abstract：BACKGROUND AND PURPOSE:Chronic nicotine exposure upregulates α4β2* nicotinic acetylcholine receptors (nAChRs) in the brain. The goal of this study was to examine the role of three serine residues in the large cytoplasmic loop of the α4 subunit on α4β2* upregulation in neurons. EXPERIMENTAL APPROACH:Serine residues S33...

journal_title：Biochemical pharmacology

authors： Zambrano CA,Escobar D,Ramos-Santiago T,Bollinger I,Stitzel J

更新日期：2019-01-01 00:00:00

abstract：:Sepsis is an etiologically complex and often fatal inflammatory process involving a multitude of cytokine signaling pathways. Tumor necrosis factor α (TNFα) acts as a central regulator of the acute-phase inflammatory response by recruiting immune cells, including circulating monocyte/macrophages, to sites of infection...

journal_title：Biochemical pharmacology

authors： Terashima-Hasegawa M,Ashino T,Kawazoe Y,Shiba T,Manabe A,Numazawa S

更新日期：2019-01-01 00:00:00

abstract：:In the present study, a screen of adenosine analogs as potential modulators of arylamine-N-acetyltransferase 1 activity identified ATP as an inhibitor within its range of physiological concentrations. Kinetically, ATP was a non-competitive inhibitor with respect to the acetyl acceptor but a competitive inhibitor with ...

journal_title：Biochemical pharmacology

authors： Minchin RF,Rosengren KJ,Burow R,Butcher NJ

更新日期：2018-12-01 00:00:00

abstract：:Drug addiction is a chronic relapsing disorder that produces a dramaticglobal health burden worldwide. Not effective treatment of drug addiction is currently available probably due to the difficulties to find an appropriate target to manage this complex disease raising the needs for further identification of novel the...

journal_title：Biochemical pharmacology

authors： Manzanares J,Cabañero D,Puente N,García-Gutiérrez MS,Grandes P,Maldonado R

更新日期：2018-11-01 00:00:00

abstract：:P-glycoprotein (P-gp) plays critical roles in mediating the cytotoxicity of many drugs that are P-gp substrates. Previously, we reported that P-glycoprotein (P-gp) is the foremost efflux transporter of deoxynivalenol (DON), which is one of the most abundant mycotoxins. However, whether DON changes the expression of P-...

journal_title：Biochemical pharmacology

authors： Li X,Mu P,Qiao H,Wen J,Deng Y

更新日期：2018-10-01 00:00:00

abstract：:Epilepsy is one of the serious neurological sequelae of bacterial meningitis. Rifampicin, the well-known broad spectrum antibiotic, is clinically used for chemoprophylaxis of meningitis. Besides its antibiotic effects, rifampicin has been proven to be an effective neuroprotective candidate in various experimental mode...

journal_title：Biochemical pharmacology

authors： Ali AE,Mahdy HM,Elsherbiny DM,Azab SS

更新日期：2018-10-01 00:00:00

abstract：:It is believed that chemotherapeutic agents can enhance the malignancy of treated cancer cells in clinical situations, which is a major problem for chemotherapy. However, the underlying molecular mechanisms are still not fully understood. Here, we demonstrated that chemotherapy up-regulates the levels of spermatogenic...

journal_title：Biochemical pharmacology

authors： Liu X,Han X,Wan X,He C,Wang Y,Mao A,Yu F,Zhou T,Feng L,Zhang P,Jin J,Ma X

更新日期：2018-10-01 00:00:00

abstract：:Metabolomics offers the opportunity to uncover endogenous biomarkers that can lead to metabolic pathways and networks and that underpin drug toxicity mechanisms. A novel protocol is presented and discussed that is applicable to drugs which generate urinary metabolites when administered to mice sensitive to its toxicit...

journal_title：Biochemical pharmacology

authors： Beyoğlu D,Zhou Y,Chen C,Idle JR

更新日期：2018-10-01 00:00:00

abstract：:Metformin, a commonly used agent in the treatment of type 2 diabetes, is also associated with reduced risk of cancer development and improvement in cancer survival. Although much is known about metformin, the mechanisms behind its anti-cancer properties are not fully understood. In this study we addressed the role of ...

