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...
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....
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...
KB02-JQ1 is a Highly Potent and Selective PROTAC BRD4 Degrader
DDB1-CUL4-associated protein 16 (DCAF16) is a 216 aa protein that is highly conserved across mammals, but absent from rodents. The DCAF16 protein has eight cysteine residues, including a cluster of four cysteines between amino acids 173-179. Especially, DCAF16 is a substrate recognition component of CUL4-DDB1 E3 ubiquitin ligases. DCAF16...