Zingerone, an Orally Active Nontoxic Methoxyphenol, Possesses Anti-Inflammatory and Anti-Tumor Properties
Humans have been using natural products for medicinal use for ages. Ginger (Zingiber officinale) is used as a condiment worldwide from times immemorial. Ginger has many health benefits in traditional medicine. It is due to diverse phytochemical constituents present in ginger which lead to promising health benefits. It is...
VU0359595 is a Selective PLD1 Inhibitor
Phospholipase is a member of a very complex group of enzymes that break down phospholipids into fatty acids and other compounds. Phospholipase D (PLD) is an enzyme of the phospholipase superfamily. There are two mammalian isoforms of PLD, coined PLD1 and PLD2, and despite conserved regulatory and catalytic domains....
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...
Tirabrutinib is a Selective BTK Inhibitor
The BTK kinases comprise 5 structural domains, including pleckstrin homology, TEC homology, Src homology, Src homology, and kinase domains. The activation of BTK kinase depends on recruitment to the plasma membrane via the pleckstrin homology domain. In humans, BTK mutations result in arrested B-cell development. Besides, it leads to...
β-Lapachone, a Naturally Occurring O-naphthoquinone, is a Topoisomerase I Inhibitor
β-Lapachone is an ortho-naphthoquinone and inhibits topoisomerase I. β-Lapachone is a classic quinone-containing antitumor NQO1-bioactivatable drug that directly kills NQO1-overexpressing cancer cells. NQO1 is an antioxidative enzyme that helps recover renal oxidative status. β-Lapachone reduces cisplatin-induced nephrotoxicity. In cancer cells, cisplatin forms cross-link with DNA, which inhibits DNA replication,...
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...