Matthew P. Patricelli

Allosteric covalent inhibition of cereblon through cryptic cysteine targeting

The paper identifies covalent ligands targeting a cryptic cysteine in CRBN, demonstrating their ability to inhibit neosubstrate degradation by trapping CRBN in an inactive conformation.

Suppression of NRF2-dependent cancer growth by a covalent allosteric molecular glue

This paper introduces VVD-065, a covalent NRF2 inhibitor that enhances NRF2 degradation and sensitizes tumors to therapy, supporting a Phase I clinical trial.

Covalent inhibitors of the RAS binding domain of PI3Ka impair tumor growth driven by RAS and HER2

The paper develops covalent inhibitors targeting the RAS binding domain of PI3Kα, showing efficacy against RAS and HER2-driven tumors without affecting glucose homeostasis.