abstract：:Tumor necrosis factor-alpha (TNF-alpha) is a mediator of multiple inflammatory diseases. Vascular endothelial growth factor (VEGF) plays a critical role in TNF-alpha-mediated diseases. We investigated the inhibitory effects of 3,3',4',5,5',7-hexahydroxyflavone (myricetin), an abundant natural flavonoid, on TNF-alpha-i...

journal_title：Biochemical pharmacology

authors： Kim JE,Kwon JY,Lee DE,Kang NJ,Heo YS,Lee KW,Lee HJ

更新日期：2009-02-01 00:00:00

abstract：:The characterization of the potent p38 inhibitor BIRB796 as a dual inhibitor of p38/Jun N-terminal kinases (JNK) mitogen-activated protein kinases (EC 2.7.11.24) has complicated the interpretation of its reported anti-inflammatory activity. To better understand the contribution of JNK2 inhibition to the anti-inflammat...

journal_title：Biochemical pharmacology

authors： Gruenbaum LM,Schwartz R,Woska JR Jr,DeLeon RP,Peet GW,Warren TC,Capolino A,Mara L,Morelock MM,Shrutkowski A,Jones JW,Pargellis CA

更新日期：2009-02-01 00:00:00

abstract：:8-Chloro-cAMP and 8-chloro-adenosine (8-Cl-Ado) are known to inhibit proliferation of cancer cells by converting 8-Cl-Ado into an ATP analog, 8-chloro-ATP (8-Cl-ATP). Because type II topoisomerases (Topo II) are ATP-dependent, we infer that 8-Cl-Ado exposure might interfere with Topo II activities and DNA metabolism i...

journal_title：Biochemical pharmacology

authors： Yang SY,Jia XZ,Feng LY,Li SY,An GS,Ni JH,Jia HT

更新日期：2009-02-01 00:00:00

abstract：:The nuclear receptors liver X receptor (LXR) alpha and LXRbeta serve as oxysterol receptors and play an important role in the regulation of lipid metabolism. We investigated the potential effects of LXRs on pathways of colon carcinogenesis and found that LXR activation suppresses the transactivation activity of beta-c...

journal_title：Biochemical pharmacology

authors： Uno S,Endo K,Jeong Y,Kawana K,Miyachi H,Hashimoto Y,Makishima M

更新日期：2009-01-15 00:00:00

abstract：:Aberrant activation of Jak/Stat signaling causes a number of hematopoietic disorders and oncogenesis, and therefore the effective inhibitors of the Jak/Stat signaling pathway may be therapeutically useful. TEL-Jak2 gene fusion, which has been identified in human leukemia, encodes a chimeric protein endowed with consti...

journal_title：Biochemical pharmacology

authors： Funakoshi-Tago M,Tago K,Nishizawa C,Takahashi K,Mashino T,Iwata S,Inoue H,Sonoda Y,Kasahara T

更新日期：2008-12-15 00:00:00

abstract：:Structurally diverse chemotherapeutic and chemopreventive drugs, including camptothecin, doxorubicin, sanguinarine, and others, were found to cause covalent crosslinking of proliferating cell nuclear antigen (PCNA) trimers in mammalian cells exposed to fluorescent light. This PCNA damage was caused by both nuclear and...

journal_title：Biochemical pharmacology

authors： Bae SI,Zhao R,Snapka RM

更新日期：2008-12-15 00:00:00

abstract：:Naturally occurring toxins are invaluable tools for exploration of the structure and function relationships of voltage-gated sodium channels (VGSCs). In this study, we isolated and characterized a novel VGSC toxin named jingzhaotoxin-II (JZTX-II) from the tarantula Chilobrachys jingzhao venom. JZTX-II consists of 32 a...

journal_title：Biochemical pharmacology

authors： Wang M,Liu Q,Luo H,Li J,Tang J,Xiao Y,Liang S

更新日期：2008-12-15 00:00:00

abstract：:Curcumin, a yellow pigment present in the Indian spice turmeric (associated with curry powder), has been linked with suppression of inflammation; angiogenesis; tumorigenesis; diabetes; diseases of the cardiovascular, pulmonary, and neurological systems, of skin, and of liver; loss of bone and muscle; depression; chron...

