abstract：:Inhibition of glycogen synthase kinase (GSK)-3 and the consequent activation of the Wnt/β-catenin signaling pathway have been reported to increase bone volume. To develop a novel pharmacotherapy for injured bone, we investigated whether GSK-3 inhibitor was effective in promoting bone formation. In in vitro experiments...

journal_title：Biochemical pharmacology

authors： Arioka M,Takahashi-Yanaga F,Sasaki M,Yoshihara T,Morimoto S,Hirata M,Mori Y,Sasaguri T

更新日期：2014-08-15 00:00:00

abstract：:Praziquantel (PZQ), prescribed as a racemic mixture, is the most readily available drug to treat schistosomiasis. In the present study, ultra-performance liquid chromatography coupled with electrospray ionization quadrupole time-of-flight mass spectrometry (UPLC-ESI-QTOFMS) based metabolomics was employed to decipher ...

journal_title：Biochemical pharmacology

authors： Wang H,Fang ZZ,Zheng Y,Zhou K,Hu C,Krausz KW,Sun D,Idle JR,Gonzalez FJ

更新日期：2014-07-15 00:00:00

abstract：:Osteosarcoma is the most common primary malignancy of bone and is characterized by a high malignant and metastatic potential. Transforming growth factor alpha (TGF-α) is classified as the EGF (epidermal growth factor)-like family, which is involved in cancer cellular activities such as proliferation, motility, migrati...

journal_title：Biochemical pharmacology

authors： Hou CH,Lin FL,Tong KB,Hou SM,Liu JF

更新日期：2014-06-15 00:00:00

abstract：:Glucocorticoids (GCs) are steroid hormones widely used as coadjuvants in the treatment of solid tumors due to their anti-inflammatory effects. However, evidence show that they also may induce chemotherapy resistance, probably through their capacity to inhibit apoptosis triggered by antineoplastic drugs. GCs exert thei...

journal_title：Biochemical pharmacology

authors： Orqueda AJ,Dansey MV,Español A,Veleiro AS,Bal de Kier Joffé E,Sales ME,Burton G,Pecci A

更新日期：2014-06-15 00:00:00

abstract：:The development of the plasma cell tumor (PCT) model was the first widely accepted in vivo model of multiple myeloma (MM). Potter and colleagues used this chemically induced PCT model to study the pathophysiology of malignant plasma cells and also used it to screen anti-MM agents. Two decades later the C57BL/KaLwRij m...

journal_title：Biochemical pharmacology

authors： Sanchez E,Chen H,Berenson JR

更新日期：2014-06-01 00:00:00

abstract：:We reported that differentiation-inducing factor-1 (DIF-1), synthesized by Dictyostelium discoideum, inhibited proliferation of various tumor cell lines in vitro by suppressing the Wnt/β-catenin signaling pathway. However, it remained unexplored whether DIF-1 also inhibits tumor growth in vivo. In the present study, t...

journal_title：Biochemical pharmacology

authors： Takahashi-Yanaga F,Yoshihara T,Jingushi K,Igawa K,Tomooka K,Watanabe Y,Morimoto S,Nakatsu Y,Tsuzuki T,Nakabeppu Y,Sasaguri T

更新日期：2014-06-01 00:00:00

abstract：:Mucosal inflammation in patients with inflammatory bowel disease (IBD) is characterized by an alteration of prohormone chromogranin A (CgA) production. The recent demonstration of an implication of CgA in collagenous colitis and immune regulation provides a potential link between CgA-derived peptides (catestatin, CTS)...

journal_title：Biochemical pharmacology

authors： Rabbi MF,Labis B,Metz-Boutigue MH,Bernstein CN,Ghia JE

更新日期：2014-06-01 00:00:00

abstract：:Catalase is an antioxidant enzyme that catalyzes mainly the transformation of hydrogen peroxide into water and oxygen. Although catalase is frequently down-regulated in tumors the underlying mechanism remains unclear. Few transcription factors have been reported to directly bind the human catalase promoter. Among them...

