Effect of anti-human immunodeficiency virus nucleoside analogs on mitochondrial DNA and its implication for delayed toxicity.

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：:The presence of DNA damage initiates signaling through the ataxia-telangiectasia mutated kinase (ATM) and the ATM- and the Rad3-related kinase (ATR), which phosphorylate, thus activating, the checkpoint kinases (Chk) 1 and 2, which leads to cell cycle arrest. The bifunctional DNA alkylator 1,3-bis(2-chloroethyl)-1-nit...

journal_title：Molecular pharmacology

authors： Cui B,Johnson SP,Bullock N,Ali-Osman F,Bigner DD,Friedman HS

更新日期：2009-06-01 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：:Neuronal cell degeneration was studied in vitro in primary rat brain neuronal cultures grown in serum-free, chemically defined, CDM R12 medium, by measuring lactate dehydrogenase (LDH) released in the culture medium. A Ca2+-dependent neuronal cell degeneration was observed after prolonged and transient exposure 30 mic...

journal_title：Molecular pharmacology

authors： Pauwels PJ,Van Assouw HP,Leysen JE,Janssen PA

更新日期：1989-10-01 00:00:00

abstract：:Upon sustained insult, kinins are released and many kinin responses, such as inflammatory pain, adapt from a B2 receptor (B2R) type in the acute phase to a B1 receptor (B1R) type in the chronic phase. In this study, we show that kinins modulate receptor endocytosis to rapidly decrease B2R and increase B1R on the cell ...

journal_title：Molecular pharmacology

authors： Enquist J,Skröder C,Whistler JL,Leeb-Lundberg LM

更新日期：2007-02-01 00:00:00

abstract：:The sympathetic nervous system modulates cardiac contractility and rate by activating beta-adrenergic receptors (beta AR) expressed on cardiac myocytes and specialized cells in the sinoatrial node and the conduction system. Recent clinical studies have suggested that beta-adrenergic receptors also play a role in cardi...

journal_title：Molecular pharmacology

authors： Devic E,Xiang Y,Gould D,Kobilka B

更新日期：2001-09-01 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：:This study describes experiments investigating the mechanism of activation of A1 adenosine receptors. Isolated rat fat cells were used as a cellular model. The A1 receptors of these cells were covalently labeled with the agonist photoaffinity label R-2-azido-N6-p-hydroxyphenylisopropyladenosine. The covalent incorpora...

journal_title：Molecular pharmacology

authors： Lohse MJ,Klotz KN,Schwabe U

更新日期：1986-10-01 00:00:00

abstract：:The nicotinic acetylcholine receptor can be expressed in Xenopus oocytes by injection of in vitro synthesized RNA for the alpha, beta, gamma, and delta mouse muscle subunits. However, detectable responses can also be obtained by injection of alpha, beta, and delta subunit RNA only. The receptors expressed in this case...

journal_title：Molecular pharmacology

authors： Charnet P,Labarca C,Lester HA

更新日期：1992-04-01 00:00:00

abstract：:Two human ovarian cancer cell lines were established from a patient before (PEO1) and after (PEO4) the onset of resistance to 5-fluorouracil (5-FU)/cisplatin-based chemotherapy. Using growth inhibition assays, we determined that the PEO4 line was almost 5-fold more resistant to 5-FU than the PEO1 line. The addition of...

journal_title：Molecular pharmacology

authors： Chu E,Lai GM,Zinn S,Allegra CJ

更新日期：1990-09-01 00:00:00

abstract：:The gamma-aminobutyric acid(A) (GABA(A)) receptor contains a binding site (or sites) for benzodiazepines and related ligands. Previous studies have shown that the residue occupying position 101 (rat numbering) of the alpha subunit is particularly important in determining how some of these compounds interact with the r...

journal_title：Molecular pharmacology

authors： Dunn SM,Davies M,Muntoni AL,Lambert JJ

更新日期：1999-10-01 00:00:00

abstract：:Receptors have well-conserved regions that are recognized and activated by hormones and neurotransmitters. Most drugs bind to these sites and mimic or block the action of the native ligands. Using a high-throughput functional screen, we identified a potent and selective M(1) muscarinic receptor agonist from a novel st...

