Copper transporters and the cellular pharmacology of the platinum-containing cancer drugs.

abstract：:In the rat isolated optic nerve, nitric oxide (NO) activates soluble guanylyl cyclase (sGC), resulting in a selective accumulation of cGMP in the axons. The axons are also selectively vulnerable to NO toxicity. The experiments initially aimed to determine any causative link between these two effects. It was shown, usi...

journal_title：Molecular pharmacology

authors： Garthwaite G,Goodwin DA,Neale S,Riddall D,Garthwaite J

更新日期：2002-01-01 00:00:00

abstract：:Signaling by the insulin-like growth factor (IGF)-1 receptor (IGF-1R) has been implicated in the promotion and aggressiveness of breast, prostate, colorectal, and lung cancers. The IGF binding proteins (IGFBPs) represent a class of natural IGF antagonists that bind to and sequester IGF-1/2 from the IGF-1R, making them...

journal_title：Molecular pharmacology

authors： Kibbey MM,Jameson MJ,Eaton EM,Rosenzweig SA

更新日期：2006-03-01 00:00:00

abstract：:The carbocyclic analogue of 5-nitro-2'-deoxyuridine (NO2dUrd), in which the sugar moiety is replaced by a cyclopentane ring and which was designated C-NO2dUrd, has been evaluated for its cytostatic, antimetabolic, and antitumor properties. The following findings are noted. C-NO2dUrd is about 500- to 2000-fold less inh...

journal_title：Molecular pharmacology

authors： Balzarini J,De Clercq E,Herdewijn P,Robins MJ

更新日期：1985-05-01 00:00:00

abstract：:CC and CXC chemokines coinduced in fibroblasts and leukocytes by cytokines and microbial agents determine the number of phagocytes infiltrating into inflamed tissues. Interleukin-8/CXCL8 and stromal cell-derived factor-1/CXCL12 significantly and dose-dependently increased the migration of monocytes, expressing the cor...

journal_title：Molecular pharmacology

authors： Gouwy M,Struyf S,Noppen S,Schutyser E,Springael JY,Parmentier M,Proost P,Van Damme J

更新日期：2008-08-01 00:00:00

abstract：:CYP3A4 is one of the major drug-metabolizing enzymes in human and is responsible for the metabolism of 60% of clinically used drugs. Many drugs are able to induce the expression of CYP3A4, which usually causes drug-drug interactions and adverse drug reactions. This study aims to explore the role of histone modificatio...

journal_title：Molecular pharmacology

authors： Yan L,Wang Y,Liu J,Nie Y,Zhong XB,Kan Q,Zhang L

更新日期：2017-08-01 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：:Previously, we reported the presence of dual promoters, referred to as distal (DP) and proximal, with a negative regulatory element between them in the mouse mu-opioid receptor (mor) gene. Here we have identified a positive regulatory element influencing mor DP transcription, which contains multiple consensus binding ...

journal_title：Molecular pharmacology

authors： Im HJ,Smirnov D,Yuhi T,Raghavan S,Olsson JE,Muscat GE,Koopman P,Loh HH

更新日期：2001-06-01 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：:Newly synthesized tocainide analogs were tested for their state-dependent affinity and use-dependent behavior on sodium currents (INa) of adult skeletal muscle fibers by means of the Vaseline-gap voltage clamp method. The drugs had the pharmacophore amino group constrained in position alpha [N-(2,6-dimethylphenyl)pyrr...

journal_title：Molecular pharmacology

authors： De Luca A,Talon S,De Bellis M,Desaphy JF,Lentini G,Corbo F,Scilimati A,Franchini C,Tortorella V,Camerino DC

更新日期：2003-10-01 00:00:00

abstract：:K201 (JTV-519) may prevent abnormal Ca(2+) leak from the sarcoplasmic reticulum (SR) in the ischemic heart and skeletal muscle (SkM) by stabilizing the ryanodine receptors (RyRs; RyR1 and RyR2, respectively). We tested direct modulation of the SR Ca(2+)-stimulated ATPase (SERCA) and RyRs by K201. In isolated cardiac a...

journal_title：Molecular pharmacology

authors： Darcy YL,Diaz-Sylvester PL,Copello JA

更新日期：2016-08-01 00:00:00

abstract：:The benzomorphan opiate, (-)N-allynormetazocine [(-)ANMC, (-)SKF10047], has been shown previously to bind two distinct sites on acetylcholine receptor (AChR)-rich membranes from Torpedo electroplaque. The low affinity site seems to correspond to the site for noncompetitive blockers on the AChR. The high affinity site,...

