Alobresib is an Orally Active BET Bromodomain Inhibitor for Uterine Serous Carcinoma Treatment
Uterine serous carcinoma is a rare and highly aggressive variant of endometrial cancer. Uterine serous carcinoma accounts for 10% of all endometrial cancer; however, it carries the poorest prognosis, with 5-year survival rates as low as 55%. Whole-exome sequencing studies have recently reported c-Myc gene amplification in a large...
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...
APG-115, an Orally Active MDM2 Inhibitor, Induces Cell-Cycle Arrest and Apoptosis in a p53-Dependent Manner
The essential all human cancers compromises the tumor suppressor function of p53. In about half of human cancers, TP53, the gene encoding p53 protein, is mutated or deleted. This inactivates the tumor suppressor function of p53. In the remaining 50%, p53 retains its wild-type status. But, murine double minute 2 (MDM2)...
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...