Molecular basis of pimarane compounds as novel activators of large-conductance Ca(2+)-activated K(+) channel alpha-subunit.

abstract：:Aldehyde hydrogenases (ALDHs) belong to a large gene family involved in oxidation of both endogenous and exogenous compounds in mammalian tissues. Among ALDHs, the rat ALDH1A7 gene displays a curious strain dependence in phenobarbital (PB)-induced hepatic expression: the responsive RR ...

journal_title：Molecular pharmacology

authors： Touloupi K,Küblbeck J,Magklara A,Molnár F,Reinisalo M,Konstandi M,Honkakoski P,Pappas P

更新日期：2019-11-01 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：:Schizophrenia (SZ), schizoaffective (SZA), and bipolar (BP) disorder are neurodevelopmental psychopathological conditions related, in part, to genetic load and, in part, to environmentally induced epigenetic dysregulation of chromatin structure and function in neocortical GABAergic, glutamatergic, and monoaminergic ne...

journal_title：Molecular pharmacology

authors： Dong E,Locci V,Gatta E,Grayson DR,Guidotti A

更新日期：2019-01-01 00:00:00

abstract：:Stimulation of alpha1-adrenoreceptors (alpha1-AR) acutely alters ion channel behavior via several signaling pathways [calcium and protein kinase C (PKC)]. Little is known about sustained alpha1-adrenergic/PKC signaling and channel regulation as may occur during cardiovascular disease states. Here we describe the effec...

journal_title：Molecular pharmacology

authors： Chen J,Chen K,Sroubek J,Wu ZY,Thomas D,Bian JS,McDonald TV

更新日期：2010-08-01 00:00:00

abstract：:[3H]Dihydroalprenolol ([3H]DHA) has been used extensively in receptor binding studies to measure beta-adrenergic receptors in the central nervous system. Usually, nonspecific binding has been defined by high concentrations of the beta-adrenergic receptor agonist isoproterenol or antagonists such as alprenolol or propr...

journal_title：Molecular pharmacology

authors： Riva MA,Creese I

更新日期：1989-07-01 00:00:00

abstract：:It is widely accepted that cAMP signaling is compartmentalized within cells. However, our knowledge of how receptors, cAMP signaling enzymes, effectors, and other key proteins form specific signaling complexes to regulate specific cell responses is limited. The multicomponent nature of these systems and the spatiotemp...

journal_title：Molecular pharmacology

authors： Johnstone TB,Agarwal SR,Harvey RD,Ostrom RS

更新日期：2018-04-01 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 role of protein kinase C (PKC) in the human aryl hydrocarbon receptor (hAhR) signal transduction pathway was examined in cell lines stably transfected with pGUDLUC6.1, in which luc+ is solely controlled by four dioxin-responsive elements (DREs). These cell lines, P5A11 and HG40/6, were derived from HeLa and HepG2 ...

journal_title：Molecular pharmacology

authors： Long WP,Pray-Grant M,Tsai JC,Perdew GH

更新日期：1998-04-01 00:00:00

abstract：:Controlled inhibition of brain acetyl- and butyrylcholinesterases (AChE and BChE, respectively) and of monoamine oxidase-B (MAO-B) may slow neurodegeneration in Alzheimer's and Parkinson's diseases. It was postulated that certain carbamate esters would inhibit AChE and BChE with the concomitant release in the brain of...

journal_title：Molecular pharmacology

authors： Groner E,Ashani Y,Schorer-Apelbaum D,Sterling J,Herzig Y,Weinstock M

更新日期：2007-06-01 00:00:00

abstract：:In an effort to combine the benefits of fibrinolytics, such as staphylokinase, with those of thrombin inhibitors for the prevention of vessel reocclusion after vascular injury, we have produced several chimeric proteins with plasminogen-activating and thrombin-inhibiting properties. Fusion proteins were constructed co...

journal_title：Molecular pharmacology

authors： Icke C,Schlott B,Ohlenschläger O,Hartmann M,Gührs KH,Glusa E

更新日期：2002-08-01 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：: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：: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：:To study the molecular pharmacology of low-voltage-activated calcium channels in biophysical detail, human medullary thyroid carcinoma (hMTC) cells were investigated using the single-channel technique. These cells had been reported to express T-type whole-cell currents and a Ca(v)3.2 (or alpha 1H) channel subunit. We ...

journal_title：Molecular pharmacology

authors： Michels G,Matthes J,Handrock R,Kuchinke U,Groner F,Cribbs LL,Pereverzev A,Schneider T,Perez-Reyes E,Herzig S

更新日期：2002-03-01 00:00:00

abstract：:Beta-L-dioxolane-cytidine (L-OddC, BCH-4556, Troxacitabine), a novel L-configuration deoxycytidine analog, is under phase III clinical trial for cancer treatment. We showed that human apurinic/apyrimidinic endonuclease (APE-1) has exonuclease activity for preferentially removing L-OddC and other L-configuration nucleo...

journal_title：Molecular pharmacology

authors： Lam W,Park SY,Leung CH,Cheng YC

更新日期：2006-05-01 00:00:00

abstract：:The gene encoding a human 5-hydroxytryptamine (5-HT)1 receptor subtype was isolated from a human placental genomic library by using oligonucleotide probes derived from transmembrane regions of the cloned human 5-HT1D beta receptor. The deduced amino acid sequence of the genomic clone hp75d is identical to that of the ...

journal_title：Molecular pharmacology

authors： Zgombick JM,Schechter LE,Macchi M,Hartig PR,Branchek TA,Weinshank RL

更新日期：1992-08-01 00:00:00

abstract：:To screen for residues of hKv1.3 important for current block by the phenylalkylamine verapamil, the inactivated-state-reduced H399T mutant was used as a background for mutagenesis studies. This approach was applied mainly to abolish the accumulation in the inactivated blocked state, recovery from which in the wild typ...