journal_title：Biochemical pharmacology

authors： Glorieux C,Auquier J,Dejeans N,Sid B,Demoulin JB,Bertrand L,Verrax J,Calderon PB

更新日期：2014-05-15 00:00:00

abstract：:Spider venoms are replete with peptidic ion channel modulators, often with novel subtype selectivity, making them a rich source of pharmacological tools and drug leads. In a search for subtype-selective blockers of voltage-gated calcium (CaV) channels, we isolated and characterized a novel 39-residue peptide, ω-TRTX-C...

journal_title：Biochemical pharmacology

authors： Klint JK,Berecki G,Durek T,Mobli M,Knapp O,King GF,Adams DJ,Alewood PF,Rash LD

更新日期：2014-05-15 00:00:00

abstract：:The transient receptor potential vanilloid-4 (TRPV4) belongs to a family of ion channels and can be activated by warm temperature, hypotonicity, cell swelling or lipid mediators of the arachidonic cascade. The metabolites or events responsible for TRPV4 activation are associated with inflammation, arguing in favor of ...

journal_title：Biochemical pharmacology

authors： Vergnolle N

更新日期：2014-05-15 00:00:00

abstract：:Pelargonidin is a natural red pigment found in fruits and vegetables, and has been reported to exhibit various effects potentially beneficial for human health. However, the possible preventive effects of pelargonidin toward atherosclerosis and mechanisms involved have not been investigated to date. Here, we compared t...

journal_title：Biochemical pharmacology

authors： Son JE,Jeong H,Kim H,Kim YA,Lee E,Lee HJ,Lee KW

更新日期：2014-05-15 00:00:00

abstract：:Multidrug resistance (MDR) is a phenomenon where cancer cells become simultaneously resistant to anticancer drugs with different structures and mechanisms of action. MDR has been shown to be associated with overexpression of ATP-binding cassette (ABC) transporters. Here, we report that telatinib, a small molecule tyro...

journal_title：Biochemical pharmacology

authors： Sodani K,Patel A,Anreddy N,Singh S,Yang DH,Kathawala RJ,Kumar P,Talele TT,Chen ZS

更新日期：2014-05-01 00:00:00

abstract：:An important pathologic hallmark of Alzheimer's disease (AD) is neuroinflammation, a process characterized in AD by disproportionate activation of cells (microglia and astrocytes, primarily) of the non-specific innate immune system within the CNS. While inflammation itself is not intrinsically detrimental, a delicate ...

journal_title：Biochemical pharmacology

authors： Cudaback E,Jorstad NL,Yang Y,Montine TJ,Keene CD

更新日期：2014-04-15 00:00:00

abstract：:The increase in life expectancy has resulted in a high occurrence of dementia and Alzheimer's disease (AD). Research on AD has undergone a paradigm shift from viewing it as a disease of old age to taking a life course perspective. Several vascular, lifestyle, psychological and genetic risk factors influencing this lat...

journal_title：Biochemical pharmacology

authors： Imtiaz B,Tolppanen AM,Kivipelto M,Soininen H

更新日期：2014-04-15 00:00:00

abstract：:Alzheimer disease (AD) is a progressive neurodegenerative disorder characterized by severe cognitive impairment, inability to perform activities of daily living and mood changes. Statins, long known to be beneficial in conditions where dyslipidemia occurs by lowering serum cholesterol levels, also have been proposed f...

journal_title：Biochemical pharmacology

authors： Barone E,Di Domenico F,Butterfield DA

更新日期：2014-04-15 00:00:00

abstract：:The tyrosine kinase inhibitors (TKIs) and multikinase inhibitors (MKIs) are oncology drugs of increasing importance that have improved the treatment of multiple tumors types. In some patients these agents produce adverse effects, including pharmacokinetic drug-drug interactions, due to cytochrome P450 (CYP) inhibition...

journal_title：Biochemical pharmacology

authors： Gu R,Hibbs DE,Ong JA,Edwards RJ,Murray M

更新日期：2014-03-15 00:00:00

abstract：:Vinorelbine (VNR), a semisynthetic vinca alkaloid acquired from vinblastine, is frequently used as the candidate for intervention of solid tumors. Nevertheless, VNR-caused endothelial injuries may lead a mitigative effect of clinical treatment efficiency. A growing body of evidence reveals that aspirin is a potent ant...

