abstract：:Inorganic polyphosphate (polyP) is a physiological polymer composed of tens to hundreds of phosphate units linked together via phosphoanhydride bonds. Here we compared the biological activity of polyP (chain length of 40 phosphate units), complexed with Gd(3+) (polyP·Gd), with the one caused by polyP (as calcium salt)...

journal_title：Biochemical pharmacology

authors： Wang X,Huang J,Wang K,Neufurth M,Schröder HC,Wang S,Müller WEG

更新日期：2016-02-15 00:00:00

abstract：:The mammalian thioredoxin reductase (TrxR) isoenzymes, TrxR1 in cytosol or nucleus, TrxR2 in mitochondria, and TrxR3 in testis, are essential seleno-flavoenzymes with a conserved penultimate selenocysteine (Sec) residue at the C-terminus, and have attracted increasing interests as potential targets for development of ...

journal_title：Biochemical pharmacology

authors： Zhang J,Li Y,Duan D,Yao J,Gao K,Fang J

更新日期：2016-02-15 00:00:00

abstract：:Pioglitazone (PIO), a PPARγ agonist that improves glycemic control in type 2 diabetes through its insulin-sensitizing action, has been shown to exhibit beneficial effects in the vessel wall. For instance, it inhibits vascular smooth muscle cell (VSMC) proliferation, a major event in atherosclerosis and restenosis afte...

journal_title：Biochemical pharmacology

authors： Osman I,Segar L

更新日期：2016-02-01 00:00:00

abstract：:Mitochondrial carriers are proteins that shuttle a variety of metabolites, nucleotides and coenzymes across the inner mitochondrial membrane. The mitochondrial ADP/ATP carriers (AACs) specifically translocate the ATP synthesized within mitochondria to the cytosol in exchange for the cytosolic ADP, playing a key role i...

journal_title：Biochemical pharmacology

authors： Todisco S,Di Noia MA,Onofrio A,Parisi G,Punzi G,Redavid G,De Grassi A,Pierri CL

更新日期：2016-01-15 00:00:00

abstract：:Lactate, once considered a metabolic dead-end, has been recently proposed to support neuron bioenergetics. To better understand how lactate specifically influences cell energy metabolism, we studied the effects of lactate supplementation on SH-SY5Y human neuroblastoma cell bioenergetic fluxes. Lactate supplementation ...

journal_title：Biochemical pharmacology

authors： E L,Swerdlow RH

更新日期：2016-01-01 00:00:00

abstract：:Autophagy is generally regarded as a mechanism to promote cell survival. However, autophagy can occasionally be the mechanism responsible of cell demise. We have found that a concomitant depletion of glucose, nutrients and growth factors provoked cell death in a variety of cell lines. This death process was contingent...

journal_title：Biochemical pharmacology

authors： Mattiolo P,Yuste VJ,Boix J,Ribas J

更新日期：2015-12-15 00:00:00

abstract：:While skin aging is a naturally occurring process by senescence, exposure to ultraviolet (UV) radiation accelerates wrinkle formation and sagging of skin. UV induces skin aging by degrading collagen via activating matrix metalloproteinases (MMPs). In this study, we show that coumestrol, a metabolite of the soybean iso...

journal_title：Biochemical pharmacology

authors： Park G,Baek S,Kim JE,Lim TG,Lee CC,Yang H,Kang YG,Park JS,Augustin M,Mrosek M,Lee CY,Dong Z,Huber R,Lee KW

更新日期：2015-12-01 00:00:00

abstract：:This Festschrift contribution summarizes the perspectives of two of David Triggle's graduate students. Both share somewhat parallel scientific and career paths-i.e., enrolling in the Biochemical Pharmacology program at the University of Buffalo, pursuing graduate training under the mentorship of David Triggle and subs...

journal_title：Biochemical pharmacology

authors： Rampe D,Gopalakrishnan M

更新日期：2015-11-15 00:00:00

abstract：:What does it mean to be a mentor in science? Definitions of mentorship are freely spouted in publications and include concepts such as academic support, professional development, role modeling, interaction, impartment of knowledge, evaluation of work, demonstration of methodology, etc. Perhaps most of us would agree w...

