Dissecting the Signaling Pathways Involved in the Crosstalk between Metabotropic Glutamate 5 and Cannabinoid Type 1 Receptors.

abstract：:As a member of the transient receptor potential (TRP) ion channel superfamily, the ligand-gated ion channel TRPA1 has been implicated in nociceptive function and pain states. The endogenous ligands that activate TRPA1 remain unknown. However, various agonists have been identified, including environmental irritants (e....

journal_title：Molecular pharmacology

authors： Niforatos W,Zhang XF,Lake MR,Walter KA,Neelands T,Holzman TF,Scott VE,Faltynek CR,Moreland RB,Chen J

更新日期：2007-05-01 00:00:00

abstract：:Resistance to cisplatin, one of the most widely used anticancer chemotherapeutic agents, is a major clinical problem. There is no effective way to predict development of cisplatin resistance in cancers. As determined by reverse transcription-polymerase chain reaction and Western blotting, the expression of gamma-caten...

journal_title：Molecular pharmacology

authors： Liang XJ,Shen DW,Gottesman MM

更新日期：2004-05-01 00:00:00

abstract：:In the present study we have investigated the capacity of various compounds sterically related to indolo[3,2-b]carbazole to inhibit specific 2,3,7,8-tetrachloro[1,6-3H]dibenzo-p-dioxin binding in rat liver cytosol, as analyzed by electrofocusing in polyacrylamide gels. When the two nitrogen atoms of indolo[3,2-b]carba...

journal_title：Molecular pharmacology

authors： Gillner M,Bergman J,Cambillau C,Alexandersson M,Fernström B,Gustafsson JA

更新日期：1993-08-01 00:00:00

abstract：:Although ATP-sensitive K+ channels continue to be explored for their therapeutic potential, developments in high-affinity radioligands to investigate native and recombinant KATP channels have been less forthcoming. This study reports the identification and pharmacological characterization of a novel iodinated 1,4-dihy...

journal_title：Molecular pharmacology

authors： Davis-Taber R,Molinari EJ,Altenbach RJ,Whiteaker KL,Shieh CC,Rotert G,Buckner SA,Malysz J,Milicic I,McDermott JS,Gintant GA,Coghlan MJ,Carroll WA,Scott VE,Gopalakrishnan M

更新日期：2003-07-01 00:00:00

abstract：:UDP-glucuronosyltransferase (UGT) 1A1 (UGT1A1) catalyzes the glucuronidation of bilirubin in liver. Among all UGT isoforms identified to date, it is the only relevant bilirubin-glucuronidating enzyme in human. Because glucuronoconjugation is the major route of bilirubin elimination, any genetic alteration that affects...

journal_title：Molecular pharmacology

authors： Bernard P,Goudonnet H,Artur Y,Desvergne B,Wahli W

更新日期：1999-09-01 00:00:00

abstract：:The glucagon-like peptide-1 receptor (GLP-1R) is a key physiological regulator of insulin secretion and a major therapeutic target for the treatment of type II diabetes. However, regulation of GLP-1R function is complex with multiple endogenous peptides that interact with the receptor, including full-length (1-37) and...

journal_title：Molecular pharmacology

authors： Koole C,Wootten D,Simms J,Valant C,Miller LJ,Christopoulos A,Sexton PM

更新日期：2011-09-01 00:00:00

abstract：:Multidrug resistance protein 1 (MRP1) is a member of the "C" branch of the ATP-binding cassette transporter superfamily. The NH(2)-proximal nucleotide-binding domain (NBD1) of MRP1 differs functionally from its COOH-proximal domain (NBD2). NBD1 displays intrinsic high-affinity ATP binding and little ATPase activity. I...

journal_title：Molecular pharmacology

authors： Payen L,Gao M,Westlake C,Theis A,Cole SP,Deeley RG

更新日期：2005-06-01 00:00:00

abstract：:A conjugate molecule was synthesized by linking the DNA-intercalative antitumor drug 4'-(9-acridinylamino)methanesulfon-manisidide (mAMSA) via a 4-carboxamide side chain to a dipyrrolecarboxamide moiety structurally related to the minor groove-binding antibiotic netropsin. The molecule (netropsin/ mAMSA) behaves as a ...

journal_title：Molecular pharmacology

authors： Henichart JP,Waring MJ,Riou JF,Denny WA,Bailly C

更新日期：1997-03-01 00:00:00

abstract：:Opioid analgesics are used extensively in the management of pain. Although the clinically effective opioids bind with high affinity to the mu-opioid receptor, studies have suggested that the delta-opioid agonists might represent more ideal analgesic agents, with fewer side effects. A limitation to opiate effectiveness...

