AT1 is a cell penetrant Proteolysis Targeting Chimera (PROTAC) that selectively targets BET4 proteins for degradation by recruitments of ubiquitin E3 ligase. AT1 comprise (+)-JQ1 as a BET4 binding domain and E3 ligase specific VHL (von Hippel-Lindau) ligand connected through a linker.
PROTAC containing (+)-JQ1 that selectively binds to BRD4
Protein degraders, also known as proteolysis targeting chimeras (PROTACs), are bifunctional small molecules that promote cellular degradation of a protein of interest (POI). PROTACs act as molecular mediators, bringing an E3 ligase and a POI into proximity, thus promoting ubiquitination
Enhancers are DNA sequences that enable complex temporal and tissue-specific regulation of genes in higher eukaryotes. Although it is not entirely clear how enhancer-promoter interactions can increase gene expression, this proximity has been observed in multiple systems at multiple loci
Nature chemical biology, 13(5), 514-521 (2017-03-14)
Inducing macromolecular interactions with small molecules to activate cellular signaling is a challenging goal. PROTACs (proteolysis-targeting chimeras) are bifunctional molecules that recruit a target protein in proximity to an E3 ubiquitin ligase to trigger protein degradation. Structural elucidation of the
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