Inhibitors of IMP dehydrogenase stimulate the phosphorylation of the anti-human immunodeficiency virus nucleosides 2',3'-dideoxyadenosine and 2',3'-dideoxyinosine.

abstract：:G-protein-coupled receptor activation is generally analyzed under equilibrium conditions. However, real-life receptor functions are often dependent on very short, transient stimuli that may not allow the achievement of a steady state. This is particularly true for synaptic receptors such as the α(2A)-adrenergic recept...

journal_title：Molecular pharmacology

authors： Ambrosio M,Lohse MJ

更新日期：2012-06-01 00:00:00

abstract：:Eukaryotic cells assemble stress granules (SGs) when translation initiation is inhibited. Different cell signaling pathways regulate SG production. Particularly relevant to this process is 5'-AMP-activated protein kinase (AMPK), which functions as a stress sensor and is transiently activated by adverse physiologic con...

journal_title：Molecular pharmacology

authors： Mahboubi H,Koromilas AE,Stochaj U

更新日期：2016-10-01 00:00:00

abstract：:Studies in vertebrate neuromuscular synapses have revealed previously that ATP, via P2Y receptors, plays a critical role in regulating postsynaptic gene expressions. An equivalent regulatory role of ATP and its P2Y receptors would not necessarily be expected for the very different situation of the brain synapses, but ...

journal_title：Molecular pharmacology

authors： Siow NL,Choi RC,Xie HQ,Kong LW,Chu GK,Chan GK,Simon J,Barnard EA,Tsim KW

更新日期：2010-12-01 00:00:00

abstract：:This article describes the expected phenotypic behavior of all types of ligands in constitutively active receptor systems and, in particular, the molecular mechanisms of inverse agonism. The possible physiological relevance of inverse agonism also is discussed. Competitive antagonists with the molecular property of ne...

journal_title：Molecular pharmacology

authors： Kenakin T

更新日期：2004-01-01 00:00:00

abstract：:Microglial activation is an invariant feature of Alzheimer's disease (AD). It is noteworthy that cannabinoids are neuroprotective by preventing β-amyloid (Aβ)-induced microglial activation both in vitro and in vivo. On the other hand, the phytocannabinoid cannabidiol (CBD) has shown anti-inflammatory properties in dif...

journal_title：Molecular pharmacology

authors： Martín-Moreno AM,Reigada D,Ramírez BG,Mechoulam R,Innamorato N,Cuadrado A,de Ceballos ML

更新日期：2011-06-01 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：: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：:A high cytoplasmic Na(+) concentration may contribute to N-methyl-D-aspartate (NMDA)-induced excitotoxicity by promoting Ca(2+) influx via reverse operation of the Na(+)/Ca(2+) exchanger (NaCaX), but may simultaneously decrease the electrochemical Ca(2+) driving force by depolarizing the plasma membrane (PM). Digital ...

journal_title：Molecular pharmacology

authors： Kiedrowski L

更新日期：1999-09-01 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：:Two forms of the multisubunit gamma-aminobutyric acid (GABA)A receptor were expressed in Xenopus oocytes by injecting mRNA encoding the bovine GABAA receptor subunit cDNAs for alpha 1 beta 1 gamma 2L and alpha 3 beta 1 gamma 2L. The properties of these two combinations were examined by electrophysiological recording o...

journal_title：Molecular pharmacology

authors： Wafford KA,Whiting PJ,Kemp JA

更新日期：1993-02-01 00:00:00

abstract：:Cocaine use poses a major health problem not only because of the dependence it causes but also because of the generation of life-threatening cardiac arrhythmias following overdose. Elucidating the molecular mechanisms of action of cocaine, therefore, remains a critical step in developing treatment for cocaine addictio...

journal_title：Molecular pharmacology

authors： Premkumar LS

更新日期：1999-12-01 00:00:00

abstract：:Cannabinoids have been implicated in the reduction of glioma growth. The present study investigated a possible relationship between the recently shown induction of cyclooxygenase (COX)-2 expression by the endocannabinoid analog R(+)methanandamide [R(+)-MA] and its effect on the viability of H4 human neuroglioma cells....

