abstract：:The action of piperine (the pungent component of pepper) and its derivative SCT-66 ((2E,4E)-5-(1,3-benzodioxol-5-yl))-N,N-diisobutyl-2,4-pentadienamide) on different gamma-aminobutyric acid (GABA) type A (GABA(A)) receptors, transient-receptor-potential-vanilloid-1 (TRPV1) receptors and behavioural effects were invest...

journal_title：Biochemical pharmacology

authors： Khom S,Strommer B,Schöffmann A,Hintersteiner J,Baburin I,Erker T,Schwarz T,Schwarzer C,Zaugg J,Hamburger M,Hering S

更新日期：2013-06-15 00:00:00

abstract：:Zinc protoporphyrin (ZnPP), a known inhibitor of heme oxygenase-1 (HO-1), has been reported to have anticancer activity in both in vitro and in vivo model systems. While the mechanisms of ZnPP's anticancer activity remain to be elucidated, it is generally believed that ZnPP suppresses tumor growth through inhibition o...

journal_title：Biochemical pharmacology

authors： Wang S,Avery JE,Hannafon BN,Lind SE,Ding WQ

更新日期：2013-06-01 00:00:00

abstract：:The aim of this work is the in vitro and ex vivo assessment of the leishmanicidal activity of camptothecin and three analogues used in cancer therapy: topotecan (Hycantim®), gimatecan (ST1481) and the pro-drug irinotecan (Camptosar®) as well as its active metabolite SN-38 against Leishmania infantum. The activity of c...

journal_title：Biochemical pharmacology

authors： Prada CF,Alvarez-Velilla R,Balaña-Fouce R,Prieto C,Calvo-Álvarez E,Escudero-Martínez JM,Requena JM,Ordóñez C,Desideri A,Pérez-Pertejo Y,Reguera RM

更新日期：2013-05-15 00:00:00

abstract：:Osteoporosis is characterized by low bone mineral density and/or poor bone microarchitecture leading to an increased risk of fractures. The skeletal alterations in osteoporosis are a consequence of a relative deficit of bone formation compared to bone resorption. Osteoporosis therapies have mostly relied on antiresorp...

journal_title：Biochemical pharmacology

authors： Esbrit P,Alcaraz MJ

更新日期：2013-05-15 00:00:00

abstract：:Prunetin is an O-methylated isoflavone, which is a type of flavonoid. There are a limited number of reports detailing the biological activities of prunetin. Although an anti-inflammatory effect of prunetin has been reported in vitro, to our knowledge, there have been no reports on anti-adipogenic effects of prunetin i...

journal_title：Biochemical pharmacology

authors： Ahn TG,Yang G,Lee HM,Kim MD,Choi HY,Park KS,Lee SD,Kook YB,An HJ

更新日期：2013-05-15 00:00:00

abstract：:Inflammatory bowel disease (IBD) is an incurable disease which affects millions of people in industrialized countries. Anecdotal and scientific evidence suggests that Cannabis use may have a positive impact in IBD patients. Here, we investigated the effect of cannabigerol (CBG), a non-psychotropic Cannabis-derived can...

journal_title：Biochemical pharmacology

authors： Borrelli F,Fasolino I,Romano B,Capasso R,Maiello F,Coppola D,Orlando P,Battista G,Pagano E,Di Marzo V,Izzo AA

更新日期：2013-05-01 00:00:00

abstract：:Heat shock protein 90 (Hsp90) is a molecular chaperone engaging in multiple cellular signaling by stabilizing oncoproteins (e.g. Akt and c-Raf) in tumor cells. Whereas Hsp90 inhibitors such as 17-AAG exert promising antitumor effects in clinical trials, current efforts focus on developing agents targeting Hsp90 with i...

journal_title：Biochemical pharmacology

authors： Lu C,Liu D,Jin J,Deokar H,Zhang Y,Buolamwini JK,Yu X,Yan C,Chen X

更新日期：2013-05-01 00:00:00

abstract：:Phospho-tyrosol-indomethacin (PTI; MPI 621), a novel anti-cancer agent, is more potent and safer than conventional indomethacin. Here, we show that PTI was extensively metabolized in vitro and in vivo. PTI was rapidly hydrolyzed by carboxylesterases to generate indomethacin as its major metabolite in the liver microso...

