Ruxolitinib (INCB018424) is an Orally Active JAK1 and JAK2 Inhibitor
The myeloproliferative neoplasms (MPNs) are a group of related clonal diseases probably arising from hematopoietic progenitor or stem cells. Patients with MPNs have an increased risk of thrombotic and bleeding complications and disease progression to acute myeloid leukemia. JAK2 is a member of the JAK family of cytoplasmic tyrosine...
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,...
WZ811 is an Orally Active CXCR4 Antagonist
The C-X-C chemokine receptor-4 (CXCR4) is a seven-transmembrane G-protein coupled receptor (GPCR). It is a member of the family I GPCR or rhodopsin-like GPCR family. The chemokine stromal cell-derived factor-1 (SDF-1 or CXCL12) is a CXC chemokine peptide. Meanwhile, it is the natural ligand for CXCR4. Importantly, the CXCR4...
NXT629 is a Selective and Competitive PPARα Antagonist
Peroxisome proliferator-activated receptors (PPARs) are ligand-activated transcription factors that belong to the nuclear hormone receptor superfamily. Of these, PPARα mainly expresses in the liver, where it activates fatty acid catabolism. PPARδ expresses ubiquitously and implicates in fatty acid oxidation and keratinocyte differentiation. PPARγ2 expresses exclusively in adipose tissue and...
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,...
MT-802 is a PROTAC Degrader of BTK for C481S Mutant CLL Treatment
The irreversible inhibitor Ibrutinib for Bruton’s tyrosine kinase (BTK) has emerged as a transformative treatment option for patients with chronic lymphocytic leukemia (CLL) and other B-cell malignancies. However, more than 80% of CLL patients develop resistance due to the mutant site in cysteine to serine covalently bound by Ibrutinib...