Showing papers in "Biochemical Pharmacology in 2010"

TL;DR: This review covers how redox-dependent transcriptional activators such as NF-E2 related factor 2, NF2, NF-κB and AP-1 along with the transcription repressor BTB and CNC homologue 1 (Bach1) control the inducible HO-1 gene expression and the role of central pro- and anti-inflammatory cellular signaling cascades including p38 MAPK and phosphatidylinositol-3 kinase (PI3K)/

TL;DR: It is demonstrated that curcumin-loaded PLGA nanoparticles formulation has enhanced cellular uptake, and increased bioactivity in vitro and superior bioavailability in vivo overCurcumin.

TL;DR: The molecular targets of the tocotrienols and their roles in cancer, bone resorption, diabetes, and cardiovascular and neurological diseases at both preclinical and clinical levels are examined.

TL;DR: It is emphasized how increased understanding of the chemopreventive effects of dietary polyphenols on specific epigenetic alterations may provide unique and yet unexplored novel and highly effective chemopresventive strategies for reducing the health burden of cancer and other diseases in humans.

TL;DR: The cellular/molecular mechanisms supporting the detrimental or beneficial features of astrogliosis have been scrutinized to gain insights on possible pharmacological approaches to enhance astrocyte neuroprotective activities.

TL;DR: The interesting timing of pro- and anti-inflammatory effects, such as those affecting lipoxygenase activity, suggests that melatonin might promote early phases of inflammation on one hand and contribute to its attenuation on the other hand, in order to avoid complications of chronic inflammation.

TL;DR: Findings demonstrate for the first time the involvement of miRNAs in multidrug resistance mediated by MRP-1 and suggest that miR-326 may be an efficient agent for preventing and reversing MDR in tumor cells.

TL;DR: The potential targeting of these essential protein kinases therapeutically is discussed, given their critical role in IL-1/TLR signalling, and the IRAK family members have been implicated in certain disease models including human immunodeficiencies.

TL;DR: The data demonstrate that Withaferin A binds Hsp90, inhibits HSp90 chaperone activity through an ATP-independent mechanism, results in Hsp 90 client protein degradation, and exhibits in vivo anticancer activity against pancreatic cancer.

TL;DR: The potential of nanotechnology to fill the gap in suppressing chronic inflammation by packaging nutraceuticals packaged as nanoparticles and proven to be useful in "nanochemoprevention" and "nano-chemotherapy" is described.

TL;DR: Gold(I) compounds were found to induce antiproliferative effects towards several human cancer cells some of which endowed with cisplatin or multidrug resistance, and were able to activate caspase-3 and induce apoptosis observed as nucleosome formation and sub-G1 cell accumulation.

TL;DR: The data suggest that isoform selective inhibition of PKM2 with small molecules is feasible and support the hypothesis that inhibition of glucose metabolism in cancer cells is a viable strategy to treat human malignancy.

TL;DR: The results indicate that many currently approved pharmaceuticals have previously unappreciated effects on NF-kappaB signaling, which may contribute to anticancer therapeutic effects.

TL;DR: The different ginsenosides in American ginseng, both the naturally occurring compounds and those resulting from steaming or biotransformation are introduced, and the possible structural-function relationship with a focus on sugar molecules, hydroxyl groups and stereoselectivity in gINSenosides is explored.

TL;DR: The results establish that protective properties of resveratrol may arise at least in part from its capability to modify the composition of microRNA populations in cells, and suggest that the manipulation of the levels of key microRNAs, such as miR-663, may help to potentiate the anti-cancer and anti-metastatic effects of resVeratrol.

TL;DR: The results show that the flow-based coculture system is capable of clearing, with improved resolution and predictive value, compounds with high, medium, and low clearance values, and when coculture is coupled with flow, higher metabolite production rates are obtained than in static systems.

TL;DR: The main thyroid-disrupting chemicals are surveyed, and the review then focuses on disrupting mechanisms known to be directly or indirectly related to the transcriptional activity of the thyroid hormone receptors.

TL;DR: Inhibitory serine-phosphorylation of GSK3 was lower in Fmr1 knockout, than wild-type, mouse brain regions and was increased by acute or chronic lithium treatment, which also increased hippocampal brain-derived neurotrophic factor levels.

TL;DR: The current understanding of GSC biology is summarized with a focus on potential anti-GSC therapies and suggests that GSCs may be important therapeutic targets not only to achieve cure but even reduce tumor relapse and improve overall survival.

TL;DR: The use of nanotechnology is reviewed as an approach to target the MAPK pathway using both genetic and pharmacological agents simultaneously targeting multiple points in the pathway or in combination with other cascades.

TL;DR: A novel small-molecule is identified that binds with a high affinity to Stat3, blocks Stat3 activation and function, and thereby induces antitumor response in human breast tumor xenografts harboring persistently active Stat3.

TL;DR: MATE1 mediates the efflux of cisPlatin and is involved in cisplatin-induced nephrotoxicity, and the combination of a selective MATE inhibitor, pyrimethamine, with cis platin also elevated creatinine and BUN levels compared to cisplasin alone.

TL;DR: The ability to selectively manipulate physiological functions, through activation of defined signalling cascades, will in all likelihood help in the development of efficacious and safe cannabinoid-based therapeutics for a variety of indications.

TL;DR: Some of the recent advances in both, the understanding of BRAF function in melanoma and the development of improved BRAF targeting inhibitors are discussed, suggesting strategies for the design of improved, more efficient combinatorial therapies.

TL;DR: A20 functions in a negative feedback loop, which mediates its inhibitory functions by downregulating key proinflammatory signaling pathways, including those controlling NF-κB- and IRF3-dependent gene expression.

TL;DR: The antioxidant N-acetyl-L-cysteine (NAC) represents a potential additional treatment option that could be considered in the case of an influenza A virus pandemic.

TL;DR: The present results suggest that nobiletin improved the hyperglycemia and insulin resistance in obese diabetic ob/ob mice by regulating expression of Glut1 and Glut4 in WAT and muscle, and expression of adipokines in W AT.

TL;DR: It is proposed that the Notch signaling pathway may represent novel therapeutic targets and will be a welcome asset to the cancer therapeutic arena.

TL;DR: The evidence from the rodent to the human implicating RAGE in the diverse disease states in which its ligands accumulate is reviewed, holding promise for the identification of potential therapeutic targets and/or biomarkers of RAGE activity in disease.

TL;DR: AICAR-initiated AMPK activation may act as a central downregulator in ongoing innate and adaptive immune responses of murine colitis, providing a novel therapeutic approach in the treatment of IBD.