Copper-dependent oxidative and topoisomerase II-mediated DNA cleavage by a netropsin/4'-(9-acridinylamino)methanesulfon-m-anisidide combilexin.

abstract：:Structural changes in the macromolecular targets of pharmacological agents can result in alterations in the efficacy of these agents. In previous studies, we identified a variant structural form of thymidylate synthase (TS) that is associated with relative resistance to 5-fluoro-2'-deoxyuridine, in a human colonic tum...

journal_title：Molecular pharmacology

authors： Barbour KW,Hoganson DK,Berger SH,Berger FG

更新日期：1992-08-01 00:00:00

abstract：:Cells of the murine neuroblastoma clone N1E-115 possess muscarinic receptors that influence the intracellular level of cyclic nucleotides. The stimulation of [3H]cyclic GMP levels occurs only with intact cells and has an EC50 near the "low-affinity" agonist equilibrium dissociation constant (KL) determined by radiolig...

journal_title：Molecular pharmacology

authors： McKinney M,Stenstrom S,Richelson E

更新日期：1984-09-01 00:00:00

abstract：:The orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) is a potent regulator of cholesterol metabolism and bile acid homeostasis. Recently, LRH-1 has been shown to play an important role in intestinal inflammation and in the progression of estrogen receptor positive and negative breast cancers and pancrea...

journal_title：Molecular pharmacology

authors： Corzo CA,Mari Y,Chang MR,Khan T,Kuruvilla D,Nuhant P,Kumar N,West GM,Duckett DR,Roush WR,Griffin PR

更新日期：2015-02-01 00:00:00

abstract：:Dietary lipids and fat-soluble micronutrients are solubilized in mixed micelles and absorbed in the small intestine. Based on an assumption that cholesterol and other fat-soluble molecules share a number of transport mechanisms and the fact that Niemann-Pick C1-like 1 (NPC1L1) is critical for intestinal cholesterol ab...

journal_title：Molecular pharmacology

authors： Narushima K,Takada T,Yamanashi Y,Suzuki H

更新日期：2008-07-01 00:00:00

abstract：:Metallothioneins (MTs) are cytoplasmic proteins that sequester certain divalent cations and are considered a primary cellular defense against the toxic transition metal cadmium (Cd(2+)). MT-I/II(-/-) knockout [MT(-/-)] cells are available and serve as an excellent tool to study non-MT-related mechanisms in metal toler...

journal_title：Molecular pharmacology

authors： Leslie EM,Liu J,Klaassen CD,Waalkes MP

更新日期：2006-02-01 00:00:00

abstract：:Studies investigating the effects of beta-naphthoflavone (beta NF) on insulin receptor binding and its intrinsic protein kinase activity in rat liver and placenta were performed. Membranes were prepared from maternal liver and placenta on gestation day 11 and used for [125I]insulin radioreceptor assay. Scatchard analy...

journal_title：Molecular pharmacology

authors： Wang SL,Raizada MK,Shiverick KT

更新日期：1988-03-01 00:00:00

abstract：:Molecular cloning of the alpha 2A-adrenergic receptor has shown that this receptor is a member of the gene superfamily of guanine nucleotide-binding protein (G protein)-coupled receptors. The alpha 2A-adrenergic receptor expressed in Chinese hamster ovary (CHO) cells attenuates and potentiates forskolin-stimulated cAM...

journal_title：Molecular pharmacology

authors： Wang CD,Buck MA,Fraser CM

更新日期：1991-08-01 00:00:00

abstract：:An 'epoxygenase' eicosanoid analog, 14, 15-cis-episulfide-eicosatrienoic acid, has several unique pharmacological effects on platelets. These include (i) inhibition of ionophore A23187- but not thrombin-induced activation, (ii) inhibition of thromboxane B2 biosynthesis derived from endogenous but not exogenous arachid...

journal_title：Molecular pharmacology

authors： Bernstrom K,Malcolm K,McGee J,Maclouf J,Levy-Toledano S,Falck JR,Fitzpatrick FA

更新日期：1991-02-01 00:00:00

abstract：:TWIK-related K(+) 1 (TREK1) potassium channels are members of the two-pore domain potassium channel family and contribute to background potassium conductances in many cell types, where their activity can be regulated by a variety of physiologic and pharmacologic mediators. Fenamates such as FFA (flufenamic acid; 2-{[3...

journal_title：Molecular pharmacology

authors： Veale EL,Al-Moubarak E,Bajaria N,Omoto K,Cao L,Tucker SJ,Stevens EB,Mathie A

更新日期：2014-05-01 00:00:00

abstract：:In this work, we evaluate the structural differences of transmembrane helix 3 in rhodopsin and the 5-hydroxytryptamine 1A (5-HT1A) receptor caused by their different amino acid sequence. Molecular dynamics simulations of helix 3 in the 5-HT1A receptor tends to bend toward helix 5, in sharp contrast to helix 3 in rhodo...

journal_title：Molecular pharmacology

authors： López-Rodríguez ML,Vicente B,Deupi X,Barrondo S,Olivella M,Morcillo MJ,Behamú B,Ballesteros JA,Sallés J,Pardo L

