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- Aacr, Ama, Proquest, Aaas, American Society for Pharmacology and Experimental Therapeutics, Csh, CSA, Highwire from 1965, Nephrology, Rupress, and Endocrine
THRX-198321 is a bifunctional muscarinic receptor antagonist and beta2-adrenoceptor agonist (MABA) that binds in a bimodal and multivalent m...
THRX-198321 is a single molecule comprised of a muscarinic acetylcholine receptor (mAChR) antagonist moiety, represented by the fragment, MA, linked by a C9 polymethylene chain to a β(2) adrenoceptor (β(2)AR) agonist moiety, represented by the fragment, BA. THRX-198321 exhibited hi...
Evidence for a second receptor for prostacyclin on human airway epithelial cells that mediates inhibition of CXCL9 and CXCL10 release.
We provide evidence for the co-expression of two, distinct, prostacyclin (PGI(2)) receptors (IP) on BEAS-2B human airway epithelial cells. IP-receptor heterogeneity initially was suggested by the finding that the rank orders of potency of PGI(2) and three structurally-similar analogs (taprostene, il...
Nitric oxide stimulates NCX1 and NCX2 but inhibits NCX3 isoform by three distinct molecular determinants.
Our data showed that (1) the NO-donor SNAP (10nM) and the NO-precursor L-arginine (10mM) were both able to increase NCX1 activity in a cGMP-independent way. Moreover, within the amino acid sequence 723-734 of the f-loop, cysteine730 resulted as the target of NO on NCX1; (2) SNAP and L-arginine were...
A common mechanism links differently acting complex II inhibitors to cardioprotection: modulation of mitochondrial reactive oxygen species p...
We have analyzed the effect of different cardioprotective complex II inhibitors on the mitochondrial production of reactive oxygen species (ROS) since ROS seem to be essential for signalling during preconditioning to prevent ischemia/reperfusion injury. Despite different binding sites and concentrat...
Robust Protective Effects of a Novel Multimodal Neuroprotectant Oxopropanoyloxy Benzoic Acid (a Salicylic Acid/Pyruvate Ester) in the Postis...
We report a novel multi-functional compound oxopropanoyloxy benzoic acid (OBA-09, a simple ester of pyruvate and salicylic acid). This protective effect was manifested by recoveries from neurological and behavioral deficits. OBA-09 exhibited anti-oxidative effects in the postischemic brain, which wa...
Epoxyeicosatrienoic Acids Prevent Cisplatin-Induced Renal Apoptosis through a p38 Mitogen-Activated Protein Kinase-Regulated Mitochondrial P...
We hypothesized that this strategy would also attenuate cisplatin-induced renal apoptosis. Inhibition of sEH with AR9273 [1-adamantan-1-yl-3-(1-methylsulfonyl-piperidin-4-yl-urea)] reduced cisplatin-induced apoptosis through mechanisms involving mitochondrial apoptotic pathways and by reducing react...
The iron-binding protein lactoferrin protects vulnerable dopamine neurons from degeneration by preserving mitochondrial calcium homeostasis.
We used midbrain cultures and experimental settings that model the progressive loss of DA neurons in this disorder. Human lactoferrin of either recombinant or natural origin provided robust protection to vulnerable DA neurons in a culture paradigm in which these neurons die spontaneously and selecti...
MONNA, a Potent and Selective Blocker for Transmembrane Protein with Unknown Function 16/Anoctamin-1.
We have developed a potent and selective blocker for endogenous ANO1 in Xenopus laevis oocytes (xANO1) using a drug screening method we previously established (Oh et al., 2008). We have synthesized a number of anthranilic acid derivatives and have determined the correlation between biological activi...
Glutamate-induced ATP synthesis: relationship between plasma membrane Na+/Ca2+ exchanger and excitatory amino acid transporters in brain and...
We investigated the role of the plasma membrane Na(+)/Ca(2+) exchanger (NCX) and the excitatory amino acid transporters (EAATs) in Glu uptake and recycling mechanisms leading to ATP synthesis. We used different cell lines, such as SH-SY5Y neuroblastoma, C6 glioma and H9c2 as neuronal, glial, and car...
Three ubiquitination sites of organic anion transporter-1 synergistically mediate protein kinase C-dependent endocytosis of the transporter.
We previously established that OAT1 constitutively internalizes from and recycles back to cell surface and that activation of protein kinase C (PKC) inhibits OAT1 activity by promoting ubiquitination of the transporter, which then leads to an accelerated internalization of the transporter from cell...