Long QT2 mutation on the Kv11.1 ion channel inhibits current activity by ablating a protein kinase Cα consensus site.

abstract：:We have previously reported that endocytic sorting of ET(A) endothelin receptors to the recycling pathway is dependent on a signal residing in the cytoplasmic carboxyl-terminal region. The aim of the present work was to characterize the carboxyl-terminal recycling motif of the ET(A) receptor. Assay of truncation mutan...

journal_title：Molecular pharmacology

authors： Paasche JD,Attramadal T,Kristiansen K,Oksvold MP,Johansen HK,Huitfeldt HS,Dahl SG,Attramadal H

更新日期：2005-05-01 00:00:00

abstract：:One-electron oxidation of several derivatives of pyrazolin-5-one, including the drug antipyrine, were studied by pulse radiolysis of aqueous solutions. All the compounds were found to be oxidized by Br2 rapidly (k approximately 3 X 10(8)-2 X 10(9) M-1 s-1) but considerably more slowly by weaker oxidants, such as perox...

journal_title：Molecular pharmacology

authors： Jovanovic SV,Neta P,Simic MG

更新日期：1985-10-01 00:00:00

abstract：:In the last years, reactive oxygen species (ROS) have been proposed as mediators of proliferative/hypertrophic responses to angiotensin II (Ang II), both in vivo and in vitro. However, the hypothesis that the Ang II-dependent cell contraction could be mediated by ROS, particularly H2O2, has not been tested. Present ex...

journal_title：Molecular pharmacology

authors： Torrecillas G,Boyano-Adánez MC,Medina J,Parra T,Griera M,López-Ongil S,Arilla E,Rodríguez-Puyol M,Rodríguez-Puyol D

更新日期：2001-01-01 00:00:00

abstract：:Thyrotropin-releasing hormone (TRH) receptors were solubilized from a rat pituitary tumor cell line, GH4C1, with digitonin. Convenient assays were developed based on the ability of hydroxylapatite and polyethyleneimine-soaked glass fiber filters to adsorb the solubilized [3H]methyl-TRH-receptor complex but not free [3...

journal_title：Molecular pharmacology

authors： Phillips WJ,Hinkle PM

更新日期：1989-04-01 00:00:00

abstract：:Lead (Pb(2+)) is a well-known inhibitor of voltage-dependent Ca(2+) channels in their native environments in several types of cells. However, its effects on discrete Ca(2+) channel phenotypes in isolation have not been well studied. We compared how specific subtypes of human neuronal high-voltage-activated Ca(2+) chan...

journal_title：Molecular pharmacology

authors： Peng S,Hajela RK,Atchison WD

更新日期：2002-12-01 00:00:00

abstract：:The flexible dopamine (DA) molecule exists in one or the other of its two conformational extremes (alpha- or beta-rotamer) and its receptor in the anterior pituitary gland exists in a high and a low affinity state. A series of novel, rigid DA congeners (2-substituted octahydrobenzo[f]quinolines) was synthesized and us...

journal_title：Molecular pharmacology

authors： Findell PR,Torkelson SM,Craig JC,Weiner RI

更新日期：1988-01-01 00:00:00

abstract：:Vinflunine, the newest fluorinated Vinca alkaloid, currently in phase III clinical trials, targets the microtubule network to induce mitotic block and apoptosis by mechanisms that remain unclear. In the current study, we investigated the apoptotic pathways induced by a wide range of vinflunine concentrations in SK-N-S...

journal_title：Molecular pharmacology

authors： Pourroy B,Carré M,Honoré S,Bourgarel-Rey V,Kruczynski A,Briand C,Braguer D

更新日期：2004-09-01 00:00:00

abstract：:A method was developed to measure the formation of glutathione adducts of 1-chloro-2,4-dinitrobenzene (CDNB) and 2,4-dichloro-1-nitrobenzene (DCNB) in periportal and pericentral regions of the liver lobule in the isolated perfused rat liver by surface reflectance spectrophotometry. Conjugates of DCNB and CDNB are rele...

journal_title：Molecular pharmacology

authors： Harris C,Thurman RG

更新日期：1986-01-01 00:00:00

abstract：:The pharmacological effects of angiotensin II (AII) are potently inhibited by several peptide and recently synthesized nonpeptide AII receptor antagonists. The interaction of sarcosine1, isoleucine8-AII (sarile), sarcosine1,O-methyltyrosine4-AII (sarmesin), and the nonpeptide AII antagonists 2-n-butyl-4-chloro-5- hydr...