journal_title：Biochemical pharmacology

authors： Anand P,Thomas SG,Kunnumakkara AB,Sundaram C,Harikumar KB,Sung B,Tharakan ST,Misra K,Priyadarsini IK,Rajasekharan KN,Aggarwal BB

更新日期：2008-12-01 00:00:00

abstract：:The discovery of caspase activation counts as one of the most important finds in the biochemistry of apoptosis. However, targeted disruption of caspases does not impair every type of apoptosis. Other proteases can replace caspases and several so called "caspase independent" pathways are now described. Here we review o...

journal_title：Biochemical pharmacology

authors： Torriglia A,Leprêtre C,Padrón-Barthe L,Chahory S,Martin E

更新日期：2008-12-01 00:00:00

abstract：:Escape from the proper control of the cell cycle by up-regulation of cyclins or aberrant activation of cyclin-dependent kinases (CDKs) as well as by inactivation of cellular inhibitors of CDKs (CKI) leads to malignant transformation. Loss of cellular CKIs in cancers provided a rationale for development of pharmacologi...

journal_title：Biochemical pharmacology

authors： Wesierska-Gadek J,Hajek SB,Sarg B,Wandl S,Walzi E,Lindner H

更新日期：2008-12-01 00:00:00

abstract：:Itch, a member of the E6AP carboxy terminus (HECT) domain-containing family of ubiquitin E3 ligases, acts in concert with the ubiquitin activating enzyme (E1) and the ubiquitin conjugating enzyme (E2) to catalyze ubiquitylation of protein targets. This sub-family of E3s shares a 350 residue C-terminal HECT domain havi...

journal_title：Biochemical pharmacology

authors： Raimondo D,Giorgetti A,Bernassola F,Melino G,Tramontano A

更新日期：2008-12-01 00:00:00

abstract：:The constitutive androstane receptor (CAR; NR1I3) is a nuclear receptor responsible for the recognition of potentially toxic endo- and exogenous compounds whose elimination from the body is accelerated by the CAR-mediated inducible expression of metabolizing enzymes and transporters. Despite the importance of CAR, few...

journal_title：Biochemical pharmacology

authors： Küblbeck J,Jyrkkärinne J,Poso A,Turpeinen M,Sippl W,Honkakoski P,Windshügel B

更新日期：2008-11-15 00:00:00

abstract：:The thiopurine drugs 6-mercaptopurine (6-MP) and 6-thioguanine (6-TG) are well-established agents for the treatment of leukaemia but their main modes of action are controversial. Thiopurine methyltransferase (TPMT) metabolises thiopurine drugs and influences their cytotoxic activity. TPMT, like DNA methyltransferases ...

journal_title：Biochemical pharmacology

authors： Hogarth LA,Redfern CP,Teodoridis JM,Hall AG,Anderson H,Case MC,Coulthard SA

更新日期：2008-10-15 00:00:00

abstract：:The insulin receptor (IR) is composed of two alpha-chains that bind ligands and two beta-chains that possess an intracellular tyrosine kinase activity. The IR is expressed in cells as two isoforms containing or not exon 11 (IRB and IRA, respectively). Several mRNA studies have demonstrated that the two isoforms are co...

journal_title：Biochemical pharmacology

authors： Blanquart C,Achi J,Issad T

更新日期：2008-10-01 00:00:00

abstract：:Oleanolic acid (OA) is a natural triperpenoid that protects against a variety of hepatotoxicants such as carbon tetrachloride, cadmium, acetaminophen, and bromobenzene. To gain insight into the molecular mechanisms of this generalized hepatoprotection, genomic analysis was performed on mouse and rat livers after OA tr...

