Category: Leukemia

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...

SIAIS178 is a Potent and Selective PROTAC-Based BCR-ABL Degrader

Proteolysis targeting chimeras (PROTACs) work by inducing selective intracellular proteolysis rather than acting as a conventional enzyme inhibitor. Besides, PROTACs consists of two covalently linked protein-binding molecules. One can engage an E3 ubiquitin ligase, and another binds to a target protein meant for degradation. Moreover, PROTACs need only to...

BETd-260 is a Potent PROTAC BET Degrader

The bromodomain and extra-terminal (BET) family proteins consist of BRD2, BRD3, BRD4, and testis-specific BRDT members. They are epigenetic “readers” and play a key role in the regulation of gene transcription. BET proteins are attractive therapeutic targets for cancer and other human diseases. In this study, BETd-260 is capable...