journal_title：Molecular pharmacology

authors： Hinz B,Ramer R,Eichele K,Weinzierl U,Brune K

更新日期：2004-12-01 00:00:00

abstract：:Compound BM5 [N-methyl-N(1-methyl-4-pyrrolidino-2-butynyl) acetamide] has previously been described as an agonist at postsynaptic muscarinic receptors and as an antagonist at presynaptic receptors. In the current work, we studied the ability of this compound to selectively stimulate phosphoinositide (PI) turnover in C...

journal_title：Molecular pharmacology

authors： Baumgold J,Drobnick A

更新日期：1989-09-01 00:00:00

abstract：:The effect of endocytosis inhibitors on 5-hydroxytryptamine(2A) (5-HT(2A)) receptor desensitization and resensitization was examined in transiently transfected human embryonic kidney (HEK) 293 cells and in C6 glioma cells that endogenously express 5-HT(2A) receptors. In HEK-293 cells, 5-HT(2A) receptor desensitization...

journal_title：Molecular pharmacology

authors： Gray JA,Sheffler DJ,Bhatnagar A,Woods JA,Hufeisen SJ,Benovic JL,Roth BL

更新日期：2001-11-01 00:00:00

abstract：:Based on the available data, we speculated that changes in brain iron metabolism induced by L-DOPA might be associated with the neurotoxicity of L-DOPA. To investigate this possibility, the effects of L-DOPA on the expression of iron influx proteins [transferrin receptor (TfR) and divalent metal transporter 1 (DMT1)],...

journal_title：Molecular pharmacology

authors： Chang YZ,Ke Y,Du JR,Halpern GM,Ho KP,Zhu L,Gu XS,Xu YJ,Wang Q,Li LZ,Wang CY,Qian ZM

更新日期：2006-03-01 00:00:00

abstract：:Past decades of cancer research have mainly focused on the role of various extracellular and intracellular biochemical signals on cancer progression and metastasis. Recent studies suggest an important role of mechanical forces in regulating cellular behaviors. This review first provides an overview of the mechanobiolo...

journal_title：Molecular pharmacology

authors： Majeski HE,Yang J

更新日期：2016-12-01 00:00:00

abstract：:Allosteric modulators of G-protein-coupled receptors can regulate conformational states involved in receptor activation ( Mol Pharmacol 58: 1412-1423, 2000 ). This hypothesis was investigated for the corticotropin-releasing factor type 1 (CRF(1)) receptor using a novel series of ligands with varying allosteric effect ...

journal_title：Molecular pharmacology

authors： Hoare SR,Fleck BA,Gross RS,Crowe PD,Williams JP,Grigoriadis DE

更新日期：2008-05-01 00:00:00

abstract：:Maurotoxin (MTX) is a potent blocker of human voltage-activated Kv1.2 and intermediate-conductance calcium-activated potassium channels, hIKCa1. Because its blocking affinity on both channels is similar, although the pore region of these channels show only few conserved amino acids, we aimed to characterize the bindin...

journal_title：Molecular pharmacology

authors： Visan V,Fajloun Z,Sabatier JM,Grissmer S

更新日期：2004-11-01 00:00:00

abstract：:The X-ray and NMR structural study of 3-carbomethoxy rifamycin S5 was undertaken in order to determine whether its low antimicrobial activity was related to a conformation of the molecule which was unfavorable for interaction with bacterial DNA-dependent RNA polymerase. However, the molecule assumes a conformation sim...

journal_title：Molecular pharmacology

authors： Brufani M,Cellai L,Cerrini S,Fedeli W,Segre A,Vaciago A

更新日期：1982-03-01 00:00:00

abstract：:Histone deacetylase inhibitors (HDACi), which have emerged as a new class of anticancer agents, act by modulating expression of genes controlling apoptosis or cell proliferation. Here, we compared the effect of HDACi on transcriptional activation by estrogen or glucocorticoid receptors (ER and GR, respectively), two m...

journal_title：Molecular pharmacology

authors： Rocha W,Sanchez R,Deschênes J,Auger A,Hébert E,White JH,Mader S

更新日期：2005-12-01 00:00:00

abstract：:The spatiotemporal dynamics of opioid signaling in the brain remain poorly defined. Photoactivatable opioid ligands provide a means to quantitatively measure these dynamics and their underlying mechanisms in brain tissue. Although activation kinetics can be assessed using caged agonists, deactivation kinetics are obsc...

