MS4322 is a First-in-Class PRMT5 PROTAC Degrader

PRMT5 is a member of type II protein arginine methyltransferases (PRMTs). When interacting with its binding partner MEP50, PRMT5 catalyzes monomethylation and symmetric dimethylation of arginine residues of its histone substrates. These substrates include H3R2, H3R8, and H4R3, and its nonhistone substrates, including p53, EGFR, N-MYC, SmD3, and RNA...

Zebularine is a DNA Methyltransferase Inhibitor

DNA methyltransferase (DNMT) family enzymes catalyze the transfer of methyl to DNA. Specifically, DNMT is a conserved cytosine methylase family, which plays a key role in epigenetic regulation. The DNMT family has four members, including DNMT1, Dnmt3a, DNMT3b, and DNMT3l. Different from other DNMTs, DNMT3l does not have any...

MRTX1133 is a Highly Selective, First-in-Class Inhibitor of KRAS G12D

Mutant KRAS is an attractive drug target for the treatment of a number of cancers for many decades. Until recently, the high affinity of KRAS for GDP/GTP and the lack of any other apparent binding pocket have significantly hampered the development of KRAS inhibitors. KRAS inhibitor relies on a...

CBL0137 is an Histone Chaperone FACT Inhibitor

Cancer harbors several characteristics, including high heterogeneity, diverse gene mutation, or rapid progression; consequently, treating cancer is difficult, and it easily relapses. Surgery, radiotherapy, chemotherapy, immunotherapy, and targeted therapy show remarkable achievements. In particular, targeted therapies promote treatment. However, we have failed to treat cancer. Chemotherapy with or without...

Trolox, an Analogue of Vitamin E, Possesses Antioxidant Effect

Oxidative stress reflects the imbalance between the systemic performance of reactive oxygen species (ROS) and the ability of biological systems to easily detoxify active intermediates or repair the resulting damage. Obviously, oxidative stress is considered to be related to the development of ADHD, cancer, Parkinson’s disease, Lafora disease, Alzheimer’s...

Lonidamine, an Antitumor Agent, is a Hexokinase, Mitochondrial Pyruvate Carrier

Targeting cancer metabolism has received interest as a strategy for anticancer therapy. Most cancers have altered metabolism and high demand for nutrients to support their rapid proliferation. There are many other metabolic alterations in cancer cells. They include a high rate of glutamine consumption, enhanced lipid synthesis, and increased...