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...
dFKBP-1 is a Potent and PROTAC-based FKBP12 Degrader
The FK506-binding protein 12 (FKBP12) is a ubiquitous abundant protein that acts as a receptor for the immunosuppressant drug FK506l FK506 binds tightly to intracellular calcium release channels and to the TGF-β type I receptor. dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. FKBP12 inhibits the basal signaling of...
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,...
GNE-987, a BET PROTAC Degrader, is a Part of PROTAC-Antibody (CLL1) Conjugate for ADC
BRD4 is a member of the BET family of proteins (BRD2, 3, 4, and T). It functions as an epigenetic “reader” of acetylated histone lysine residues via its two bromodomain motifs (BD1 and BD2). Disruption of BRD4-histone interactions is an attractive strategy for the development of novel anti-cancer agents....
SIAIS178 is a Potent and Selective PROTAC-Based BCR-ABL Degrader
Proteolysis targeting chimeras (PROTACs) work by inducing selective intracellular proteolysis rather than acting as a conventional enzyme inhibitor. Besides, PROTACs consists of two covalently linked protein-binding molecules. One can engage an E3 ubiquitin ligase, and another binds to a target protein meant for degradation. Moreover, PROTACs need only to...
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...