AUTAC2 is a FKBP12-Targeting Autophagy-Mediated Degrader (AUTAC)
Autophagy-targeting chimera (AUTAC) is a technology that selectively degrades intracellular proteins and intracellular debris through the autophagy pathway. An AUTAC molecule contains a degradation tag (guanine derivative) and a ligand of the protein of interest (POI) to provide target specificity. AUTAC can selectively recognize and degrades a broad range...
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...
RapaLink-1, a Third-Generation Bivalent mTOR Inhibitor, Combines Rapamycin with MLN0128
Glioblastoma (GBM), the most common primary brain tumor, represents one of the most aggressive cancers. The signaling from PI3K and AKT to mTOR is commonly dysregulated in GBM. But, blockade of these upstream targets minimally affects mTOR activity in glioma. Allosteric mTOR inhibitors, such as rapamycin, incompletely block mTORC1...