Category: Acute Lymphoblastic Leukemia

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)...

CKI-7 is a Dual CK1 and Cdc7 Kinase Inhibitor

Protein phosphorylation plays a fundamental role in the regulation of a variety of cellular processes. Casein kinase I (CK1) is a cyclic nucleotide independent kinase. It is highly purified from various tissues, including calf thymus, rabbit reticulocytes, liver, and skeletal muscle. The widespread distribution of CK1 suggests its importance...

SI-109, a STAT3 Transcription Inhibitor, is the Ligand of PROTAC Degrader SD-36

As we have written in the article “SD-36 is a Selective PROTAC STAT3 Degrader”, proteolysis targeting chimera (PROTAC) technology has been a type of therapeutics that induces targeted protein degradation. Signal transducer and activator of transcription 3 (STAT3) is an attractive cancer therapeutic target. Longchuan Bai, et al have...