journal_title：Molecular pharmacology

authors： Spalding TA,Trotter C,Skjaerbaek N,Messier TL,Currier EA,Burstein ES,Li D,Hacksell U,Brann MR

更新日期：2002-06-01 00:00:00

abstract：:Recently we demonstrated that the effects of beta 2-adrenoceptor (AR) stimulation to augment Ca2+ current (ICa), cytosolic Ca2+ (Cai) transients, and contractility in rat ventricular myocytes are largely dissociated from its effect to increase cellular cAMP levels. This result suggested that beta 2ARs might be coupled...

journal_title：Molecular pharmacology

authors： Xiao RP,Ji X,Lakatta EG

更新日期：1995-02-01 00:00:00

abstract：:The beta 3-adrenergic receptor (beta 3AR) is a member of the super-family of G protein-coupled receptors that are characterized by seven putative transmembrane helices connected by hydrophilic loops. The mechanism by which the activated beta ARs transmit the signals across the plasma membrane involves the stimulation ...

journal_title：Molecular pharmacology

authors： Guan XM,Amend A,Strader CD

更新日期：1995-09-01 00:00:00

abstract：:Corticotropin-releasing factor (CRF) receptors encoded by two distinct genes have recently been identified and termed CRF1 and CRF2. CRF and the non-mammalian-related peptide sauvagine bind to and activate CRF1 receptors with high affinity and equal potency. Although CRF is significantly weaker at the CRF2 receptor, s...

journal_title：Molecular pharmacology

authors： Grigoriadis DE,Liu XJ,Vaughn J,Palmer SF,True CD,Vale WW,Ling N,De Souza EB

更新日期：1996-09-01 00:00:00

abstract：:Amitriptyline is a classic tricyclic antidepressant (TCA) and has been used to treat the depression and anxiety of patients with cancer, but its relevance to cancer cell apoptosis is not known. In the present study, we demonstrated that amitriptyline inhibited cyclin D2 transactivation and displayed potential antimyel...

journal_title：Molecular pharmacology

authors： Mao X,Hou T,Cao B,Wang W,Li Z,Chen S,Fei M,Hurren R,Gronda M,Wu D,Trudel S,Schimmer AD

更新日期：2011-04-01 00:00:00

abstract：:Notch-1 (Notch) is a cell surface receptor that regulates cell-fate decisions in the developing nervous system, and it may also have roles in synaptic plasticity in the adult brain. Binding of its ligands results in the proteolytic cleavage of Notch by the γ-secretase enzyme complex, thereby causing the release of a N...

journal_title：Molecular pharmacology

authors： Arumugam TV,Cheng YL,Choi Y,Choi YH,Yang S,Yun YK,Park JS,Yang DK,Thundyil J,Gelderblom M,Karamyan VT,Tang SC,Chan SL,Magnus T,Sobey CG,Jo DG

更新日期：2011-07-01 00:00:00

abstract：:Tetrodotoxin-sensitive Na(+) currents have been extensively studied because they play a major role in neuronal firing and bursting. In this study, we showed that voltage-dependent Na(+) currents are regulated in a slow manner by oxotremorine (oxo-M) and angiotensin II in rat sympathetic neurons. We found that these cu...

journal_title：Molecular pharmacology

authors： Puente EI,De la Cruz L,Arenas I,Elias-Viñas D,Garcia DE

更新日期：2016-04-01 00:00:00

abstract：:The interaction of hormones acting via the mobilization of calcium and stimulation of cAMP levels in cells was examined by determining the effects of carbachol and forskolin on cAMP and cGMP accumulation in mouse parotid gland. Treatment of isolated acini with either carbachol (0.01 to 20 microM) or forskolin (1 micro...

journal_title：Molecular pharmacology

authors： Watson EL,Singh JC,McPhee C,Beavo J,Jacobson KL

更新日期：1990-10-01 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 anti-arrhythmic quinidine has been reported to be a competitive inhibitor of the catalytic activities of human liver P-450DB, including sparteine delta 2-oxidation and bufuralol 1'-hydroxylation, and we confirmed the observation that submicromolar concentrations are strongly inhibitory. Human liver microsomes oxid...

