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...
SRX3207 is an Orally Active and First-in-Class Dual Syk/PI3K Inhibitor
Macrophages (MΦ) not only play a role in host defense and tumor growth, metastasis, and immunosuppression. Many studies have demonstrated that targeting the molecular pathways/signaling nodes in the MΦs that regulate the transition of protumorigenic MΦs into anti-tumorigenic MΦs will activate the immune response in cancer. Syk kinase has...
GSK143 is an Orally Active and Highly Selective Spleen Tyrosine Kinase (SYK) Inhibitor
Tyrosine-protein kinase SYK is an enzyme that in humans is encoded by the SYK gene. Specifically, Syk is a 72 kDa cytoplasmic non-receptor tyrosine kinase and it is relevant to in a variety of signal transduction cell types. Besides, Syk and ZAP-70, which are related to the zeta chain,...
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...
TAK-659 is a Dual SYK and FLT-3 Kinase Inhibitor for Leukemia Treatment
Acute Myelogenous Leukemia (AML) is a disease driven by SYK and/or FLT3-mediated signaling. In particular, spleen tyrosine kinase (SYK) is a 72 kD non-receptor cytoplasmic tyrosine kinase. SYK is a key mediator for a variety of inflammatory cells and immunology signaling pathways, including B cell receptor in B cells,...