The description of the crystal structure of the Brd4 PROTAC compound MZ1 in complex with the human E3 ubiquitin ligase VHL and the Brd4 bromodomain shines new light onto how PROTACs work and ...

NanoBRET can also be performed in permeabilized cells to examine the impact of PROTAC permeability. In live cells, the MZ1 PROTAC shows right-shifted IC 50 compared to precursor VH298 (Figure 3B).

PROTAC cooperative recognition for selective protein degradation Date: March 13, 2017 ... BRD4, which is an attractive drug target for cancer, with a selective BRD4 `degrader' called MZ1.

Overcome Roadblocks to PROTAC Characterization. How To Guide . Last Updated: September 4, 2023 (+ more) Published: August 4, 2023 Credit: Nanotemper. Proteolysis-targeting chimeras (PROTACs) are ...

NEW HAVEN, Conn., June 21, 2024 (GLOBE NEWSWIRE) -- Arvinas, Inc. (Nasdaq: ARVN), a clinical-stage biotechnology company creating a new class of drugs based on targeted protein degradation, today ...

Once PROTAC binds to its target protein and the ubiquitin ligase, the ligase will attach ubiquitin groups to the surface of the target protein, which tags it for degradation by the proteasome inside ...

This guide highlights how an innovative, plate-based, and automation-ready affinity screening solution helps you overcome roadblocks in your PROTAC characterization projects.