Author

L. van der Veen

2 papers indexed here

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Clinical trial Open access Oct 2026

The conformation-selective PI3Kδ inhibitor roginolisib in patients with advanced or metastatic cancer, including metastatic uveal melanoma: first-in-human clinical trial

Phosphatidylinositol 3-kinase delta (PI3Kδ) promotes tumour cell growth directly or indirectly by activating immune-suppressive cells. In contrast to previous PI3Kδ inhibitors, roginolisib is a selective, non-ATP competitive inhibitor, which locks PI3Kδ into an inactive state and causes an allosteric modulation. In a F...

A. D. Di Giacomo, M. Simonelli, A. Losurdo et al. · Nature Communications · 2 citations

Open access Oct 2026

PI3Kδ is selectively inhibited by roginolisib by stabilizing the C-terminal helix kα12

Phosphoinositide 3-kinases (PI3Ks) are major regulators of cell growth, proliferation and signalling, constituting key therapeutic targets in cancer, inflammation, and other diseases. Individual class I PI3K isoforms control key cellular functions, imposing the need to generate isoform-specific inhibition for therapeut...

O. Vadas, S. Tiede, Maria Chaouki et al. · Nature Communications · 1 citation