更新日期：2002-07-01 00:00:00

abstract：:Inhibition of multidrug resistance protein 1 (MRP1) mediated cytostatic drug efflux might be useful in the treatment of drug resistant tumors. Because the glutathione (GSH) conjugate of ethacrynic acid (EA), GS-EA, is a good substrate of MRP1, GS-EA derivatives are expected to be good inhibitors of MRP1. To study stru...

journal_title：Molecular pharmacology

authors： Burg D,Wielinga P,Zelcer N,Saeki T,Mulder GJ,Borst P

更新日期：2002-11-01 00:00:00

abstract：:Peroxisome proliferator-activated receptors (PPARs) are a family of nuclear receptors that are involved in lipid metabolism, differentiation, proliferation, cell death, and inflammation. Three subtypes have been identified: PPAR-alpha, -delta, and -gamma. We have previously shown presence of PPAR-gamma mRNA in the amn...

journal_title：Molecular pharmacology

authors： Berry EB,Eykholt R,Helliwell RJ,Gilmour RS,Mitchell MD,Marvin KW

更新日期：2003-12-01 00:00:00

abstract：:Prostaglandin E(2) (PGE(2)), originally discovered as a pro-inflammatory mediator, also inhibits several chemoattractant-elicited neutrophil functions, including adhesion, secretion of cytotoxic enzymes, production of superoxide anions, and chemotaxis. In this study, we have examined the effects of PGE(2) and prostagl...

journal_title：Molecular pharmacology

authors： Burelout C,Thibault N,Levasseur S,Simard S,Naccache PH,Bourgoin SG

更新日期：2004-08-01 00:00:00

abstract：:We examined the subtype-selective binding site of the beta-adrenergic receptors (betaARs). The beta(1)/beta(2)-chimeric receptors showed the importance of the second and seventh transmembrane domains (TM2 and TM7) of the beta(2)AR for the binding of the beta(2)-selective agonists such as formoterol and procaterol. Ala...

journal_title：Molecular pharmacology

authors： Isogaya M,Sugimoto Y,Tanimura R,Tanaka R,Kikkawa H,Nagao T,Kurose H

更新日期：1999-11-01 00:00:00

abstract：:We demonstrated previously that nonsteroidal anti-inflammatory drugs (NSAIDs) increased p27(Kip1) by inhibiting protein degradation to suppress the proliferation of human lung cancer cells. In this study, we elucidate the molecular mechanism by which NSAIDs modulate p27(Kip1) proteolysis. Immunoblotting and in vitro u...

journal_title：Molecular pharmacology

authors： Huang YC,Chuang LY,Hung WC

更新日期：2002-12-01 00:00:00

abstract：:Capsaicin (vanilloid) sensitivity has long served as the functional signature of a subset of nociceptive sensory neurons. Mutagenesis studies have revealed seemingly distinct regions involved in mediating ligand binding and channel activation at the capsaicin binding site. Residue 547 (transmembrane region 4) mediates...

journal_title：Molecular pharmacology

authors： Johnson DM,Garrett EM,Rutter R,Bonnert TP,Gao YD,Middleton RE,Sutton KG

更新日期：2006-09-01 00:00:00

abstract：:The microtubule-binding taxanes, docetaxel and cabazitaxel, are administered intravenously for the treatment of castration-resistant prostate cancer (CRPC) as the oral administration of these drugs is largely hampered by their low and highly variable bioavailabilities. Using a simple, rapid, and environmentally friend...

journal_title：Molecular pharmacology

authors： Liao VWY,Kumari A,Narlawar R,Vignarajan S,Hibbs DE,Panda D,Groundwater PW

更新日期：2020-06-01 00:00:00

abstract：:Several novel phenylaminotetralins (PATs) cause functional changes in brain that are associated with binding to saturable, high affinity sites that are not identical to any known central nervous system receptor. These PATs were tested for their ability to cause receptor-mediated functional effects on tyrosine hydroxyl...

journal_title：Molecular pharmacology

authors： Booth RG,Wyrick SD,Baldessarini RJ,Kula NS,Myers AM,Mailman RB

更新日期：1993-12-01 00:00:00

abstract：:We have used two experimental approaches--receptor inactivation with an irreversible antagonist and changes in receptor expression during passage of cells through the cell cycle--to explore the relationship between beta-adrenergic receptor number and response in intact S49 lymphoma cells. beta-Receptors in asynchronou...

journal_title：Molecular pharmacology

authors： Mahan LC,Insel PA

更新日期：1986-01-01 00:00:00

abstract：:Avermectins are a family of potent broad-spectrum anthelmintic compounds, which bind with high affinity to membranes isolated from the free-living nematode Caenorhabditis elegans. Binding of avermectins is thought to modulate chloride channel activity, but the exact mechanism for anthelmintic activity remains to be de...

