CZS-241 is an Orally Active and Selective PLK4 Inhibitor
PLK4 (polo-like kinase 4) is an enzyme that encodes a member of the polo family of serine/threonine protein kinases. Importantly, PLK4 protein localizes to centrioles—complex microtubule-based structures found in centrosomes-and regulates centriole duplication during the cell cycle. Particularly, PLK4 has been regarded as an extremely potential anticancer target, and...
MC2590, a Potent HDAC Inhibitor, inhibits HDAC1-3, -6, -8, and -10
Histone deacetylase (HDAC) is an epigenetic enzyme that regulates gene expression through histone deacetylation. It leads to more closed chromatin structure and gene expression inhibition. Many non-histones are also targets of HDAC, such as α Microtubulin, heat shock protein (HSP) 90, and hypoxia-inducible factor HIF-1 α. Specifically, HDAC is...
SIAIS100 is a Potent BCR-ABL PROTAC Degrader
Chronic myeloid leukemia (CML) is a kind of myeloproliferative neoplasms (MPN). It is characterized by the proliferation of a pluripotential stem cell that can differentiate along the granulocytic lineage. In terms of mechanism, it is consistently related to the BCR-ABL1 fusion gene. CML is typically relevant to a balanced...
Vamotinib (PF-114) is a Potent, Selective and Orally Active Tyrosine Kinase Inhibitor
BCR-ABL, a fusion gene, is a mutation that is formed by the combination of two genes, BCR and ABL. The BCR gene is normally on chromosome number 22. The ABL gene is normally on chromosome number 9. The BCR-ABL mutation happens when pieces of BCR and ABL genes break...
Dasatinib is an Orally Active Dual Bcr-Abl and Src Family Tyrosine Kinase Inhibitor
Src is an important member of the non-receptor protein tyrosine kinase. Furthermore, Src plays a key role in the regulation of many cells through the extracellular ligand binding to the receptor and the cell adhesion molecule activation in cell cycle-specific stage. Src can affect cell adhesion, motility, proliferation, and...
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...
GMB-475, a BCR-ABL1 Inhibitor Based on PROTAC, Has Potential to Overcome BCR-ABL1-Dependent Drug Resistance
Chronic myeloid leukemia is a myeloproliferative disorder characterized by the presence of the oncogenic fusion protein BCR-ABL1. ABL1, one of the fusion partners in the BCR-ABL1 protein, contains an allosteric myristoylation binding site. Especially, the proteolysis targeting chimera (PROTAC) technology provides a unique toolkit for probing the non-kinase roles...