journal_title：Molecular pharmacology

authors： Wienen W,Mauz AB,Van Meel JC,Entzeroth M

更新日期：1992-06-01 00:00:00

abstract：:Dysregulation of the chemokine system is implicated in a number of autoimmune and inflammatory diseases, as well as cancer. Modulation of chemokine receptor function is a very promising approach for therapeutic intervention. Despite interest from academic groups and pharmaceutical companies, there are currently few ap...

journal_title：Molecular pharmacology

authors： Bobkov V,Arimont M,Zarca A,De Groof TWM,van der Woning B,de Haard H,Smit MJ

更新日期：2019-12-01 00:00:00

abstract：:To identify novel factors or mechanisms that are important for the resistance of tissues to chemical toxicity, we have determined the mechanisms underlying the previously observed increases in resistance to acetaminophen (APAP) toxicity in the lateral nasal gland (LNG) of the male Cyp2g1-null/Cyp2a5-low mouse. Initial...

journal_title：Molecular pharmacology

authors： Zhou X,Wei Y,Xie F,Laukaitis CM,Karn RC,Kluetzman K,Gu J,Zhang QY,Roberts DW,Ding X

更新日期：2011-04-01 00:00:00

abstract：:N-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) induces Parkinson-like symptoms in humans, nonhuman primates, and mice. Several studies suggest that MPTP is metabolized by monoamine oxidase (MAO) type B to yield N-methyl-4-phenyl-pyridinium (MPP+), which is responsible for the neurotoxic effects of the drug. In th...

journal_title：Molecular pharmacology

authors： Itzhak Y,Mash D,Zhang SH,Stein I

更新日期：1991-03-01 00:00:00

abstract：:Adenine-uridine rich elements (AREs) play an important role in modulating mRNA stability, being the target site of many ARE-binding proteins (AUBPs) that are involved in the decay process. Three 26-mer 2'-O-methyl oligoribonucleotides (ORNs) homologous to the core region of ARE of bcl2 mRNA have been studied for decoy...

journal_title：Molecular pharmacology

authors： Bevilacqua A,Ghisolfi L,Franzi S,Maresca G,Gherzi R,Capaccioli S,Nicolin A,Canti G

更新日期：2007-02-01 00:00:00

abstract：:Rat liver and brain membrane alpha 1-adrenergic receptors were purified greater than 500-fold by successive chromatographic steps using heparin-agarose, an affinity matrix constructed by coupling a novel derivative of the alpha 1-selective antagonist prazosin to Affigel-102 and wheat germ agglutinin-agarose. Several l...

journal_title：Molecular pharmacology

authors： Terman BI,Riek RP,Grodski A,Hess HJ,Graham RM

更新日期：1990-04-01 00:00:00

abstract：:Diltiazem is a widely prescribed Ca2+ antagonist drug for cardiac arrhythmia, hypertension, and angina pectoris. Using the ancestral CaV channel construct CaVAb as a molecular model for X-ray crystallographic analysis, we show here that diltiazem targets the central cavity of the voltage-gated Ca2+ channel underneath ...

journal_title：Molecular pharmacology

authors： Tang L,Gamal El-Din TM,Lenaeus MJ,Zheng N,Catterall WA

更新日期：2019-10-01 00:00:00

abstract：:A cDNA encoding the human liver phenol-sulfating form of phenol sulfotransferase (P-PST) has been isolated and characterized from a lambda Uni-Zap XR human liver cDNA library. P-PST is the major form of phenol sulfotransferase involved in drug and xenobiotic metabolism in human liver. P-PST is also responsible for the...

journal_title：Molecular pharmacology

authors： Wilborn TW,Comer KA,Dooley TP,Reardon IM,Heinrikson RL,Falany CN

更新日期：1993-01-01 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：:The binding of [3H]quinuclidinyl benzilate ([3H]QNB) to cardiac muscarinic receptors was inhibited not only by classical muscarinic antagonists but also by nicotinic blocking agents and inhibitors of acetylcholinesterase. Gallamine, pancuronium, ambenonium, and decamethonium were the most potent of these agents examin...

journal_title：Molecular pharmacology

authors： Dunlap J,Brown JH

更新日期：1983-07-01 00:00:00

abstract：:Resveratrol (RES), a natural plant polyphenol, has gained interest as a nontoxic chemopreventive agent capable of inducing tumor cell death in a variety of cancer types. However, the early molecular mechanisms of RES-induced apoptosis are not well defined. Using the human breast cancer cell lines MDA-MB-231 and MCF-7,...

journal_title：Molecular pharmacology

authors： Sareen D,Darjatmoko SR,Albert DM,Polans AS

更新日期：2007-12-01 00:00:00

abstract：:Immune-mediated drug hypersensitivity reactions (IDHRs) represent a significant problem due to their unpredictable and severe nature, as well as the lack of understanding of the pathogenesis. Sulfamethoxazole (SMX), a widely used antibiotic, has been used as a model compound to investigate the underlying mechanism of ...

