Tag: PROTAC

XZ739 is a PROTAC BCL-XL Degrader

PROTAC is an emerging therapeutic modality. PROTAC is a feasible solution to reduce platelet toxicity associated with BCL-XL inhibition. BCL-XL plays a key role in tumorigenesis and cancer chemotherapy resistance. As a result, BCL-XL is an attractive target for cancer treatment. Specifically, XZ739 is a CRBN-dependent BCL-XL degrader. XZ739,...

ARCC-4 is a Highly Potent PROTAC Androgen Receptor Degrader

Androgen receptor (AR) signaling is crucial for normal prostate development. It also drives the growth and survival of prostate cancer cells. AR signaling suppression is a common strategy for treating prostate cancer. Like other occupancy-based inhibitors, the antiandrogen enzalutamide requires high saturating drug concentrations to achieve its clinical benefit....

TL13-12 is a Selective ALK-PROTAC Degrader

Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase. ALK is an attractive target for cancer therapies not only for its prominent role in a number of malignancies but also for its scant expression in normal adult tissue. Therapeutic strategies that target ALK may provide ways to further delay...

TL13-112 is a PROTAC Degrader of ALK

Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase and its mutation in domains. ALK Chromosomal translocations involve the kinase domain of ALK in many cancers. In addition to ALCL, ALK fusion proteins are seen in diffuse large B-cell lymphoma (DLBCL), inflammatory myofibroblastic tumor (IMT), breast cancer, colorectal cancer,...

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...