Tag: PROTAC

MZP-54 is a Selective BRD3/4 PROTAC Degrader

PROTACs are bivalent chemical protein degraders. In particular, PROTACs degrade a specific endogenous protein of interest (POI) by harnessing the E3 ubiquitin ligase pathway. Especially, PROTACs is a powerful small-molecule approach for inducing protein degradation. Moreover, PROTACs conjugate a target warhead to an E3 ubiquitin ligase ligand via a...

VZ185 is a Selective Dual BRD7/9 PROTAC Degrader

Targeted protein degradation is an emerging strategy to use small molecules to knock down a protein by hijacking the ubiquitin-proteasome system. PROTACs are bifunctional degrader molecules. They compose a ligand for the target protein and a ligand for E3 ligase recruitment, connected by a linker. An attractive feature of...

UNC6852 is a Selective Rolycomb Repressive Complex 2 (PRC2) PROTAC Degrader

Polycomb repressive complex 2 (PRC2) is a multicomponent complex with histone methyltransferase (HMT) activity. H3K27 trimethylation (H3K27me3) is a key mechanism responsible for gene repression. In this study, researchers report the discovery of an EED-targeted bivalent chemical degrader. Researchers show that UNC6852 potently binds EED in vitro, degrades EED...

BI-3663 is a Highly Selective PTK2/FAK PROTAC

Focal adhesion tyrosine kinase (PTK2) is a cytoplasmic protein tyrosine kinase. PTK2 plays an important role in adhesion, spreading, motility, invasion, metastasis, survival, angiogenesis, epithelial to mesenchymal transition, cancer stem cells, and the tumor microenvironment. Overexpression and activation of PTK2 connect with several human malignant diseases, including colorectal, ovarian,...

BETd-260 is a Potent PROTAC BET Degrader

The bromodomain and extra-terminal (BET) family proteins consist of BRD2, BRD3, BRD4, and testis-specific BRDT members. They are epigenetic “readers” and play a key role in the regulation of gene transcription. BET proteins are attractive therapeutic targets for cancer and other human diseases. In this study, BETd-260 is capable...

ZXH-3-26 is a Selective PROTAC BRD4 Degrader

Targeting protein degradation refers to small molecule induces ubiquitination and degradation of disease targets. These small molecules simultaneously recruit both a ubiquitin E3 ligase and the target protein, then to be ubiquitinated. Therefore, PROTACs represent a functional application of chemically induced protein dimerization. BRD4 acts as an attractive target...

dTRIM24 is a Selective PROTAC Degrader of TRIM24

TRIM24 is a multidomain protein characterized as a co-regulator of transcription. Especially, dTRIM24 acts as a chemical probe of an emerging cancer dependency. Recruitment of the VHL E3 ubiquitin ligase by dTRIM24 elicits potent and selective degradation of TRIM24. TRIM24 has been posited as a dependency in numerous cancers,...