Characterization of an NBS1 C-terminal peptide that can inhibit ataxia telangiectasia mutated (ATM)-mediated DNA damage responses and enhance radiosensitivity.

abstract：:In this study, we investigated the effects of single alanine substitutions of amino acid residues in the supposed ATP binding site of the human P2X3 receptor on the agonistic effect of nucleotide analogs. The wild-type and mutant receptors were expressed in HEK293 cells, and the nucleotide effects were measured by mea...

journal_title：Molecular pharmacology

authors： Riedel T,Wiese S,Leichsenring A,Illes P

更新日期：2012-07-01 00:00:00

abstract：:The pharmacological preservation of bone in the ovariectomized rat by estrogen, selective estrogen receptor modulators (SERMs), and bisphosphonates has been well described. However, comprehensive molecular analysis of the effects of these pharmacologically diverse antiresorptive agents on gene expression in bone has n...

journal_title：Molecular pharmacology

authors： Helvering LM,Liu R,Kulkarni NH,Wei T,Chen P,Huang S,Lawrence F,Halladay DL,Miles RR,Ambrose EM,Sato M,Ma YL,Frolik CA,Dow ER,Bryant HU,Onyia JE

更新日期：2005-11-01 00:00:00

abstract：:Nitric oxide (NO) promotes retinal and choroidal neovascularization, although different isoforms of nitric-oxide synthetase (NOS) are critical in each. Deficiency of endothelial NOS (eNOS) suppresses retinal but not choroidal neovascularization, whereas deficiency of neuronal NOS (nNOS) or inducible NOS (iNOS) suppres...

journal_title：Molecular pharmacology

authors： Ando A,Yang A,Nambu H,Campochiaro PA

更新日期：2002-09-01 00:00:00

abstract：:We used transcript-specific oligonucleotides to examine the localization in the rat nervous system of the corresponding mRNAs for the two P2X purinoceptor genes cloned recently from the rat vas deferens and PC12 cells. PC12 P2X purinoceptor mRNA was labeled in the olfactory tubercle, striatum, hypothalamus, hippocampu...

journal_title：Molecular pharmacology

authors： Kidd EJ,Grahames CB,Simon J,Michel AD,Barnard EA,Humphrey PP

更新日期：1995-10-01 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：:Dysfunction of p53 and resistance to cancer drugs can arise through mutually exclusive overexpression of MDM2 or MDM4. Cisplatin-resistant cells, however, can demonstrate increased binding of both MDM2 and MDM4 to p53 but in absence of cellular overexpression. Whether MDM2 inhibitors alone can activate p53 in these re...

journal_title：Molecular pharmacology

authors： Xie X,He G,Siddik ZH

更新日期：2020-04-01 00:00:00

abstract：:Mechanistic studies are presented of a novel class of aminophosphine platinum(II) complexes as potential anticancer agents. These new agents, which have demonstrated activity against murine and human tumor cells including those resistant to cisplatin are cis-[PtCl2(Me2N(CH2)3PPh2-P)2] (Com1) and cis-[PtCl(C6H11NH(CH2)...

journal_title：Molecular pharmacology

authors： Neplechová K,Kaspárková J,Vrána O,Nováková O,Habtemariam A,Watchman B,Sadler PJ,Brabec V

更新日期：1999-07-01 00:00:00

abstract：:Bitopic binding properties apply to a variety of muscarinic compounds that span and simultaneously bind to both the orthosteric and allosteric receptor sites. We provide evidence that fluorescent pirenzepine derivatives, with the M1 antagonist fused to the boron-dipyrromethene [Bodipy (558/568)] fluorophore via spacer...

journal_title：Molecular pharmacology

authors： Daval SB,Kellenberger E,Bonnet D,Utard V,Galzi JL,Ilien B

更新日期：2013-07-01 00:00:00

abstract：:Differential display reverse transcription-polymerase chain reaction was used to identify mRNAs that are differentially expressed in the brain of rats treated chronically with the reference tricyclic antidepressant, imipramine, in comparison with control rats. The gene encoding for a mutation suppressor for Sec4-8 yea...

journal_title：Molecular pharmacology

authors： Andriamampandry C,Muller C,Schmidt-Mutter C,Gobaille S,Spedding M,Aunis D,Maitre M

更新日期：2002-12-01 00:00:00

abstract：:The aim of this study was to clarify the mechanism by which cytochrome P450 (P450)-mediated catalytic activity is decreased following interferon (IFN) administration. Microsomal steroid hydroxylation was assessed to test the hypothesis that IFN selectively decreases the activities of individual P450 isozymes in male r...

journal_title：Molecular pharmacology

authors： Craig PI,Mehta I,Murray M,McDonald D,Aström A,van der Meide PH,Farrell GC

