Month: July 2019

MT-802 is a PROTAC Degrader of BTK for C481S Mutant CLL Treatment

The irreversible inhibitor Ibrutinib for Bruton’s tyrosine kinase (BTK) has emerged as a transformative treatment option for patients with chronic lymphocytic leukemia (CLL) and other B-cell malignancies. However, more than 80% of CLL patients develop resistance due to the mutant site in cysteine to serine covalently bound by Ibrutinib...

GSK3368715 is an Orally Active Type I PRMT Inhibitor

GSK3368715 is an orally active type I PRMT inhibitor. Protein arginine methyltransferases (PRMTs) transfer a methyl group from S-adenosyl-L-methionine (SAM) to the substrate arginine side chain. All PRMTs can generate ω-NG-monomethyl-arginine (MMA) through a single methylation event. However, type I and II enzymes catalyze progression from MMA to NG-asymmetric...

MBM-55 is a Potent Nek2 Inhibitor for Cancer Therapy

NIMA-related kinase 2 (Nek2) is a serine/threonine kinase. It serves as a key regulator of mitotic processes such as centrosome duplication and spindle assembly. Deregulation of mitotic processes can lead to genomic instability and aneuploidy. It is a characteristic of all tumors and is a hallmark of cancer. Nek2...

M-89, a Specific Menin inhibitor, Has Potential to Treat MLL Leukemia

Mixed lineage leukemia (MLL) protein is a histone methyltransferase and specifically methylates histone H3 lysine 4 residue (H3K4). MLL gene rearrangement accounts 5-10% in acute myeloid leukemia in adults and almost 70% of acute lymphoblastic leukemia in infants. As far as the current treatment regimen is concerned, adult leukemia...

GSK2643943A is a Novel DUB Inhibitor

The ubiquitin proteasome system participates in a variety of biological functions including cell cycle progression, intracellular signaling and protein degradation. Therefore, it is not surprising to find many misregulation of this system in cancer. Fortunately, the first-generation deubiquitylating enzyme (DUB) inhibitors are now approaching clinical trials. For instance, the...