journal_title：Biochemical pharmacology

authors： Tsai KL,Huang PH,Kao CL,Leu HB,Cheng YH,Liao YW,Yang YP,Chien Y,Wang CY,Hsiao CY,Chiou SH,Chen JW,Lin SJ

更新日期：2014-03-15 00:00:00

abstract：:Stroke is a neurological condition and may cause changes in hepatic drug-metabolizing enzymes. Hepatic CYP2B is involved in the metabolism of a variety of centrally active substances. The purpose of this study was to investigate the possible down-regulation mechanism of hepatic CYP2B after acute stroke. Using a rat mo...

journal_title：Biochemical pharmacology

authors： Bing Y,Zhu S,Jiang K,Dong G,Li J,Yang Z,Yang J,Yue J

更新日期：2014-02-15 00:00:00

abstract：:B-cell activating factor (BAFF) is involved in not only the physiology of normal B cells, but also the pathophysiology of aggressive B cells related to malignant and autoimmune diseases. However, how excessive BAFF promotes aggressive B-cell proliferation and survival is not well understood. Here we show that excessiv...

journal_title：Biochemical pharmacology

authors： Liang D,Zeng Q,Xu Z,Zhang H,Gui L,Xu C,Chen S,Zhang S,Huang S,Chen L

更新日期：2014-01-15 00:00:00

abstract：:There is intense interest in the development and application of animal models of CNS disorders to explore pathology and molecular mechanisms, identify potential biomarkers, and to assess the therapeutic utility, estimate safety margins and establish pharmacodynamic and pharmacokinetic parameters of new chemical entiti...

journal_title：Biochemical pharmacology

authors： McGonigle P

更新日期：2014-01-01 00:00:00

abstract：:Melatonin (MEL) has been proposed as a therapeutic agent for the oral cavity, due to its antioxidant and anti-inflammatory effects since periodontal diseases are aggravated by free radicals, and by disproportionate immunological response to plaque microorganism. In addition, MEL promotes bone formation. This study aim...

journal_title：Biochemical pharmacology

authors： Gómez-Florit M,Ramis JM,Monjo M

更新日期：2013-12-15 00:00:00

abstract：:To identify needed human equilibrative nucleoside transporter 4 (hENT4) inhibitors, we cloned and stably expressed the recombinant protein in PK15NTD (nucleoside transporter deficient) cells, and, investigated its interaction with a series of dipyridamole analogs synthesized in our laboratory. Compounds were tested in...

journal_title：Biochemical pharmacology

authors： Wang C,Lin W,Playa H,Sun S,Cameron K,Buolamwini JK

更新日期：2013-12-01 00:00:00

abstract：:Urotensin-II (UII), a cyclic undecapeptide, selectively binds the urotensin-II receptor (UT receptor), a G protein-coupled receptor (GPCR) involved in cardiovascular effects and associated with numerous pathophysiological conditions including hypertension, atherosclerosis, heart failure, pulmonary hypertension and oth...

journal_title：Biochemical pharmacology

authors： Sainsily X,Cabana J,Boulais PE,Holleran BJ,Escher E,Lavigne P,Leduc R

更新日期：2013-12-01 00:00:00

abstract：:Ibuprofen and related 2-arylpropanoic acid (2-APA) drugs are often given as a racemic mixture and the R-enantiomers undergo activation in vivo by metabolic chiral inversion. The chiral inversion pathway consists of conversion of the drug to the coenzyme A ester (by an acyl-CoA synthetase) followed by chiral inversion ...

journal_title：Biochemical pharmacology

authors： Qu X,Allan A,Chui G,Hutchings TJ,Jiao P,Johnson L,Leung WY,Li PK,Steel GR,Thompson AS,Threadgill MD,Woodman TJ,Lloyd MD

