abstract：:There is a strong association between tobacco smoking and the consumption of alcoholic beverages. When compared to the effects of either drug on its own, the combined use may lead to worsened outcomes, such as less successful quitting attempts and increased likelihood of developing mood disorders. Co-consumption most ...

journal_title：Biochemical pharmacology

authors： Abreu-Villaça Y,Manhães AC,Krahe TE,Filgueiras CC,Ribeiro-Carvalho A

更新日期：2017-11-15 00:00:00

abstract：:The NADPH oxidases (NOXs) play a recognized role in the development and progression of inflammation-associated disorders, as well as cancer. To date, several NOX inhibitors have been developed, through either high throughput screening or targeted disruption of NOX interaction partners, although only a few have reached...

journal_title：Biochemical pharmacology

authors： Lu J,Risbood P,Kane CT Jr,Hossain MT,Anderson L,Hill K,Monks A,Wu Y,Antony S,Juhasz A,Liu H,Jiang G,Harris E,Roy K,Meitzler JL,Konaté M,Doroshow JH

更新日期：2017-11-01 00:00:00

abstract：:"Are new neurons added in the adult mammalian brain?" "Do neural stem cells activate following CNS diseases?" "How can we modulate their activation to promote recovery?" Recent findings in the field provide novel insights for addressing these questions from a new perspective. In this review, we will summarize the curr...

journal_title：Biochemical pharmacology

authors： Pino A,Fumagalli G,Bifari F,Decimo I

更新日期：2017-10-01 00:00:00

abstract：:Andrographis paniculata has long been part of the traditional herbal medicine system in Asia and in Scandinavia. Andrographolide was isolated as a major bioactive constituent of A. paniculata in 1951, and since 1984, andrographolide and its analogs have been scrutinized with modern drug discovery approach for anti-inf...

journal_title：Biochemical pharmacology

authors： Tan WSD,Liao W,Zhou S,Wong WSF

更新日期：2017-09-01 00:00:00

abstract：:Diabetic retinopathy (DR) is the most frequent complication of diabetes and one of leading causes of blindness worldwide. Early phases of DR are characterized by retinal pericyte loss mainly related to concurrent inflammatory process. Recently, an important link between P2X7 receptor (P2X7R) and inflammation has been ...

journal_title：Biochemical pharmacology

authors： Platania CBM,Giurdanella G,Di Paola L,Leggio GM,Drago F,Salomone S,Bucolo C

更新日期：2017-08-15 00:00:00

abstract：:Indole alkaloids possess a large spectrum of biological activities including anti-protozoal action. Here we report for the first time that voacamine, isolated from the plant Tabernaemontana coronaria, is an antiprotozoal agent effective against a large array of trypanosomatid parasites including Indian strain of Leish...

journal_title：Biochemical pharmacology

authors： Chowdhury SR,Kumar A,Godinho JLP,De Macedo Silva ST,Zuma AA,Saha S,Kumari N,Rodrigues JCF,Sundar S,Dujardin JC,Roy S,De Souza W,Mukhopadhyay S,Majumder HK

更新日期：2017-08-15 00:00:00

abstract：:Extrahepatic cytochrome P450 enzymes (CYP450) are pivotal in the metabolism of endogenous substrates and xenobiotics. CYP2J2 is a major cardiac CYP450 and primarily metabolizes polyunsaturated fatty acids such as arachidonic acid to cardioactive epoxyeicosatrienoic acids. Due to its role in endobiotic metabolism, CYP2...

journal_title：Biochemical pharmacology

authors： Karkhanis A,Hong Y,Chan ECY

更新日期：2017-07-01 00:00:00

abstract：:Understanding the mechanism of resistance to tubulin-targeted anticancer drugs is important for improved chemotherapy. In this work, a colchicine-resistant MCF-7 cell line (MCF-7Col30) was generated by the gradual increment of colchicine treatment and the MCF-7Col30 showed ∼8-fold resistance towards colchicine. MCF-7C...