journal_title：Biochemical pharmacology

authors： Xie G,Zhou D,Cheng KW,Wong CC,Rigas B

更新日期：2013-04-15 00:00:00

abstract：:The phenolic glucoside gastrodin, a main constituent of a Chinese traditional herbal medicine, has been known to display several biological and pharmacological properties. However, the role and precise molecular mechanisms explaining how gastrodin suppresses the inflammatory response in septic cardiac dysfunction are ...

journal_title：Biochemical pharmacology

authors： Yang P,Han Y,Gui L,Sun J,Chen YL,Song R,Guo JZ,Xie YN,Lu D,Sun L

更新日期：2013-04-15 00:00:00

abstract：:Previously we reported that liposomal cisplatin (CDDP) overcomes CDDP resistance of ovarian A2780cis cancer cells (Krieger et al., Int. J. Pharm. 389, 2010, 10-17). Here we find that the cytotoxic activity of liposomal CDDP is not associated with detectable DNA platination in resistant ovarian cancer cells. This sugge...

journal_title：Biochemical pharmacology

authors： Koch M,Krieger ML,Stölting D,Brenner N,Beier M,Jaehde U,Wiese M,Royer HD,Bendas G

更新日期：2013-04-15 00:00:00

abstract：:Poor prognosis in patients with later stage colorectal cancer (CRC) necessitates the search for new treatment strategies. Ceramide, because of its role in orchestrating death cascades in cancer cells, is a versatile alternative. Ceramide can be generated by exposure to chemotherapy or ionizing radiation, or it can be ...

journal_title：Biochemical pharmacology

authors： Morad SA,Madigan JP,Levin JC,Abdelmageed N,Karimi R,Rosenberg DW,Kester M,Shanmugavelandy SS,Cabot MC

更新日期：2013-04-15 00:00:00

abstract：:Breast cancer is the leading cause of cancer death among females, and novel chemotherapeutic drugs for treating breast cancer are needed urgently. Saxifragifolin D (SD) was isolated by our group from Androsace umbellata which is commonly used to treat solid tumor. In this study, we evaluated its growth inhibitory effe...

journal_title：Biochemical pharmacology

authors： Shi JM,Bai LL,Zhang DM,Yiu A,Yin ZQ,Han WL,Liu JS,Li Y,Fu DY,Ye WC

更新日期：2013-04-01 00:00:00

abstract：:The homomeric α7 nicotinic acetylcholine receptor is a well-studied therapeutic target, though its characteristically rapid desensitization complicates the development of drugs with specific agonist effects. Moreover, some experimental compounds such as GTS-21 (2,4diMeOBA), a derivative of the α7-selective partial ago...

journal_title：Biochemical pharmacology

authors： Isaacson MD,Horenstein NA,Stokes C,Kem WR,Papke RL

更新日期：2013-03-15 00:00:00

abstract：:Valine residues in the pore region of SK2 (V366) and SK3 (V520) were replaced by either an alanine or a phenylalanine to evaluate the impact on the interactions with the allosteric blocker apamin. Unlike TEA which showed high sensitivity to phenylalanine mutated channels, the binding affinity of apamin to the phenylal...

journal_title：Biochemical pharmacology

authors： Dilly S,Philippart F,Lamy C,Poncin S,Snyders D,Seutin V,Liégeois JF

更新日期：2013-02-15 00:00:00

abstract：:Thiazolidinediones (also referred to as glitazones), agonists for Peroxisome Proliferator-Activated Receptor gamma (PPARγ), are used for treating type 2 diabetes mellitus, where they decrease insulin resistance and cardiovascular risk. Compounds bearing the thiazolidinedione structure have also been shown to inhibit p...

journal_title：Biochemical pharmacology

authors： Sinagra T,Tamburella A,Urso V,Siarkos I,Drago F,Bucolo C,Salomone S

更新日期：2013-02-15 00:00:00

abstract：UNLABELLED:Non-steroidal anti-inflammatory drugs (NSAIDs) induce the shedding of L-selectin in human neutrophils through a mechanism still not well understood. In this work we studied both the functional effect of NSAIDs on the neutrophils/endothelial cells dynamic interaction, and the potential involvement of reactive...