journal_title：Biochemical pharmacology

authors： Smith SL

更新日期：2015-11-15 00:00:00

abstract：:During tumor progression, hypoxia-inducible factor 1 (HIF-1) plays a critical role in tumor angiogenesis and tumor growth by regulating the transcription of several genes in response to a hypoxic environment and changes in growth factors. This study was designed to investigate the effects of cinnamic aldehyde (CA) on ...

journal_title：Biochemical pharmacology

authors： Bae WY,Choi JS,Kim JE,Jeong JW

更新日期：2015-11-01 00:00:00

abstract：:The constitutive androstane receptor (CAR) modulates the transcription of numerous genes involving drug metabolism, energy homeostasis, and cell proliferation. Most functions of CAR however were defined from animal studies. Given the known species difference of CAR and the significant cross-talk between CAR and the pr...

journal_title：Biochemical pharmacology

authors： Li D,Mackowiak B,Brayman TG,Mitchell M,Zhang L,Huang SM,Wang H

更新日期：2015-11-01 00:00:00

abstract：:The challenges associated with developing more effective treatments for neurologic and psychiatric illness such as Alzheimer's disease and schizophrenia are considerable. Both the symptoms and the pathophysiology of these conditions are complex and poorly understood and the clinical presentations across different pati...

journal_title：Biochemical pharmacology

authors： Terry AV Jr,Callahan PM,Hernandez CM

更新日期：2015-10-15 00:00:00

abstract：:Nicotinic acetylcholine receptors (nAChRs) are widely distributed throughout the central nervous system, being expressed in neurons and non-neuronal cells, where they participate in a variety of physiological responses like memory, learning, locomotion, attention, among others. We will focus on the α7 nAChR subtype, w...

journal_title：Biochemical pharmacology

authors： Egea J,Buendia I,Parada E,Navarro E,León R,Lopez MG

更新日期：2015-10-15 00:00:00

abstract：:Minocycline is a semisynthetic tetracycline derivative; it has anti-inflammatory and anti-cancer effects distinct from its antimicrobial function. However, the molecular mechanism of minocycline-induced cytotoxicity in non-small cell lung cancer (NSCLC) cells has not been identified. Rad51 plays a central role in homo...

journal_title：Biochemical pharmacology

authors： Ko JC,Wang TJ,Chang PY,Syu JJ,Chen JC,Chen CY,Jian YT,Jian YJ,Zheng HY,Chen WC,Lin YW

更新日期：2015-10-01 00:00:00

abstract：:The prevalence of hyperuricemia/gout increases with aging. However, the effect of aging on function for excretion of uric acid to out of the body has not been clarified. We found that ileal uric acid clearance in middle-aged rats (11-12 months) was decreased compared with that in young rats (2 months). In middle-aged ...

journal_title：Biochemical pharmacology

authors： Ogura J,Kuwayama K,Sasaki S,Kaneko C,Koizumi T,Yabe K,Tsujimoto T,Takeno R,Takaya A,Kobayashi M,Yamaguchi H,Iseki K

更新日期：2015-09-01 00:00:00

abstract：:Microtubules are critical elements that are involved in a wide range of cellular processes, and thus, they have become an attractive target for many anticancer drugs. A novel synthesised compound, 12P, was identified as new microtubule inhibitor. This compound inhibits tubulin polymerisation through binding to the col...

journal_title：Biochemical pharmacology

authors： Yan J,Pang Y,Sheng J,Wang Y,Chen J,Hu J,Huang L,Li X

更新日期：2015-09-01 00:00:00

abstract：:Several drug compounds have failed in clinical trials due to extensive biotransformation by aldehyde oxidase (AOX) (EC 1.2.3.1). One of the main reasons is the difficulty in scaling clearance for drugs metabolised by AOX, from preclinical species to human. Using methotrexate as a probe substrate, we evaluated AOX meta...

