The Role of ACKR3 in Breast, Lung, and Brain Cancer.

abstract：:Phosphorylation of tau protein promotes stability of the axonal cytoskeleton; aberrant tau phosphorylation is implicated in the biogenesis of paired helical filaments (PHF) seen in Alzheimer's disease. Protein kinases and phosphatases that modulate tau phosphorylation have been identified using in vitro techniques; ho...

journal_title：Molecular pharmacology

authors： Garver TD,Kincaid RL,Conn RA,Billingsley ML

更新日期：1999-04-01 00:00:00

abstract：:2-Methyl-2-nitrosopropane (MNP) has long been known to undergo photochemical and thermal decomposition, generating di-tert-butyl nitroxide, in organic solvent. The present study was undertaken to demonstrate that MNP can be used as a caged-nitric oxide (NO), which can liberate NO upon illumination. Photolysis of MNP l...

journal_title：Molecular pharmacology

authors： Pou SJ,Anderson DE,Surichamorn W,Keaton LL,Tod ML

更新日期：1994-10-01 00:00:00

abstract：:Acetylsalicylic acid (aspirin) is a cyclooxygenase (COX) inhibitor, yet some of its therapeutic effects are thought to derive from mechanisms unrelated to prostaglandin synthesis inhibition. In human intestinal myofibroblasts, aspirin, at therapeutic doses, had the unexpected effect of inducing prolonged COX-2 express...

journal_title：Molecular pharmacology

authors： Mifflin RC,Saada JI,Di Mari JF,Valentich JD,Adegboyega PA,Powell DW

更新日期：2004-02-01 00:00:00

abstract：:The ability of four antidepressant drugs, imipramine, alaproclate, norzimelidine, and fluvoxamine, to inhibit serotonin transport into platelet plasma membrane vesicles was tested over a range of external Na+ concentrations. Imipramine affinity, as we previously reported [J. Biol. Chem. 258:6115-6119 (1983)] increases...

journal_title：Molecular pharmacology

authors： Humphreys CJ,Levin J,Rudnick G

更新日期：1988-06-01 00:00:00

abstract：:Retina from 1-day-old chicks is a valuable tissue model for studying neuronal nicotinic receptors because it expresses a large number of the developmentally regulated high affinity [(3)H]epibatidine labeled nicotinic receptors. Most of these receptors contain the beta4 subunit associated with different alpha subunits....

journal_title：Molecular pharmacology

authors： Barabino B,Vailati S,Moretti M,McIntosh JM,Longhi R,Clementi F,Gotti C

更新日期：2001-06-01 00:00:00

abstract：:The efficacy of antineoplastic compounds can depend heavily on the genetic background of the cells exposed to the drugs. This becomes evident by the fact that HT-29 human colon cancer cells but not primary murine nontransformed colonocytes are efficiently submitted to apoptosis by the flavonoid flavone. By determining...

journal_title：Molecular pharmacology

authors： Wenzel U,Kuntz S,Daniel H

更新日期：2003-12-01 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：:Our laboratory recently isolated and sequenced cDNAs encoding the microsomal flavin-containing monooxygenases (FMOs) from rabbit liver and rabbit lung. As a first step in understanding the molecular bases for the catalytic and physical differences between these enzymes, we have expressed them in COS-1 cells and compar...

journal_title：Molecular pharmacology

authors： Lawton MP,Kronbach T,Johnson EF,Philpot RM

更新日期：1991-11-01 00:00:00

abstract：:We examined the effect of trichosporin-B-III, an alpha-aminoisobutyric acid-containing antibiotic peptide consisting of 19 amino acid residues and a phenylalaninol, on catecholamine secretion from cultured bovine adrenal chromaffin cells. Incubation of the cells with trichosporin-B-III (3-20 microM) caused an increase...

journal_title：Molecular pharmacology

authors： Tachikawa E,Takahashi S,Furumachi K,Kashimoto T,Iida A,Nagaoka Y,Fujita T,Takaishi Y

更新日期：1991-11-01 00:00:00

abstract：:Extracellular protons inhibit N-methyl-D-aspartate (NMDA) receptors with an IC50 value in the physiological pH range. To identify the molecular determinants of proton sensitivity, we used scanning mutagenesis of the NR1 subunit to search for residues that control proton inhibition of NMDA receptors. Homology modeling ...

