abstract：:CREB-mediated transcription can be initiated by membrane receptor stimulation and subsequent activation of intracellular pathways to the cell nucleus, and has been described as a molecular switch required for learning and memory. While CREB dimers are thought to be constitutively bound to response elements on DNA unde...

journal_title：Biochemical pharmacology

authors： Scott Bitner R

更新日期：2012-03-15 00:00:00

abstract：:Angiogenesis, the development of neovessels from pre-existing vessels, is obligatory for solid tumors survival, growth, invasion, and metastasis. Many anti-angiogenic agents are small molecules originated from natural sources. Recently, angiosuppressive effects of indirubin and its derivatives, the active components i...

journal_title：Biochemical pharmacology

authors： Chan YK,Kwok HH,Chan LS,Leung KS,Shi J,Mak NK,Wong RN,Yue PY

更新日期：2012-03-01 00:00:00

abstract：:The peptide hormone gastrin binds two ferric ions with high affinity, and iron binding is essential for the biological activity of non-amidated gastrins in vitro and in vivo. Bi3+ ions also bind to glycine-extended gastrin17 (Ggly), but inhibit Ggly-induced cell proliferation and migration in gastrointestinal cell lin...

journal_title：Biochemical pharmacology

authors： Kovac S,Loh SW,Lachal S,Shulkes A,Baldwin GS

更新日期：2012-02-15 00:00:00

abstract：:Multiple sclerosis (MS) is a severe chronic T cell-mediated autoimmune inflammatory disease of the central nervous system (CNS), the existing therapy of which is only partially effective and is associated with undesirable side effects. Euphol, an alcohol tetracyclic triterpene, has a wide range of pharmacological prop...

journal_title：Biochemical pharmacology

authors： Dutra RC,de Souza PR,Bento AF,Marcon R,Bicca MA,Pianowski LF,Calixto JB

更新日期：2012-02-15 00:00:00

abstract：:The PI3K/AKT/mTOR signaling pathway regulates cell proliferation, survival and angiogenesis. The mammalian target of rapamycin (mTOR) is a protein kinase ubiquitously expressed within cells that regulates cell growth and survival by integrating nutrient and hormonal signals. mTOR exists in two complexes, mTORC1 and mT...

journal_title：Biochemical pharmacology

authors： Espona-Fiedler M,Soto-Cerrato V,Hosseini A,Lizcano JM,Guallar V,Quesada R,Gao T,Pérez-Tomás R

更新日期：2012-02-15 00:00:00

abstract：:A set of sulfamides designed, synthesized and evaluated against maximal electroshock seizure (MES) and pentilenetetrazol (PTZ) tests with promising results, were tested for their affinity for the benzodiazepine binding site of the GABA(A) receptor. The most active compounds, N,N'-dicyclohexylsulfamide (7) and N,N'-dip...

journal_title：Biochemical pharmacology

authors： Wasowski C,Gavernet L,Barrios IA,Villalba ML,Pastore V,Samaja G,Enrique A,Bruno-Blanch LE,Marder M

更新日期：2012-01-15 00:00:00

abstract：:We previously demonstrated that the widely used immunosuppressive drugs cyclosporin A (CsA) and tacrolimus (FK506), independent of immunophilin binding, can activate profibrogenic transforming growth factor β (TGFβ)/Smad signaling cascades in rat renal mesangial cells (MC). Here we report that both peptidyl-prolyl cis...

journal_title：Biochemical pharmacology

authors： Akool el-S,Gauer S,Osman B,Doller A,Schulz S,Geiger H,Pfeilschifter J,Eberhardt W

更新日期：2012-01-15 00:00:00

abstract：:5-Lipoxygenase (5-LO) is a crucial enzyme of the arachidonic acid (AA) cascade and catalyzes the formation of bioactive leukotrienes (LTs) which are involved in inflammatory diseases and allergic reactions. The pathophysiological effects of LTs are considered to be prevented by 5-LO inhibitors. In this study we presen...

