Nitric oxide levels in human preneoplastic colonocytes determine their susceptibility toward antineoplastic agents.

abstract：:The endocannabinoids anandamide and 2-arachidonyl glycerol (2-AG) bind to G protein-coupled central and peripheral cannabinoid receptors CB1 and CB2, respectively. Due to the relatively high expression of the CB2 isotype on peripheral immune cells, it has been hypothesized that this receptor mediates the immunosuppres...

journal_title：Molecular pharmacology

authors： Gonsiorek W,Lunn C,Fan X,Narula S,Lundell D,Hipkin RW

更新日期：2000-05-01 00:00:00

abstract：:Lysophosphatidic acid (LPA) and sphingosine-1-phosphate (S1P) are members of the phospholipid growth factor family. A major limitation in the field to date has been a lack of receptor subtype-specific agonists and antagonists. Here, we report that dioctylglycerol pyrophosphate and dioctylphosphatidic acid are selectiv...

journal_title：Molecular pharmacology

authors： Fischer DJ,Nusser N,Virag T,Yokoyama K,Wang Da,Baker DL,Bautista D,Parrill AL,Tigyi G

更新日期：2001-10-01 00:00:00

abstract：:Poly(ADP-ribose) polymerase-1 (PARP-1) is a NAD-consuming enzyme with an emerging key role in epigenetic regulation of gene transcription. Although PARP-1 expression is characteristically restricted to the nucleus, a few studies report the mitochondrial localization of the enzyme and its ability to regulate organelle ...

journal_title：Molecular pharmacology

authors： Lapucci A,Pittelli M,Rapizzi E,Felici R,Moroni F,Chiarugi A

更新日期：2011-06-01 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：:G protein-coupled receptor (GPCR) kinases (GRKs) play a key role in terminating signals initiated by agonist-bound GPCRs. However, chronic stimulation of GPCRs, such as that which occurs during heart failure, leads to the overexpression of GRKs and maladaptive downregulation of GPCRs on the cell surface. We previously...

journal_title：Molecular pharmacology

authors： Bouley RA,Weinberg ZY,Waldschmidt HV,Yen YC,Larsen SD,Puthenveedu MA,Tesmer JJG

更新日期：2020-06-01 00:00:00

abstract：:Celecoxib (CE) is a nonsteroidal anti-inflammatory drug (NSAID) that is a specific inhibitor of cyclooxygenase 2 (COX2). It is indicated for a variety of chronic inflammatory conditions, including rheumatoid arthritis. Over the last few years, adverse cardiovascular effects and increased risk for heart attacks have be...

journal_title：Molecular pharmacology

authors： Alloza I,Baxter A,Chen Q,Matthiesen R,Vandenbroeck K

更新日期：2006-05-01 00:00:00

abstract：:Mitsuya and Broder [Proc. Natl. Acad. Sci. USA 83:1911-1915 (1986)] demonstrated that every purine (adenosine, guanosine, and inosine) and pyrimidine (cytidine and thymidine) nucleoside containing the 2',3'-dideoxyribose configuration, when evaluated against human immunodeficiency virus (HIV) in vitro, significantly s...

journal_title：Molecular pharmacology

authors： Hao Z,Cooney DA,Hartman NR,Perno CF,Fridland A,DeVico AL,Sarngadharan MG,Broder S,Johns DG

更新日期：1988-10-01 00:00:00

abstract：:Stimulatory effects of spermine at heteromeric N-methyl-D-aspartate (NMDA) receptors expressed from cloned subunits were studied by voltage-clamp recording in Xenopus oocytes. At NR1A/NR2B receptors, in the presence of a saturating concentration of glycine, the magnitude of spermine stimulation was dependent on the co...

journal_title：Molecular pharmacology

authors： Williams K

更新日期：1994-07-01 00:00:00

abstract：:The purpose of these studies was to support the hypothesis that an undiscovered cannabinoid receptor exists in brain. [(35)S]GTP gamma S binding was stimulated by anandamide and WIN55212-2 in brain membranes from both CB(1)(+/+) and CB(1)(-/-) mice. In contrast, a wide variety of other compounds that are known to acti...

journal_title：Molecular pharmacology

authors： Breivogel CS,Griffin G,Di Marzo V,Martin BR

更新日期：2001-07-01 00:00:00

abstract：:For several GPCRs, discrimination between agonism and antagonism is possible on the basis of thermodynamics parameters, such as binding enthalpy and entropy. In this study, we analyze whether agonists and antagonists can also be discriminated thermodynamically at the histamine H(1) receptor (H(1)R). Because previous s...

journal_title：Molecular pharmacology

authors： Wittmann HJ,Seifert R,Strasser A

更新日期：2009-07-01 00:00:00

abstract：:High-throughput screening has led to the identification of small-molecule blockers of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel, but the structural basis of blocker binding remains to be defined. We developed molecular models of the CFTR channel on the basis of homology to the bac...

