BPK-29, a NR0B1 Ligand, Disrupts Protein Interactions for NR0B1-WT
Nuclear factor (erythroid-derived 2)-like 2 (NRF2) is a master regulator of the cellular antioxidant response. It is genetically activated in Non-Small Cell Lung Cancers (NSCLCs) by, for instance, mutations in the interacting protein KEAP1. Its aberrant activation rewires biochemical networks in cancer cells that may create special vulnerabilities. KEAP1-mutant...
CSRM617 is a Transcription Factor ONECUT2 Inhibitor for Prostate Cancer
The transcription factor ONECUT2 (OC2) is a master regulator of androgen receptor networks in mCRPC (metastatic castration-resistant prostate cancer ). OC2 acts as a survival factor in mCRPC models. OC2 is a potential drug target in the metastatic phase of aggressive PC. CSRM617, a well-tolerated novel small-molecule inhibitor of...
PTC596 is an Orally Active and Selective BMI-1 Inhibitor
BMI-1 is a highly conserved class II member of the Polycomb group of genes, regulating diverse aspects of transcription, stem cell maintenance, cell proliferation, and oncogenesis. BMI-1 has vital functions in the self-renewal and maintenance of AML and normal hematopoietic stem cells. The first BMI inhibitor PCT-209 has a...
SS-208 is a Selective HDAC6 Inhibitor for Melanoma
Malignant melanoma represents the most aggressive and deadliest form of cutaneous cancer. This disease possesses the characteristic of increasing incidence, high metastasis, rapid disease progression, poor prognosis, and high mortality. The latest data showed that patients with metastatic melanoma have a poor prognosis with a 5-year survival rate of...
AZD0424 is an Orally Active and Dual Selective Src/Abl Kinase Inhibitor
A study from Victoria K Woodcock suggested that AZD0424 is an inhibitor of the proto-oncogenic non-receptor tyrosine kinases Src and ABL1. The kinase plays an indefensible role in cancer. Src expresses lowly in the majority of cell types and participates in regulating bone metabolism, proliferation, and angiogenesis. Src also...
BY27 is a Selective and Orally Active BET BD2 Inhibitor
BET (Bromodomain and extra terminal domain) is a well-known member of the bromodomain family. It contains BRD2, BRD3, BRD4, and BRDT, which have two tandem bromodomains (BD1 and BD2). BD1 and BD2 are recognition motifs for the acetyl-lysine residues of N terminuses of histones as well as other proteins....
KPT-6566 is a Selective PIN1 Inhibitor
PIN1 is a prolyl isomerase, which binds to several proteins, acts as a post phosphorylation control and regulates protein function. PIN1 targets proteins containing phosphorylated S/T-P sites firstly via the WW domain to bind to the protein. Next, the enzyme catalyzes the cis/trans isomerization via the catalytic PPIase domain....