journal_title：Biochemical pharmacology

authors： Wisniewska JM,Rödl CB,Kahnt AS,Buscató El,Ulrich S,Tanrikulu Y,Achenbach J,Rörsch F,Grösch S,Schneider G,Cinatl J Jr,Proschak E,Steinhilber D,Hofmann B

更新日期：2012-01-15 00:00:00

abstract：:Carbonyl reductase activity catalyzes the two electron reduction of several endogenous and exogenous carbonyl substrates. Recent data indicate that the expression of human carbonyl reductase 3 (CBR3) is regulated by the master redox switch Nrf2. Nrf2 binds to conserved antioxidant response elements (AREs) in the promo...

journal_title：Biochemical pharmacology

authors： Cheng Q,Kalabus JL,Zhang J,Blanco JG

更新日期：2012-01-01 00:00:00

abstract：:The Phosphatidylinositol 3-kinase (PI3K) inhibitor, LY294002 (LY2), has been previously reported to inhibit nuclear factor κB (NFκB) activity, in a PI3K-independent mechanism. The goals of the current research were to determine the specificity of LY2 regarding NFκB subunits, and to identify relevant modulation of cyto...

journal_title：Biochemical pharmacology

authors： Avni D,Glucksam Y,Zor T

更新日期：2012-01-01 00:00:00

abstract：:Vascular disrupting agents show selective effects on tumor established vasculature, and achieve encouraging results in both pre-clinical and clinical experiments. In the present study, we investigated the effects of a new CA4 derivative MDS-11 and its prodrug MDS-11P on vascular disrupting activity in vitro and in viv...

journal_title：Biochemical pharmacology

authors： Deng ZT,Feng T,Wang P,Qi X,Chen XH,Li YX,Song CL,Geng MY,Li J

更新日期：2011-12-15 00:00:00

abstract：:The so-called human xenosensors, constitutive androstane receptor (hCAR), pregnane X receptor (hPXR) and aryl hydrocarbon receptor (hAhR), participate in drug metabolism and transport as well as in several endogenous processes by regulating the expression of their target genes. While the ligand specificities for hPXR ...

journal_title：Biochemical pharmacology

authors： Küblbeck J,Laitinen T,Jyrkkärinne J,Rousu T,Tolonen A,Abel T,Kortelainen T,Uusitalo J,Korjamo T,Honkakoski P,Molnár F

更新日期：2011-12-15 00:00:00

abstract：:Hepatocellular carcinoma (HCC) is one of the most common causes of cancer-related death. Different signaling pathways are de-regulated in this pathogenesis, among them the epidermal growth factor receptor one (EGFR/Erb1). Here we show that blockage of this pathway by the tyrphostin 4-(3-chloroanilino)-6,7-dimethoxyqui...

journal_title：Biochemical pharmacology

authors： Caja L,Sancho P,Bertran E,Ortiz C,Campbell JS,Fausto N,Fabregat I

更新日期：2011-12-01 00:00:00

abstract：:Antibiotic resistance issues necessitate the continued discovery and development of new antibacterial agents. Efforts are ongoing in two approaches to find new compounds that are effective against antibiotic-resistant pathogens. These efforts involve modification of existing classes including fluoroquinolones, tetracy...

journal_title：Biochemical pharmacology

authors： Bush K,Pucci MJ

更新日期：2011-12-01 00:00:00

abstract：:Alzheimer's disease (AD), the most common form of dementia, is characterized by the deposition of amyloid plaques, accumulation of fibrillary tangles in neurons, neurite degeneration, loss of neurons, and a progressive loss of cognitive function. The pathogenesis of AD is not fully understood, and no strong disease-mo...

journal_title：Biochemical pharmacology

authors： Zeng F,Lu JJ,Zhou XF,Wang YJ

更新日期：2011-11-15 00:00:00

abstract：:The Wnt/Frizzled signaling pathway plays multiple functions in animal development and, when deregulated, in human disease. The G-protein coupled receptor (GPCR) Frizzled and its cognate heterotrimeric Gi/o proteins initiate the intracellular signaling cascades resulting in cell fate determination and polarization. In ...