journal_title：Molecular pharmacology

authors： Low CM,Lyuboslavsky P,French A,Le P,Wyatte K,Thiel WH,Marchan EM,Igarashi K,Kashiwagi K,Gernert K,Williams K,Traynelis SF,Zheng F

更新日期：2003-06-01 00:00:00

abstract：:Previously, we showed that the human kappa-opioid receptor (hkor) stably expressed in Chinese hamster ovary (CHO) cells underwent down-regulation after prolonged U50,488H treatment. In the present study, we determined the mechanisms underlying this process. U50, 488H caused a significant down-regulation of the hkor, a...

journal_title：Molecular pharmacology

authors： Li JG,Benovic JL,Liu-Chen LY

更新日期：2000-10-01 00:00:00

abstract：:Previous studies have shown that at least two subtypes of somatostatin (SRIF) receptors (SRIF1 and SRIF2) are expressed in mammalian cells. SRIF1 receptors have high affinity for MK 678, whereas SRIF2 receptors have no affinity for MK 678 but selectively bind peptides with structures similar to that of CGP 23996. Rece...

journal_title：Molecular pharmacology

authors： Rens-Domiano S,Law SF,Yamada Y,Seino S,Bell GI,Reisine T

更新日期：1992-07-01 00:00:00

abstract：:Nicotine can enhance working memory and attention. Activation of both alpha7 and beta2(*) nicotinic acetylcholine receptors (nAChRs) in the prefrontal cortex (PFC) has been implicated in these processes. The ability of presynaptic nAChRs to modulate neurotransmitter release, notably glutamate release, is postulated to...

journal_title：Molecular pharmacology

authors： Dickinson JA,Kew JN,Wonnacott S

更新日期：2008-08-01 00:00:00

abstract：:Recently we identified the serotonin reuptake inhibitor paroxetine as an inhibitor of G protein-coupled receptor kinase 2 (GRK2) that improves cardiac performance in live animals. Paroxetine exhibits up to 50-fold selectivity for GRK2 versus other GRKs. A better understanding of the molecular basis of this selectivity...

journal_title：Molecular pharmacology

authors： Homan KT,Wu E,Wilson MW,Singh P,Larsen SD,Tesmer JJ

更新日期：2014-02-01 00:00:00

abstract：:The ADP-sensitive and K+ -sensitive phosphorylated forms of Na,K-ATPase (E1P and E2P, respectively) are believed to be the main phosphorylated intermediates of Na,K-ATPase. In the presence of 100 mM Na+, E2P is the major component of the phosphorylated form in all native Na,K-ATPase preparations known, including the m...

journal_title：Molecular pharmacology

authors： Yoda A,Yoda S

更新日期：1982-11-01 00:00:00

abstract：:The peroxisome proliferator-activated receptors (PPARs) represent pharmacological target molecules to improve insulin resistance in type 2 diabetes mellitus. Here we assessed a functional connection between pharmacological activation of PPAR and vascular endothelial growth factor (VEGF) expression in keratinocytes and...

journal_title：Molecular pharmacology

authors： Schiefelbein D,Seitz O,Goren I,Dissmann JP,Schmidt H,Bachmann M,Sader R,Geisslinger G,Pfeilschifter J,Frank S

更新日期：2008-10-01 00:00:00

abstract：:Psoralen plus UVA light (PUVA) is commonly used to treat psoriasis, a common skin disorder associated with rapid proliferation of cells. PUVA exerts its antiproliferative activity through formation of DNA monoadducts and interstrand cross-links (ICLs). However, this treatment may lead to skin malignancies as a direct ...

journal_title：Molecular pharmacology

authors： Derheimer FA,Hicks JK,Paulsen MT,Canman CE,Ljungman M

更新日期：2009-03-01 00:00:00

abstract：:Inhibitors of the serotonin transporter (SERT) are widely used antidepressant agents, but the structural mechanism for inhibitory activity and selectivity over the closely related norepinephrine transporter (NET) is not well understood. Here we use a combination of chemical, biological, and computational methods to de...

journal_title：Molecular pharmacology

authors： Andersen J,Stuhr-Hansen N,Zachariassen LG,Koldsø H,Schiøtt B,Strømgaard K,Kristensen AS

更新日期：2014-05-01 00:00:00

abstract：:We examined the block of N-methyl-D-aspartate (NMDA) receptors by n-alkyl (straight chain) diamines and related monoamines and triamines using whole-cell voltage clamp recording of NMDA receptor currents in cultured rat hippocampal neurons and [3H] dizocilpine binding to rat forebrain homogenates. At -60 mV, the diami...

