Category: PROTAC

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,...

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...

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,...

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,...