journal_title：Biochemical pharmacology

authors： Choughule KV,Joswig-Jones CA,Jones JP

更新日期：2015-08-01 00:00:00

abstract：:Innovative crystallographic techniques have resulted in an exponential growth in the number of solved G-protein coupled receptor (GPCR) structures and a better understanding of the mechanisms of class A receptor activation and G protein binding. The recent release of the type 1 receptor for the corticotropin-releasing...

journal_title：Biochemical pharmacology

authors： Cordomí A,Ismail S,Matsoukas MT,Escrieut C,Gherardi MJ,Pardo L,Fourmy D

更新日期：2015-08-01 00:00:00

abstract：:Kidney cancer, also known as renal cell carcinoma (RCC), is one of the top 10 diagnosed cancers in the USA, and the incidence is rising. Despite major improvements in drug therapy strategies, RCC remains a deadly malignancy if not found and removed in its early stages. RCC is so highly drug-resistant that no effective...

journal_title：Biochemical pharmacology

authors： Singhal SS,Singhal J,Figarola JL,Riggs A,Horne D,Awasthi S

更新日期：2015-08-01 00:00:00

abstract：:The present study was aimed to investigate the metabolomics of sulfur amino acids in Zucker diabetic fatty (ZDF) rats, an obese type 2 diabetic animal model. Plasma levels of total cysteine, homocysteine and methionine, but not glutathione (GSH) were markedly decreased in ZDF rats. Hepatic methionine, homocysteine, cy...

journal_title：Biochemical pharmacology

authors： Kwak HC,Kim YM,Oh SJ,Kim SK

更新日期：2015-08-01 00:00:00

abstract：:Tumor cell growth requires large iron quantities and the deprivation of this metal induced by synthetic metal chelators is therefore an attractive method for limiting the cancer cell proliferation. The antiproliferative effect of the Quilamine HQ1-44, a new iron chelator vectorized toward tumor cells by a polyamine ch...

journal_title：Biochemical pharmacology

authors： Renaud S,Corcé V,Cannie I,Ropert M,Lepage S,Loréal O,Deniaud D,Gaboriau F

更新日期：2015-08-01 00:00:00

abstract：:Anticoagulants and anti-platelet agents are simultaneously administrated in clinical practice (i.e. percutaneous coronary intervention), which cause significant risk of systemic bleeding. Targeted delivery of anticoagulants to the activated platelets at sites of vascular injuries may condense the site-specific anticoa...

journal_title：Biochemical pharmacology

authors： Zhu Y,Lin Y,Liu A,Shui M,Li R,Liu X,Hu W,Wang Y

更新日期：2015-06-15 00:00:00

abstract：:Inflammation, especially chronic inflammation, is directly involvement in the pathogenesis of many diseases including cancer. An effective approach for managing inflammation is to employ chemicals to block activation of nuclear factor-κB (NF-κB), a key regulator for inflammatory processes. Piperlongumine (piplartine, ...

journal_title：Biochemical pharmacology

authors： Sun LD,Wang F,Dai F,Wang YH,Lin D,Zhou B

更新日期：2015-06-01 00:00:00

abstract：:Most human UDP-glucuronosyltransferase (UGT; EC 2.4.1.17) genes contain non-synonymous single nucleotide polymorphisms (nsSNPs) which cause amino acid substitutions. Allelic variants caused by nsSNPs may exhibit absent or reduced enzyme activity. UGT2B7 is one of the most important UGTs that glucuronidates abundant en...

journal_title：Biochemical pharmacology

authors： Yuan L,Qian S,Xiao Y,Sun H,Zeng S

更新日期：2015-05-01 00:00:00

abstract：:For several years the IMP/GMP-preferring cytosolic 5'-nucleotidase II (cN-II) has been considered as a therapeutic target in oncology. Indeed, various reports have indicated associations between cN-II expression level and resistance to anticancer agents in several cancer cell lines and in patients affected with neopla...

