Showing papers in "Biochemical Pharmacology in 2013"

TL;DR: Evidence supporting Keap1-dependent and -independent mechanisms of Nrf2 regulation are dissected, which highlight key knowledge gaps in this important field of biology, and suggest how these may be addressed experimentally.

TL;DR: The stemness properties of a few cancer cells as well as components of the tumor stroma, like fibroblasts and tumor-associated macrophages but also hypoxia, also help tumor to resist to anticancer agents.

TL;DR: In conclusion, CGA improved glucose and lipid metabolism, via the activation of AMPK, in Lepr(db/db) mice.

TL;DR: In this review, the chemistry and biological activity of some natural and synthetic H2S-donating compounds have been summarized and the newly reported NOSH-aspirin that releases both NO and H 2S has been discussed.

TL;DR: This review not only summarizes the diverse molecular targets of ursolic acid, but also provides an insight into the various preclinical and clinical studies that have been performed in the last decade with this promising triterpenoid.

TL;DR: Cannabigerol attenuated murine colitis, reduced nitric oxide production in macrophages (effect being modulated by the CB2 receptor) and reduced ROS formation in intestinal epithelial cells, and could be considered for clinical experimentation in IBD patients.

TL;DR: Genetic evidence supporting amyloid causality in AD is reviewed in the context of the clinical failures, and progress in tau-based and alternative approaches to AD, where an evolving modus operandi in biomedical research fosters excessive optimism and a preoccupation with unproven and often ephemeral, biomarker/genome-based approaches.

TL;DR: This is the first report on aspects of substituted methcathinone efficacies at serotonin (5-HT) receptors and in superfusion release assays, and indicates direct interactions with hVMAT2 and serotonin, dopamine, and hSigma1 receptors may not explain psychoactive effects.

TL;DR: SFN regulates Nrf2's CpGs demethylation and reactivation in TRAMP C1 cells, suggesting SFN may exert its chemopreventive effect in part via epigenetic modifications of NRF2 gene with subsequent induction of its downstream anti-oxidative stress pathway.

TL;DR: The need to develop tumor-targeting drug carrier systems affecting both the tumor cells and the tumor environment is highlighted and some newly identified putatively targetable ER partners are reviewed.

TL;DR: The reactivity of ebselen with protein thiols has helped to identify novel, selective targets for inhibitory actions on several enzymes of importance in pharmacology and toxicology, and initial concerns about selenium toxicity, fortunately, were unfounded.

TL;DR: The goal would be to further aggravate the pre-existing stress conditions in tumor cells with appropriate pharmacological agents, so that the already engaged pro-survival mechanism would be overwhelmed and the ER stress response forced to switch to its pro-apoptotic mode.

TL;DR: Gen knock out studies suggest that AhR is indispensable for the postnatal maintenance of intestinal intraepithelial lymphocytes and skin-resident dendritic epidermal gamma delta T cells, providing a potential link between AhR and gut immunity and wound healing.

TL;DR: Impaired activity of SIRT1 induces endothelial dysfunction and up-regulates NADPH oxidase-derived ROS production in the vascular wall, mimicking the vascular aging phenotype.

TL;DR: OCT1 plays an important role in the hepatocellular uptake of morphine and carriers of loss-of-function OCT1 polymorphisms may be at higher risk of adverse effects after codeine administration, especially if they are also ultra-rapid CYP2D6 metabolizers.

TL;DR: Glycogen synthase kinase-3 (GSK-3) is a serine/threonine protein kinase that phosphorylates and inhibits GSK-3, thereby inhibiting glycogen synthesis from glucose as mentioned in this paper.

TL;DR: Using a murine model of acute liver injury caused by overdose of acetaminophen, mechanistic studies suggest that hypoxia-inducible factor (HIF) may be involved in regulating the angiogenic effect of hepatic macrophages (Macs) and indicate an important role for hepatic Macs in liver blood vessel repair, thereby contributing to tissue recovery from acute injury.

TL;DR: The major advances in the study of GSC role in GBM and the therapeutic implications resulting from them are discussed, thus reporting the latest strategies applied to counteract and overcome GBM intrinsic resistance to therapy for a better management of patients.

TL;DR: The tumor promoting function of TGF-β and its possible promise as a therapeutic target in high grade gliomas, including glioblastoma multiforme (GBM), a disease with very poor prognosis is reviewed.

TL;DR: A conserved cation-π interaction between ligand and aromatic residues of the ligand binding site critically contributes to ligand recognition, as revealed by X-ray crystal structures of acetylcholine binding proteins, as well as the integral pLGICs, ELIC and GluCl.

TL;DR: Laboratory and clinical evidence suggest that NAG-1, like other TGF-β family members, may have different or pleiotropic functions in the early and late stages of carcinogenesis and may serve as a potential biomarker for the diagnosis and prognosis of cancer.

TL;DR: The present review summarizes the discoveries made to date regarding PIM kinases as driving oncogenes in the process of tumorigenesis and their validation as drug targets.

TL;DR: The mechanisms by which tumor cells exposed to targeted therapies co-opt the host leading to therapeutic escape and resistance are outlined and the idea that long-term responses to targeted anticancer therapies will only be achieved through strategies that target both the tumor and host is discussed.

TL;DR: Antiviral therapy is obviously needed to control those infections that are not amenable to prophylaxis by vaccination, but is also highly desirable for those infections where vaccination has not been implemented or did not fulfill its premises for complete protection.

TL;DR: New evidence supports enhancement of mitochondrial respiratory function as a generalizable therapeutic principle relevant to highly adaptable systems that are exquisitely sensitive to energy availability such as the nervous system.

TL;DR: The efforts that have been made to target FOXM1 in cancer and the consequences ofFOXM1 suppression in human cancer cells are described and summarized.

TL;DR: It is suggested that AMPK activation by ROS can promote cell survival by inducing autophagy, mitochondrial biogenesis and expression of genes involved in antioxidant defense, and increased intracellular concentrations of ROS may represent a general mechanism for enhancement of AMPK-mediated cellular adaptation, including maintenance of redox homeostasis.

TL;DR: In this work, how nicotinic agonists may be acting in the PFC to influence cognitive function is reviewed, in light of the latest findings.

TL;DR: The accumulating evidence is positive, but more work is required using positron emission tomography to understand current alterations in α7 nAChR expression and their relationship to symptoms, and cross-species behavioral tasks should be used more regularly to determine the predictive efficacy of treatments.

TL;DR: Results strongly indicate that the co-treatment strategy with rapamycin can attenuate the cardiotoxic effects of DXR in a tumour-bearing mouse model.