journal_title：Biochemical pharmacology

authors： Liu J,Wu Q,Lu YF,Pi J

更新日期：2008-10-01 00:00:00

abstract：:The glycolipid alpha-galactosylceramide (alpha-GalCer), when presented on CD1 molecules by antigen presenting cells (APCs) to invariant NKT (iNKT cells), is a potent immunomodulator. Indoleamine 2,3-dioxygenase (IDO), an enzyme catalyzing the catabolism of L-tryptophan along the kynurenine pathway, is inducible in APC...

journal_title：Biochemical pharmacology

authors： Fallarini S,Paoletti T,Panza L,Lombardi G

更新日期：2008-09-15 00:00:00

abstract：:Cyclophosphamides are pro-drugs whose killing agent is produced from an aldehyde that is formed by the action of a P450 oxidation step. The mustard from the aldehyde can destroy bone marrow cells as well as the tumor. Aldehyde dehydrogenase (EC 1.2.1.3) can oxidize the aldehyde and hence inactivate the cytotoxic inter...

journal_title：Biochemical pharmacology

authors： Ho KK,Mukhopadhyay A,Li YF,Mukhopadhyay S,Weiner H

更新日期：2008-09-01 00:00:00

abstract：:We have previously found that repeated exposure to heroin reduces liver synthesis of morphine-3-glucuronide (M3G) and increases the production of morphine-6-glucuronide (M6G), which normally is not formed in the rat. By contrast repeated exposure to naltrexone does not activate M6G synthesis but increases the V(max) o...

journal_title：Biochemical pharmacology

authors： Antonilli L,Brusadin V,Milella MS,Sobrero F,Badiani A,Nencini P

更新日期：2008-09-01 00:00:00

abstract：:Benzoxathiolone derivatives have been reported to show pharmacological potentials in the psoriasis and acne. However, molecular basis for these pharmacological properties is little known. We postulated that the derivatives could mediate some of their pharmacological actions by modulating nuclear factor (NF)-kappaB act...

journal_title：Biochemical pharmacology

authors： Kim MH,Lee HY,Roh E,Kim BH,Chung EY,Lee YR,Lee IJ,Lee H,Lee CK,Han SB,Kim Y

更新日期：2008-08-01 00:00:00

abstract：:Anti-angiogenic therapy mediated by drugs and food components is an established strategy for cancer prevention. Our previous cell-culture studies identified a food-derived anti-angiogenic compound, tocotrienol (T3, an unsaturated vitamin E), as a potential angiogenic inhibitor. Among T3 isomers, delta-T3 is considered...

journal_title：Biochemical pharmacology

authors： Shibata A,Nakagawa K,Sookwong P,Tsuzuki T,Oikawa S,Miyazawa T

更新日期：2008-08-01 00:00:00

abstract：:The discipline of biochemical pharmacology emerged in the late 1940s as a result of an increasing emphasis on understanding drug mechanisms at the cellular level. This research approach has contributed significantly to the development of many new drug classes including antihypertensive, antifective, cholesterol loweri...

journal_title：Biochemical pharmacology

authors： Enna SJ,Feuerstein GZ,Piette J,Williams M

更新日期：2008-07-01 00:00:00

abstract：:Poly(ADPR)polymerases' (PARPs) inhibitors potentiate the cytotoxic effects of chemotherapeutic agents like alkylating compounds and TOPO I poisons, while their action in combination with cisplatin still needs investigation. In fact, one of the earliest responses to DNA single- or double-strand breaks is the synthesis ...

journal_title：Biochemical pharmacology

authors： Gambi N,Tramontano F,Quesada P

更新日期：2008-06-15 00:00:00

abstract：:Elongator, a multi-subunit complex assembled by the IkappaB kinase-associated protein (IKAP)/hELP1 scaffold protein is involved in transcriptional elongation in the nucleus as well as in tRNA modifications in the cytoplasm. However, the biological processes regulated by Elongator in human cells only start to be elucid...

journal_title：Biochemical pharmacology

authors： Cornez I,Creppe C,Gillard M,Hennuy B,Chapelle JP,Dejardin E,Merville MP,Close P,Chariot A

