Tag: PROTAC

CCT36776 is a PROTAC-based Pirin Protein Degradation Probe

Proteolysis targeting chimeras (PROTACs) are heterobifunctional molecules. It induces rapid and selective protein degradation, via the proteasome. PROTACs contain two different ligands connected by a linker, one portion of the molecule engages the target protein. While the other, attach via a flexible linker, recruits an E3 ubiquitin ligase to...

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...

MS432 is a Highly Selective PROTAC Degrader for MEK1 and MEK2

Chemical induced protein knockdown via the proteolysis targeting chimera (PROTAC) technology is a promising approach to target dysregulated proteins. Moreover, MEK1/2 proteins are the only RAF substrates. MEK1/2 proteins are the crucial “gatekeepers” of ERK activity. The classic RAS-RAF-MEK-ERK signaling pathway is common in mammals, plays critical roles in...

MG-277, a PROTAC Molecular Glue, Exhibits Anti-cancer Activity by Inhibiting GSPT1

Proteolysis targeting chimeras (PROTACs) induce protein degradation. A typical PROTAC small-molecule degrader consists of three essential components: a ligand that binds the protein of interest, a second ligand that binds to and recruits an E3 ligase degradation complex, and a linker tethering the two ligands together. MD-222, a bona...

SI-109, a STAT3 Transcription Inhibitor, is the Ligand of PROTAC Degrader SD-36

As we have written in the article “SD-36 is a Selective PROTAC STAT3 Degrader”, proteolysis targeting chimera (PROTAC) technology has been a type of therapeutics that induces targeted protein degradation. Signal transducer and activator of transcription 3 (STAT3) is an attractive cancer therapeutic target. Longchuan Bai, et al have...

SD-36 is a Selective PROTAC STAT3 Degrader

Proteolysis targeting chimera (PROTAC) technology has been a type of therapeutics that induces targeted protein degradation. Signal transducer and activator of transcription 3 (STAT3) is an attractive cancer therapeutic target. In this study, Longchuan Bai, et al developed a potent and specific PROTAC degrader of STAT3 and evaluate its...

CP5V is a Specific PROTAC Degrader of Cdc20

The cell-division cycle protein 20 (Cdc20) is the substrate receptor of anaphase synthesis complex (APC) or cyclosome (APC/C). Besides, it coordinates late initiation and exit of mitosis through safety and time-dependent degradation. Cdc20 is a key mitotic factor, which controls the beginning of anaphase and the exit of mitosis....