Vijayaratnam Santhakumar

Nov 23, 2024 | nature.com | Serah Kimani |Laurent Hoffer |Stuart Green |Dalia Barsyte-Lovejoy |Vijayaratnam Santhakumar |Suzanne Ackloo | +5 more

AbstractProteolysis-targeting chimeras (PROTACs) have been explored for the degradation of drug targets for more than two decades. However, only a handful of E3 ligase substrate receptors have been efficiently used. Downregulation and mutation of these receptors would reduce the effectiveness of such PROTACs. We recently developed potent ligands for DCAF1, a substrate receptor of EDVP and CUL4 E3 ligases.

Sep 25, 2023 | nature.com | Stuart Green |Vijayaratnam Santhakumar

AbstractE3 ubiquitin ligases are critical to the protein degradation pathway by catalyzing the final step in protein ubiquitination by mediating ubiquitin transfer from E2 enzymes to target proteins. Nedd4 is a HECT domain-containing E3 ubiquitin ligase with a wide range of protein targets, the dysregulation of which has been implicated in myriad pathologies, including cancer and Parkinson's disease.