Showing papers in "Biochemical Pharmacology in 2015"

TL;DR: A profound insight is provided into the role of the α7 nAChR subtype in microglia and point out to microglial α7/HO-1 pathway as an anti-inflammatory therapeutic target.

TL;DR: The aim of the present review is to present the main evidences of the pro-oxidant-related cytotoxic activity of naturally occurring polyphenols and their underlying mechanisms.

TL;DR: The pharmacological profiles of compounds that derived from these strategies and have been recently tested in clinical trials are reviewed and future directions for antidepressant research are outlined.

TL;DR: The aim in this article is to review important aspects of the pharmacological diversity of nAChR allosteric modulators and to describe recent evidence aimed at identifying binding sites at the same site as acetylcholine at the interface between two subunits.

TL;DR: It is proposed that atherosclerosis is associated with reduced ACE2 expression in heart and kidney and an unexplored potential of atorvastatin to up-regulate ACE2 via epigenetic histone modifications is shown.

TL;DR: There is reason to be optimistic that new technology for GPCR ligand discovery will help reverse the current narrowing of the pharmaceutical pipeline.

TL;DR: The effects of pharmacologically active compounds as modulators of different types of cancer cell death depending on the cellular context are summarized to highlight the potential role of these compounds for context-specific anticancer therapy.

TL;DR: Preeclampsia is a pregnancy-associated disorder characterized by hypertension, and could lead to maternal and fetal morbidity and mortality; however, the pathophysiological mechanisms involved are unclear.

TL;DR: It is demonstrated that wogonoside may exert its anti-inflammatory effect via dual inhibition of NF-κB and NLRP3 inflammasome, suggesting that woside might be a potential effective drug for inflammatory bowel diseases.

TL;DR: This study is the first to show that certain flavonoids are inhibitors of SASP production, partially related to NF-κB p65 and IκBζ signaling pathway, and may effectively protect or alleviate chronic low-grade inflammation in degenerative diseases such as cardiovascular diseases and late-stage cancer.

TL;DR: It is demonstrated that resveratrol can potentiate the anti-tumor effects of 5-FU on CRC cells by chemosensitizing them, inhibiting an EMT phenotype via up- regulation of intercellular junctions and by down-regulation of NF-κB pathway.

TL;DR: The pharmacological potential of selective mPGES-1 inhibitor classes as well as dual mPGes-1/5-lipoxygenase inhibitors is reviewed and pitfalls in their development, including species discrepancies and loss of in vivo activity, are discussed.

TL;DR: The inhibitory potency of a series of polyoxometalates as well as chalcogenide hexarhenium cluster complexes at a broad range of ecto-nucleotidases was evaluated and the polyoxoanionic compounds displayed a non-competitive mechanism of inhibition of NPPs and eN, but appeared to be competitive inhibitors of TNAP.

TL;DR: Oral administration of COS prevented the development of aberrant crypt foci in a mouse model of colitis-associated colorectal cancer (CRC) via a mechanism involving AMPK activation-induced β-catenin suppression and caspase-3 activation.

TL;DR: The role of DJ-1 in transformation is discussed, some of the significant aspects of and prospects for therapeutically targeting theDJ-1 signaling in cancer are highlighted, and what the future may hold are described.

TL;DR: The results suggest that the inhibitory effect of CUR on anchorage-independent growth of HT29 cells could, at least in part, involve the epigenetic demethylation and up-regulation of DLEC1.

TL;DR: Copy number variants have been implicated in multiple neuropsychiatric conditions, including autism spectrum disorder (ASD), schizophrenia, and intellectual disability, and Chromosome 15q13 is a hotspot for such CNVs due to the presence of low copy repeat (LCR) elements, which facilitate non-allelic homologous recombination (NAHR).

TL;DR: It is suggested that α7 nAChRs may be useful targets for reducing Parkinson's disease progression and for the management of the dyskinesias that arise with l-dopa therapy.

TL;DR: EGCG possesses cardioprotective action against DOX-induced cardiotoxicity by suppressing oxidative stress, inflammation and apoptotic signals as well as activation of pro-survival pathways.

TL;DR: The role of IGF-1 signaling cascade in the prevalence of metabolic syndrome in particular the susceptibility to overnutrition and sedentary life style-induced obesity, dyslipidemia, insulin resistance and other features of metabolic Syndrome will be discussed.

TL;DR: Recent advances in developing inhibitors of MmpL proteins are reviewed, in the challenging context of targeting membrane proteins and the future prospects for potential antituberculosis drug candidates are reviewed.

TL;DR: Different mitochondrial functions that are affected during bacterial infection as well as different strategies developed by bacterial pathogens to subvert functions related to calcium homeostasis, maintenance of redox status and mitochondrial morphology are discussed.

TL;DR: The results indicate that the enhanced cytotoxicity of the Pt(IV)-VPA conjugates is a consequence of several processes involving enhanced cellular accumulation, downregulation of HDACs and yet other biochemical processes (not involvingHDACs) which may potentiate antitumor effects.

TL;DR: Overall, the studies reviewed here suggest that nicotine alters behaviors related to fear and anxiety and that nicotine contributes to the development, maintenance, and reoccurrence of anxiety disorders.

TL;DR: In this article, the authors used siRNA to knockdown TAS2R38 from NCI-H716 cells, which showed that siRNA knockdown of the TAS 2R38 reduced berberine-induced GLP-1 secretion.

TL;DR: Data indicate that nitrogen-atom-lacking pattern is a successful strategy to improve anti- inflammatory property of PL, and that the novel molecule, PL-0N may be served as a promising lead for developing natural product-directed anti-inflammatory agents.

TL;DR: Mechanisms whereby WA reduces necrotic hepatocyte injury, and demonstrate that WA has therapeutic potential in AILI are shown.

TL;DR: This commentary provides a useful overview of the role of IL-6 in both autoimmune diseases and cancers from the laboratory as well as clinical perspectives.

TL;DR: Although EBOV is highly contagious and transmitted by direct contact with body fluids, it could be counteracted by the adequate chemoprophylactic and -therapeutic interventions: vaccines, antibodies, siRNAs (small interfering RNAs), interferons and chemical substances.

TL;DR: NBS-1120 was better than aspirin as a chemopreventive agent; it dose-dependently inhibited tumor growth and tumor mass and showed similar anti-inflammatory, analgesic, anti-pyretic, and anti-platelet activities.