journal_title：Molecular pharmacology

authors： Bot G,Blake AD,Li S,Reisine T

更新日期：1997-08-01 00:00:00

abstract：:Because cytotoxicity by an alkylating agent such as N-methyl-N'-nitrosoguanidine is markedly increased in adenine methylase-deficient dam-3 Escherichia coli, it was of interest to assess whether mismatch repair was similarly important in the repair of DNA damage induced by cis-diamminedichloroplatinum(II) (CDDP). The ...

journal_title：Molecular pharmacology

authors： Fram RJ,Cusick PS,Wilson JM,Marinus MG

更新日期：1985-07-01 00:00:00

abstract：:Although α7 nicotinic acetylcholine receptors are considered potentially important therapeutic targets, the development of selective agonists has been stymied by the α7 receptor's intrinsically low probability of opening (P(open)) and the concern that an agonist-based therapeutic approach would disrupt endogenous chol...

journal_title：Molecular pharmacology

authors： Williams DK,Wang J,Papke RL

更新日期：2011-12-01 00:00:00

abstract：:The incorporation of leucine into protein was studied in Ca2+-depleted and Ca2+-restored preparations of normal liver cells isolated from fed, adult male rats. Ca2+-restored cells incorporated amino acid 5-10-fold more rapidly than did Ca2+-depleted cells for incubation periods up to 1 hr. Readdition of Ca2+ at suprap...

journal_title：Molecular pharmacology

authors： Brostrom CO,Bocckino SB,Brostrom MA,Galuska EM

更新日期：1986-01-01 00:00:00

abstract：:To understand the molecular mechanism by which the angiotensin II (AII) type 1 receptor (AT1 receptor) transduces its biological signal, we examined the role of various signaling molecules involved in AT1 receptor signaling in Chinese hamster ovary cells stably transfected with the AT1 receptor. AT1 receptor-transfect...

journal_title：Molecular pharmacology

authors： Arai H,Escobedo JA

更新日期：1996-09-01 00:00:00

abstract：:P-glycoprotein, an ATP-driven efflux pump, regulates permeability of the blood-brain barrier (BBB). Sphingolipids, endogenous to brain tissue, influence inflammatory responses and cell survival in vitro. Our laboratory has previously shown that sphingolipid signaling by sphingosine 1-phosphate decreases basal P-glycop...

journal_title：Molecular pharmacology

authors： Mesev EV,Miller DS,Cannon RE

更新日期：2017-04-01 00:00:00

abstract：:Although nonsteroidal anti-inflammatory drugs (NSAIDs) are used as cancer chemopreventative agents, their mechanism is unclear because NSAIDs have cyclooxygenase-independent actions. We investigated an alternative target for NSAIDs, peroxisome proliferator-activated receptor-gamma (PPARgamma), activation of which decr...

journal_title：Molecular pharmacology

authors： Adamson DJ,Frew D,Tatoud R,Wolf CR,Palmer CN

更新日期：2002-01-01 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：:The ability of dopamine agonists and antagonists to compete with [3H]spiperone binding to rat striatal membrane preparations at 4, 15, 26, and 37 degrees varied markedly with temperature. Dopamine and the dopamine agonist 2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene hydrobromide (ADTN) were more potent at lower...

journal_title：Molecular pharmacology

authors： Kilpatrick GJ,el Tayar N,Van de Waterbeemd H,Jenner P,Testa B,Marsden CD

更新日期：1986-09-01 00:00:00

abstract：:We have identified four new mu-opiod receptor (MOR)-1 exons, indicating that the gene now contains at least nine exons spanning more than 200 kilobases. Replacement of exon 4 by combinations of the new exons yields three new receptors. When expressed in Chinese hamster ovary cells, all three variants displayed high af...

journal_title：Molecular pharmacology

authors： Pan YX,Xu J,Bolan E,Abbadie C,Chang A,Zuckerman A,Rossi G,Pasternak GW

更新日期：1999-08-01 00:00:00

abstract：:Tienilic acid-induced hepatitis is characterized by the presence of anti-liver and -kidney microsomal (anti-LKM2) autoantibodies in patient sera. Cytochrome P4502C9(CYP2C9), involved in the metabolism of tienilic acid, was shown to be a target for tienilic acid-reactive metabolites and for autoantibodies. To further i...

