- cancer agents by inducing apoptosis in different cancer cell models. In this study, we have considered EOs as a potential resource of new kinase inhibitors with a polypharmacological profile. On the other hand,...

Università della Svizzera italiana

The novel TORC1/2 kinase inhibitor PQR620 has anti-tumor activity in lymphomas as a single agent and in combination with venetoclax

Tarantelli, Chiara ; Gaudio, Eugenio ; Hillmann, Petra ; Spriano, Filippo ; Sartori, Giulio ; Aresu, Luca ; Cascione, Luciano ; Rageot, Denise ; Kwee, Ivo ; Beaufils, Florent ; Zucca, Emanuele ; Stathis, Anastasios ; Wymann, Matthias P. ; Cmiljanovic, Vladimir ; Fabbro, Doriano ; Bertoni, Francesco

In: Cancers, 2019, vol. 11, no. 6, p. 775

The phosphatidylinositol 3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) signaling cascade is an important therapeutic target for lymphomas. Rapamycin-derivates as allosteric mTOR complex 1 (TORC1) inhibitors have shown moderate preclinical and clinical anti-lymphoma activity. Here, we assessed the anti-tumor activity of PQR620, a novel brain penetrant dual TORC1/2 inhibitor, in 56...