journal_title：Biochemical pharmacology

authors： Rai A,Kapoor S,Naaz A,Kumar Santra M,Panda D

更新日期：2017-05-15 00:00:00

abstract：:Bradykinin (BK) induces inflammation in rheumatoid arthritis (RA). Resveratrol is a potent activator of Sirt1 which could modulate inflammation through deacetylating histones of transcription factors. Here, we investigated the mechanisms underlying BK-induced COX-2 expression which is modulated by resveratrol/Sirt1 in...

journal_title：Biochemical pharmacology

authors： Yang CM,Chen YW,Chi PL,Lin CC,Hsiao LD

更新日期：2017-05-15 00:00:00

abstract：:B-Raf kinase is the key point in a main branch of mitogen-activated protein kinase pathways and some of its mutations, such as the V600E mutation, lead to the persistent activation of ERK signaling and the trigger of severe diseases, including melanoma and other somatic cancers. Several potent drugs have been approved...

journal_title：Biochemical pharmacology

authors： Wang PF,Qiu HY,Wang ZF,Zhang YJ,Wang ZC,Li DD,Zhu HL

更新日期：2017-05-15 00:00:00

abstract：:DNA methylation is a mammalian epigenetic mark that participates to define where and when genes are expressed, both in normal cells and in the context of diseases. Like other epigenetic marks, it is reversible and can be modulated by chemical agents. Because it plays an important role in cancer by silencing certain ge...

journal_title：Biochemical pharmacology

authors： Pechalrieu D,Etievant C,Arimondo PB

更新日期：2017-04-01 00:00:00

abstract：:Hyperglycaemia increases the generation of reactive oxidants in blood vessels and is a major cause of endothelial dysfunction. A water-soluble selenium-containing sugar (1,4-Anhydro-4-seleno-d-talitol, SeTal) has potent antioxidant activity in vitro and is a promising treatment to accelerate wound healing in diabetic ...

journal_title：Biochemical pharmacology

authors： Ng HH,Leo CH,O'Sullivan K,Alexander SA,Davies MJ,Schiesser CH,Parry LJ

更新日期：2017-03-15 00:00:00

abstract：:Most of diabetic cardiovascular complications are attributed to endothelial dysfunction and impaired angiogenesis. Endoplasmic Reticulum (ER) and oxidative stresses were shown to play a pivotal role in the development of endothelial dysfunction in diabetes. Hemeoxygenase-1 (HO-1) was shown to protect against oxidative...

journal_title：Biochemical pharmacology

authors： Maamoun H,Zachariah M,McVey JH,Green FR,Agouni A

更新日期：2017-03-01 00:00:00

abstract：:Leukemia cells aberrantly overexpress senescence-suppression telomerase reverse transcriptase (TERT) and down-regulate key senescence-promoting genes to escape complete senescence, resulting in immortalization and malignant progression. Accordingly, induction of complete senescence is a sensible strategy for anti-leuk...

journal_title：Biochemical pharmacology

authors： Pan Y,Meng M,Zheng N,Cao Z,Yang P,Xi X,Zhou Q

更新日期：2017-02-15 00:00:00

abstract：:We have previously reported that Gen-27, a newly synthesized flavonoid, exhibits anticancer effects against human colorectal cancer cells. In this study, we investigated the anticancer effects in human breast cancer cell lines and its underlying mechanisms. We demonstrated that Gen-27 inhibited the growth and prolifer...

journal_title：Biochemical pharmacology

authors： Tao L,Wei L,Liu Y,Ding Y,Liu X,Zhang X,Wang X,Yao Y,Lu J,Wang Q,Hu R

更新日期：2017-02-01 00:00:00

abstract：:Thromboxane A2 is a potent mediator of inflammation and platelet aggregation exerting its effects through the activation of a G protein-coupled receptor (GPCR), termed TP. Although the existence of dimers/oligomers in Class A GPCRs is widely accepted, their functional significance still remains controversial. Recently...

journal_title：Biochemical pharmacology

authors： Capra V,Mauri M,Guzzi F,Busnelli M,Accomazzo MR,Gaussem P,Nisar SP,Mundell SJ,Parenti M,Rovati GE