journal_title：Biochemical pharmacology

authors： Zhao Q,Zhou X,Curbo S,Karlsson A

更新日期：2018-10-01 00:00:00

abstract：:Aflatoxin B1 (AFB1) is bioactivated by cytochrome P450 (CYP) 3A isoforms in humans to generate the highly reactive epoxide intermediate AFB1-8,9-epoxide (AFBO), causing hepatotoxicity and hepatocarcinoma. Due to the unavoidable contamination in their feed, pigs are more likely to be exposed to AFB1 and indirectly harm...

journal_title：Biochemical pharmacology

authors： Jiang H,Wu J,Zhang F,Wen J,Jiang J,Deng Y

更新日期：2018-10-01 00:00:00

abstract：:Hyperactivated macrophages play a key role in the initiation and perpetuation of mucosal inflammation in Crohn's disease (CD). Increasing evidence suggests that the basic helix-loop-helix (bHLH) repressor Twist1 can suppress activation of nuclear factor-κB (NF-κB) and the subsequent production of TNF-α, which are both...

journal_title：Biochemical pharmacology

authors： Tu T,Yu M,Zhang Y,Shi X,Xu J,Hu J,Gan J,He W,Dong L,Han J,Huang Z,Pan Y,Zhang J

更新日期：2018-09-01 00:00:00

abstract：:S-Nitrosothiols, a class of NO donors, demonstrate potential benefits for cardiovascular diseases. Drugs for such chronic diseases require long term administration preferentially through the oral route. However, the absorption of S-nitrosothiols by the intestine, which is the first limiting barrier for their vascular ...

journal_title：Biochemical pharmacology

authors： Bonetti J,Zhou Y,Parent M,Clarot I,Yu H,Fries-Raeth I,Leroy P,Lartaud I,Gaucher C

更新日期：2018-09-01 00:00:00

abstract：:Acute respiratory distress syndrome threatens public health with high morbidity and mortality due to ineffective intervention whereby lipopolysaccharide (LPS) induced acute lung injury (ALI) in mice provides a research model. The seeds of Euphorbia lathyris L. have a long history of usage in Traditional Chinese Medici...

journal_title：Biochemical pharmacology

authors： Zhang Q,Zhu S,Cheng X,Lu C,Tao W,Zhang Y,William BC,Cao X,Yi S,Liu Y,Zhao Y,Luo Y

更新日期：2018-09-01 00:00:00

abstract：:Thrombospondin (TSP)-2, a matricellular glycoprotein of the TSP family, regulates multiple biological functions, including proliferation, angiogenesis, cell adhesion, and extracellular matrix (ECM) modeling. The clinical relevance of TSP-2 has been explored in many different cancers. TSP-2 expression levels vary betwe...

journal_title：Biochemical pharmacology

authors： Liu JF,Lee CW,Tsai MH,Tang CH,Chen PC,Lin LW,Lin CY,Lu CH,Lin YF,Yang SH,Chao CC

更新日期：2018-09-01 00:00:00

abstract：:The current obesity epidemic is a major worldwide health and economic burden. In the modern environment, an increase in the intake of high-fat and high-sugar foods plays a crucial role in the development of obesity by disrupting the mechanisms governing food intake and energy balance. Food intake and whole-body energy...

journal_title：Biochemical pharmacology

authors： Zagmutt S,Mera P,Soler-Vázquez MC,Herrero L,Serra D

更新日期：2018-09-01 00:00:00

abstract：:Diabetic nephropathy (DN) is one of the most prevalent lethal complications of diabetes that leads to end stage renal disease. Although several clinical approaches exist to attenuate DN, there is not curative treatment to date. DN is complicated, as it involves several simultaneous molecular pathways. Some natural and...

journal_title：Biochemical pharmacology

authors： Dewanjee S,Bhattacharjee N

更新日期：2018-09-01 00:00:00

abstract：:Sulfasalazine (SF) promotes remyelination and improves the outcome of multiple sclerosis (MS) patients. However, the underlining mechanism remains elusive. Here, we examined whether SF blocks microglia switching to a pro-inflammatory M1-like phenotype through a competing endogenous RNA (ceRNA) effects in cuprizone-ind...