journal_title：Biochemical pharmacology

authors： Domínguez-Luis M,Herrera-García A,Arce-Franco M,Armas-González E,Rodríguez-Pardo M,Lorenzo-Díaz F,Feria M,Cadenas S,Sánchez-Madrid F,Díaz-González F

更新日期：2013-01-15 00:00:00

abstract：:The human ether-a-go-go-related gene (hERG) encodes the rapidly activating, delayed rectifier potassium channel (IKr) important for cardiac repolarization. Dysfunction of the hERG channel can cause Long QT Syndrome (LQTS). A wide variety of structurally diverse therapeutic compounds reduce the hERG current by acute di...

journal_title：Biochemical pharmacology

authors： Zhang Y,Dong Z,Jin L,Zhang K,Zhao X,Fu J,Gong Y,Sun M,Yang B,Li B

更新日期：2013-01-01 00:00:00

abstract：:20-Hydroxyvitamin D(3) (20(OH)D(3)), the major product of CYP11A1 action on vitamin D(3), is biologically active and is produced in vivo. As well as potentially having important physiological actions, it is of interest as a therapeutic agent due to its lack of calcemic activity. In the current study we have examined t...

journal_title：Biochemical pharmacology

authors： Tieu EW,Tang EK,Chen J,Li W,Nguyen MN,Janjetovic Z,Slominski A,Tuckey RC

更新日期：2012-12-15 00:00:00

abstract：:Rosuvastatin increased vascular endothelial NO and attenuated platelet activation after ischemia-reperfusion in mice; nevertheless, the influence of rosuvastatin on the activation of human platelets and the underlying mechanism has never been investigated. In an in vitro study platelets from 8 healthy donors were incu...

journal_title：Biochemical pharmacology

authors： Pignatelli P,Carnevale R,Di Santo S,Bartimoccia S,Nocella C,Vicario T,Loffredo L,Angelico F,Violi F

更新日期：2012-12-15 00:00:00

abstract：:Physiological levels of wild-type (wt) apolipoprotein E (apoE) in plasma mediate the clearance of cholesterol-rich atherogenic lipoprotein remnants while higher than normal plasma apoE concentrations fail to do so and trigger hypertriglyceridemia. This property of wt apoE reduces significantly its therapeutic value as...

journal_title：Biochemical pharmacology

authors： Lampropoulou A,Zannis VI,Kypreos KE

更新日期：2012-12-01 00:00:00

abstract：:Epothilones constitute a novel class of antitubulin agents that are active in patients who relapse after treatment with other chemotherapeutics. This study investigated the molecular mechanisms leading to the onset of epothilone-B (patupilone) resistance in ovarian cancer. Results demonstrated that the Gli family of t...

journal_title：Biochemical pharmacology

authors： Mozzetti S,Martinelli E,Raspaglio G,Prislei S,De Donato M,Filippetti F,Shahabi S,Scambia G,Ferlini C

更新日期：2012-12-01 00:00:00

abstract：:Lesions to DNA trigger the DNA-damage response (DDR), a complex, multi-branched cell-intrinsic process targeted to DNA repair, or elimination of the damaged cells by apoptosis. DDR aims at reducing permanence of mutated cells, decreasing the risk of tumor development: the more stringent the response, the lower the lik...

journal_title：Biochemical pharmacology

authors： Caputo F,Vegliante R,Ghibelli L

更新日期：2012-11-15 00:00:00

abstract：:Chemokines and their receptors play fundamental roles in many physiological and pathological processes such as leukocyte trafficking, inflammation, cancer and HIV-1 infection. Chemokine-receptor interactions are particularly intricate and therefore require precise orchestration. The flexible N-terminal domain of human...

journal_title：Biochemical pharmacology

authors： Szpakowska M,Fievez V,Arumugan K,van Nuland N,Schmit JC,Chevigné A

更新日期：2012-11-15 00:00:00

abstract：:Chemical compounds derived from plants have been used since the origin of human beings to counteract a number of diseases. Among them, the natural isoquinoline alkaloid berberine has been employed in Ayurvedic and Chinese Medicine for hundreds of years with a wide range of pharmacological and biochemical effects. More...