journal_title：Molecular pharmacology

authors： Arena JP,Liu KK,Paress PS,Cully DF

更新日期：1991-09-01 00:00:00

abstract：:The effects of the non-tumor-promoting protein kinase C (PKC) activator bryostatin 1 and the PKC inhibitors staurosporine and UCN-01 were examined with respect to modulation of 1-[beta-D-arabinofuranosyl]cytosine (ara-C)-induced apoptosis in human myeloid leukemia cells (HL-60) overexpressing the antiapoptotic protein...

journal_title：Molecular pharmacology

authors： Wang S,Vrana JA,Bartimole TM,Freemerman AJ,Jarvis WD,Kramer LB,Krystal G,Dent P,Grant S

更新日期：1997-12-01 00:00:00

abstract：:The involvement of mitogen-activated protein (MAP) kinases in the mitogenic effect of thyrotropin (TSH) is not fully elucidated. In FRTL-5 cells, we found that the MAP kinase kinase (MEK) inhibitors UO126 and PD98059 substantially decreased TSH-induced DNA synthesis, indicating that MAP kinases are involved in the TSH...

journal_title：Molecular pharmacology

authors： Iacovelli L,Capobianco L,Salvatore L,Sallese M,D'Ancona GM,De Blasi A

更新日期：2001-11-01 00:00:00

abstract：:The UGT1 locus is felt to be highly conserved between species, as is evident from the characterization of the locus in rodents and humans. In rabbits, cDNAs encoding proteins homologous to human UGT1A4, UGT1A6, and UGT1A7 have previously been identified. Here we demonstrate by Southern blot analysis, using exon 1 dive...

journal_title：Molecular pharmacology

authors： Li Q,Lamb G,Tukey RH

更新日期：2000-07-01 00:00:00

abstract：:The retinoid (visual) cycle consists of a series of biochemical reactions needed to regenerate the visual chromophore 11-cis-retinal and sustain vision. Genetic or environmental factors affecting chromophore production can lead to blindness. Using animal models that mimic human retinal diseases, we previously demonstr...

journal_title：Molecular pharmacology

authors： Gao S,Kahremany S,Zhang J,Jastrzebska B,Querubin J,Petersen-Jones SM,Palczewski K

更新日期：2018-05-01 00:00:00

abstract：:Rates of glucuronidation were measured at high substrate concentrations in specific zones of the liver lobule using micro-light guides placed on periportal and pericentral regions on the surface of livers from phenobarbital-treated rats. Livers were perfused with sulfate-free buffer under normoxic conditions, and fluo...

journal_title：Molecular pharmacology

authors： Conway JG,Kauffman FC,Tsukada T,Thurman RG

更新日期：1984-05-01 00:00:00

abstract：:The P2Y(1) receptor is responsible for the initiation of platelet aggregation in response to ADP and plays a key role in thrombosis. Although this receptor is expressed early in the platelet lineage, the regulation of its expression during megakaryocyte differentiation is unknown. In the mouse megakaryocytic cell line...

journal_title：Molecular pharmacology

authors： Hechler B,Toselli P,Ravanat C,Gachet C,Ravid K

更新日期：2001-11-01 00:00:00

abstract：:Pyrethroid insecticides are synthetic neurotoxins patterned after the naturally occurring pyrethrins. Their mechanism of action is thought to involve effects primarily at the voltage-sensitive sodium channel of both insect and mammalian neurons, although recent studies have raised the possibility that these compounds ...

journal_title：Molecular pharmacology

authors： Brown GB,Gaupp JE,Olsen RW

更新日期：1988-07-01 00:00:00

abstract：:The effect of the neuromuscular blocker alcuronium on the binding of N-[3H]-methylscopolamine [( 3H]NMS) and l-[3H]quinuclidinylbenzilate ([3H]QNB) to muscarinic binding sites in rat heart atria, longitudinal smooth muscle of the ileum, cerebral cortex, cerebellum, and submaxillary glands was measured using filtration...

journal_title：Molecular pharmacology

authors： Tucek S,Musílková J,Nedoma J,Proska J,Shelkovnikov S,Vorlícek J

更新日期：1990-11-01 00:00:00

abstract：:One-electron oxidation of several derivatives of pyrazolin-5-one, including the drug antipyrine, were studied by pulse radiolysis of aqueous solutions. All the compounds were found to be oxidized by Br2 rapidly (k approximately 3 X 10(8)-2 X 10(9) M-1 s-1) but considerably more slowly by weaker oxidants, such as perox...

journal_title：Molecular pharmacology

authors： Jovanovic SV,Neta P,Simic MG

更新日期：1985-10-01 00:00:00

abstract：:Reversible binding of warfarin to defatted serum albumin was studied by equilibrium dialysis at pH 7.4, in a 66 mM sodium phosphate buffer at 37 degrees. The binding isotherm could be described by two stoichiometric binding constants, K1 in the range 141,000 to 192,000 M-1 and K2 at 39,000 to 57,000 M-1. At least two ...

journal_title：Molecular pharmacology

authors： Larsen FG,Larsen CG,Jakobsen P,Brodersen R

更新日期：1985-02-01 00:00:00