journal_title：Molecular pharmacology

authors： Banghart MR,Williams JT,Shah RC,Lavis LD,Sabatini BL

更新日期：2013-11-01 00:00:00

abstract：:Serotonin 5-HT(2B) receptors are often coexpressed with 5-HT(1B) receptors, and cross-talk between the two receptors has been reported in various cell types. However, many mechanistic details underlying 5-HT(1B) and 5-HT(2B) receptor cross-talk have not been elucidated. We hypothesized that 5-HT(2B) and 5-HT(1B) recep...

journal_title：Molecular pharmacology

authors： Janoshazi A,Deraet M,Callebert J,Setola V,Guenther S,Saubamea B,Manivet P,Launay JM,Maroteaux L

更新日期：2007-06-01 00:00:00

abstract：:Small-molecule restoration of wild-type structure and function to mutant p53 (so-called mutant reactivation) is a highly sought-after goal in cancer drug development. We previously discovered that small-molecule zinc chelators called zinc metallochaperones (ZMCs) reactivate mutant p53 by restoring zinc binding to zinc...

journal_title：Molecular pharmacology

authors： Yu X,Blanden A,Tsang AT,Zaman S,Liu Y,Gilleran J,Bencivenga AF,Kimball SD,Loh SN,Carpizo DR

更新日期：2017-06-01 00:00:00

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：:The powerful analgesic effects of opioid drugs have captivated the interest of physicians and scientists for millennia, and the ability of opioid drugs to produce serious undesired effects has been recognized for a similar period of time (Kieffer and Evans, 2009). Many of these develop progressively with prolonged or ...

journal_title：Molecular pharmacology

authors： Jullié D,Gondin AB,von Zastrow M,Canals M

更新日期：2020-10-01 00:00:00

abstract：:The mechanisms underlying mastoparan-induced elevation of the intracellular free calcium concentration ([Ca2+]i) were investigated in the insulin-secreting cell lines RINm5F and HIT. In both cell types, micromolar concentrations of mastoparan induced a prompt increase of [Ca2+]i, measured as an increase in fura-2 fluo...

journal_title：Molecular pharmacology

authors： Eddlestone GT,Komatsu M,Shen L,Sharp GW

更新日期：1995-04-01 00:00:00

abstract：:Several lines of evidence suggest that G-protein-coupled receptors can adopt different active conformations, but their direct demonstration in intact cells is still missing. Using a fluorescence resonance energy transfer (FRET)-based approach we studied conformational changes in alpha(2A)-adrenergic receptors in intac...

journal_title：Molecular pharmacology

authors： Zürn A,Zabel U,Vilardaga JP,Schindelin H,Lohse MJ,Hoffmann C

更新日期：2009-03-01 00:00:00

abstract：:The chelator di-2-pyridylketone 4,4-dimethyl-3-thiosemicarbazone (Dp44mT) shows potent and selective anticancer and antimetastatic activity. However, the mechanism by which it is initially transported into cells to induce cytotoxicity is unknown. Hence, the current investigation examined the cellular uptake of ¹⁴C-Dp4...

journal_title：Molecular pharmacology

authors： Merlot AM,Pantarat N,Menezes SV,Sahni S,Richardson DR,Kalinowski DS

更新日期：2013-12-01 00:00:00

abstract：:We describe the receptor binding and antagonistic properties of two novel nonpeptide antagonists, FR167344 (3-bromo-8-[2,6-dichloro-3-[N-[(E)-4-(N,N-dimethylcarbamoyl)cinnamido acetyl]-N-methylamino]benzyloxy]-2-methylimidazo[1,2-a]pyridine hydrochloride) and FR173657 (8-[3-[N-[(E)-3-(6-acetamidopyridin-3-yl)acryloylg...

journal_title：Molecular pharmacology

authors： Aramori I,Zenkoh J,Morikawa N,O'Donnell N,Asano M,Nakamura K,Iwami M,Kojo H,Notsu Y

更新日期：1997-02-01 00:00:00

abstract：:The biliary excretion of several organic anions is mediated by the canalicular multispecific organic anion transporter (cMOAT), which is hereditarily defective in mutant rats such as Eisai hyperbilirubinemic rats (EHBR). In addition, using a kinetic study with isolated canalicular membrane vesicles, we recently sugges...

journal_title：Molecular pharmacology

authors： Hirohashi T,Suzuki H,Ito K,Ogawa K,Kume K,Shimizu T,Sugiyama Y

更新日期：1998-06-01 00:00:00