A Lead PROTAC BRD9 Chemical Degrader

The bromodomain-containing protein BRD9, a recently identified mSWI/SNF subunit, is a novel complex configuration distinct from BAF and PBAF. The mSWI/SNF (BAF) complex comprises at least 15 subunits of ~2 MDa in size. The BAF complex has an autonomous capacity to specifically regulate gene expression patterns in a cell...

BR351 is a Brain Penetrant MMP Inhibitor

Matrix metalloproteinases (MMPs) are a family of zinc- and calcium-dependent endopeptidases. They are responsible for the degradation of most extracellular matrix proteins during organogenesis, growth and normal tissue turnover. Elevated MMP expression and activity has existed in numerous disease processes, including inflammation, tumor cell metastasis, and atherosclerosis. Currently, synthetic...

AZD3229 is a Potent Pan-KIT Mutant Inhibitor

Gastrointestinal stromal tumors (GISTs) are the most common mesenchymal neoplasms of the gastrointestinal tract. While the application of targeted tyrosine kinase inhibitors has revolutionized the treatment of gastrointestinal stromal tumors (GISTs). The targeted tyrosine kinase inhibitors inhibit KIT-driven proliferation, diverse mutations to this kinase drive resistance to established therapies....

CCB02, a Tubulin Binder Inhibits Cancer Cells with Extra Centrosomes

Centrosome is an important organelle. It acts as the main microtubule organizing center (MTOC), regulates cell-cycle progression in mammalian cells. In normal cells, centrosome duplication occurs in the early phase of cell cycle. It ensures each daughter cell to have one centrosome after cell division. CPAP (centrosomal P4.1-associated protein)...

Optimization of HJB97 for The Design of PROTAC Degraders of BET Proteins

The Bromodomain and Extra-Terminal Domain (BET) family of proteins comprises BRD2, BRD3, BRD4, and BRDT. The BET proteins are epigenetic readers and play a key role in the regulation of gene transcription. BET proteins are considered to be attractive therapeutic targets for cancer. The targeted degradation of BET proteins...

CF53, a Potent and Orally Active BET Inhibitor

Bromodomain and extra-terminal (BET) family is a well-known member of bromodomain family. Proteins of this family include BRD2, BRD3, BRD4 and a testis-specific protein, BRDT. BET proteins act as important epigenetic “readers” and play a vital role in regulating gene transcription. Thus, they are becoming hot targets for cancer...