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...
GNE-987, a BET PROTAC Degrader, is a Part of PROTAC-Antibody (CLL1) Conjugate for ADC
BRD4 is a member of the BET family of proteins (BRD2, 3, 4, and T). It functions as an epigenetic “reader” of acetylated histone lysine residues via its two bromodomain motifs (BD1 and BD2). Disruption of BRD4-histone interactions is an attractive strategy for the development of novel anti-cancer agents....
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...