Category: Acute Lymphoblastic Leukemia

Reversine is a ATP-Competitive Aurora Kinase Inhibitor

Aurora kinases are serine/threonine kinases that play a prominent role in mitotic regulation. The Aurora A kinase, the “polar” kinase resides at spindle poles during mitosis. It is implicated in the control of centrosome duplication, maturation, and separation. Aurora A is important for the formation of a bipolar mitotic...

Daunorubicin is a Topoisomerase II Inhibitor with potent Antineoplastic Activities

Topoisomerases are enzymes that regulate the overwinding or underwinding of DNA. The winding problem of DNA arises due to the intertwined nature of its double-helical structure. Topoisomerases are isomerase enzymes that act on the topology of DNA. Type I topoisomerase cuts one strand of a DNA double helix, relaxation...

DT2216 is a Selective PROTAC Degrader of BCL-XL

BCL-XL is a member of the Bcl-2 protein family and a transmembrane molecule in mitochondria. Specifically, it acts as an anti-apoptotic protein by blocking the release of mitochondrial contents such as cytochrome c. Besides, BCL-XL is a well-validated cancer target and eventually leads to caspase activation and eventually programmed...

DI-87 is an Orally Active and Selective Deoxycytidine Kinase (dCK) Inhibitor

Deoxyribonucleotide triphosphates (dNTPs) are essential for tumor growth, and DNA replication and repair also is essential dNTPs.  Parallel and convergent de novo and salvage pathways redundantly produce the same dNTPs using different substrates.  The de novo pathway produces dNTPs from glucose and amino acids and is dependent upon ribonucleotide reductase (RNR)....

THZ-P1-2 is a Selective PI5P4K Inhibitor

Phosphatidylinositol 5-phosphate (PI-5-P) is one of the seven phosphoinositides. They regulate a wide range of cellular functions. They localize in the nucleus, Golgi, endoplasmic reticulum, and at the plasma membrane. PI-5-P is an oxidative stress-induced regulator of AKT activation. The phosphorylation of the low abundance phosphoinositide PI-5-P at the...

EB-3D, a ChoKα1 Inhibitor, Induces AMPK-mTOR Pathway Deregulation and Apoptosis

T-cell acute lymphoblastic leukemia (T-ALL) is an aggressive hematologic disorder. It results from the malignant transformation of T-cell progenitors. Since the overexpression of choline kinase alpha 1 (ChoKa1) has been associated with tumorigenesis in many cancers, it becomes an interesting therapeutic target. ChoK catalyzes the phosphorylation of choline (Cho)...