Here we explore peptide inhibitors of Cdc20, a substrate-recognition subunit and activator of the E3 ubiquitin ligase the anaphase promoting complex/cyclosome (APC/C) that is essential in mitosis and ...
The clinical success in hematological malignancies of bortezomib has bolstered interest in the development of a new generation of proteasome inhibitors, varying in their mode of action through ...
There are also ubiquitin-like proteins such as NEDD8, ISG15 or SUMO that act as homologous pathways for ubiquitination. Bortezomib was the first-in-class proteasome inhibitor and is currently ...
CG001419 is a highly active small molecule designed to selectively degrade both mutant and wild-type TRK proteins and is being developed to be a new, non-opioid, non-NSAID analgesic therapy as part of ...
Enzyme kinetics and hydrogen–deuterium eXchange mass spectrometry indicated that the inhibitor binds tightly to regions surrounding the USP30 catalytic cysteine and positions itself to form a binding ...
These results suggest that, in the recruitment of K63 and K27 ubiquitin chains to PDE9A, CHIP triggers its sequential ubiquitination and subsequent degradation via the autophagy–lysosomal pathway.
Deshaies was studying how E3 ubiquitin ligase enzymes can label proteins to be dispatched ... Wertz, Chen and colleagues discovered that peptides formed when the proteasome chopped up BET were killing ...