journal_title：Molecular pharmacology

authors： Lecoeur S,André C,Beaune PH

更新日期：1996-08-01 00:00:00

abstract：:EM-652 (SCH 57068) is a new orally active antiestrogen that demonstrates pure antagonistic effects in the mammary gland and endometrium. In vivo studies have shown that EM-652 is primarily glucuronidated at the 7-hydroxy position in rats and that the metabolite is present in the plasma of female monkeys and human subj...

journal_title：Molecular pharmacology

authors： Barbier O,Albert C,Martineau I,Vallée M,High K,Labrie F,Hum DW,Labrie C,Bélanger A

更新日期：2001-03-01 00:00:00

abstract：:Recombinant interferon-alpha (IFN) enhances the cytotoxic effects of the fluorinated pyrimidine, 5-fluorouracil (5FU), against two human colon cancer cell lines. The aspartate transcarbamylase (ATCase) inhibitor, N-(phosphonacetyl)-L-aspartate (PALA), was studied in combination with 5FU/IFN to determine whether furthe...

journal_title：Molecular pharmacology

authors： Wadler S,Mao X,Bajaj R,Hallam S,Schwartz EL

更新日期：1993-11-01 00:00:00

abstract：:Stimulation of beta2-adrenoceptors with the selective beta2 agonist procaterol caused a biphasic decrease in cell surface M2 muscarinic receptor number in human embryonic lung 299 cells when measured with the hydrophilic antagonist [3H]N-methylscopolamine. In contrast, total muscarinic receptor number, measured with t...

journal_title：Molecular pharmacology

authors： Rousell J,Haddad EB,Mak JC,Webb BL,Giembycz MA,Barnes PJ

更新日期：1996-04-01 00:00:00

abstract：:Previous studies have shown that the transcription factor signal transducer and activator of transcription-3 (STAT3) in podocytes plays an important role in progression of HIV nephropathy and in collapsing forms of glomerulonephritis. Here, we have observed that application of 100 nM angiotensin II (Ang II) to culture...

journal_title：Molecular pharmacology

authors： Abkhezr M,Dryer SE

更新日期：2014-08-01 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：:Multiple lines of evidence indicate that the platinum-containing cancer drugs enter cells, are distributed to various subcellular compartments, and are exported from cells via transporters that evolved to manage copper homeostasis. The cytotoxicity of the platinum drugs is directly related to how much drug enters the ...

journal_title：Molecular pharmacology

authors： Howell SB,Safaei R,Larson CA,Sailor MJ

更新日期：2010-06-01 00:00:00

abstract：:We recently reported the cloning of a novel alpha 1-adrenergic receptor (AR), the alpha 1CAR. By transient and stable expression of the alpha 1CAR and the previously cloned alpha 1BAR in COS-7 and HeLa cells, respectively, we have now compared their ability to interact with major signal-transduction pathways (includin...

journal_title：Molecular pharmacology

authors： Schwinn DA,Page SO,Middleton JP,Lorenz W,Liggett SB,Yamamoto K,Lapetina EG,Caron MG,Lefkowitz RJ,Cotecchia S

更新日期：1991-11-01 00:00:00

abstract：:Despite some blockbuster G protein-coupled receptor (GPCR) drugs, only a small fraction (∼ 15%) of the more than 390 nonodorant GPCRs have been successfully targeted by the pharmaceutical industry. One way that this issue might be addressed is via translation of recent deorphanization programs that have opened the pro...

journal_title：Molecular pharmacology

authors： Bolognini D,Tobin AB,Milligan G,Moss CE

更新日期：2016-03-01 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：:[3H]P1075 binding to membrane preparations of rabbit skeletal muscle were observed in the presence of nucleotide triphosphates or diphosphates but not AMP, cAMP, adenosine, tripolyphosphate, or pyrophosphate. Nonhydrolyzable or poorly hydrolyzable ATP analogs inhibited MgATP-supported binding. The EC50 value for MgATP...

journal_title：Molecular pharmacology

authors： Dickinson KE,Bryson CC,Cohen RB,Rogers L,Green DW,Atwal KS

更新日期：1997-09-01 00:00:00

abstract：:Four piperazinoquinolone antibacterial drugs (norfloxacin, ciprofloxacin, enoxacin, and pipemidic acid), known to be gamma-aminobutyric acid (GABA) antagonists, fully reversed the inhibitory effect of GABA on [35S]t-butylbicyclophosphorothionate ([35S] TBPS) binding to rat brain membranes in vitro. Twelve indomethacin...

journal_title：Molecular pharmacology

authors： Squires RF,Saederup E

更新日期：1993-05-01 00:00:00