Golcadomide is an Orally Active CRBN E3 Ligase Modulator (CELMoD)
Protein degradation agents based on the ubiquitin-proteasome pathway include a part of molecular glues. A molecular glue is a small molecule that stabilizes the interaction between two proteins that do not normally interact. If one of the proteins is ubiquitin ligase, molecular glue can cause another protein to undergo...
MS170 is a PROTAC AKT Degrader
The alternative name of serine/threonine kinase AKT is protein kinase B (PKB). Three closely related genes in humans: AKT1 (PKB-α), AKT2 (PKB-β), and AKT3 (PKB-γ) encode PKB. AKT is an important component of the PI3K/AKT/mammalian target of rapamycin (m-TOR) signaling pathway. It also regulates fundamental cellular and physiological processes,...
Iberdomide (CC-220) is an Orally Active Cereblon (CRBN) E3 Ligase Modulator (CELMoD)
Cereblon (CRBN) is a key protein in autosomal recessive nonsyndromic mental retardation. Specifically, it plays an intermediary role in helping immunomodulatory drugs play their immunomodulatory and tumor-killing roles. Besides, CRBN is highly conserved from plants to mammals, and mRNA expression in humans, rats, and mice is common. CRBN interacts...
SJ6986 is a Selective and Orally Active GSPT1/2 Degrader
Targeted protein degradation (TPD) is a novel chemical biology approach. Molecular glues (MGs) are small molecules that can bind to E3 ligase and change their surface and specificity, leading to the recruitment, ubiquitination, and subsequent degradation of substrates that are normally not targeted by the ligase (neosubstrates). Immunomodulatory imide...
Lenalidomide, a Ligand of CRBN, is an Orally Active Immunomodulator
Immunomodulatory imide drugs (IMiDs) are a class of immunomodulatory drugs containing an imide group. The discovery of anti-angiogenic and anti-inflammatory properties promoted the development of Thalidomide analogs. These compounds bind Cereblon (CRBN), the substrate adaptor for the CRBN-CRL4 E3 ubiquitin ligase, and modulate the substrate specificity of the enzyme....
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...