journal_title：Biochemical pharmacology

authors： Koval A,Purvanov V,Egger-Adam D,Katanaev VL

更新日期：2011-11-15 00:00:00

abstract：:PI3K cascade is a central signaling pathway regulating cell proliferation, growth, differentiation, and survival. Tight regulation of the PI3K signaling pathway is necessary to avoid aberrant cell proliferation and cancer development. Together with SHIP-1, the inositol phosphatases PTEN and SHIP-2 are the gatekeepers ...

journal_title：Biochemical pharmacology

authors： Condé C,Gloire G,Piette J

更新日期：2011-11-15 00:00:00

abstract：:Neutrophils play a key role in host defense and inflammation through the production of superoxide anion and other reactive oxygen species (ROS) by the enzyme complex NADPH oxidase. The cytosolic NADPH oxidase component, p67phox, has been shown to be phosphorylated in human neutrophils but the pathways involved in this...

journal_title：Biochemical pharmacology

authors： Dang PM,Raad H,Derkawi RA,Boussetta T,Paclet MH,Belambri SA,Makni-Maalej K,Kroviarski Y,Morel F,Gougerot-Pocidalo MA,El-Benna J

更新日期：2011-11-01 00:00:00

abstract：:Son of Sevenless (SOS) was discovered in Drosophila melanogaster. Essential for normal eye development in Drosophila, SOS has two human homologues, SOS1 and SOS2. The SOS1 gene encodes the Son of Sevenless 1 protein, a Ras and Rac guanine nucleotide exchange factor. This protein is composed of several important domain...

journal_title：Biochemical pharmacology

authors： Pierre S,Bats AS,Coumoul X

更新日期：2011-11-01 00:00:00

abstract：:The peroxisome proliferator activated receptor-γ (PPAR-γ) is involved in the pathogenesis of diabetic retinopathy. Diabetic retinopathy is a preventable microvascular diabetic complication that damages human retinal pigment epithelial cells. Taurine is abundant in the fruit of Lycium barbarum (Goji Berry), and is repo...

journal_title：Biochemical pharmacology

authors： Song MK,Salam NK,Roufogalis BD,Huang TH

更新日期：2011-11-01 00:00:00

abstract：:The human α7 neuronal nicotinic acetylcholine receptor gene (CHRNA7) is a candidate gene for schizophrenia and an important drug target for cognitive deficits in the disorder. Activation of the α7*nAChR, results in opening of the channel and entry of mono- and divalent cations, including Ca(2+), that presynaptically p...

journal_title：Biochemical pharmacology

authors： Araud T,Graw S,Berger R,Lee M,Neveu E,Bertrand D,Leonard S

更新日期：2011-10-15 00:00:00

abstract：:Neuronal nicotinic acetylcholine receptors (nAChR), recognized targets for drug development in cognitive and neuro-degenerative disorders, are allosteric proteins with dynamic interconversions between multiple functional states. Activation of the nAChR ion channel is primarily controlled by the binding of ligands (ago...

journal_title：Biochemical pharmacology

authors： Williams DK,Wang J,Papke RL

更新日期：2011-10-15 00:00:00

abstract：:Protein kinase D (PKD) is a subfamily of serine/threonine specific family of kinases, comprised of PKD1, PKD2 and PKD3 (PKCμ, PKD2 and PKCv in humans). It is known that PKCs activate PKD, but the relative expression of isoforms of PKD or the specific PKC isoform/s responsible for its activation in platelets is not kno...

journal_title：Biochemical pharmacology

authors： Bhavanasi D,Kim S,Goldfinger LE,Kunapuli SP

更新日期：2011-10-01 00:00:00

abstract：:Current epidemiological and experimental studies support a beneficial role of dietary polyphenols in several gastrointestinal diseases, including inflammatory bowel disease. The aim of this study was to gain a better understanding of the effects of a naturally occurring polyphenol, ellagic acid, present in some fruits...

journal_title：Biochemical pharmacology

authors： Rosillo MA,Sanchez-Hidalgo M,Cárdeno A,de la Lastra CA

更新日期：2011-10-01 00:00:00

abstract：:Nonsteroidal anti-inflammatory drugs (NSAIDs) are now understood to fall into one of two agent classes in clinical use. Traditional NSAIDs inhibit both cyclooxygenases-1 and 2 (COX-1, 2), which act as key enzymes catalyzing the same reaction in the production of prostaglandins (PGs), while the second class of NSAIDs s...