journal_title：Molecular pharmacology

authors： Norimatsu Y,Ivetac A,Alexander C,O'Donnell N,Frye L,Sansom MS,Dawson DC

更新日期：2012-12-01 00:00:00

abstract：:Differential display reverse transcription-polymerase chain reaction was used to identify mRNAs that are differentially expressed in the brain of rats treated chronically with the reference tricyclic antidepressant, imipramine, in comparison with control rats. The gene encoding for a mutation suppressor for Sec4-8 yea...

journal_title：Molecular pharmacology

authors： Andriamampandry C,Muller C,Schmidt-Mutter C,Gobaille S,Spedding M,Aunis D,Maitre M

更新日期：2002-12-01 00:00:00

abstract：:In vivo administration of the porphyrogenic agent allylisopropylacetamide (AIA) to phenobarbital-pretreated rats results in marked loss of hepatic cytochrome P-450 content. Using isozyme-selective functional markers, we now show that such loss reflects inactivation of several phenobarbital-inducible and constitutive i...

journal_title：Molecular pharmacology

authors： Bornheim LM,Underwood MC,Caldera P,Rettie AE,Trager WF,Wrighton SA,Correia MA

更新日期：1987-08-01 00:00:00

abstract：:There are now several examples of single G protein-coupled receptors to which binding of specific agonists causes differential effects on the associated signaling pathways. The dopamine D(2) receptor is of special importance because the selective activation of functional pathways has been shown both in vitro and in si...

journal_title：Molecular pharmacology

authors： Gay EA,Urban JD,Nichols DE,Oxford GS,Mailman RB

更新日期：2004-07-01 00:00:00

abstract：:A family of five cholinergic muscarinic receptor genes (m1, m2, m3, m4, and m5) has recently been identified and cloned. In order to investigate the pharmacological properties of the individual muscarinic receptors, we have transfected each of these genes into Chinese hamster ovary cells (CHO-K1) and have established ...

journal_title：Molecular pharmacology

authors： Buckley NJ,Bonner TI,Buckley CM,Brann MR

更新日期：1989-04-01 00:00:00

abstract：:The aliphatic adenine analogues, D-eritadenine, L-eritadenine, L-threoeritadenine, and 9-(S)-(2,3-dihydroxypropyl)adenine [(S)DHPA] function as inhibitors/inactivators of purified S-adenosylhomocysteine (AdoHcy) hydrolase, but these compounds did not induce reduction of enzyme-bound NAD+. D-Eritadenine, L-eritadenine,...

journal_title：Molecular pharmacology

authors： Schanche JS,Schanche T,Ueland PM,Holý A,Votruba I

更新日期：1984-11-01 00:00:00

abstract：:Sazetidine-A has been recently proposed to be a "silent desensitizer" of alpha4beta2 nicotinic acetylcholine receptors (nAChRs), implying that it desensitizes alpha4beta2 nAChRs without first activating them. This unusual pharmacological property of sazetidine-A makes it, potentially, an excellent research tool to dis...

journal_title：Molecular pharmacology

authors： Zwart R,Carbone AL,Moroni M,Bermudez I,Mogg AJ,Folly EA,Broad LM,Williams AC,Zhang D,Ding C,Heinz BA,Sher E

更新日期：2008-06-01 00:00:00

abstract：:Amphetamine congeners [e.g., 3,4-methylenedioxymetamphetamine (MDMA), or "ecstasy"] are substrates for monoamine transporters (i.e., the transporters for serotonin, norepinephrine, and dopamine); however, their in vivo-action relies on their ability to promote monoamine efflux. The mechanistic basis for this counter t...

journal_title：Molecular pharmacology

authors： Seidel S,Singer EA,Just H,Farhan H,Scholze P,Kudlacek O,Holy M,Koppatz K,Krivanek P,Freissmuth M,Sitte HH

更新日期：2005-01-01 00:00:00

abstract：:The aim of this study was to clarify the mechanism by which cytochrome P450 (P450)-mediated catalytic activity is decreased following interferon (IFN) administration. Microsomal steroid hydroxylation was assessed to test the hypothesis that IFN selectively decreases the activities of individual P450 isozymes in male r...

journal_title：Molecular pharmacology

authors： Craig PI,Mehta I,Murray M,McDonald D,Aström A,van der Meide PH,Farrell GC

更新日期：1990-09-01 00:00:00

abstract：:The human monoamine oxidase (MAO) B plays a major role in the degradation of biogenic and dietary amines such as phenylethylamine, benzylamine, dopamine, and tyramine. We previously showed that the -246/-99 MAO B promoter region exhibited the highest activity and contained two clusters of overlapping Sp1 sites, a CACC...

