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...

Université de Fribourg

Cell-Permeant and photocleavable chemical inducer of dimerization

Zimmermann, Mirjam ; Cal, Ruben ; Janett, Elia ; Hoffmann, Viktor ; Bochet, Christian G. ; Constable, Edwin ; Beaufils, Florent ; Wymann, Matthias P.

In: Angewandte Chemie International Edition, 2014, vol. 53, no. 18, p. 4717–4720

Chemical inducers of dimerization (CIDs) have been developed to orchestrate protein dimerization and translocation. Here we present a novel photocleavable HaloTag- and SNAP-tag-reactive CID (MeNV-HaXS) with excellent selectivity and intracellular reactivity. Excitation at 360 nm cleaves the methyl-6-nitroveratryl core of MeNV-HaXS. MeNV-HaXS covalently links HaloTag- and SNAP-tag fusion...