Showing papers in "Biochemical Pharmacology in 2004"

TL;DR: Inactivation of the acetyltransferase function of either CBP or p300 in various experimental systems will no doubt teach us more about the specific biological roles of these proteins.

TL;DR: Oxidative stress regulates both signal transduction and chromatin remodeling which in turn impacts on pro-inflammatory responses in the lungs.

TL;DR: It is concluded that prodrugs offer a viable strategy to disentangle pharmacodynamic and pharmacokinetic optimization and to demonstrate some of the therapeutic benefits afforded by successful pro drug candidates.

TL;DR: There is obviously no direct structure-activity relationship for the various interactions of human AChE, OPs and oximes, indicating the superior inhibitory potency of organophosphonates.

TL;DR: Celecoxib, the first US FDA approved selective COX-2 inhibitor, initially developed for the treatment of adult rheumatoid arthritis and osteoarthritis, has been reported to reduce the formation of polyps in patients with familial adenomatous polyposis.

TL;DR: It is found that copper-mediated inhibition of purified 20S proteasome cannot be blocked by a reducing agent and that organic copper compounds do not generate hydrogen peroxide in the cells, suggesting that proteasomesome inhibition and apoptosis induction are not due to copper- mediated oxidative damage of proteins.

TL;DR: Investigation of the effects of resveratrol on the colon injury caused by intracolonic instillation of trinitrobenzenesulphonic acid in rats found it reduces the damage in experimentally induced colitis, alleviates the oxidative events and stimulates apoptosis.

TL;DR: The current review is an attempt to describe two sides of the NF-κB coin, as a friend and as a foe, which can mediate a wide variety of diseases including cancer.

TL;DR: Recent data obtained on the role of protein acetylation in the regulation of the NF-kappaB cascade are discussed, including reports of potentiation of NF- kappaB-mediated gene induction following deacetylase inhibition by trichostatin A or sodium butyrate.

TL;DR: A hypothesis is proposed that GABAergic interactions with the brain stress neurotransmitter corticotropin-releasing factor in specific elements of the extended amygdala may be an important component for the motivation for excessive drinking associated with the transition from social drinking to addiction.

TL;DR: It is shown that ART inhibited the growth of normal human umbilical endothelial cells and of KS-IMM cells that have been established from a Kaposi's sarcoma lesion obtained from a renal transplant patient, and its growth inhibitory activity correlated with the induction of apoptosis in KS- IMM cells.

TL;DR: It is demonstrated that P-gp modulation of opioid brain uptake varies substantially within this class of compounds, regardless of receptor subtype, which may influence the onset, magnitude, and duration of analgesic response.

TL;DR: Demethylation inhibitors are proposed here to be potential novel candidate antimetastatic agents, which would bring about methylation and silencing of metastatic genes.

TL;DR: Curcumin I is the most effective MDR modulator among curcuminoids, and may be used in combination with conventional chemotherapeutic drugs to reverse MDR in cancer cells.

TL;DR: Electrophysiologic and pharmacologic studies suggest that the vulnerable NMDA receptors in schizophrenia may be concentrated on cortico-limbic GABAergic interneurons, thereby linking these two neuropathologic features of the disorder.

TL;DR: It is demonstrated that C-PC induces apoptosis in K562 cells by cytochrome c release from mitochondria into the cytosol, PARP cleavage and down regulation of Bcl-2.

TL;DR: A molecular mechanism based on the effect of these compounds on the structure of biological membranes is proposed to account for their multiple biological activities.

TL;DR: The concept that the endogenous cannabinoid system is activated on demand suggests that a promising strategy to alleviate seizure frequency is the enhancement of endocannabinoid levels by inhibiting the cellular uptake and the degradation of these endogenous compounds.

TL;DR: The results suggest that flavonols derivatives as quercetin and kaempferol can stimulate osteoblastic activity, and such compounds may represent new pharmacological tools for the treatment of osteoporosis.

TL;DR: It is suggested that the IGF system and IGF-IR signalling may play a role in hepatocarcinogenesis and in deregulated proliferation and apoptosis of HCC cells, and care must be taken when designing combinations of antitumoural molecules for antineoplastic treatment.

TL;DR: Post-translational modification of chromatin histones governs a key mechanism of transcriptional regulation of nuclear receptors and cell-cycle control proteins, which alter the access of transcription factors and nuclear receptors to the promoters of target genes.

TL;DR: In a Phase II double-blind, placebo-controlled study in 110 patients with mild cognitive impairment (MCI), oral administration of SGS742 at a dose of 600 mg t.i.d. for 8 weeks significantly improved attention, in particular choice reaction time and visual information processing as well as working memory measured as pattern recognition speed.

TL;DR: The result suggests that curcumin most likely inhibits cell proliferation, cell-mediated cytotoxicity (CMC), and cytokine production by inhibiting NF-kappaB target genes involved in induction of these immune responses.

TL;DR: These new actions of niacin on several key effectors of reverse cholesterol transport out of the vessel wall provide a rational to expect regression of atherosclerosis and test the combination of niakin with statins for an overadditive clinical benefit.

TL;DR: Using the recombinant enzyme methioninase, methylselenol-generating chemiluminesence by superoxide (O2*-) is shown to be catalytic alone in oxidizing thiols, i.e. GSH, generating superoxide and inducing oxidative stress in direct proportion to its concentration.

TL;DR: The data indicate that apoptosis-inducing effects of celecoxib partly depend on COX-2 expression of the cells, whereas induction of a cell cycle block occurred COx-2 independently, which indicates that the anticarinogenic effects of Celecoxib can be explained by both COZ-2-dependent and -independent mechanisms.

TL;DR: In order to estimate the relationships between the amounts of resveratrol taken up by food or drink intake, and the several possible benefits illustrated from in vitro/in vivo experiments and from epidemiological studies, it is essential to demonstrate step by step the route of res veratrol from plasma to the cell active site.

TL;DR: This enzyme assay provides a useful method for future inhibition studies of 2-AG degrading enzyme(s) in brain membrane preparation having considerably higher MGL-like activity when compared to FAAH activity.

TL;DR: It is proposed that YC-1 is a good lead compound for the development of new anti-HIF-1, anticancer agents, which would improve the prognoses of many cancer patients.

TL;DR: Glyoxal cytotoxic effects of glyoxal and its ability to overcome cellular resistance to oxidative stress are focused on.