journal_title：Biochemical pharmacology

authors： Tillhon M,Guamán Ortiz LM,Lombardi P,Scovassi AI

更新日期：2012-11-15 00:00:00

abstract：:Glutamatergic hypofunction and elevated levels of kynurenic acid (KYNA) in the brain are common features of patients with schizophrenia. In vivo studies indicate that in the hippocampus KYNA decreases glutamate levels, presumably via inhibition of α7 nicotinic receptors (nAChRs). Here we tested the hypothesis that bas...

journal_title：Biochemical pharmacology

authors： Banerjee J,Alkondon M,Albuquerque EX

更新日期：2012-10-15 00:00:00

abstract：:The biological mechanisms underlying castration resistance of prostate cancer are not fully understood. In the present study, we examined the role of organic anion transporting polypeptides (OATPs) as importers of dehydroepiandrosterone sulfate (DHEAS) into cells to support growth under androgen-depleted conditions. C...

journal_title：Biochemical pharmacology

authors： Arakawa H,Nakanishi T,Yanagihara C,Nishimoto T,Wakayama T,Mizokami A,Namiki M,Kawai K,Tamai I

更新日期：2012-10-15 00:00:00

abstract：:Andrographolide, a novel nuclear factor-κB (NF-κB) inhibitor, is isolated from leaves of Andrographis paniculata. Platelet activation is relevant to a variety of coronary heart diseases. Our recent studies revealed that andrographolide possesses potent antiplatelet activity by activating the endothelial nitric oxide s...

journal_title：Biochemical pharmacology

authors： Lu WJ,Lin KH,Hsu MJ,Chou DS,Hsiao G,Sheu JR

更新日期：2012-10-01 00:00:00

abstract：:OSI-930, a dual c-Kit and KDR tyrosine kinase inhibitor, is reported to have undergone a Phase I dose escalation study in patients with advanced solid tumors. A series of fifteen pyridyl and phenyl analogues of OSI-930 were designed and synthesized. Extensive screening of these compounds led to the discovery that nitr...

journal_title：Biochemical pharmacology

authors： Kuang YH,Patel JP,Sodani K,Wu CP,Liao LQ,Patel A,Tiwari AK,Dai CL,Chen X,Fu LW,Ambudkar SV,Korlipara VL,Chen ZS

更新日期：2012-09-15 00:00:00

abstract：:Histone deacetylases (HDAC) play a key role in regulating gene expression by deacetylating histones. Some HDAC isoforms can also modulate the function of nonhistone proteins implicated in regulatory processes, and therefore HDACs are recognized as useful targets for therapeutic purposes. HDAC inhibitors have generated...

journal_title：Biochemical pharmacology

authors： Dallavalle S,Pisano C,Zunino F

更新日期：2012-09-15 00:00:00

abstract：:The β2-adrenergic receptor (β2AR) is the prototypical member of the heptahelical G protein-coupled receptor (GPCR) superfamily and is well-known to elicit biological effects through both G protein-dependent and G protein-independent signaling cascades. Agonism of β2AR has been described to promote phosphorylation and ...

journal_title：Biochemical pharmacology

authors： Singh M,Moniri NH

更新日期：2012-09-01 00:00:00

abstract：:Invasion of normal brain tissue by tumor cells is a major contributing factor to the recurrence of glioblastoma and its resistance to therapy. Here, we have assessed the efficacy of the microtubule (MT) targeting agent Epothilone B (patupilone) on glioblastoma cell migration, a prerequisite for invasive tumor cell beh...

journal_title：Biochemical pharmacology

authors： Pagano A,Honoré S,Mohan R,Berges R,Akhmanova A,Braguer D

更新日期：2012-08-15 00:00:00

abstract：:Human ABCG2 is a plasma membrane glycoprotein that provides physiological protection against xenobiotics. ABCG2 also significantly influences biodistribution of drugs through pharmacological tissue barriers and confers multidrug resistance to cancer cells. Moreover, ABCG2 is the molecular determinant of the side popul...

