TAI-1 is an Orally Active and Highly Potent Hec1 Inhibitor
Hec1 (Ndc80) is one of the outer kinetochore proteins and forms heterotetramers with proteins NUF2, SPC25, and SPC24. Specifically, drugs that interfere with mitosis are part of the most successful chemotherapeutic compounds for cancer in clinical practice. Hec1, a component of mitochondria, is overexpressed in a variety of human...
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...
BAY 61-3606, a Syk Inhibitor, Sensitizes TRAIL-Induced Apoptosis by Downregulating Mcl-1 in Breast Cancer
Breast cancer cells usually develop resistance to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL). TRAIL shows cancer-selective killing activity. TRAIL ligand selectively kills cancer cells by initiating apoptotic signaling through the engagement of its pro-apoptotic receptors, death receptors-4 and -5. In particular, myeloid cell leukemia sequence-1 (Mcl-1) is a member...