更新日期：2017-01-15 00:00:00

abstract：:Cannabis and cannabinoids are known to affect female reproduction. However, the role of the endocannabinoid system in mouse uterine contractility in the dioestrus and oestrus phases has not been previously investigated. The present study aimed at filling this gap. Endocannabinoid (anandamide and 2-arachidonoylglycerol...

journal_title：Biochemical pharmacology

authors： Pagano E,Orlando P,Finizio S,Rossi A,Buono L,Iannotti FA,Piscitelli F,Izzo AA,Di Marzo V,Borrelli F

更新日期：2017-01-15 00:00:00

abstract：:The nuclear retinoid X receptor-α (RXRα) plays critical roles in cell homeostasis and in many physiological processes mainly through its transcriptional function. However, an N-terminal truncated form of RXRα, tRXRα, was frequently described in various cancer cells and tumor tissues, thus representing a new promising ...

journal_title：Biochemical pharmacology

authors： Wang PY,Zeng WJ,Liu J,Wu YL,Ma Y,Zeng Z,Pang JY,Zhang XK,Yan X,Wong AST,Zeng JZ

更新日期：2017-01-15 00:00:00

abstract：:MRP1 overexpression in multidrug-resistant cancer cells has been shown to be responsible for collateral sensitivity to some flavonoids that stimulate a huge MRP1-mediated GSH efflux. This massive GSH depletion triggers the death of these cancer cells. We describe here that bivalent flavonoid dimers strikingly stimulat...

journal_title：Biochemical pharmacology

authors： Dury L,Nasr R,Lorendeau D,Comsa E,Wong I,Zhu X,Chan KF,Chan TH,Chow L,Falson P,Di Pietro A,Baubichon-Cortay H

更新日期：2017-01-15 00:00:00

abstract：:Bupropion is a widely used antidepressant and smoking cessation aid and a strong inhibitor of CYP2D6 in vivo. Bupropion is administered as a racemic mixture of R- and S-bupropion and has stereoselective pharmacokinetics. Four primary metabolites of bupropion, threo- and erythro-hydrobupropion and R,R- and S,S-OH-bupro...

journal_title：Biochemical pharmacology

authors： Sager JE,Tripathy S,Price LS,Nath A,Chang J,Stephenson-Famy A,Isoherranen N

更新日期：2017-01-01 00:00:00

abstract：:Salinomycin, a polyether antibiotic, acts as a highly selective potassium ionophore and has anticancer activity on various cancer cell lines. Cisplatin has been proved as chemotherapy drug for advanced human non-small cell lung cancer (NSCLC). Thymidylate synthase (TS) is a key enzyme in the pyrimidine salvage pathway...

journal_title：Biochemical pharmacology

authors： Ko JC,Zheng HY,Chen WC,Peng YS,Wu CH,Wei CL,Chen JC,Lin YW

更新日期：2016-12-15 00:00:00

abstract：:Cisplatin is a potent chemotherapeutic drug widely used for the treatment of human cancer. However, its efficacy against hepatocellular carcinoma (HCC) is poor for reasons that remain unclear. We show here that prothymosin-alpha (PTMA) is overexpressed in HCC cell lines. Silencing PTMA using short-hairpin RNA sensitiz...

journal_title：Biochemical pharmacology

authors： Lin YT,Liu YC,Chao CC

更新日期：2016-12-15 00:00:00

abstract：:The need to protect human spermatozoa from oxidative stress during assisted reproductive technology, has prompted a detailed analysis of the impacts of phenolic compounds on the functional integrity of these cells. Investigation of 16 individual compounds revealed a surprising variety of negative effects including: (i...

journal_title：Biochemical pharmacology

authors： Aitken RJ,Muscio L,Whiting S,Connaughton HS,Fraser BA,Nixon B,Smith ND,De Iuliis GN

更新日期：2016-12-01 00:00:00

abstract：:β1-Adrenergic receptor (β1-AR) agonists and antagonists are widely used in the treatment of major cardiovascular diseases such as heart failure and hypertension. The β1-AR like other G protein-coupled receptors (GPCRs) are endocytosed in response to intense agonist activation. Recycling of the agonist-internalized β1-...