更新日期：2013-12-01 00:00:00

abstract：:Resveratrol, a natural phytoalexin that shows health-promoting benefits, is an inhibitor of store-operated calcium entry (SOCE). Knowledge of the molecular mechanism underlying this inhibition is required for the proper design of therapies that include resveratrol or related stilbenoids, but remains largely unknown. T...

journal_title：Biochemical pharmacology

authors： Casas-Rua V,Alvarez IS,Pozo-Guisado E,Martín-Romero FJ

更新日期：2013-12-01 00:00:00

abstract：:Diabetic retinopathy is one of the leading causes of blindness and the most common complication of diabetes with no cure available. We investigated the role of phospholipases A2 (PLA2) in diabetic retinopathy using an in vitro blood-retinal barrier model (BRB) and an in vivo streptozotocin (STZ)-induced diabetic model...

journal_title：Biochemical pharmacology

authors： Lupo G,Motta C,Giurdanella G,Anfuso CD,Alberghina M,Drago F,Salomone S,Bucolo C

更新日期：2013-12-01 00:00:00

abstract：:Polyphenolic anthocyanins are major colorful compounds in red fruits, known to prevent cardiovascular and other diseases. Grape polyphenols are a mixture of various molecules and their exact contribution to above bioactivities remains to be clarified. In the present study, we first analyzed the effect of purified grap...

journal_title：Biochemical pharmacology

authors： Decendit A,Mamani-Matsuda M,Aumont V,Waffo-Teguo P,Moynet D,Boniface K,Richard E,Krisa S,Rambert J,Mérillon JM,Mossalayi MD

更新日期：2013-11-15 00:00:00

abstract：:Nicotine has been shown in a variety of studies to improve cognitive function including learning, memory and attention. Nicotine both stimulates and desensitizes nicotinic receptors, thus acting both as an agonist and a net antagonist. The relative roles of these two actions for nicotine-induced cognitive improvement ...

journal_title：Biochemical pharmacology

authors： Levin ED

更新日期：2013-10-15 00:00:00

abstract：:AMP-activated protein kinase (AMPK) activates endothelial nitric oxide synthase (eNOS) via phosphorylation at the activating site. The eNOS-nitric oxide (NO)/soluble guanylate cyclase (sGC)-cGMP/cGMP-dependent protein kinase (PKG) signaling axis is a major antiaggregatory mechanism residing in platelets. Based on the ...

journal_title：Biochemical pharmacology

authors： Liu Y,Oh SJ,Chang KH,Kim YG,Lee MY

更新日期：2013-10-01 00:00:00

abstract：:Pregnancy is associated with uteroplacental and vascular remodeling in order to adapt for the growing fetus and the hemodynamic changes in the maternal circulation. We have previously shown upregulation of uterine matrix metalloproteinases (MMPs) during pregnancy. Whether pregnancy-associated changes in MMPs are local...

journal_title：Biochemical pharmacology

authors： Dang Y,Li W,Tran V,Khalil RA

更新日期：2013-09-15 00:00:00

abstract：:We investigated whether morphine and its pro-drug codeine are substrates of the highly genetically polymorphic organic cation transporter OCT1 and whether OCT1 polymorphisms may affect morphine and codeine pharmacokinetics in humans. Morphine showed low transporter-independent membrane permeability (0.5 × 10⁻⁶ cm/s). ...

journal_title：Biochemical pharmacology

authors： Tzvetkov MV,dos Santos Pereira JN,Meineke I,Saadatmand AR,Stingl JC,Brockmöller J

更新日期：2013-09-01 00:00:00

abstract：:The human P2Y₁₁ nucleotide receptor mRNA was found in virtually all human tissues, and the receptor serves many physiological roles, such as immune response regulation. The Ala-87-Thr-P2Y₁₁ receptor single nucleotide polymorphism was linked to increased risk for acute myocardial infarction. To facilitate the developme...

journal_title：Biochemical pharmacology

authors： Haas M,Ben-Moshe I,Fischer B,Reiser G

更新日期：2013-09-01 00:00:00

abstract：:7-Ketocholesterol (7-KC) is found at an elevated level in patients with cancer and chronic liver disease. The up-regulation of an efflux pump, P-glycoprotein (P-gp) leads to drug resistance. To elucidate the effect of 7-KC on P-gp, P-gp function and expression were investigated in hepatoma cell lines Huh-7 and HepG2 a...