journal_title：Molecular pharmacology

authors： Guengerich FP,Müller-Enoch D,Blair IA

更新日期：1986-09-01 00:00:00

abstract：:It has long been believed that the cortical actin cytoskeleton plays an important role in regulating the secretion of hormones and neurotransmitters. In this study, we investigated the control of actin dynamics in primary neuroendocrine cells and determined the relationship of actin dynamics to various components of t...

journal_title：Molecular pharmacology

authors： Bittner MA,Holz RW

更新日期：2005-04-01 00:00:00

abstract：:Epoxyeicosatrienoic acids (EETs), products of the cytochrome P-450 monooxygenase metabolism of arachidonic acid, can regulate the activity of ion channels. We examined the effects of EETs on cardiac L-type Ca2+ channels that play important roles in regulating cardiac contractility, controlling heart rate, and mediatin...

journal_title：Molecular pharmacology

authors： Chen J,Capdevila JH,Zeldin DC,Rosenberg RL

更新日期：1999-02-01 00:00:00

abstract：:Human serum butyrylcholinesterase (Hu BChE) is a promising therapeutic against the toxicity of chemical warfare nerve agents. We have showed previously that recombinant (r) Hu BChE can be expressed at very high levels, 400 to 600 U/ml in mouse blood, by delivering the Hu BChE gene using adenovirus (Ad). Here, we repor...

journal_title：Molecular pharmacology

authors： Chilukuri N,Duysen EG,Parikh K,diTargiani R,Doctor BP,Lockridge O,Saxena A

更新日期：2009-09-01 00:00:00

abstract：:We have, in the accompanying work, demonstrated the coexistence of M2 and M3 muscarinic receptors in the circular smooth muscle of canine colon. In the present study, the effects of muscarinic receptor stimulation on phosphoinositide turnover and adenylate cyclase activity were examined. In myo-[3H]inositol-labeled ci...

journal_title：Molecular pharmacology

authors： Zhang LB,Buxton IL

更新日期：1991-12-01 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：:We determined the effect of flufenamic acid (FFA) and related derivatives on gap junction channel currents, applying the dual whole-cell patch-clamp technique to pairs of N2A neuroblastoma cells transfected with various connexins. FFA reduced gap junction channel currents in a reversible and concentration-dependent ma...

journal_title：Molecular pharmacology

authors： Srinivas M,Spray DC

更新日期：2003-06-01 00:00:00

abstract：:alpha4beta2 nicotinic acetylcholine receptors (nAChRs) are recognized as the principal nicotine binding site in brain. Recombinant alpha4beta2 nAChR demonstrate biphasic concentration-response relationships with low- and high-EC50 components. This study shows that untranslated regions (UTR) can influence expression of...

journal_title：Molecular pharmacology

authors： Briggs CA,Gubbins EJ,Marks MJ,Putman CB,Thimmapaya R,Meyer MD,Surowy CS

更新日期：2006-07-01 00:00:00

abstract：:[3H]-d-cis-Diltiazem binds to canine cardiac sarcolemma in a specific, saturable, and reversible manner with a KD = 58.0 +/- 9.5 nM and a receptor site density (maximum binding) of 2.19 +/- 0.24 pmol/mg of protein. Bepridil and verapamil, Ca2+ channel inhibitors, can completely inhibit this binding at nM concentration...

journal_title：Molecular pharmacology

authors： Balwierczak JL,Johnson CL,Schwartz A

更新日期：1987-02-01 00:00:00

abstract：:The delta family of ionotropic glutamate receptors consists of glutamate delta-1 (GluD1) and glutamate delta-2 receptors. We have previously shown that GluD1 knockout mice exhibit features of developmental delay, including impaired spine pruning and switch in the N-methyl-D-aspartate receptor subunit, which are releva...

journal_title：Molecular pharmacology

authors： Suryavanshi PS,Gupta SC,Yadav R,Kesherwani V,Liu J,Dravid SM

更新日期：2016-08-01 00:00:00