Allele-specific activators and inhibitors for kinesin.

Effect of Activators and Inhibitors on Lactase Activities to Determine its Kinetic Model

Accelerated Cytotoxicity Mechanism Screening

By discovering how chemical compounds/xenobiotics cytotoxicity is affected when their metabolic pathways are inhibited or activated, the metabolic pathways that activate versus detoxify chemical compound can be identified. Reactive metabolites contributing to cytotoxicity can also be identified. In this lecture, the pretreatment of inhibitors and activators of xenobiotic metabolizing enzymes as...

Modulation of estrogen related receptor alpha activity by the kinesin KIF17

Estrogen-related receptor alpha (ERR1) is an orphan nuclear receptor that can bind transcriptional co-activators constitutively. ERR1 expression correlates with poor patient outcomes in breast cancer, heightening interest in this nuclear receptor as a therapeutic target. Because ERR1 has no known regulatory ligand, a major challenge in targeting its activity is to find cellular or synthetic mod...

Downregulation of Kinesin Spindle Protein Inhibits Proliferation, Induces Apoptosis and Increases Chemosensitivity in Hepatocellular Carcinoma Cells

Background: Kinesin spindle protein (KSP) plays a critical role in mitosis. Inhibition of KSP function leads to cell cycle arrest at mitosis and ultimately to cell death. The aim of this study was to suppress KSP expression by specific small-interfering RNA (siRNA) in Hep3B cells and evaluate its anti-tumor activity. Methods: Three siRNA targeting KSP (KSP-siRNA #1-3) and one mismatched-siRNA (...

Engineered kinesin motor proteins amenable to small-molecule inhibition.

The human genome encodes 45 kinesin motor proteins that drive cell division, cell motility, intracellular trafficking and ciliary function. Determining the cellular function of each kinesin would benefit from specific small-molecule inhibitors. However, screens have yielded only a few specific inhibitors. Here we present a novel chemical-genetic approach to engineer kinesin motors that can carr...