Showing papers in "Biochemical Pharmacology in 2007"

TL;DR: The hypothesis that metallo-beta-lactamases may be the result of divergent evolution starting from an ancestral protein which did not have a beta- lactamase activity is suggested.

TL;DR: HMATE1 and hMATE2-K function together as a detoxication system, by mediating the tubular secretion of intracellular ionic compounds across the brush-border membranes of the kidney.

TL;DR: The full potential of these inhibitors (epigenetic modulators) is still on the horizon, as the true breadth of their utility as anti-cancer agents will be determined by the careful analysis of gene expression changes generated by these inhibitors and then combined with conventional chemotherapy to synergistically improve response and toxicity for an overall enhanced therapeutic benefit to the patient.

TL;DR: This review will critically discuss the applications of chemical and dietary chemoprevention, intending the protecting effects against cancer of chemically synthesized molecules, or phytochemicals present in the regular diet.

TL;DR: Results indicate that curcumin has nutritional potential as a naturally occurring anti-inflammatory agent for treating OA through suppression of NF-kappaB mediated IL-1beta/TNF-alpha catabolic signalling pathways in chondrocytes.

TL;DR: Tightened coupling between Phases I and II by AhR- and Nrf2-induced XMEs may greatly attenuate health risks posed by CYP1A1-generated toxic intermediates and reactive oxygen species, and better recognition of coordinate Phase I andII metabolisms may improve risk assessment of reactive toxic intermediate in the extrapolation to low level endo- and xenobiotic exposure.

TL;DR: In this article, a review of rodent brain subtypes is presented by discussing their subunit composition, pharmacology and localisation and, when possible, comparing them with the same subtypes present in the brain of other mammalian species or chick.

TL;DR: Anthocyanin (cyanidin 3-glucoside; C3G) which is a pigment widespread in the plant kingdom, ameliorates hyperglycemia and insulin sensitivity due to the reduction of retinol binding protein 4 (RBP4) expression in type 2 diabetic mice.

TL;DR: An emerging hypothesis is that PAX proteins play an essential role in maintaining tissue specific stem cells by inhibiting terminal differentiation and apoptosis and that these functional characteristics may facilitate the development and progression of specific cancers.

TL;DR: Given the important role of FAK in a large number of processes involved in tumorigenesis, metastasis and survival signalling FAK should be regarded as a potential target in the development of anti-cancer drugs.

TL;DR: The results indicated that the neuroprotective effect of UA against D-gal induced neurotoxicity might be caused, at least in part, by the increase in the activity of antioxidant enzymes with a reduction in lipid peroxidation.

TL;DR: This review summarizes studies that attempted to determine the subtypes of nicotinic acetylcholine receptors (nAChR) expressed in the dopaminergic nerve terminals in the mouse, finding three subtypes that contain the alpha6 subunit and bind alpha-CtxMII with high affinity.

TL;DR: The evidence that norepinephrine (NE) is neuroprotective and that LC degeneration sensitizes DA neurons to damage is examined, and the potential contribution of NE loss to the behavioral symptoms associated with PD is examined.

TL;DR: It is found that cinnamaldehyde perturbs the Z-ring morphology in vivo and reduces the frequency of the Z ring per unit cell length of Escherichia coli and GTP dependent FtsZ polymerization is inhibited by cinn amaldehyde.

TL;DR: The nephrotoxicity of platinum agents was closely associated with their renal accumulation, which is determined by the substrate specificity of the OCT and MATE families.

TL;DR: The calcium channel antagonists are a mature group of drugs directed at cardiovascular diseases including hypertension, angina, peripheral vascular disorders and some arrhythmic conditions and potential new directions are indicated including male fertility, bone growth, immune disorders, cancer and schistosomiasis.

TL;DR: The recent discovery of chemically heterogeneous group of molecules capable of differentially modifying nAChR properties without interacting at the ligand binding site illustrates the adequacy of the allosteric model to predict functional consequences.

TL;DR: Over the next decade, it is anticipated that additional NCEs including antagonists and allosteric modulators (both positive and negative), interacting with various nAChR subtypes, will be advanced to the clinic in areas of high unmet medical need, e.g., pain, neurodegeneration, to provide novel medications with improved efficacy.

TL;DR: Sr(2+) is a full CaR agonist in HEK-CaR and POB, and, therefore, the anabolic effect of Sr( 2+) on bone in vivo could be mediated, in part, by the CaR.

TL;DR: Examination of additional flavone structures indicated that methylated flavones in general have antiproliferative properties, and it was demonstrated that 5,7-dimethoxyflavone was well absorbed and had high oral bioavailability as well as tissue accumulation in vivo in the rat.

TL;DR: It is found that resveratrol prevented accumulation of reactive oxygen species, depletion of cellular glutathione, and cellular oxidative damage induced by MPP(+), suggesting involvement of antioxidative properties in the neuroprotective action of resver atrol.

TL;DR: A striking finding is that variations in maternal separation and handling cause changes in ethanol and cocaine self-administration, which indicates that various manipulations in the perinatal period can have long lasting effects of interest to biochemical pharmacologists.

TL;DR: It is suggested that cucurbitacin glucosides exhibit pleiotropic effects on cells, causing both cell cycle arrest and apoptosis, and might have therapeutic value against breast cancer cells.

TL;DR: The investigation of a new bis-chelated Au(I) bidentate phosphine complex of the novel water soluble ligand 1,3-bis(di-2-pyridylphosphino)propane (d2pypp) shows that this gold complex, at submicromolar concentrations, selectively induces apoptosis in breast cancer cells but not in normal breast cells.

TL;DR: Together, the presynaptic and postsynaptic effects of nAChRs generate and facilitate the induction of long-term changes in synaptic transmission, which may prove efficacious in the treatment of neuropathologies where synaptic transmission is compromised, as in Alzheimer's or Parkinson's disease.

TL;DR: Evidence is provided for a reversible crosstalk between histone acetylation and DNA demethylation, which has significant implications on the use of HDAC inhibitors as therapeutic agents.

TL;DR: A dose- and time-dependent down-regulation of expression of cyclin E by curcumin is demonstrated that correlates with the decrease in the proliferation of human prostate and breast cancer cells, suggesting the role of ubiquitin-dependent proteasomal pathway.

TL;DR: Two classes of wake-improving agents are distinguished: the first acting through non-histaminergic mechanisms and the second acting via histamine and supports brain H(3)-receptors as potentially novel therapeutic targets for vigilance and sleep-wake disorders.

TL;DR: This is the first study to provide comprehensive information on the P- gp interaction profile of anti-HIV drugs under identical assay conditions and reveals that many compounds may indeed inhibit P-gp substantially and indicates that of the various systems tested, the calcein assay in P388/dx/P388 cells is the most suitable and reliable in vitro model for the quantification of P-GP inhibition.

TL;DR: This review summarizes the expression of individual PLA(2) in cancers, focuses on the potential mechanisms by which these esterases mediate carcinogenesis, and suggests that select PLA( 2) isoforms may be targets for anti-cancer drugs.