journal_title：Molecular pharmacology

authors： Dreker T,Grissmer S

更新日期：2005-10-01 00:00:00

abstract：:Expression of the angiotensin II type 1 receptor (AT1-R) mRNA in vascular smooth muscle cells (VSMC) is down-regulated by a variety of agonists, including growth factors, agonists of Galphaq protein-coupled receptors, and activators of adenylyl cyclase. To determine whether cAMP-dependent protein kinases (PKA) partici...

journal_title：Molecular pharmacology

authors： Wang X,Murphy TJ

更新日期：1998-09-01 00:00:00

abstract：:When expressed via an inducible promoter in human embryonic kidney 293 cells, the rat Mas-related gene D (rMrgD) receptor responded to beta-alanine but not L-alanine by elevating intracellular [Ca(2+)], stimulating phosphorylation of the mitogenactivated protein kinases known as extracellular signal-regulated kinase (...

journal_title：Molecular pharmacology

authors： Milasta S,Pediani J,Appelbe S,Trim S,Wyatt M,Cox P,Fidock M,Milligan G

更新日期：2006-02-01 00:00:00

abstract：:A recently isolated monoclonal antibody was found to be a potent and powerful inhibitor of the catalytic activity of rabbit brain acetylcholinesterase (AChE; acetylcholine acetylhydrolase, EC 3.1.1.7), with an IC50 of about 1 nM and a maximal inhibition of at least 90%. The antibody increased the optimal concentration...

journal_title：Molecular pharmacology

authors： Brimijoin S,Mintz KP,Prendergast FG

更新日期：1985-12-01 00:00:00

abstract：:Two peptides, which have no significant homology with known protein structures, were obtained by microsequencing of a mu-opioid binding protein purified to homogeneity from bovine striatal membranes. Polyclonal antibodies generated against portions of these peptides immunoprecipitated up to 65% of radiolabeled purifie...

journal_title：Molecular pharmacology

authors： Gioannini TL,Yao YH,Hiller JM,Taylor LP,Simon EJ

更新日期：1993-10-01 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：:PDE4A11 is a novel cAMP-specific phosphodiesterase that is conserved in humans, mouse, rat, pig, and bat. Exon-1(4A11) encodes its unique, 81 amino acid N-terminal region. Reverse-transcriptase polymerase chain reaction performed across the splice junction, plus identification of expressed sequence tags, identifies PD...

journal_title：Molecular pharmacology

authors： Wallace DA,Johnston LA,Huston E,MacMaster D,Houslay TM,Cheung YF,Campbell L,Millen JE,Smith RA,Gall I,Knowles RG,Sullivan M,Houslay MD

更新日期：2005-06-01 00:00:00

abstract：:The mechanism underlying the crosstalk between multiple G protein-coupled receptors remains poorly understood. We previously reported that prostaglandin E receptor EP1 facilitates dopamine D1 receptor signaling in striatal slices and promotes behavioral responses induced by D1 receptor agonists. Here, using human embr...

journal_title：Molecular pharmacology

authors： Ehrlich AT,Furuyashiki T,Kitaoka S,Kakizuka A,Narumiya S

更新日期：2013-09-01 00:00:00

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：:Consequent to agonist exposure, many G protein-coupled receptors undergo sequestration or internalization. Results with receptors linked to adenylate cyclase, such as the beta 2-adrenergic receptor, or receptors linked to phospholipase C (PLC) have provided conflicting results regarding the role of second messenger-de...

journal_title：Molecular pharmacology

authors： Benya RV,Akeson M,Mrozinski J,Jensen RT,Battey JF

更新日期：1994-09-01 00:00:00

abstract：:15-Deoxy delta(12,14)-prostaglandin J(2) (15d-PGJ(2)), an activator of peroxisome proliferator-activated receptor (PPAR)-gamma and -delta, is a prostanoid metabolite with anti-inflammatory actions. In intrauterine tissues, proinflammatory cytokines and prostaglandins have been identified as playing key roles in the ma...

journal_title：Molecular pharmacology

authors： Berry EB,Keelan JA,Helliwell RJ,Gilmour RS,Mitchell MD

更新日期：2005-07-01 00:00:00

abstract：:Adenosine acting via A2a receptors (A2aR) is a potent cerebral vasodilator that relaxes vascular smooth muscle cells (VSMCs) by a mechanism attributed to activation of cAMP-dependent protein kinase (cAK). We examined effects of adenosine and its mechanism of action on L-type Ca2+ channels in native VSMCs from rat basi...

journal_title：Molecular pharmacology

authors： Murphy K,Gerzanich V,Zhou H,Ivanova S,Dong Y,Hoffman G,West GA,Winn HR,Simard JM

更新日期：2003-09-01 00:00:00

abstract：:The relationship between the phospholipase-stimulating and immunosuppressive properties of cyclosporin A (CsA) has been investigated in vitro. At concentrations of 0.025 microM and upwards, CsA caused dose-related inhibition of both mitogen- and alloantigen-stimulated uptake of tritiated thymidine by human mononuclear...

journal_title：Molecular pharmacology

authors： Anderson R,Smit MJ,Van Rensburg CE

更新日期：1993-09-01 00:00:00

abstract：:We show here that arsenite (As(3+)) elicits multiple effects on gene control, such as the interruption of cell cycle control by initiating G(2)/M arrest as well as inhibiting the aryl hydrocarbon (Ah) receptor-mediated 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD)-inducible expression of CYP1A1. This raises the question ...

journal_title：Molecular pharmacology

authors： Bonzo JA,Chen S,Galijatovic A,Tukey RH

更新日期：2005-04-01 00:00:00