journal_title：Molecular pharmacology

authors： Coleman BA,Michel L,Oswald R

更新日期：1987-10-01 00:00:00

abstract：:cRNAs encoding the kappa-opioid receptor and an inwardly rectifying, G protein-coupled, K+ channel were coinjected into Xenopus oocytes. The effects of kappa-opioid receptor agonists and antagonists on the membrane currents in these oocytes were studied using the two-electrode voltage-clamp technique. The kappa-opioid...

journal_title：Molecular pharmacology

authors： Ma GH,Miller RJ,Kuznetsov A,Philipson LH

更新日期：1995-05-01 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：:It has been demonstrated previously that cannabinol (CBN) differentially modulates interleukin-2 (IL-2) protein secretion by T cells with a corresponding change in extracellular signal-regulated kinase activity. The objective of the present studies was to further investigate the molecular mechanism by which CBN enhanc...

journal_title：Molecular pharmacology

authors： Jan TR,Rao GK,Kaminski NE

更新日期：2002-02-01 00:00:00

abstract：:Previous biochemical studies have demonstrated that synergy between non-nucleoside reverse transcriptase (RT) inhibitors (NNRTI) and nucleoside RT inhibitors (NRTIs) is due to inhibition by the NNRTI of the rate at which HIV-1 RT facilitates ATP-mediated excision of NRTIs from chain-terminated template/primers (T/P). ...

journal_title：Molecular pharmacology

authors： Radzio J,Sluis-Cremer N

更新日期：2008-02-01 00:00:00

abstract：:Dilute formalin injected into the rat hindpaw as a nociceptive stimulus increases neurokinin-1 receptor (NK-1R) mRNA levels in the dorsal horn of the spinal cord. Increased NK-1R mRNA levels could result from increased mRNA stability or an increased rate of NK-1R mRNA transcription. In this study, RNA samples prepared...

journal_title：Molecular pharmacology

authors： McCarson KE,Krause JE

更新日期：1996-11-01 00:00:00

abstract：:Mitochondrial disorders are devastating genetic diseases for which efficacious therapies are still an unmet need. Recent studies report that increased availability of intracellular NAD obtained by inhibition of the NAD-consuming enzyme poly(ADP-ribose) polymerase (PARP)-1 or supplementation with the NAD-precursor nico...

journal_title：Molecular pharmacology

authors： Felici R,Lapucci A,Cavone L,Pratesi S,Berlinguer-Palmini R,Chiarugi A

更新日期：2015-06-01 00:00:00

abstract：:Previous analyses suggested that potent aryl hydrocarbon receptor (AhR) antagonists were planar, with a lateral electron-rich center. To further define structural requirements and mechanism for antagonism, ten additional flavone derivatives were synthesized. Based on their ability to 1) compete with 2,3,7, 8-tetrachlo...

journal_title：Molecular pharmacology

authors： Henry EC,Kende AS,Rucci G,Totleben MJ,Willey JJ,Dertinger SD,Pollenz RS,Jones JP,Gasiewicz TA

更新日期：1999-04-01 00:00:00

abstract：:The binding of two anthranilic acid derivatives, glafenic and floctafenic acids, to human erythrocytes and plasma proteins has been investigated in vitro by equilibrium dialysis. Despite their close chemical structures it was shown that the binding of the two compounds to serum albumin, lipoproteins, and erythrocytes ...

journal_title：Molecular pharmacology

authors： Albengres E,Urien S,Riant P,Marcel GA,Tillement JP

更新日期：1987-03-01 00:00:00

abstract：:We reported previously the formation of a glutathionyl conjugate of the active metabolite (AM) of clopidogrel and the covalent modification of a cysteinyl residue of human cytochrome P450 2B6 in a reconstituted system (Mol Pharmacol 80:839-847, 2011). In this work, we extended our studies of the metabolism of clopidog...

journal_title：Molecular pharmacology

authors： Zhang H,Lau WC,Hollenberg PF

更新日期：2012-08-01 00:00:00

abstract：:Cytosolic sulfotransferase (SULT)-mediated sulfation plays an essential role in the detoxification of bile acids and is necessary to avoid pathological conditions, such as cholestasis, liver damage, and colon cancer. In this study, using transgenic mice bearing conditional expression of the activated constitutive andr...

