Category: Leukemia

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...

Ilorasertib is an Orally Active ATP-Competitive Multitargeted Kinase Inhibitor

Aurora kinases are key regulators of mitosis that overexpress in many cancer types. Ilorasertib (ABT-348) is a potent inhibitor of all three Aurora kinases, although it has greater activity versus Aurora B and C than Aurora-A. In addition, Ilorasertib also inhibits VEGFRs and PDGFRs, and the Src families of...

S2116 is a Potent Lysine-Specific Demethylase 1 (LSD1) Inhibitor

Lysine-specific demethylase 1 (LSD1) is a human protein encoded by the kdm1a gene. Specifically, LSD1 is a flavin-dependent monoamine oxidase that demethylates monomethyl and dimethyllysine, especially H3K4 and H3K9. Besides, LSD1 regulates a variety of biological processes through dual function regulation of enhancer function. Overexpression of LSD1 is a...

M-808 is a Highly Potent and Efficacious Covalent Menin-MLL Interaction Inhibitor

Menin is a putative tumor suppressor associated with multiple endocrine tumor type 1 (MEN-1 syndrome). Specifically, Menin has two functional nuclear localization signals and inhibits JunD transcriptional activation. MLL1, a histone methyltransferase, is an active global regulator of gene transcription. Besides, the protein belongs to histone-modifying enzyme and contains...