journal_title：Biochemical pharmacology

authors： Cividini F,Pesi R,Chaloin L,Allegrini S,Camici M,Cros-Perrial E,Dumontet C,Jordheim LP,Tozzi MG

更新日期：2015-03-15 00:00:00

abstract：:Adiponectin blocks hepatocellular carcinoma (HCC) progression by inducing cell apoptosis through the modulation of C-Jun N-terminal kinase and mammalian target of rapamycin. However, the precise upstream signaling pathways or molecules remain elusive. In the present study, we analyzed the role of antioxidant protein t...

journal_title：Biochemical pharmacology

authors： Xing SQ,Zhang CG,Yuan JF,Yang HM,Zhao SD,Zhang H

更新日期：2015-01-15 00:00:00

abstract：:Hepatic stellate cells (HSCs) are the primary source of matrix components in hepatic fibrosis. Ferulic acid (FA) has antifibrotic potential in renal and cardiac disease. However, whether FA comprises inhibitive effects of HSCs activation remains to be clarified. This study aims at evaluating the hypothesis that FA inh...

journal_title：Biochemical pharmacology

authors： Xu T,Pan Z,Dong M,Yu C,Niu Y

更新日期：2015-01-01 00:00:00

abstract：:Growing evidence suggests that hepatic-insulin resistance is sufficient to promote progression to cardiovascular disease. We have shown previously that liver-specific protein-tyrosine-phosphatase 1B (PTP1B) deficiency improves hepatic-insulin sensitivity and whole-body glucose homeostasis. The aim of this study was to...

journal_title：Biochemical pharmacology

authors： Agouni A,Tual-Chalot S,Chalopin M,Duluc L,Mody N,Martinez MC,Andriantsitohaina R,Delibegović M

更新日期：2014-12-15 00:00:00

abstract：BACKGROUND:Salvinorin A (SA) is a potent anti-inflammatory diterpene isolated from the Mexican plant S. divinorum. Recently we showed that the novel SA analog, PR-38 has an inhibitory effect on mouse gastrointestinal (GI) motility mediated by opioid and cannabinoid (CB) receptors. The aim of the study was to characteri...

journal_title：Biochemical pharmacology

authors： Sałaga M,Polepally PR,Zakrzewski PK,Cygankiewicz A,Sobczak M,Kordek R,Zjawiony JK,Krajewska WM,Fichna J

更新日期：2014-12-15 00:00:00

abstract：:CUDC-101 is the first small-molecule inhibitor designed to simultaneously inhibit epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2) and histone deacetylase (HDAC) in cancer cells. Recently, in its first in human phase I study, CUDC-101 showed promising single agent activity again...

journal_title：Biochemical pharmacology

authors： Wu CP,Hsiao SH,Su CY,Luo SY,Li YQ,Huang YH,Hsieh CH,Huang CW

更新日期：2014-12-15 00:00:00

abstract：:Hepcidin is a peptide hormone that controls systemic iron availability and is upregulated by iron and inflammation. Heparins have been shown to be efficient hepcidin inhibitors both in vitro and in vivo, even when their anticoagulant activity has been abolished by chemical reactions of oxidation/reduction (glycol-spli...

journal_title：Biochemical pharmacology

authors： Poli M,Asperti M,Ruzzenenti P,Mandelli L,Campostrini N,Martini G,Di Somma M,Maccarinelli F,Girelli D,Naggi A,Arosio P

更新日期：2014-12-01 00:00:00

abstract：:The vasoactive urotensin-II (UII), a cyclic undecapeptide widely distributed in cardiovascular, renal and endocrine systems, specifically binds the UII receptor (UT receptor), a G protein-coupled receptor (GPCR). The involvement of this receptor in numerous pathophysiological conditions including atherosclerosis, hear...