journal_title：Molecular pharmacology

authors： Saini SP,Sonoda J,Xu L,Toma D,Uppal H,Mu Y,Ren S,Moore DD,Evans RM,Xie W

更新日期：2004-02-01 00:00:00

abstract：:We cloned and expressed a human metabotropic glutamate receptor 1 alpha (HmGluR1 alpha) in a novel cell line. The human mGluR1 alpha cDNA was found to be 86% identical to rat mGluR1 alpha, and the predicted protein sequence was found to be 93% identical to rat mGluR1 alpha. We expressed HmGluR1 alpha in AV12-664, an a...

journal_title：Molecular pharmacology

authors： Desai MA,Burnett JP,Mayne NG,Schoepp DD

更新日期：1995-10-01 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 nuclear receptor peroxisome proliferator-activated receptor (PPAR) is activated by a diverse group of acidic ligands, including many peroxisome proliferator chemicals present in the environment. Janus tyrosine kinase-signal transducer and activator of transcription (JAK-STAT) signaling is activated by multiple cyt...

journal_title：Molecular pharmacology

authors： Shipley JM,Waxman DJ

更新日期：2003-08-01 00:00:00

abstract：:The human CYP2C9 plays a crucial role in the metabolic clearance of a wide range of clinical therapeutics. The *2 allele is a prevalent genetic variation in CYP2C9 that is found in various populations. A marked reduction of catalytic activity toward many important drug substrates has been demonstrated by CYP2C9*2, whi...

journal_title：Molecular pharmacology

authors： Parikh SJ,Evans CM,Obi JO,Zhang Q,Maekawa K,Glass KC,Shah MB

更新日期：2020-11-01 00:00:00

abstract：:Peroxisome proliferator-activated receptor δ (PPARδ) has been implicated in vascular pathophysiology. However, its functions in atherogenic changes of the vascular wall have not been fully elucidated. PPARδ activated by GW501516 (2-[2-methyl-4-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]methylsulfanyl]ph...

journal_title：Molecular pharmacology

authors： Hwang JS,Ham SA,Yoo T,Lee WJ,Paek KS,Lee CH,Seo HG

更新日期：2016-11-01 00:00:00

abstract：:15-Deoxy-Delta(12,14)-prostaglandin J(2) (15d-PGJ(2)) is a cyclopentenonic prostaglandin endowed with powerful anti-inflammatory activities, as shown in animal models of inflammatory/autoimmune diseases, where pharmacological administration of this prostanoid can ameliorate inflammation and local tissue damage via act...

journal_title：Molecular pharmacology

authors： Fionda C,Nappi F,Piccoli M,Frati L,Santoni A,Cippitelli M

更新日期：2007-11-01 00:00:00

abstract：:Regulators of G-protein signaling (RGS) proteins are important components of signal transduction pathways initiated through G-protein-coupled receptors (GPCRs). RGS proteins accelerate the intrinsic GTPase activity of G-protein alpha-subunits (Galpha) and thus shorten the time course and reduce the magnitude of G-prot...

journal_title：Molecular pharmacology

authors： Roman DL,Talbot JN,Roof RA,Sunahara RK,Traynor JR,Neubig RR

更新日期：2007-01-01 00:00:00

abstract：:GH3 cells show spontaneous activity characterized by bursts of action potentials and oscillations in [Ca 2+]i. This activity is modulated by the activation of exogenously expressed opioid receptors. In GH3 cells expressing only micro receptors (GH3MOR cells), the micro receptor-specific ligand [D-Ala2,N-Me-Phe4,Gly5-o...

journal_title：Molecular pharmacology

authors： Charles AC,Mostovskaya N,Asas K,Evans CJ,Dankovich ML,Hales TG

更新日期：2003-01-01 00:00:00

abstract：:AM1710 (3-(1,1-dimethyl-heptyl)-1-hydroxy-9-methoxy-benzo(c) chromen-6-one), a cannabilactone cannabinoid receptor 2 (CB2) agonist, suppresses chemotherapy-induced neuropathic pain in rodents without producing tolerance or unwanted side effects associated with CB1 receptors; however, the signaling profile of AM1710 re...

journal_title：Molecular pharmacology

authors： Li AL,Lin X,Dhopeshwarkar AS,Thomaz AC,Carey LM,Liu Y,Nikas SP,Makriyannis A,Mackie K,Hohmann AG

更新日期：2019-02-01 00:00:00