Responsiveness of an SV40-immortalized hepatocyte cell line to growth hormone.

abstract：:The effects of two new phthalazinone derivatives, azelastine (AZ) and flezelastine (FZ), on the reversal of resistance to doxorubicin (dox) were studied using two variants of the rat C6 glioblastoma cell line, selected with dox (C6 0.5) or with vincristine (C6 1V). Both lines presented a multidrug-resistant phenotype ...

journal_title：Biochemical pharmacology

authors： Hu YP,Robert J

更新日期：1995-07-17 00:00:00

abstract：:Tachykinin NK receptors (NKRs) differ to a large degree among species with respect to their affinities for small molecule antagonists. The aims of the present study were to clone NKRs from gerbil (NK2R and NK3R) and dog (NK1R, NK2R and NK3R) in which the sequence was previously unknown and to investigate the potency o...

journal_title：Biochemical pharmacology

authors： Leffler A,Ahlstedt I,Engberg S,Svensson A,Billger M,Oberg L,Bjursell MK,Lindström E,von Mentzer B

更新日期：2009-05-01 00:00:00

abstract：:Within the tissue surrounding the necrotic lesion, following a cryogenic injury of the brain, there is a definite activation of phospholipase A2 (at 2 and 4 hr post lesion) that accounts, at least in part, for the phospholipid breakdown. There is also an activation of cholinephosphotransferase (at 2 hr post lesion) th...

journal_title：Biochemical pharmacology

authors： Arrigoni E,Averet N,Cohadon F

更新日期：1987-11-01 00:00:00

abstract：:Ribonucleotide reductase is the rate-limiting enzyme for the de novo synthesis of deoxynucleoside triphosphates and therefore represents a good target for cancer chemotherapy. Trimidox (3,4,5-trihydroxybenzamidoxime) was identified as a potent inhibitor of this enzyme and was shown to significantly decrease deoxycytid...

journal_title：Biochemical pharmacology

authors： Fritzer-Szekeres M,Salamon A,Grusch M,Horvath Z,Höchtl T,Steinbrugger R,Jäger W,Krupitza G,Elford HL,Szekeres T

更新日期：2002-08-01 00:00:00

abstract：:Radioligand binding techniques are commonly used in the characterization of beta-adrenergic receptors on human peripheral leukocytes. Accurate interpretation of receptor binding parameters necessitates appropriate radioligand selection. In addition, cell isolation techniques should have minimal effect on the binding p...

journal_title：Biochemical pharmacology

authors： Szefler SJ,Edwards CK 3rd,Haslett C,Zahniser NR,Miller JA,Henson PM

更新日期：1987-05-15 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：: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：:Multidrug resistance (MDR) is a phenomenon where cancer cells become simultaneously resistant to anticancer drugs with different structures and mechanisms of action. MDR has been shown to be associated with overexpression of ATP-binding cassette (ABC) transporters. Here, we report that telatinib, a small molecule tyro...

journal_title：Biochemical pharmacology

authors： Sodani K,Patel A,Anreddy N,Singh S,Yang DH,Kathawala RJ,Kumar P,Talele TT,Chen ZS

更新日期：2014-05-01 00:00:00

abstract：:Rational approaches to targeted cancer therapy have begun to predominate the pipelines of oncology drug development. Our rapidly increasing understanding of the "wiring" of tumor cells and the vulnerabilities of such cells that can potentially be exploited through targeted treatments has opened up enormous opportuniti...

journal_title：Biochemical pharmacology

authors： Sharma SV,Settleman J

更新日期：2010-09-01 00:00:00

abstract：:Resistance to anti-cancer chemotherapies often leads to regional failure, and can be caused by biochemical and/or physiological mechanisms. Biochemical mechanisms include the overexpression of resistance-conferring proteins. In contrast, physiological resistance involves the tumor microenvironment, and can be caused b...

journal_title：Biochemical pharmacology

authors： Mahoney BP,Raghunand N,Baggett B,Gillies RJ

更新日期：2003-10-01 00:00:00

abstract：:Augmented endothelium-dependent contractions (EDC) contributes to endothelial dysfunction and vascular disease progression. An early signal in EDC is cytosolic [Ca2+]i rise in endothelial cells, which stimulates the production of contractile prostanoids, leading to vascular contraction. In this study, the molecular id...

