Category: Leukemia

Cytochalasin B is a Mycotoxin binding to the Barbed end of Actin Filaments

Actin, a family of globular multi-functional proteins, is the most abundant protein in most eukaryotic cells. It forms microfilaments in the cytoskeleton, and the thin filaments in muscle fibrils. Actin participates in many important cellular processes, including muscle contraction, cell motility, cell division and cytokinesis, vesicle and organelle movement,...

Atuveciclib is a Highly Selective and Orally Active PTEFb, CDK9 Inhibitor

Positive transcription elongation factor P-TEFb is a kinase composed of CDK9 and cyclin T. Specifically, P-TEFb plays an important role in the transcriptional regulation of RNA polymerase II (pol II) in eukaryotes. Besides, P-TEFb mediates the positive transcriptional extension of the new mRNA chain by phosphorylating the S2 residue...

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...

GSK2606414 is an Orally Available PERK Inhibitor

PERK (Protein kinase R (PKR)-like endoplasmic reticulum kinase) is a type I endoplasmic reticulum transmembrane protein. Generally, PERK contains a stress-sensing domain facing the endoplasmic reticulum lumen and a cytosolic kinase domain. Interestingly, PERK is a major component of the unfolded protein response (UPR), which promotes the adaptation of...

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...

SIM1 is a PROTAC Based BET Family Degrader

Proteolytic targeting chimera (PROTAC) is a heterobifunctional small molecule that acts by inducing selective intracellular proteolysis. Specifically, bifunctional PROTAC molecule is including ligands of target protein (POI) and covalent ligands of E3 ubiquitin ligase (E3). After binding to POI, PROTAC can recruit E3 for POI ubiquitination. This ubiquitination is...

DCH36_06 is a Selective p300/CBP Inhibitor

Histone acetyltransferases (HATs) are epigenetic enzymes that relieve transcriptional repression by preferentially acetylation of ε-amino group of lysine residues on histones. In general, HATs are crucial for chromatin restructuring and transcriptional regulation in eukaryotic cells. HATs can be grouped into at least five different subfamilies (HAT1, Gcn5/PCAF, MYST, p300/CBP,...