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...
Bestatin is a Broad-Spectrum, and Competitive Aminopeptidase Inhibitor
Aminopeptidases catalyze the cleavage of amino acids from the amino terminus of protein or peptide substrates. Regarding catalytic mechanism, most of the aminopeptidases are metallo-enzymes. In addition, aminopeptidase is widely present in animal and plant kingdomsis widely present in , found in many subcellular organelles, in cytoplasm, and as...
Repotrectinib is a potent ROS1 and TRK Inhibitor
Repotrectinib is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. The IC50 values are 0.83/0.05/0.1 nM for TRKA/B/C, respectively. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib inhibits mutant ALKs. It inhibits ALK G1202R with an IC50 of 1.26 nM. Besides, it inhibits ALK L1196M with an IC50 of 1.08 nM)....
Almonertinib is an Orally Active and Irreversible EGFR Inhibitor
Lung cancer is one of the most common malignant tumors in the world. Its lethality ranks the first among many malignant tumors. In addition, the overexpression of the human ATP-binding cassette (ABC) drug transporter ABCB1 (P-gp) or ABCG2 (BCRP) in cancer cells often contributes significantly to the development of...
AZD1390 is a Highly Selective, Orally Active and Brain-Penetrant ATM Inhibitor
Glioblastoma multiforme (GBM) is a lethal form of brain tumor arising from malignant glial cells. this disease affects 2 to 3 per 100,000 adults per year and accounts for 52% of all primary brain tumors. ATM plays a central role in the detection, signaling, and repair of DNA double-strand...
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...