journal_title：Biochemical pharmacology

authors： Wang SF,Chou YC,Mazumder N,Kao FJ,Nagy LD,Guengerich FP,Huang C,Lee HC,Lai PS,Ueng YF

更新日期：2013-08-15 00:00:00

abstract：:The genus Mycobacterium includes non-pathogenic species such as M. smegmatis, and pathogenic species such as M. tuberculosis, the causative agent of tuberculosis (TB). Treatment of TB requires a lengthy regimen of several antibiotics, whose effectiveness has been compromised by the emergence of resistant strains. New ...

journal_title：Biochemical pharmacology

authors： Lee Y,Mootien S,Shoen C,Destefano M,Cirillo P,Asojo OA,Yeung KR,Ledizet M,Cynamon MH,Aristoff PA,Koski RA,Kaplan PA,Anthony KG

更新日期：2013-07-15 00:00:00

abstract：:Cancer metastasis is a major cause for cancer-related death and inhibiting cancer metastasis is an alternative way to treat cancer. Several lines of reported evidence suggest that NADPH oxidase 4 (NOX4) is a potential target for intervention of cancer metastasis, as the reactive oxygen species (ROS) generated by this ...

journal_title：Biochemical pharmacology

authors： Zhang B,Liu Z,Hu X

更新日期：2013-07-15 00:00:00

abstract：:Lipids play a complex role in prostate cancer (PCa). Increased de novo synthesis of fatty acids and/or cholesterol is associated with the development of prostate tumors. Liver X Receptors (LXRs) are members of the nuclear receptor family that regulates intracellular lipid homeostasis. Targeting the transcriptional act...

journal_title：Biochemical pharmacology

authors： Hoang JJ,Baron S,Volle DH,Lobaccaro JM,Trousson A

更新日期：2013-07-01 00:00:00

abstract：:The disturbances of the cholesterol synthesis and metabolism described in Alzheimer's disease (AD) may be both a consequence of the neurodegenerative process and a contributor to the pathogenesis. These putative relationships and their underlying mechanisms are not well understood. The aim of this study was to evaluat...

journal_title：Biochemical pharmacology

authors： Popp J,Meichsner S,Kölsch H,Lewczuk P,Maier W,Kornhuber J,Jessen F,Lütjohann D

更新日期：2013-07-01 00:00:00

abstract：:Oxysterols possess anti-proliferative properties that may be used with much effect in the treatment of cancer. We have demonstrated previously that 7 beta-hydroxycholesterol (7b-HC) provokes both metabolic stress, as witnessed by AMPK activation, and changes in lipid raft composition in C6 glioblastoma cells. These ob...

journal_title：Biochemical pharmacology

authors： de Weille J,Fabre C,Gaven C,Bakalara N

更新日期：2013-07-01 00:00:00

abstract：:Tamoxifen (Tam) is a selective estrogen receptor modulator (SERM) that remains one of the major drugs used in the hormonotherapy of breast cancer (BC). In addition to its SERM activity, we recently showed that the oxidative metabolism of cholesterol plays a role in its anticancer pharmacology. We established that thes...

journal_title：Biochemical pharmacology

authors： Segala G,de Medina P,Iuliano L,Zerbinati C,Paillasse MR,Noguer E,Dalenc F,Payré B,Jordan VC,Record M,Silvente-Poirot S,Poirot M

更新日期：2013-07-01 00:00:00

abstract：:Flavin-containing monooxygenases (FMOs), drug-metabolizing enzymes essential for the metabolism of endogenous biochemicals and foreign compounds, have been characterized in human (including FMO1-5 and FMO6P), but remain to be investigated in cynomolgus macaque. In this study, cDNAs of cynomolgus FMO1-5 and FMO6 were i...

journal_title：Biochemical pharmacology

authors： Uno Y,Shimizu M,Yamazaki H

更新日期：2013-06-15 00:00:00