journal_title：Molecular pharmacology

authors： Subramaniam S,Donevan SD,Rogawski MA

更新日期：1994-01-01 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：:Anthracyclines are potent anticancer agents, but their use is limited by cardiotoxicity at high cumulative doses. The mechanisms involved in anthracycline-mediated cardiotoxicity are still poorly understood, but numerous investigations have indicated a role for iron in this process. Our previous studies using neoplast...

journal_title：Molecular pharmacology

authors： Kwok JC,Richardson DR

更新日期：2004-01-01 00:00:00

abstract：:Bupropion is an atypical antidepressant that also has usefulness as a smoking-cessation aid. Because hydroxybupropion, a major metabolite of bupropion, is believed to contribute to its antidepressant activity, this metabolite may also contribute to the smoking-cessation properties of bupropion. This study investigated...

journal_title：Molecular pharmacology

authors： Damaj MI,Carroll FI,Eaton JB,Navarro HA,Blough BE,Mirza S,Lukas RJ,Martin BR

更新日期：2004-09-01 00:00:00

abstract：:Up-regulation of fractalkine is involved in vascular and tissue damage in inflammatory conditions. Resveratrol has been shown to have anti-inflammatory, antioxidant, and antitumor activities. Its regulatory effects on expression of fractalkine in vascular endothelial cells and fractalkine receptor CX3CR1 in monocytes ...

journal_title：Molecular pharmacology

authors： Moon SO,Kim W,Sung MJ,Lee S,Kang KP,Kim DH,Lee SY,So JN,Park SK

更新日期：2006-07-01 00:00:00

abstract：:Cytotoxic effects of quinones are thought to be mediated by redox cycles between quinones and quinols whereby reactive oxygen species are generated. The role of glucuronidation in preventing these toxic redox cycles was investigated by using benzo(a)pyrene-3,6-quinone and isolated rat hepatocytes or Reuber hepatoma ce...

journal_title：Molecular pharmacology

authors： Lilienblum W,Bock-Hennig BS,Bock KW

更新日期：1985-04-01 00:00:00

abstract：:In previous studies, it was shown that the overexpression of beta2-adrenoceptor (beta2AR) in the hearts of transgenic mice (Tg) leads to agonist-independent activation of adenylate cyclase and enhanced myocardial function. Here, we measured the physical coupling of beta2AR and Gs by evaluating the coimmunoprecipitatio...

journal_title：Molecular pharmacology

authors： Gürdal H,Bond RA,Johnson MD,Friedman E,Onaran HO

更新日期：1997-08-01 00:00:00

abstract：:The insecticide imidacloprid and structurally related neonicotinoids act selectively on insect nicotinic acetylcholine receptors (nAChRs). To investigate the mechanism of neonicotinoid selectivity, we have examined the effects of mutations to basic amino acid residues in loop D of the nAChR acetylcholine (ACh) binding...

journal_title：Molecular pharmacology

authors： Shimomura M,Yokota M,Ihara M,Akamatsu M,Sattelle DB,Matsuda K

更新日期：2006-10-01 00:00:00

abstract：:Fusion proteins were generated between the human 5-hydroxytryptamine (5-HT)(1A) receptor and both wild-type (Cys(351)) and pertussis toxin-resistant (Gly(351) and Ile(351)) forms of G(i1). These were expressed stably. Pertussis toxin treatment substantially reduced basal high-affinity GTPase activity in clones express...

journal_title：Molecular pharmacology

authors： Kellett E,Carr IC,Milligan G

更新日期：1999-10-01 00:00:00

abstract：:Aflatrem, a mycotoxin from Aspergillus flavus, potentiates the gamma-aminobutyric acid (GABA)-induced chloride current. This positive allosteric regulatory action of aflatrem was quantitatively studied on the GABAA receptor channel expressed in Xenopus oocytes after injection with chick brain mRNA under voltage-clamp ...

journal_title：Molecular pharmacology

authors： Yao Y,Peter AB,Baur R,Sigel E

更新日期：1989-03-01 00:00:00

abstract：:The diphosphoinositol polyphosphates ("inositol pyrophosphates") are a specialized subgroup of the inositol phosphate signaling family. This review proposes that many of the current data concerning the metabolic turnover and biological effects of the diphosphoinositol polyphosphates are linked by a common theme: these...

journal_title：Molecular pharmacology

authors： Shears SB

更新日期：2009-08-01 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