journal_title：Biochemical pharmacology

authors： Duan C,Liu Y,Li Y,Chen H,Liu X,Chen X,Yue J,Zhou X,Yang J

更新日期：2018-09-01 00:00:00

abstract：:The International Diabetes Federation predicts that by 2045 the number of individuals afflicted with diabetes will increase to 629 million. Furthermore, ∼352 million individuals with impaired glucose tolerance are at increased risk for developing diabetes. Several mechanisms have been proposed for the onset of metabol...

journal_title：Biochemical pharmacology

authors： Kowluru A,Kowluru RA

更新日期：2018-08-01 00:00:00

abstract：:Chondrosarcoma is a common primary malignant tumor of the bone that can metastasize through the vascular system to other organs. A key step in the metastatic process, lymphangiogenesis, involves vascular endothelial growth factor-C (VEGF-C). However, the effects of lymphangiogenesis in chondrosarcoma metastasis remain...

journal_title：Biochemical pharmacology

authors： Su CM,Tang CH,Chi MJ,Lin CY,Fong YC,Liu YC,Chen WC,Wang SW

更新日期：2018-08-01 00:00:00

abstract：:Hypertension is considered as one of the cancer progressive factors, and often found comorbidity in cancer patients. Renin-angiotensin system (RAS) plays an important role in the regulation of blood pressure, and angiotensin II (Ang II) is well known pressor peptide associated with RAS. Ang II has been reported to acc...

journal_title：Biochemical pharmacology

authors： Ishikane S,Hosoda H,Nojiri T,Tokudome T,Mizutani T,Miura K,Akitake Y,Kimura T,Imamichi Y,Kawabe S,Toyohira Y,Yanagihara N,Takahashi-Yanaga F,Miyazato M,Miyamoto K,Kangawa K

更新日期：2018-08-01 00:00:00

abstract：:Tanshinone I (Tanshinone-1), a major active principle of the traditional Chinese medicine Salvia miltiorrhiza, possesses excellent anticancer properties, including inhibiting proliferation, angiogenesis and metastasis and overcoming multidrug resistance (MDR). However, its direct anticancer molecular target(s) remain ...

journal_title：Biochemical pharmacology

authors： Tian QT,Ding CY,Song SS,Wang YQ,Zhang A,Miao ZH

更新日期：2018-08-01 00:00:00

abstract：:Sorafenib is the only FDA approved drug for the treatment of advanced hepatocellular carcinoma (HCC) and other malignancies. Studies indicate that TGF-β signalling is associated with tumour progression in HCC. Autocrine and paracrine TGF-β promotes tumour growth and malignancy by inducing epithelial-mesenchymal transi...

journal_title：Biochemical pharmacology

authors： Chung CL,Wang SW,Sun WC,Shu CW,Kao YC,Shiao MS,Chen CL

更新日期：2018-08-01 00:00:00

abstract：:The maintenance of the characteristic lipid compositions and physicochemical properties of biological membranes is essential for their proper function. Mechanisms allowing to sense and restore membrane homeostasis have been identified in prokaryotes for a long time and more recently in eukaryotes. A membrane remodelin...

journal_title：Biochemical pharmacology

authors： Gianfrancesco MA,Paquot N,Piette J,Legrand-Poels S

更新日期：2018-07-01 00:00:00

abstract：:Common marmosets (Callithrix jacchus) are potentially useful nonhuman primate models for preclinical studies. An anti-inflammatory drug, diclofenac is reportedly metabolized mainly by human cytochrome P450 (P450) 2C9 to 4'-hydroxydiclofenac and minorly by P450 3A4 to 5-hydroxydiclofenac that leads to reactive intermed...

journal_title：Biochemical pharmacology

authors： Nakanishi K,Uehara S,Kusama T,Inoue T,Shimura K,Kamiya Y,Murayama N,Shimizu M,Uno Y,Sasaki E,Yamazaki H

更新日期：2018-06-01 00:00:00

abstract：:Only limited data are available on the inhibition of the sugar transporter GLUT5 by flavonoids or other classes of bioactives. Intestinal GLUT7 is poorly characterised and no information exists concerning its inhibition. We aimed to study the expression of GLUT7 in Caco-2/TC7 intestinal cells, and evaluate inhibition ...

