BSJ-03-204 is a Selective Palbociclib-Based CDK4/6 Dual Degrader (PROTAC)
The chimeric proteolytic enzyme (PROTAC) is a heterobifunctional small molecule. Specifically, it is composed of two active domains and an adaptor that can remove specific proteins that are not needed. Besides, PROTAC does not act as a conventional enzyme inhibitor, but by inducing selective intracellular proteolysis. Moreover, PROTAC includes...
GSK778 is a Potent and Selective Inhibitor of BET BD1
The bromodomain is a protein domain of about 110 amino acids, which can recognize acetylated lysine residues. Specifically, the bet (Bromo- and terminal domain) family consists of germ cell-specific (BRDT) and ubiquitously expressed (BRD2, BRD3, Brd4) epigenetic reader proteins. As a “reader” of lysine acetylation, bromodomain is responsible for...
PRN1008 is a Reversible Covalent and Oral Active Inhibitor of Bruton’s Tyrosine Kinase (BTK)
Bruton’s tyrosine kinase (BTK) is a nonreceptor tyrosine kinase in human encoded by BTK gene. Besides, the kinase belongs to the TEC protein tyrosine kinase family of kinases. Additionally, this kind of tyrosine kinase plays a crucial role in B cell maturation as well as mast cell activation through...