更新日期：2008-06-01 00:00:00

abstract：:Hsp90 is a protein chaperone regulating the stability and activity of many signalling molecules. The requirement of Hsp90 activity in the NF-kappaB pathway has been recently reported by several authors using the Hsp90 ATPase inhibitor geldanamycin (GA), an anti-tumor drug. Hsp90 inhibition blocks the synthesis and act...

journal_title：Biochemical pharmacology

authors： Crèvecoeur J,Merville MP,Piette J,Gloire G

更新日期：2008-06-01 00:00:00

abstract：:Arsenic trioxide (ATO) is an effective therapeutic agent for the treatment of acute promyelocytic leukemia, but successful application of this agent may occasionally require the use of sensitizing strategies. The present work demonstrates that the flavonoids quercetin and chrysin cooperate with ATO to induce apoptosis...

journal_title：Biochemical pharmacology

authors： Ramos AM,Aller P

更新日期：2008-05-15 00:00:00

abstract：:Sustained activation of AMP-activated protein kinase (AMPK) induces apoptosis in several cell types. In pancreatic beta cells this occurs under glucose limitation, or in the presence of the pharmacological AMPK activator 5-aminoimidazole-4-carboxamide-riboside (AICAR). It is unknown whether Akt activation can countera...

journal_title：Biochemical pharmacology

authors： Cai Y,Wang Q,Ling Z,Pipeleers D,McDermott P,Pende M,Heimberg H,Van de Casteele M

更新日期：2008-05-15 00:00:00

abstract：:Vectorial secretion of cationic compounds across tubular epithelial cells is an important function of the kidney. This uni-directed transport is mediated by two cooperative functions, which are membrane potential-dependent organic cation transporters at the basolateral membranes and H+/organic cation antiporters at th...

journal_title：Biochemical pharmacology

authors： Terada T,Inui K

更新日期：2008-05-01 00:00:00

abstract：:In this study, the differentiation-promoting effects of terbinafine (Lamisil), TB) were investigated in human epithelioid squamous carcinoma (A431) cells. The polyhydroxyethylmethacrylate (poly-HEMA)- and type-I collagen-coated culture plate models were adapted to harvest the TB-induced differentiated cells by agitati...

journal_title：Biochemical pharmacology

authors： Huang CS,Ho WL,Lee WS,Sheu MT,Wang YJ,Tu SH,Chen RJ,Chu JS,Chen LC,Lee CH,Tseng H,Ho YS,Wu CH

更新日期：2008-05-01 00:00:00

abstract：:Herbal antidiabetic preparations are often used as an add-on therapy in diabetes and such herbal preparations often contains quercetin that can inhibit cytochrome P450 (CYP) 3A4. This enzyme is responsible for metabolizing pioglitazone, a commonly used antidiabetic agent. Hence, it was speculated that quercetin may in...

journal_title：Biochemical pharmacology

authors： Umathe SN,Dixit PV,Kumar V,Bansod KU,Wanjari MM

更新日期：2008-04-15 00:00:00

abstract：:A growing body of evidence suggests that mitochondria take up calcium upon receptor (agonist) stimulation and that this contributes to the dynamics of spatiotemporal calcium signaling. We have previously shown that engagement of the high-affinity receptor for immunoglobulin E (FcepsilonRI) stimulates mitochondrial cal...

journal_title：Biochemical pharmacology

authors： Suzuki Y,Yoshimaru T,Inoue T,Nunomura S,Ra C

更新日期：2008-04-01 00:00:00

abstract：:The aim of the present study was to estimate the relative contribution of rat P450 isoforms to the metabolism of caffeine and to assess the usefulness of caffeine as a marker substance for estimating the activity of P450 in rat liver and its potential for pharmacokinetic interactions in pharmacological experiments. Th...

journal_title：Biochemical pharmacology

authors： Kot M,Daniel WA

更新日期：2008-04-01 00:00:00

abstract：:There is increasing evidence that human arylamine N-acetyltransferase type 1 (NAT1, EC 2.3.1.5), although first identified as a homologue of a drug-metabolising enzyme, appears to be a marker in human oestrogen receptor positive breast cancer. Mouse Nat2 is the mouse equivalent of human NAT1. The development of mouse ...