journal_title：Biochemical pharmacology

authors： Nooh MM,Mancarella S,Bahouth SW

更新日期：2016-11-15 00:00:00

abstract：:The formyl peptide receptor (FPR) gene family has a complex evolutionary history and comprises eight murine members but only three human representatives. To enable translation of results obtained in mouse models of human diseases, more comprehensive knowledge of the pharmacological similarities/differences between the...

journal_title：Biochemical pharmacology

authors： Skovbakke SL,Winther M,Gabl M,Holdfeldt A,Linden S,Wang JM,Dahlgren C,Franzyk H,Forsman H

更新日期：2016-11-01 00:00:00

abstract：:Tenofovir alafenamide (TAF) can be considered a new prodrug of tenofovir (TFV), as successor of tenofovir disoproxil fumarate (TDF). It is in vivo as potent against human immunodeficiency virus (HIV) at a 30-fold lower dose (10mg) than TDF (300mg). TAF has been approved in November 2015 (in the US and EU), as a single...

journal_title：Biochemical pharmacology

authors： De Clercq E

更新日期：2016-11-01 00:00:00

abstract：:Cytogenetic lesions often alter kinase signaling in acute myeloid leukemia (AML) and the addition of kinase inhibitors to the treatment arsenal is of interest. We have screened a kinase inhibitor library and performed combination testing to find promising drug-combinations for synergistic killing of AML cells. Cytotox...

journal_title：Biochemical pharmacology

authors： Österroos A,Kashif M,Haglund C,Blom K,Höglund M,Andersson C,Gustafsson MG,Eriksson A,Larsson R

更新日期：2016-10-15 00:00:00

abstract：:Increased matrix metalloproteinase (MMP)-2 is implicated in the vascular remodeling of hypertension. Calponin-1 is a contractile protein, and its absence is associated with vascular smooth muscle cell (VSMC) phenotype switch, which leads to migration and remodeling. We evaluated whether increased MMP-2 activity preced...

journal_title：Biochemical pharmacology

authors： Belo VA,Parente JM,Tanus-Santos JE,Castro MM

更新日期：2016-10-15 00:00:00

abstract：:Ligand-receptor binding kinetics (i.e. association and dissociation rates) are emerging as important parameters for drug efficacy in vivo. Awareness of the kinetic behavior of endogenous ligands is pivotal, as drugs often have to compete with those. The binding kinetics of neurokinin 1 (NK1) receptor antagonists have ...

journal_title：Biochemical pharmacology

authors： Nederpelt I,Bleeker D,Tuijt B,IJzerman AP,Heitman LH

更新日期：2016-10-15 00:00:00

abstract：:The lack of effective chemotherapies in hepatocellular carcinoma (HCC) is still an unsolved problem and underlines the need for new strategies in liver cancer treatment. In this study, we present a novel approach to improve the efficacy of Sorafenib, today's only routinely used chemotherapeutic drug for HCC, in combin...

journal_title：Biochemical pharmacology

authors： Lange M,Abhari BA,Hinrichs TM,Fulda S,Liese J

更新日期：2016-10-15 00:00:00

abstract：:GABAA receptors are ligand-gated ion channels that form a fundamental component of inhibitory neurotransmission in the central and peripheral nervous systems. However, since the initial recordings of inhibitory electrical activity of neurons in response to GABA, these receptors have been found to play a more complex r...

journal_title：Biochemical pharmacology

authors： Knoflach F,Hernandez MC,Bertrand D

更新日期：2016-09-01 00:00:00

abstract：:Chemokine receptor (CKR) signaling forms the basis of essential immune cellular functions, and dysregulated CKR signaling underpins numerous disease processes of the immune system and beyond. CKRs, which belong to the seven transmembrane domain receptor (7TMR) superfamily, initiate signaling upon binding of endogenous...

journal_title：Biochemical pharmacology

authors： Kleist AB,Getschman AE,Ziarek JJ,Nevins AM,Gauthier PA,Chevigné A,Szpakowska M,Volkman BF

