Abexinostat is an Orally Available Pan-HDAC Inhibitor
HDAC (Histone deacetylases) are a class of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone. To date, There are 18 human HDACs. Besides, HDACs include four classes on the basis of their homology with yeast proteins. Class I HDACs (HDAC1, 2, 3, and...
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...
Tirabrutinib is a Selective BTK Inhibitor
The BTK kinases comprise 5 structural domains, including pleckstrin homology, TEC homology, Src homology, Src homology, and kinase domains. The activation of BTK kinase depends on recruitment to the plasma membrane via the pleckstrin homology domain. In humans, BTK mutations result in arrested B-cell development. Besides, it leads to...
Apitolisib is an Orally Active Class I PI3K and mTORC1/2 Inhibitor
Activation of the pathway occurs following activating point mutations or amplification of the PIK3CA gene encoding the p110a PI3K isoform. Oncogenes such as PI3K, AKT, epidermal growth factor receptor (EGFR), and human epithelial growth factor receptor 2 (HER2) stimulate proliferation, growth, and survival by activating mTOR kinase. The mTOR...
CJ-2360 is a Potent and Orally Active ALK Inhibitor
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase belonging to the insulin receptor (IR) kinase superfamily. It highly expresses in adult brain tissue and exerts an important role in the development of the nervous system. Deregulation of ALK originally presents by the identification of at (2;5) chromosomal translocation...
BI-3802-Induced Polymerization Triggers Degradation of BCL6
PROTAC has been developed to degrade a wide range of clinically relevant targets. These small-molecule degraders engage both the E3 ligase and the target protein to promote the formation of a substrate–drug–ligase ternary complex. Although degraders can show notable efficacy and sustained depletion of targets, some proteins are resistant....