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
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
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
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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