更新日期：2016-08-15 00:00:00

abstract：:Ischemia/reperfusion (I/R) injury constitutes a major reason for failure of liver surgeries and transplantation. I/R injury is more severe in steatotic livers and limits their use in transplantation. Here, we present a novel and selective Toll-like receptor 9 (TLR9) antagonist COV08-0064 and test its potential to prot...

journal_title：Biochemical pharmacology

authors： Shaker ME,Trawick BN,Mehal WZ

更新日期：2016-07-15 00:00:00

abstract：:Poly (ADP-ribose) polymerases (PARPs) facilitate repairing of cancer cell DNA damage as a mean to promote cancer proliferation and metastasis. Inhibitors of PARPs which interfering DNA repair, in context of defects in other DNA repair mechanisms, can thus be potentially exploited to inhibit or even kill cancer cells. ...

journal_title：Biochemical pharmacology

authors： Zhou Q,Ji M,Zhou J,Jin J,Xue N,Chen J,Xu B,Chen X

更新日期：2016-05-01 00:00:00

abstract：:PepT1 (SLC15A1) is a high-capacity low-affinity transporter that is important in the absorption of digested di/tripeptides from dietary protein in the small intestine. PepT1 is also crucial for the intestinal uptake and absorption of therapeutic agents such as the β-lactam aminocephalosporins and antiviral prodrugs. S...

journal_title：Biochemical pharmacology

authors： Hu Y,Smith DE

更新日期：2016-05-01 00:00:00

abstract：:The regulation of tissue transglutaminase (TG2) activity by the GPCR family is poorly understood. In this study, we investigated the modulation of TG2 activity by the A1 adenosine receptor in cardiomyocyte-like H9c2 cells. H9c2 cells were lysed following stimulation with the A1 adenosine receptor agonist N(6)-cyclopen...

journal_title：Biochemical pharmacology

authors： Vyas FS,Hargreaves AJ,Bonner PL,Boocock DJ,Coveney C,Dickenson JM

更新日期：2016-05-01 00:00:00

abstract：:Bromodomains are epigenetic readers of histone acetylation involved in chromatin remodeling and transcriptional regulation. The human proteome comprises 46 bromodomain-containing proteins with a total of 61 bromodomains, which, despite highly conserved structural features, recognize a wide array of natural peptide lig...

journal_title：Biochemical pharmacology

authors： Ferri E,Petosa C,McKenna CE

更新日期：2016-04-15 00:00:00

abstract：:Disturbed redox homeostasis with both elevated reactive oxygen species (ROS) levels and antioxidant defense mechanisms has been reported in acute lymphoblastic leukemia (ALL). We therefore hypothesized that inhibition of pathways responsible for ROS detoxification renders ALL cells more susceptible for cell death. Her...

journal_title：Biochemical pharmacology

authors： Haß C,Belz K,Schoeneberger H,Fulda S

更新日期：2016-04-01 00:00:00

abstract：:Glucagon-like peptide-1 (GLP-1) is a neuroendocrine hormone produced by gastrointestinal tract in response to food ingestion. GLP-1 plays a very important role in the glucose homeostasis by stimulating glucose-dependent insulin secretion, inhibiting glucagon secretion, inhibiting gastric emptying, reducing appetite an...

journal_title：Biochemical pharmacology

authors： Torres G,Morales PE,García-Miguel M,Norambuena-Soto I,Cartes-Saavedra B,Vidal-Peña G,Moncada-Ruff D,Sanhueza-Olivares F,San Martín A,Chiong M

更新日期：2016-03-15 00:00:00

abstract：:The reaction mechanism of DNA topoisomerase II (TOP2) involves a covalent double-strand break intermediate in which the enzyme is coupled to DNA via a 5'-phosphotyrosyl bond. This normally transient enzyme-bridged break is stabilised by drugs such as mitoxantrone, mAMSA, etoposide, doxorubicin, epirubicin and idarubic...

journal_title：Biochemical pharmacology

authors： Lee KC,Bramley RL,Cowell IG,Jackson GH,Austin CA

更新日期：2016-03-01 00:00:00