Tag: FKBP12

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...

KB02-SLF is a PROTAC-Based Nuclear FKBP12 Degrader (Molecular Glue)

Conventional small-molecule probes play their roles by perturbing the functions of proteins, including blocking enzyme catalysis or antagonizing receptor signaling. However, a compound only binds to only one of these domains that may can not fully inactivate the protein. There exist a novel strategy, chemical probes, which direct proteins...