H3B-5942, a Selective Estrogen Receptor Covalent Antagonist for ERα Breast Cancer Treatment
Estrogen receptor is a nuclear receptor activated by estrogen, existing inside cells. The receptor contains two types, ERα and ERβ. The former is always expressed in breast cancer, which causes great death among women around the world. Consequently, trying to find a potent ERα inhibitor is a possible...
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...
A Novel and Efficacious RAF Inhibitor RAF709
The mitogen-activated protein kinase pathway regulates lots of multiple biological functions. In addition, RAF inhibitors activate the MAPK pathway. Interestingly, the MAPK pathway in turn induces the RAS proteins to exchange GDP for GTP. The RAF proteins are serine-threonine specific protein kinases. They activate the MEK/ERK cascade downstream of...
Action Mechanism of a Mcl-1 Inhibitor AZD5991
Apoptosis is a highly regulated program of cell death. Apoptosis occurs in multicellular organisms. Mcl-1 plays an important role in apoptosis. Mechanically, Mcl-1 promotes cell survival by preventing induction of apoptosis in many cancers. In addition, Mcl-1 is a member of the Bcl-2 family of proteins. In contrast to...
Alofanib, An Allosteric Inhibitor of FGFR2
FGF family participates in a variety of physiological processes in adult organism including regulation of angiogenesis. FGF acts via high affinity binding to specific receptors (FGFR) in various cells and stimulates cell proliferation, differentiation, and migration. Angiogenesis plays a pivotal role in the development of various physiological and pathological...