journal_title：Molecular pharmacology

authors： Wong WK,Chen K,Shih JC

更新日期：2001-04-01 00:00:00

abstract：:Metabolism of [3H]-(+/-)-trans-1,2-dihydroxy-1,2-dihydrobenz[a] anthracene by liver microsomes isolated from control, phenobarbital-treated, and 3-methylcholanthrene-treated Long-Evans rats and from 3-methylcholanthrene-treated Sprague-Dawley rats was examined. Liver microsomes from both control and phenobarbital-trea...

journal_title：Molecular pharmacology

authors： Vyas KP,van Bladeren PJ,Thakker DR,Yagi H,Sayer JM,Levin W,Jerina DM

更新日期：1983-07-01 00:00:00

abstract：:Na+-d-glucose cotransporter 1 (SGLT1) is rate-limiting for glucose absorption in the small intestine. Shortly after intake of glucose-rich food, SGLT1 abundance in the luminal membrane of the small intestine is increased. This upregulation occurs via glucose-induced acceleration of the release of SGLT1-containing vesi...

journal_title：Molecular pharmacology

authors： Chintalapati C,Keller T,Mueller TD,Gorboulev V,Schäfer N,Zilkowski I,Veyhl-Wichmann M,Geiger D,Groll J,Koepsell H

更新日期：2016-11-01 00:00:00

abstract：:Sulfation is an important pathway in the biotransformation of many drugs, xenobiotic compounds, neurotransmitters, and hormones. The sulfate donor for these reactions is 3'-phosphoadenosine-5'-phosphosulfate (PAPS). We set out to determine whether PAPS might serve as a photoaffinity ligand for sulfotransferase enzymes...

journal_title：Molecular pharmacology

authors： Otterness DM,Powers SP,Miller LJ,Weinshilboum RM

更新日期：1991-01-01 00:00:00

abstract：:Stimulation of N-methyl-D-aspartate (NMDA) receptors is believed to underlie long-term memory formation, and excessive NMDA receptor activation has been linked to several neuropathological conditions. Phosphorylation and activation of p42/44 mitogen-activated protein kinase (ERK) is believed to mediate many of these e...

journal_title：Molecular pharmacology

authors： Rakhit S,Clark CJ,O'shaughnessy CT,Morris BJ

更新日期：2005-04-01 00:00:00

abstract：:We have investigated various nitric oxide (NO) synthase inhibitors for their affinity and selectivity toward the three human isoenzymes in radioligand binding experiments. Therefore, we developed the new radioligand [(3)H]2-amino-4-picoline to measure binding of these compounds to the three human NO synthase (NOS) iso...

journal_title：Molecular pharmacology

authors： Boer R,Ulrich WR,Klein T,Mirau B,Haas S,Baur I

更新日期：2000-11-01 00:00:00

abstract：:The neuropeptides vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase-activating peptide (PACAP) and their class II G protein-coupled receptors VPAC(1), VPAC(2), and PAC(1) play important roles in human physiology. No small molecule modulator has ever been reported for the VIP/PACAP receptors, and ther...

journal_title：Molecular pharmacology

authors： Chu A,Caldwell JS,Chen YA

更新日期：2010-01-01 00:00:00

abstract：:We previously described the development of genetic models to study the in vivo functions of the hepatic cytochrome P450 (P450) system, through the hepatic deletion of either cytochrome P450 oxidoreductase [POR; HRN (hepatic reductase null) line] or cytochrome b(5) [HBN (hepatic cytochrome b(5) null) line]. However, HR...

journal_title：Molecular pharmacology

authors： Henderson CJ,McLaughlin LA,Wolf CR

更新日期：2013-06-01 00:00:00

abstract：:N-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) induces Parkinson-like symptoms in humans, nonhuman primates, and mice. Several studies suggest that MPTP is metabolized by monoamine oxidase (MAO) type B to yield N-methyl-4-phenyl-pyridinium (MPP+), which is responsible for the neurotoxic effects of the drug. In th...

journal_title：Molecular pharmacology

authors： Itzhak Y,Mash D,Zhang SH,Stein I

更新日期：1991-03-01 00:00:00

abstract：:The effects of ethanol on a number of electrophysiological parameters were examined in 10 different voltage-gated potassium channels expressed in Xenopus oocytes. None of the channels examined was highly sensitive to ethanol, but there was significant variability among the channels tested at concentrations of ethanol ...

journal_title：Molecular pharmacology

authors： Anantharam V,Bayley H,Wilson A,Treistman SN

更新日期：1992-09-01 00:00:00

abstract：:The cytochrome P450 26 family is believed to be responsible for all-trans-retinoic acid (atRA) metabolism and elimination in the human fetus and adults. CYP26A1 and CYP26B1 mRNA is expressed in a tissue-specific manner, and mice in which the CPY26 isoform has been knocked out show distinct malformations and lethality....

journal_title：Molecular pharmacology

authors： Tay S,Dickmann L,Dixit V,Isoherranen N

更新日期：2010-02-01 00:00:00