journal_title：Biochemical pharmacology

authors： Kawamura A,Westwood I,Wakefield L,Long H,Zhang N,Walters K,Redfield C,Sim E

更新日期：2008-04-01 00:00:00

abstract：:Deoxyelephantopin (ESD) was reported to potentiate apoptosis, inhibit invasion and abolish osteoclastogenesis but no target protein was disclosed. Here, we discovered that ESD could significantly inhibit the proliferation of different cancer cells and induce apoptosis and cell cycle arrest at G(2)/M phase in HeLa cell...

journal_title：Biochemical pharmacology

authors： Zou G,Gao Z,Wang J,Zhang Y,Ding H,Huang J,Chen L,Guo Y,Jiang H,Shen X

更新日期：2008-03-15 00:00:00

abstract：:Four pseudo-symmetrical tamoxifen derivatives, RID-B (13), RID-C (14), RID-D (15), and bis(dimethylaminophenetole) (16), were synthesized via the novel three-component coupling reaction, and the structure-activity relationships of these pseudo-symmetrical tamoxifen derivatives were examined. It was discovered that 13 ...

journal_title：Biochemical pharmacology

authors： Shiina I,Sano Y,Nakata K,Kikuchi T,Sasaki A,Ikekita M,Nagahara Y,Hasome Y,Yamori T,Yamazaki K

更新日期：2008-03-01 00:00:00

abstract：:We recently found that simvastatin can modulate the nuclear factor-kappaB (NF-kappaB) activation pathway, but whether other statins have similar effects to those of simvastatin is unknown. Therefore, we evaluated the effect six different statins on TNF-induced NF-kappaB activation in human myeloid leukemia cells. We t...

journal_title：Biochemical pharmacology

authors： Ahn KS,Sethi G,Aggarwal BB

更新日期：2008-02-15 00:00:00

abstract：:The present study was designed to evaluate the radioprotective effect of N- acetylcysteine (NAC) on gamma-radiation induced toxicity in hepatic tissue in rat. The cellular changes were estimated using malondialdehyde (MDA, an index of lipid peroxidation), superoxide dismutase (SOD), glutathione peroxidase (GSHPx), red...

journal_title：Biochemical pharmacology

authors： Mansour HH,Hafez HF,Fahmy NM,Hanafi N

更新日期：2008-02-01 00:00:00

abstract：:5-Aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR) is a commonly used pharmacological agent to study physiological effects which are similar to those of exercise. However, signal transduction pathways by which AICAR elicits downstream effects in liver are poorly understood. We report here that AICAR not on...

journal_title：Biochemical pharmacology

authors： Wang HM,Mehta S,Bansode R,Huang W,Mehta KD

更新日期：2008-01-15 00:00:00

abstract：:Thermodynamic parameters DeltaG degrees , DeltaH degrees and DeltaS degrees of the binding equilibrium of 12 ligands (six agonists and six antagonists) to the A(2B) adenosine receptor subtype have been determined by affinity measurements carried out on HEK 293 cells stably transfected with human A(2B) adenosine recept...

journal_title：Biochemical pharmacology

authors： Gessi S,Fogli E,Sacchetto V,Varani K,Merighi S,Leung E,Lennan SM,Borea PA

更新日期：2008-01-15 00:00:00

abstract：:To uncover the full spectrum of its pharmacological activities, the selective COX-2 inhibitor celecoxib is routinely being used at concentrations of up to 100 microM in cell culture. At these elevated concentrations, several COX-2-independent effects were identified, although many details of these events have remained...

journal_title：Biochemical pharmacology

authors： Pyrko P,Kardosh A,Schönthal AH

更新日期：2008-01-15 00:00:00

abstract：:The discovery and development of medications to treat addiction and notably, cocaine addiction, have been frustrated by both the complexity of the disorder and the lack of target validation in human subjects. The dopamine transporter has historically been a primary target for cocaine abuse medication development, but ...

journal_title：Biochemical pharmacology

authors： Rothman RB,Baumann MH,Prisinzano TE,Newman AH

更新日期：2008-01-01 00:00:00