journal_title：Biochemical pharmacology

authors： Imanishi J,Morita Y,Yoshimi E,Kuroda K,Masunaga T,Yamagami K,Kuno M,Hamachi E,Aoki S,Takahashi F,Nakamura K,Miyata S,Ohkubo Y,Mutoh S

更新日期：2011-10-01 00:00:00

abstract：:Evasion of cell death by overexpression of anti-apoptotic proteins, such as Bcl-2, is commonly observed in cancer cells leading to a lack of response to chemotherapy. Hence, there is a need to find new chemotherapeutic agents that are able to overcome chemoresistance mediated by Bcl-2 and to understand their mechanism...

journal_title：Biochemical pharmacology

authors： Hoffmann R,von Schwarzenberg K,López-Antón N,Rudy A,Wanner G,Dirsch VM,Vollmar AM

更新日期：2011-09-01 00:00:00

abstract：:Polyamines (putrescine, spermidine and spermine) are aliphatic amines that are produced by the action of ornithine decarboxylase (ODC) in a rate-limiting and protein kinase C (PKC)-regulated step. Because high levels of polyamines are found in the synovial fluid of arthritic patients, the aim of the present study was ...

journal_title：Biochemical pharmacology

authors： Silva MA,Klafke JZ,Rossato MF,Gewehr C,Guerra GP,Rubin MA,Ferreira J

更新日期：2011-08-01 00:00:00

abstract：:It has become apparent of late that even in tamoxifen and/or aromatase resistant breast cancers, ERα remains a bona fide therapeutic target. Not surprisingly, therefore, there has been considerable interest in developing Selective ER Degraders (SERDs), compounds that target the receptor for degradation. Currently, ICI...

journal_title：Biochemical pharmacology

authors： Wardell SE,Marks JR,McDonnell DP

更新日期：2011-07-15 00:00:00

abstract：:Breast cancer resistance protein (BCRP; ABCG2), a clinical marker for identifying the side population (SP) cancer stem cell subgroup, affects intestinal absorption, brain penetration, hepatobiliary excretion, and multidrug resistance of many anti-cancer drugs. Nutlin-3a is currently under pre-clinical investigation in...

journal_title：Biochemical pharmacology

authors： Zhang F,Throm SL,Murley LL,Miller LA,Steven Zatechka D Jr,Kiplin Guy R,Kennedy R,Stewart CF

更新日期：2011-07-01 00:00:00

abstract：:It was previously shown that [Pt(O,O'-acac)(γ-acac)(DMS)] induces apoptosis in various cancer cells and exerts antimetastatic responses in vitro. In rats, [Pt(O,O'-acac)(γ-acac)(DMS)] reaches the central nervous system in quantities higher than cisplatin causing less excitotoxicity. The aim of the present paper was to...

journal_title：Biochemical pharmacology

authors： Muscella A,Calabriso N,Vetrugno C,Fanizzi FP,De Pascali SA,Marsigliante S

更新日期：2011-06-01 00:00:00

abstract：:Cudratricusxanthone G (CTXG), a natural bioactive cudratricusxanthone extracted from C. tricuspidata, has shown anti-cancer properties. However, the function and mechanism of CTXG in tumor invasion have not been elucidated to date. In this study, we investigated the inhibitory effect of CTXG on the proliferation, migr...

journal_title：Biochemical pharmacology

authors： Kuang L,Wang L,Wang Q,Zhao Q,Du B,Li D,Luo J,Liu M,Hou A,Qian M

更新日期：2011-05-15 00:00:00

abstract：:Angiogenesis has emerged as a critical process for tumour progression. Identifying key pathways involved in the regulation and promotion of angiogenesis has resulted in the development of numerous approaches targeting pro-angiogenic signalling pathways. The most prominent and characterised pro-angiogenic pathway is th...

