Category: Acute Lymphoblastic Leukemia

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...

Optimization of HJB97 for The Design of PROTAC Degraders of BET Proteins

The Bromodomain and Extra-Terminal Domain (BET) family of proteins comprises BRD2, BRD3, BRD4, and BRDT. The BET proteins are epigenetic readers and play a key role in the regulation of gene transcription. BET proteins are considered to be attractive therapeutic targets for cancer. The targeted degradation of BET proteins...