journal_title：Biochemical pharmacology

authors： Gauer JS,Tumova S,Lippiat JD,Kerimi A,Williamson G

更新日期：2018-06-01 00:00:00

abstract：:Interleukin (IL)-22 plays protective roles in infections and in inflammatory diseases that have been linked to its meditation of innate immunity via multiple mechanisms. IL-22 binds specifically to its heterodimeric receptor, which is expressed on a variety of epithelial tissues. UTTR1147A is a recombinant fusion prot...

journal_title：Biochemical pharmacology

authors： Stefanich EG,Rae J,Sukumaran S,Lutman J,Lekkerkerker A,Ouyang W,Wang X,Lee D,Danilenko DM,Diehl L,Loyet KM,Herman A

更新日期：2018-06-01 00:00:00

abstract：:A2B adenosine receptor (A2BAR) activation induces Gs-dependent cyclic AMP accumulation. However, A2BAR G protein-coupling to other signaling events, e.g. ERK1/2 and calcium, is not well documented. We explored Gi, Gq/11 and Gs coupling in 1321 N1 astrocytoma, HEK293, and T24 bladder cancer cells endogenously expressin...

journal_title：Biochemical pharmacology

authors： Gao ZG,Inoue A,Jacobson KA

更新日期：2018-05-01 00:00:00

abstract：:(R,E)-N-(3-(2-acetamido-3-(benzyloxy) propanamido)propyl)-2-cyano-3-(4-hydroxy phenyl)acrylamide (hr5F) was design-synthesized based on bioactivity focus strategy as a potential agent to treat diabetic complicates. With in vitro enzyme assay, it is confirmed that hr5F is an effective ALR2 inhibitor with IC50 value of ...

journal_title：Biochemical pharmacology

authors： Wang Z,Yuan S,Li Y,Zhang Z,Xiao W,Tang D,Ye K,Liu Z,Wang C,Zheng Y,Nie H,Chen H

更新日期：2018-04-01 00:00:00

abstract：:Gastric cancer is the third common cause of cancer mortality in the world with poor prognosis and high recurrence due to lack of effective medicines. Our studies revealed that lanatoside C, a FDA-approved cardiac glycoside, had an anti-proliferation effect on different human cancer cell lines (MKN-45; SGC-7901; HN4; M...

journal_title：Biochemical pharmacology

authors： Hu Y,Yu K,Wang G,Zhang D,Shi C,Ding Y,Hong D,Zhang D,He H,Sun L,Zheng JN,Sun S,Qian F

更新日期：2018-04-01 00:00:00

abstract：:Class B peptide hormone GPCRs are targets for the treatment of major chronic disease. Peptide ligands of these receptors display biased agonism and this may provide future therapeutic advantage. Recent active structures of the calcitonin (CT) and glucagon-like peptide-1 (GLP-1) receptors reveal distinct engagement of ...

journal_title：Biochemical pharmacology

authors： Dal Maso E,Zhu Y,Pham V,Reynolds CA,Deganutti G,Hick CA,Yang D,Christopoulos A,Hay DL,Wang MW,Sexton PM,Furness SGB,Wootten D

更新日期：2018-04-01 00:00:00

abstract：:Acetaminophen (APAP)-induced hepatotoxicity is the main cause of drug-induced liver injury. This study investigated the protection of baicalin and its aglycone baicalein against APAP-induced hepatotoxicity and its mechanism. Baicalein and baicalin alleviated APAP-induced hepatotoxicity both in vitro and in vivo. Moreo...

journal_title：Biochemical pharmacology

authors： Shi L,Hao Z,Zhang S,Wei M,Lu B,Wang Z,Ji L

更新日期：2018-04-01 00:00:00

abstract：:Transient outward potassium current (Ito) contributes to early repolarization of many mammalian cardiac action potentials, including human, whilst the rapid delayed rectifier K+ current (IKr) contributes to later repolarization. Fast Ito channels can be produced from the Shal family KCNDE gene product Kv4.3s, although...