journal_title：Biochemical pharmacology

authors： Liang C,Zhang Y,Zhuo D,Lo CY,Yu L,Lau CW,Kwan YW,Tse G,Huang Y,Yao X

更新日期：2019-01-01 00:00:00

abstract：:"Ecstasy" [(+/-)-3,4-methylenedioxymethamphetamine or MDMA] is a CNS stimulant, whose use is increasing despite evidence of long-term neurotoxicity. In vitro, the majority of MDMA is demethylenated to (+/-)-3,4-dihydroxymethamphetamine (DHMA) by the polymorphic cytochrome P450 2D6 (CYP2D6). We investigated the demethy...

journal_title：Biochemical pharmacology

authors： Ramamoorthy Y,Yu AM,Suh N,Haining RL,Tyndale RF,Sellers EM

更新日期：2002-06-15 00:00:00

abstract：:Dicumarol is routinely added to the 3-[4,4-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay to study the role of NAD(P)H:quinone oxido-reductase in drug activation and detoxification. We assessed the direct impact of dicumarol (a mitochondrial uncoupler) on the MTT assay. Mouse mammary tumor (EMT6) an...

journal_title：Biochemical pharmacology

authors： Collier AC,Pritsos CA

更新日期：2003-07-15 00:00:00

abstract：:Nobiletin is a polymethoxylated flavone found in certain citrus fruits that exhibits various pharmacological effects including anti-inflammatory, antitumor and neuroprotective properties. The present study investigated the effects of nobiletin on insulin sensitivity in obese diabetic ob/ob mice, and the possible mecha...

journal_title：Biochemical pharmacology

authors： Lee YS,Cha BY,Saito K,Yamakawa H,Choi SS,Yamaguchi K,Yonezawa T,Teruya T,Nagai K,Woo JT

更新日期：2010-06-01 00:00:00

abstract：:Casein-elicited mouse peritoneal macrophages cultured in the presence of phorbol 12-myristate 13-acetate (PMA) express u-PA. Induction is maximal after 4 hr of stimulation and u-PA activity is mainly recovered with the membrane fraction of the cellular lysate. This enzymatic activity is inhibited by isopropylmethylpho...

journal_title：Biochemical pharmacology

authors： Dubois P,Lison D,Lauwerys R

更新日期：1988-06-01 00:00:00

abstract：:The role of Ca2+ and protein kinase C (PKC) activity in the release of immunoreactive endothelin-1 (ET-1) from cultured porcine aortic endothelial cells of first or second passage has been studied. ET-1 accumulation within cells and secretion into cell-conditioned medium over 3 and/or 5 hr was measured. Confluent cell...

journal_title：Biochemical pharmacology

authors： Brunner F

更新日期：1995-06-16 00:00:00

abstract：:The oxidative metabolism of more than 20 drugs (e.g. sparteine, debrisoquine, dextromethorphan) is mediated by cytochrome P450IID6. Codeine O-demethylation to morphine was recently demonstrated to co-segregate with the polymorphic metabolism of debrisoquine and dextromethorphan. The female Dark-Agouti rat (DA) is an a...

journal_title：Biochemical pharmacology

authors： Mikus G,Somogyi AA,Bochner F,Eichelbaum M

更新日期：1991-03-01 00:00:00

abstract：:HeLa S3 cells exposed to Adriamycin and Daunomycin for 3 hr at EC90 and 10 x EC90 concentrations and incubated in drug-free medium demonstrated the characteristics of apoptosis, morphological changes and fragmentation of DNA into oligonucleosome-sized fragments. The kinetics of DNA degradation after incubation with Ad...

journal_title：Biochemical pharmacology

authors： Skladanowski A,Konopa J

更新日期：1993-08-03 00:00:00

abstract：:Sulphate conjugation was investigated using extracts of human foetal liver cells in culture. The three reactions which are involved in sulphate conjugation were measured singly or in combination: they are (i) the PAPS generation catalyzed by ATP-sulphurylase and adenosine 5'-phosphosulphate (APS)-kinase, (ii) the phen...

journal_title：Biochemical pharmacology

authors： Tan TM,Sit KH,Wong KP

更新日期：1988-12-15 00:00:00

abstract：:Targeting of deregulated protein tyrosine kinases has been proposed as a new approach in the therapeutic intervention against pathological processes including proliferative disorders and cancer. Using a screening approach based on a comparative evaluation of antiproliferative effects in a panel of tumor cells with dif...

journal_title：Biochemical pharmacology

authors： Cassinelli G,Lanzi C,Pensa T,Gambetta RA,Nasini G,Cuccuru G,Cassinis M,Pratesi G,Polizzi D,Tortoreto M,Zunino F

