Category: Breast Cancer

SD-1029 is a JAK2/STAT3 Activation Inhibitor

Janus kinase (JAK) is a family of intracellular, nonreceptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT pathway. JAK includes JAK1, JAK2, JAK3 and TYK2. JAK serves as the cytoplasmic signaling components of cytokine receptors and are activated through cytokine-mediated trans-phosphorylation. The pseudokinase domain of JAKs is crucial...

Rucaparib is a PARP Inhibitor

PARP is a family of proteins involved in many cellular processes, such as DNA repair, genomic stability, and programmed cell death. At least 18 members of the PARP family are encoded by different genes and have homology in conserved catalytic domains. Specifically, PARPs play an important role in various...

Dovitinib is a Multi-Targeted Tyrosine Kinase Inhibitor

Tyrosine kinase is an enzyme that can transfer phosphate groups from ATP to tyrosine residues of specific proteins in cells. Specifically, this covalent post-translational modification is a key component of normal cell communication and homeostasis maintenance. Tyrosine kinase is an important mediator of signal cascade reaction. Besides, it plays...

Deguelin, a Naturally Occurring Rotenoid, Acts as a Chemopreventive Agent

Head and neck squamous cell carcinoma (HNSCC) represents more than 5% of all cancers each year. In addition, breast cancer is a heterogeneous group of diseases. Approximately 60-70% of breast cancers express estrogen receptors (ER) and/or progesterone receptors (PR). About 20-30% of breast cancers have amplified levels of the...

Apitolisib is an Orally Active Class I PI3K and mTORC1/2 Inhibitor

Activation of the pathway occurs following activating point mutations or amplification of the PIK3CA gene encoding the p110a PI3K isoform. Oncogenes such as PI3K, AKT, epidermal growth factor receptor (EGFR), and human epithelial growth factor receptor 2 (HER2) stimulate proliferation, growth, and survival by activating mTOR kinase. The mTOR...

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...

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...