journal_title：Biochemical pharmacology

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

更新日期：2014-11-15 00:00:00

abstract：:Multiple lines of compelling evidence from clinical and population-based studies support that hyperinsulinemia often accompanying obesity-associated insulin insensitivity promotes colon carcinogenesis. Insulin can acetylate, thereby activating sterol regulator element-binding protein 1 (SREBP-1), a prime transcription...

journal_title：Biochemical pharmacology

authors： Song NY,Na HK,Baek JH,Surh YJ

更新日期：2014-11-01 00:00:00

abstract：:Metabolic and cardiovascular disease patients have increased plasma levels of lipids and, specifically, of palmitate, which can be toxic for several tissues. Trimetazidine (TMZ), a partial inhibitor of lipid oxidation, has been proposed as a metabolic modulator for several cardiovascular pathologies. However, its mech...

journal_title：Biochemical pharmacology

authors： Kuzmicic J,Parra V,Verdejo HE,López-Crisosto C,Chiong M,García L,Jensen MD,Bernlohr DA,Castro PF,Lavandero S

更新日期：2014-10-01 00:00:00

abstract：:GABAB receptors assemble from GABAB1 and GABAB2 subunits. GABAB2 additionally associates with auxiliary KCTD subunits (named after their K(+) channel tetramerization-domain). GABAB receptors couple to heterotrimeric G-proteins and activate inwardly-rectifying K(+) channels through the βγ subunits released from the G-p...

journal_title：Biochemical pharmacology

authors： Adelfinger L,Turecek R,Ivankova K,Jensen AA,Moss SJ,Gassmann M,Bettler B

更新日期：2014-10-01 00:00:00

abstract：:The nitroderivative 1-nitro-2-phenylethane (NPE) was recently described as a compound possessing heme-dependent soluble guanylyl cyclase (sGC) stimulating properties in vascular smooth muscle cells. In this study, we tested such pharmacological property of NPE in mice pancreatic acinar cells subjected to the bile salt...

journal_title：Biochemical pharmacology

authors： Cosker F,Lima FJ,Lahlou S,Magalhães PJ

更新日期：2014-09-15 00:00:00

abstract：:CYP2C19 (formerly known as CYP2C75), highly homologous to human CYP2C19, has been identified in cynomolgus and rhesus macaques, non-human primate species widely used in drug metabolism studies. CYP2C19 is predominantly expressed in liver and encodes a functional drug-metabolizing enzyme. Genetic variants in human CYP2...

journal_title：Biochemical pharmacology

authors： Uno Y,Matsushita A,Shukuya M,Matsumoto Y,Murayama N,Yamazaki H

更新日期：2014-09-15 00:00:00

abstract：:The peroxisome proliferator-activated receptors (PPARs) are ligand-dependent transcription factors involved in lipid metabolism and glucose utilization, in cell growth, differentiation and apoptosis, and in the regulation of pro-inflammatory genes expression such as cyclooxygenase-2 (COX-2). PPARγ is the main isoform ...

journal_title：Biochemical pharmacology

authors： Casali CI,Weber K,Faggionato D,Gómez EM,Tome MC

更新日期：2014-08-15 00:00:00

abstract：:Phospholipase A2 (PLA2) cleave phospholipids preferentially at the sn-2 position, liberating free fatty acids and lysophospholipids. They are classified into six main groups based on size, location, function, substrate specificity and calcium requirement. These classes include secretory PLA2 (sPLA2), cytosolic (cPLA2)...

journal_title：Biochemical pharmacology

authors： Quach ND,Arnold RD,Cummings BS

更新日期：2014-08-15 00:00:00

abstract：:The aim of this study was to find the peptide ligands to inhibit Candida albicans secreted aspartyl proteinase 2 (Sap2). First, a ligand library, containing 300 different peptides, was constructed, and their interaction with Sap2 was separately calculated by molecular dynamic software. Second, 10 peptide ligands with ...

journal_title：Biochemical pharmacology

authors： Jebali A,Hajjar FH,Hekmatimoghaddam S,Kazemi B,De La Fuente JM,Rashidi M

更新日期：2014-08-15 00:00:00