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BRD2 – MZ1 (PROTAC) – VCB (VHL) E3 Ligase protocol

A proteolysis targeting chimera (PROTAC) is a heterobifunctional small molecule composed of two active domains and a linker, capable of removing specific unwanted proteins. Rather than acting as a conventional enzyme inhibitor, a PROTAC works by inducing selective intracellular proteolysis. PROTACs consist of two covalently linked protein-binding molecules: one capable of engaging an E3 ubiquitin ligase, and another one that binds to a target protein meant for degradation. The von Hippel-Lindau E3 Ligase (VHL) and the elongin BC proteins form together the functional VCB complex which is able to use the PROTAC MZ1 to bind to the bromodomain of BRD2.

The two attached documents investigate this interaction via labeling of BRD2 (MOX-P-101) and VCB (MOX-P-102), respectively.

protein – small molecule | PROTACs | ternary complex | Hook effect | MOX-P-101 | MOX-P-102

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