A Novel Cytosolic Isoform of Mitochondrial Trans-2-Enoyl-CoA Reductase Enhances Peroxisome Proliferator-Activated Receptor α Activity.

Background: Mitochondrial trans-2-enoyl-CoA reductase (MECR) is involved in mitochondrial synthesis of fatty acids and is highly expressed in mitochondria. MECR is also known as nuclear receptor binding factor-1, which was originally reported with yeast two-hybrid screening as a binding protein of the nuclear hormone receptor peroxisome proliferator-activated receptor α (PPARα). However, MECR and PPARα are localized at different compartment, mitochondria, and the nucleus, respectively.

Diclofenac, a Non-steroidal Anti-inflammatory Drug, Inhibits L-type Ca Channels in Neonatal Rat Ventricular Cardiomyocytes.

A non-steroidal anti-inflammatory drug (NSAID) has many adverse effects including cardiovascular (CV) risk. Diclofenac among the nonselective NSAIDs has the highest CV risk such as congestive heart failure, which resulted commonly from the impaired cardiac pumping due to a disrupted excitation-contraction (E-C) coupling. We investigated the effects of diclofenac on the L-type calcium channels which are essential to the E-C coupling at the level of single ventricular myocytes isolated from neonatal rat heart, using the whole-cell voltage-clamp technique.

Cloning and characterization of rat transient receptor potential-melastatin 4 (TRPM4).

Transient receptor potential-melastatin 4 (TRPM4) is a Ca(2+)-activated, but Ca(2+)-impermeable, cation channel. Increasing [Ca(2+)](i) induce current activation and reduction through TRPM4 channels. Several TRPM4 isoforms are expressed in mice and humans, but rat TRPM4 (rTRPM4) has not been previously identified.

Silencing of Kv4.1 potassium channels inhibits cell proliferation of tumorigenic human mammary epithelial cells.

Potassium channel activity has been shown to facilitate cell proliferation in cancer cells. In the present study, the role of Kv4.1 channels in immortal and tumorigenic human mammary epithelial cells was investigated.

Endogenous TRPM4-like channel in Chinese hamster ovary (CHO) cells.

Chinese hamster ovary (CHO) cells used in many transfection studies have been found to endogenously express channels permeable to monovalent cations, but not to divalent cations. In the presence of intracellular Ca(2+), 23-pS channel with a linear current-voltage (I-V) relationship could be frequently observed in inside-out patches but not in cell-attached patches. The open probability was voltage-dependent, which is higher at positive potentials.

Sulfonate chalcone as new class voltage-dependent K+ channel blocker.

Chalcone derivatives 1-17 were synthesized and their voltage-dependent K+ channel inhibitory activities were investigated. The effective K+ channel blockers were shown to be sulfonate chalcones 9-17, in which the sulfonyloxy group is placed on the A-ring. The 3'-(p-aminobenzene-sulfonylhydroxy)-4-hydroxychalcone 17 (IC50 = 0.