-
Article
Open AccessProteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies
Proteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that utilize the ubiquitin proteasome system (UPS) to degrade proteins of interest (POI). PROTACs are potentially superior to con...
-
Article
Open AccessDT2216—a Bcl-xL-specific degrader is highly active against Bcl-xL-dependent T cell lymphomas
Patients with advanced T cell lymphomas (TCLs) have limited therapeutic options and poor outcomes in part because their TCLs evade apoptosis through upregulation of anti-apoptotic Bcl-2 proteins. Subsets of TC...
-
Article
PROteolysis TArgeting Chimeras (PROTACs) as emerging anticancer therapeutics
Using PROteolysis TArgeting Chimeras (PROTACs) to degrade proteins that are important for tumorigenesis has emerged as a potential therapeutic strategy for cancer. PROTACs are heterobifunctional molecules cons...
-
Article
Open AccessUsing proteolysis-targeting chimera technology to reduce navitoclax platelet toxicity and improve its senolytic activity
Small molecules that selectively kill senescent cells (SCs), termed senolytics, have the potential to prevent and treat various age-related diseases and extend healthspan. The use of Bcl-xl inhibitors as senol...
-
Chapter
Senolytic Drug Development
Cellular senescence is a hallmark of aging because senescent cells (SnCs) accumulate with age and play a causative role in many age-related diseases. Selectively eliminating SnCs has been emerging as a new str...
-
Article
A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity
B-cell lymphoma extra large (BCL-XL) is a well-validated cancer target. However, the on-target and dose-limiting thrombocytopenia limits the use of BCL-XL inhibitors, such as ABT263, as safe and effective antican...
