5-Azacytidine, a Nucleoside Analogue of Cytidine, Inhibits DNA Methylation
In the mammalian genome, DNA methylation is an epigenetic mechanism involving the transfer of a methyl group onto the C5 position of the cytosine to form 5-methylcytosine. DNA methylation regulates gene expression by recruiting proteins involved in gene repression or by inhibiting the binding of transcription factor(s) to DNA....
HM43239 is an Orally Active and Selective FLT3 Inhibitor
Acute myeloid leukemia (AML) is the most common acute leukemia in adults, with an incidence of over 20 000 cases per year in the United States alone. Large chromosomal translocations, as well as mutations in the genes involved in hematopoietic proliferation and differentiation, result in the accumulation of poorly...
Dovitinib is a Multi-Targeted Tyrosine Kinase Inhibitor
Tyrosine kinase is an enzyme that can transfer phosphate groups from ATP to tyrosine residues of specific proteins in cells. Specifically, this covalent post-translational modification is a key component of normal cell communication and homeostasis maintenance. Tyrosine kinase is an important mediator of signal cascade reaction. Besides, it plays...
Flavopiridol (Alvocidib) is a pan CDK Inhibitor
The cyclin-dependent kinases (CDKs) are serine/threonine protein kinases. And it exhibits drives force behind the cell cycle and cell proliferation. CDKs contain at least a catalytic subunit (CDK) and a regulatory subunit (cyclin). To date, at least 10 CDKs and 15 cyclins have been identified. Once activation, CDKs phosphorylate...
Quizartinib (AC220) is an Orally Active and Highly Selective FLT3 Tyrosine Kinase Inhibitor
Receptor tyrosine kinase FMS like tyrosine kinase 3 (FLT3) is a member of the class III receptor tyrosine kinase family. The family also includes FMS, kit, and platelet-derived growth factor (PDGF) receptors. Specifically, FLT3 is relevant to regulating the survival, proliferation, and differentiation of hematopoietic stem/progenitor cells. The normal...
Elesclomol (STA-4783) is an Oxidative Stress Inducer and Induces Apoptosis
Modulating reactive oxygen species (ROS) levels has been proposed as a therapeutic strategy for cancer. In normal cells, ROS are produced at low concentrations and cancer cells produce elevated levels of ROS due to increased metabolic activity, resulting in a state of chronic oxidative stress. Recent studies showed the...
Infigratinib (BGJ-398) is an Orally Active FGFR Inhibitor
The fibroblast growth factor receptor (FGFR) family of receptor tyrosine kinases (RTKs) comprises four members (FGFR1, FGFR2, FGFR3, and FGFR4) that share significant sequence homology. This family of RTKs serves as high-affinity receptors for the fibroblast growth factors (FGFs) that control cell proliferation, apoptosis, and differentiation and are involved...