Category: Leukemia

Rosabulin is a Potent Microtubule Inhibitor

Chemotherapy is a cornerstone in the development of present-day cancer therapy. Moreover, Chemotherapy is one of the most effective and potent strategies to treat malignant tumors. However, Chemotherapy resistance occurs when cancers that have been responding to therapy suddenly begin to grow. Rosabulin is a potent tubulin inhibitor. In...

AZD1208 is an Orally Bioavailable and Highly Selective PIM Kinases Inhibitor

Pim kinases, also known as serine/threonine kinases, have three highly homologous isoforms namely Pim-1, Pim-2, and Pim-3. And Pim-1, Pim-2, and Pim-3 are recurrent proviral integration locus in Moloney murine leukemia virus. The overexpression of Pim kinases occurs when viral inserts at this site. Pim kinases are overexpressed in...

Dasatinib is an Orally Active Dual Bcr-Abl and Src Family Tyrosine Kinase Inhibitor

Src is an important member of the non-receptor protein tyrosine kinase. Furthermore, Src plays a key role in the regulation of many cells through the extracellular ligand binding to the receptor and the cell adhesion molecule activation in cell cycle-specific stage. Src can affect cell adhesion, motility, proliferation, and...

Piclidenoson is a First-in-Class and Orally Active A3AR Agonist

One of the main strategies for cancer research is the identification of drugs that can cause apoptotic death in malignant cells. Additionally, Adenosine 5′-triphosphate (ATP), UTP, and adenosine are considered that inhibit the growth of several cancerous cell lines. Adenosine has several physiological and pharmacological functions. It can modulate...

ICCB280 is a Potent C/EBPα Inducer with Anti-Leukemic Properties

Knowledge of the pathogenesis of AML has seen great progress due to recent advances in genetic studies. However, the long-term survival of AML patients is still unsatisfactory. A block in differentiation is one of the characteristics of leukemia. C/EBPα is an essential transcription factor for the differentiation of cells...

MZP-54 is a Selective BRD3/4 PROTAC Degrader

PROTACs are bivalent chemical protein degraders. In particular, PROTACs degrade a specific endogenous protein of interest (POI) by harnessing the E3 ubiquitin ligase pathway. Especially, PROTACs is a powerful small-molecule approach for inducing protein degradation. Moreover, PROTACs conjugate a target warhead to an E3 ubiquitin ligase ligand via a...

dFKBP-1 is a Potent and PROTAC-based FKBP12 Degrader

The FK506-binding protein 12 (FKBP12) is a ubiquitous abundant protein that acts as a receptor for the immunosuppressant drug FK506l FK506 binds tightly to intracellular calcium release channels and to the TGF-β type I receptor. dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. FKBP12 inhibits the basal signaling of...