Category: Acute Lymphoblastic Leukemia

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...