The von Hippel-Lindau (VHL) Cullin RING E3 ligase is an essential enzyme in the ubiquitin-
proteasome system that recruits substrates such as the hypoxia inducible factor for …

Abstract PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules
consisting of two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to …

Bivalent proteolysis-targeting chimeras (PROTACs) drive protein degradation by
simultaneously binding a target protein and an E3 ligase and forming a productive ternary …

Constraining a molecule in its bioactive conformation via macrocyclization represents an
attractive strategy to rationally design functional chemical probes. While this approach has …

Clinical development of bromodomain and extra‐terminal (BET) protein inhibitors differs
from the traditional course of drug development. These drugs are simultaneously being …

The BET family of proteins consists of BRD2, BRD3, BRD4, and BRDt. Each protein contains
two distinct bromodomains (BD1 and BD2). BET family bromodomain inhibitors under …

Small-molecule-induced protein depletion technologies, also called inducible degrons,
allow degradation of genetically engineered target proteins within cells and animals. Here …

Blocking the interactions between bromodomain and extraterminal (BET) proteins and
acetylated lysines of histones by small molecules has important implications for the …

Epigenetic mechanisms for controlling gene expression through heritable modifications to
DNA, RNA, and proteins, are essential processes in maintaining cellular homeostasis. As a …

Epigenetic modulators perform critical functions in gene expression for rapid adaption to
external stimuli and are prevalent in all higher-order organisms. The establishment of a link …