journal_title：Biochemical pharmacology

authors： Bridges EM,Harris AL

更新日期：2011-05-15 00:00:00

abstract：:Hepatic fibrosis is characterized by excess type I collagen deposition and exacerbated inflammatory response. Naltrexone, an opioid receptor antagonist used for treating alcohol abuse, attenuates hepatocellular injury in fibrotic animal models, which can be accompanied by deleterious side effects. Additionally, opioid...

journal_title：Biochemical pharmacology

authors： Day SA,Lakner AM,Moore CC,Yen MH,Clemens MG,Wu ES,Schrum LW

更新日期：2011-04-15 00:00:00

abstract：:Targeted drug therapy or "smart" drug delivery, potentially combined with simultaneous imaging modalities to monitor the delivery of drugs to specific tissues, is arguably the "holy grail" of pharmacology. Therapeutic approaches that exploit nanoparticles to deliver drugs selectively to cancer cells are currently cons...

journal_title：Biochemical pharmacology

authors： Garcia-Bennett A,Nees M,Fadeel B

更新日期：2011-04-15 00:00:00

abstract：:We previously demonstrated that prostaglandin (PG) E₂ stimulates adhesion of mastocytoma P-815 cells (P-815 cells) to the Arg-Gly-Asp (RGD)-enriched matrix via the PGE₂ receptor subtype EP4 [Hatae N, Kita A, Tanaka S, Sugimoto Y, Ichikawa A. Induction of adherent activity in mastocytoma P-815 cells by the cooperation ...

journal_title：Biochemical pharmacology

authors： Okada Y,Nishikawa J,Semma M,Ichikawa A

更新日期：2011-04-01 00:00:00

abstract：:Following our observation that erythrosine B (FD&C Red No. 3) is a relatively potent inhibitor of the TNF-R-TNFα and CD40-CD154 protein-protein interactions, we investigated whether this inhibitory activity extends to any other protein-protein interactions (PPI) as well as whether any other approved food colors posses...

journal_title：Biochemical pharmacology

authors： Ganesan L,Margolles-Clark E,Song Y,Buchwald P

更新日期：2011-03-15 00:00:00

abstract：:The pregnane X-receptor (PXR) is a promiscuous nuclear receptor primarily responsible for the induction of genes from the cytochrome P450 3A family. In this study, we used a previously described PXR/SRC tethered protein to establish two in vitro assays for identifying PXR ligands: automated ligand identification syste...

journal_title：Biochemical pharmacology

authors： Xiao L,Nickbarg E,Wang W,Thomas A,Ziebell M,Prosise WW,Lesburg CA,Taremi SS,Gerlach VL,Le HV,Cheng KC

更新日期：2011-03-01 00:00:00

abstract：:This study demonstrates that a long-lasting co-culture of neutrophil surrogates (HL-60 cells), minimally primed by platelet activating factor (PAF), and resting endothelial cells (EC) results in the elaboration of an hyper-adhesive endothelial surface, as measured by the increase in the expression of endothelial adhes...

journal_title：Biochemical pharmacology

authors： Allegra M,D'Acquisto F,Tesoriere L,Livrea MA,Perretti M

更新日期：2011-02-01 00:00:00

abstract：:Thioredoxin reductase (TR1) is a selenoprotein that is involved in cellular redox status control and deoxyribonucleotide biosynthesis. Many cancers, including lung, overexpress TR1, making it a potential cancer therapy target. Previous work has shown that TR1 knockdown enhances the sensitivity of cancer cells to antic...

journal_title：Biochemical pharmacology

authors： Poerschke RL,Moos PJ

更新日期：2011-01-15 00:00:00

abstract：:The well-known analgesic and antipyretic drug N-acetyl-p-aminophenol (acetaminophen; APAP) has been previously reported to affect MDR1 expression in rat liver. In this study, we have investigated the effect of subtoxic doses of APAP on MDR1 expression and activity in rat intestine and human intestinal cells. Administr...

journal_title：Biochemical pharmacology

authors： Ghanem CI,Arias A,Novak A,Carpini GD,Villanueva S,Blazquez AG,Marin JJ,Mottino AD,Rubio MC

更新日期：2011-01-15 00:00:00