更新日期：2000-06-15 00:00:00

abstract：:A sesquiterpene furanoic acid (SFA) marine natural product isolated from soft corals of the genus Sinularia (Bowden et al., Aust J Chem 36: 371-376, 1983) was found to inactivate bee venom phospholipase A2 (bvPLA2, EC 3.1.1.4) in vitro. In this study, we characterized the kinetics of inactivation of bvPLA2 by this com...

journal_title：Biochemical pharmacology

authors： Grace KJ,Zavortink D,Jacobs RS

更新日期：1994-04-20 00:00:00

abstract：:Activation of the P2Y(1) nucleotide receptor in platelets by ADP causes changes in shape and aggregation, mediated by activation of phospholipase C (PLC). Recently, MRS2500(2-iodo-N(6)-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate) was introduced as a highly potent and selective antagonist for this rece...

journal_title：Biochemical pharmacology

authors： Cattaneo M,Lecchi A,Ohno M,Joshi BV,Besada P,Tchilibon S,Lombardi R,Bischofberger N,Harden TK,Jacobson KA

更新日期：2004-11-15 00:00:00

abstract：:The turnover rate of vitamin E is slow in nerve tissue. Therefore, we have developed in vitro techniques to study the biochemical reactions of this nutrient in brain. Subcellular fractions were isolated from the cerebral hemispheres of 4-month-old, male, Fisher 344 rats. Aliquots of fractions (500 micrograms protein) ...

journal_title：Biochemical pharmacology

authors： Vatassery GT

更新日期：1993-06-09 00:00:00

abstract：:In our search for NF-kappaB inhibitors from natural resources, we have previously identified two structurally related dilignans, manassantin A and B as specific inhibitors of NF-kappaB activation from Saururus chinensis. However, their molecular mechanism of action remains unclear. We here demonstrate that manassantin...

journal_title：Biochemical pharmacology

authors： Lee JH,Hwang BY,Kim KS,Nam JB,Hong YS,Lee JJ

更新日期：2003-11-15 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：:A compound, YM-53792, was identified as an inhibitor of interleukin-2 (IL-2) gene promoter activity, using a Jurkat cell-based reporter system in which the luciferase gene is regulated by the IL-2 gene promoter. Production of IL-2, interleukin-4 (IL-4) and interleukin-5 (IL-5) from human peripheral blood mononuclear c...

journal_title：Biochemical pharmacology

authors： Kuromitsu S,Fukunaga M,Lennard AC,Masuho Y,Nakada S

更新日期：1997-11-01 00:00:00

abstract：:Recently, the marked decline in renal carnitine reabsorption has been thought to account fotr the systemic carnitine deficiency in juvenile visceral steatosis (JVS) mice. We have conducted a kinetic analysis using embryonic fibroblasts derived from normal, heterozygous, and homozygous jvs mice and found that the high-...

journal_title：Biochemical pharmacology

authors： Hashimoto N,Suzuki F,Tamai I,Nikaido H,Kuwajima M,Hayakawa J,Tsuji A

更新日期：1998-05-15 00:00:00

abstract：:The effects of delta 8-tetrahydrocannabinol (delta 8-THC) and its major and active metabolite, 11-hydroxy-delta 8-tetrahydrocannabinol (11-OH-delta 8-THC), on the hepatic microsomal drug-metabolizing enzyme system were studied in mice. The repeated administration of 11-OH-delta 8-THC (5 mg/kg/day, i.v.) for 3 or 7 day...

journal_title：Biochemical pharmacology

authors： Watanabe K,Arai M,Narimatsu S,Yamamoto I,Yoshimura H

更新日期：1986-06-01 00:00:00

abstract：:The transcription factor NF-kappaB plays a key role in a wide variety of cellular processes such as innate and adaptive immunity, cellular proliferation, apoptosis and development. In unstimulated cells, NF-kappaB is sequestered in the cytoplasm through its tight association with inhibitory proteins called IkappaBs, c...

journal_title：Biochemical pharmacology

authors： Gloire G,Dejardin E,Piette J

更新日期：2006-10-30 00:00:00

abstract：:We tested the influence of IFNgamma on proteasome activity in parental Hep G2 cells that do not metabolize ethanol, as well as in recombinant Hep G2-derived cells that express either or both alcohol dehydrogenase (ADH) and cytochrome P4502E1 (CYP2E1). IFNgamma treatment increased proteasome activity in VL-17A (ADH(+),...

journal_title：Biochemical pharmacology

authors： Osna NA,Clemens DL,Donohue TM Jr

更新日期：2003-09-01 00:00:00