journal_title：Molecular pharmacology

authors： Cheng L,Stewart BJ,You Q,Petersen DR,Ware JA,Piccotti JR,Kawabata TT,Ju C

更新日期：2008-06-01 00:00:00

abstract：:The heptadecapeptide orphanin FQ (OFQ) has been identified as the endogenous ligand for a G protein-coupled receptor (OFQ-R), which, despite its high degree of sequence similarity to opioid receptors, fails to bind opioid ligands. We developed two radioligands for the OFQ-R: a tritiated native OFQ peptide ([3H]OFQ) an...

journal_title：Molecular pharmacology

authors： Ardati A,Henningsen RA,Higelin J,Reinscheid RK,Civelli O,Monsma FJ Jr

更新日期：1997-05-01 00:00:00

abstract：:Opioid drugs, such as morphine, and the endogenous opioid peptides, namely the enkephalins, endorphins, and dynorphins, exert a wide spectrum of physiological and behavioral effects, including effects on pain perception, mood, motor control, and autonomic functions. These effects are mediated via membrane-bound recept...

journal_title：Molecular pharmacology

authors： Raynor K,Kong H,Chen Y,Yasuda K,Yu L,Bell GI,Reisine T

更新日期：1994-02-01 00:00:00

abstract：:We describe the structural and functional features of the human alpha3 nicotinic receptor subunit promoter. A 0.35-kb region immediately upstream of the start codon was identified that when transfected in human neuroblastoma cells was able to drive the expression of the luciferase reporter gene with a strength compara...

journal_title：Molecular pharmacology

authors： Fornasari D,Battaglioli E,Flora A,Terzano S,Clementi F

更新日期：1997-02-01 00:00:00

abstract：:Activation of synthesis-modulating dopamine autoreceptors by dopamine or its agonists has been shown to inhibit dopamine synthesis in the rat striatum. However, systemic administration of the direct-acting dopamine agonist apomorphine failed to inhibit dopamine synthesis in striata from rats that had received local un...

journal_title：Molecular pharmacology

authors： Bean AJ,Shepard PD,Bunney BS,Nestler EJ,Roth RH

更新日期：1988-12-01 00:00:00

abstract：:The functional significance of the conserved amino acids within transmembrane regions II and VII of the human 5-hydroxytryptamine (5-HT)1A receptor was analyzed by oligonucleotide-directed mutagenesis followed by transient expression of the mutated receptor genes in COS-1 cells. The substitution of a conserved asparag...

journal_title：Molecular pharmacology

authors： Chanda PK,Minchin MC,Davis AR,Greenberg L,Reilly Y,McGregor WH,Bhat R,Lubeck MD,Mizutani S,Hung PP

更新日期：1993-04-01 00:00:00

abstract：:Cross-talk between G protein-coupled receptors and protein tyrosine kinases is well established, but the phenotypic consequences of these signaling interactions are not completely understood. To investigate the role of Src family kinases in mitogenic signaling by G protein-coupled receptors, we used genetic and pharma...

journal_title：Molecular pharmacology

authors： Mishra R,Wang Y,Simonson MS

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：:Effects of pimaric acid (PiMA) and eight closely related compounds on large-conductance K(+) (BK) channels were examined using human embryonic kidney (HEK) 293 cells, in which either the alpha subunit of BK channel (HEKBKalpha) or both alpha and beta1 (HEKBKalphabeta1) subunits were heterologously expressed. Effects o...

journal_title：Molecular pharmacology

authors： Imaizumi Y,Sakamoto K,Yamada A,Hotta A,Ohya S,Muraki K,Uchiyama M,Ohwada T

更新日期：2002-10-01 00:00:00

abstract：:K-252b, a member of the staurosporine family of protein kinase inhibitors, selectively potentiates the activation of the nerve growth factor receptor, TrkA, by a nonpreferred ligand, neurotrophin-3 (NT-3), in a variety of cell types. At higher (micromolar) concentrations of K-252b, an inhibitory effect occurs because ...

journal_title：Molecular pharmacology

authors： Pollack S,Young L,Bilsland J,Wilkie N,Ellis S,Hefti F,Broughton H,Harper S

更新日期：1999-07-01 00:00:00

abstract：:Sulfated polymannuroguluronate (SPMG) has entered the phase II clinical trial as the first anti-AIDS drug candidate in China. Herein, we report that SPMG was effective at protecting T lymphocytes against apoptosis. Further studies indicated that SPMG significantly elevated mitochondrial membrane potential (MMP) of T c...

journal_title：Molecular pharmacology

authors： Miao B,Li J,Fu X,Gan L,Xin X,Geng M

更新日期：2005-12-01 00:00:00