journal_title：Biochemical pharmacology

authors： Hegedüs C,Truta-Feles K,Antalffy G,Várady G,Német K,Ozvegy-Laczka C,Kéri G,Orfi L,Szakács G,Settleman J,Váradi A,Sarkadi B

更新日期：2012-08-01 00:00:00

abstract：:Work published over the past 10-15 years has caused the neuroscience community to engage in a process of constant re-evaluation of the roles of glial cells in the mammalian central nervous system. Recent emerging evidence suggests that, in addition to carrying out various homeostatic functions within the CNS, astrocyt...

journal_title：Biochemical pharmacology

authors： Bradley SJ,Challiss RA

更新日期：2012-08-01 00:00:00

abstract：:Deoxycytidine kinase (dCK) (EC 2.7.1.74) is a key enzyme in the activation of several therapeutic nucleoside analogs (NA). Its activity can be increased in vivo by Ser-74 phosphorylation, a property that could be used for enhancing NA activation and clinical efficacy. In line with this, studies with recombinant dCK sh...

journal_title：Biochemical pharmacology

authors： Amsailale R,Van Den Neste E,Arts A,Starczewska E,Bontemps F,Smal C

更新日期：2012-07-01 00:00:00

abstract：:Triapine is an α-N-heterocyclic thiosemicarbazone with promising anticancer activity against hematologic malignancies but widely ineffective against solid tumor types in clinical trials. The anticancer activity of thiosemicarbazones can be dramatically increased by terminal dimethylation. KP1089 is a gallium compound ...

journal_title：Biochemical pharmacology

authors： Heffeter P,Pirker C,Kowol CR,Herrman G,Dornetshuber R,Miklos W,Jungwirth U,Koellensperger G,Keppler BK,Berger W

更新日期：2012-06-15 00:00:00

abstract：:Neutrophil serine proteases (NSPs), including elastase, proteinase 3 and cathepsin G, play critical roles in the pathogenesis of chronic inflammatory lung diseases. The release of excess NSPs leads to the destruction of lung tissue and an overexuberant, sustained inflammatory response. Antiproteases could be valuable ...

journal_title：Biochemical pharmacology

authors： Tanga A,Saidi A,Jourdan ML,Dallet-Choisy S,Zani ML,Moreau T

更新日期：2012-06-15 00:00:00

abstract：:Apo 2 ligand/tumor necrosis factor (TNF)-related apoptosis-inducing ligand (Apo2L/TRAIL), is a member of the TNF family of cytokines, which can induce apoptotic cell death in cells expressing at least one of their specific death receptors, DR4 (TRAIL-R1) or DR5 (TRAIL-R2). In the last decade, the Apo2L/TRAIL system of...

journal_title：Biochemical pharmacology

authors： Martinez-Lostao L,Marzo I,Anel A,Naval J

更新日期：2012-06-01 00:00:00

abstract：:Vinca alkaloids are clinically used to inhibit the growth of malignancy by interfering with microtubule polymerization. The purpose of this study was to identify the molecular mechanisms underlying growth inhibition as well as apoptosis in vinca alkaloid-treated lung adenocarcinoma cells. Consistent with nocodazole, t...

journal_title：Biochemical pharmacology

authors： Chiu WH,Luo SJ,Chen CL,Cheng JH,Hsieh CY,Wang CY,Huang WC,Su WC,Lin CF

更新日期：2012-05-01 00:00:00

abstract：:Arsenic, still a significant environmental threat in several regions in the world, induces various cancers, including lungs, skin, and bladder. Arsenic-induced Bowen's disease (As-BD) is generally an indolent cutaneous intraepithelial carcinoma in susceptible people. Patients with As-BD have been found to have attenua...

journal_title：Biochemical pharmacology

authors： Lee CH,Hong CH,Yu CL,Wang LF,Clausen BE,Liao WT,Huang SK,Chen GS,Yu HS

更新日期：2012-05-01 00:00:00

abstract：:Quinones are ubiquitously present in mammals and their environment. They are involved in physiologic functions such as electron transport but are also toxic compounds. In particular, quinone-quinol redox cycles may lead to oxidative stress, and arylating quinones have been demonstrated to activate endoplasmic reticulu...

journal_title：Biochemical pharmacology

authors： Bock KW

更新日期：2012-04-01 00:00:00