journal_title：Biochemical pharmacology

authors： Lainez S,Doray A,Hancox JC,Cannell MB

更新日期：2018-04-01 00:00:00

abstract：:The capacity of G protein-coupled receptors to modulate mechanistic target of rapamycin (mTOR) activity is a newly emerging paradigm with the potential to link cell surface receptors with cell survival. Cardiomyocyte viability is linked to signalling pathways involving Akt and mTOR, as well as increased glucose uptake...

journal_title：Biochemical pharmacology

authors： Sato M,Evans BA,Sandström AL,Chia LY,Mukaida S,Thai BS,Nguyen A,Lim L,Tan CYR,Baltos JA,White PJ,May LT,Hutchinson DS,Summers RJ,Bengtsson T

更新日期：2018-02-01 00:00:00

abstract：:HO-1 (heme oxygenase-1), an antioxidant enzyme, induced by rosiglitazone (PPAR ligands) can be a potential treatment of inflammation. However, the mechanisms of rosiglitazone-induced HO-1 expression in human pulmonary alveolar epithelial cells (HPAEpiCs) remain largely unknown. In this study, we found that upregulatio...

journal_title：Biochemical pharmacology

authors： Cho RL,Lin WN,Wang CY,Yang CC,Hsiao LD,Lin CC,Yang CM

更新日期：2018-02-01 00:00:00

abstract：:The signal transducer and activator of transcription 3 is a constitutively activated oncogenic protein in various human tumors and represents a valid target for anticancer drug design. In this study, we have achieved a new type of STAT3 inhibitors based on structural modifications on shikonin scaffold, guided by compu...

journal_title：Biochemical pharmacology

authors： Qiu HY,Fu JY,Yang MK,Han HW,Wang PF,Zhang YH,Lin HY,Tang CY,Qi JL,Yang RW,Wang XM,Zhu HL,Yang YH

更新日期：2017-12-15 00:00:00

abstract：:Multidrug resistance (MDR) represents a serious problem in cancer treatment. One strategy to overcome this obstacle is to identify agents that are selectively lethal to MDR cells. The aim of this study was to discover novel compounds against MDR leukemia and to determine the molecular mechanisms behind collateral sens...

journal_title：Biochemical pharmacology

authors： Hamdoun S,Fleischer E,Klinger A,Efferth T

更新日期：2017-12-15 00:00:00

abstract：:Telbivudine (LdT), a widely prescribed anti-hepatitis B virus (HBV) drug for the treatment of chronic Hepatitis B (CHB), causes adverse reactions ranging from creatine kinase (CK) elevation to myopathy. The purpose of this study was to explore the mechanism(s) of LdT induced CK elevation. The effects of LdT on mitocho...

journal_title：Biochemical pharmacology

authors： Jianfei L,Min W,Chunlai M,Bicui C,Jiming Z,Bin W

更新日期：2017-12-15 00:00:00

abstract：:The incidence, severity and progression of autoimmune diseases (e.g. scleroderma, multiple sclerosis, rheumatoid arthritis) and certain inflammatory diseases (e.g. asthma) are sex-biased where these pathologies dominate in women. However, other immune disorders such as sepsis, post-surgery infections and gout display ...

journal_title：Biochemical pharmacology

authors： Pace S,Sautebin L,Werz O

更新日期：2017-12-01 00:00:00

abstract：:Aldehyde oxidase (AOX) is a cytosolic enzyme responsible for the metabolism of some drugs and drug candidates. AOX catalyzes the oxidative hydroxylation of substrates including several aliphatic and aromatic aldehydes, and nitrogen-containing heterocyclic compounds. AOX is also reported to catalyze the reductive metab...

journal_title：Biochemical pharmacology

authors： Paragas EM,Humphreys SC,Min J,Joswig-Jones CA,Jones JP

更新日期：2017-12-01 00:00:00

abstract：:Here we report on the induction of resistance to photodynamic therapy (PDT) in the ABCG2-high human breast cancer cell line MA11 after repetitive PDT, using either Pheophorbide A (PhA) or di-sulphonated meso-tetraphenylchlorin (TPCS2a) as photosensitizer. Resistance to PhA-PDT was associated with enhanced expression o...

journal_title：Biochemical pharmacology

authors： Olsen CE,Weyergang A,Edwards VT,Berg K,Brech A,Weisheit S,Høgset A,Selbo PK

更新日期：2017-11-15 00:00:00