更新日期：1990-09-01 00:00:00

abstract：:To determine the role of C-Rel in nitric-oxide synthase-2 (NOS-2) transcriptional activation, we evaluated the effect of lipopolysaccharide and interferon-gamma (LPS/IFNgamma) on C-Rel DNA binding in RAW 264.7. LPS/IFNgamma-stimulated C-Rel binding peaked at 4 to 8 h and declined at 24 h. Transfection of cells with a ...

journal_title：Molecular pharmacology

authors： Cieslik KA,Deng WG,Wu KK

更新日期：2006-12-01 00:00:00

abstract：:2-Hydroxy-4(-2,2,3,3,3-pentafluoropropoxy)-benzoic acid (UR-1505), a new molecule chemically related to salicylic acid, has immunomodulator properties and is currently under clinical development for treatment of atopic dermatitis. The present work describes the immunomodulatory profile of UR-1505. UR-1505 targets T ce...

journal_title：Molecular pharmacology

authors： Román J,de Arriba AF,Barrón S,Michelena P,Giral M,Merlos M,Bailón E,Comalada M,Gálvez J,Zarzuelo A,Ramis I

更新日期：2007-08-01 00:00:00

abstract：:Dynamin is a GTPase enzyme involved in membrane constriction and fission during endocytosis. Phospholipid binding via its pleckstrin homology domain maximally stimulates dynamin activity. We developed a series of surface-active small-molecule inhibitors, such as myristyl trimethyl ammonium bromide (MiTMAB) and octadec...

journal_title：Molecular pharmacology

authors： Quan A,McGeachie AB,Keating DJ,van Dam EM,Rusak J,Chau N,Malladi CS,Chen C,McCluskey A,Cousin MA,Robinson PJ

更新日期：2007-12-01 00:00:00

abstract：:We have investigated the effect of chronic flurazepam HCl treatment on the gamma-aminobutyric acid (GABA)A receptor complex in cultured mammalian cortical neurons. Chronic flurazepam (1-5 microM, for 1-10 days) treatment did not produce any changes in the morphological appearance or the cell protein content of cortica...

journal_title：Molecular pharmacology

authors： Hu XJ,Ticku MK

更新日期：1994-04-01 00:00:00

abstract：:Melanocortins (MCs) have various physiological actions on the brain. The recent cloning of neural MC receptors opened new avenues to study the effects of these neuropeptides on the nervous system. Here we investigated the structure-activity relationships (SARs) of peptides derived from adrenocorticotropic hormone (ACT...

journal_title：Molecular pharmacology

authors： Adan RA,Cone RD,Burbach JP,Gispen WH

更新日期：1994-12-01 00:00:00

abstract：:3H-Neurokinin A (3H-NKA) with high specific activity (75 Ci/mmol) was synthesized to study NKA (NK-2)-binding sites on membrane preparations of various tissues in the rat, including brain, spinal cord, duodenum, vas deferens, and ileum. The binding capacity of 3H-NKA (0.9 nM) was very low in membrane preparations of d...

journal_title：Molecular pharmacology

authors： Bergström L,Beaujouan JC,Torrens Y,Saffroy M,Glowinski J,Lavielle S,Chassaing G,Marquet A,D'Orleans-Juste P,Dion S

更新日期：1987-12-01 00:00:00

abstract：:Recent studies from our laboratory have provided evidence that multiple states of the phencyclidine (PCP) receptor exist. In addition, several compounds such as PCP and the novel anticonvulsant MK-801 were found to inhibit binding more potently in the presence of Mg2+ and L-glutamate (L-GLU) than when these agents wer...

journal_title：Molecular pharmacology

authors： Sills MA,Loo PS

更新日期：1989-07-01 00:00:00

abstract：:The Notch family consists of four highly conserved transmembrane receptors. The release of the active intracellular domain requires the enzymatic activity of γ-secretase. Notch is involved in embryonic development and in many physiologic processes of normal cells, in which it regulates growth, apoptosis, and different...

journal_title：Molecular pharmacology

authors： Gharaibeh L,Elmadany N,Alwosaibai K,Alshaer W

更新日期：2020-11-01 00:00:00

abstract：:The phenylalkylamine emopamil prevents brain damage due to experimental cerebral ischemia. Stereoselective, high affinity, binding sites for (-)-[3H]emopamil in guinea pig brain cortex and liver membranes have been proposed to mediate its antiischemic effect. Using [N-methyl-3H]LU49888 as a photoaffinity probe we now ...

journal_title：Molecular pharmacology

authors： Moebius FF,Burrows GG,Striessnig J,Glossmann H

更新日期：1993-02-01 00:00:00

abstract：:Mitochondria contain specific Ca2+ antagonist binding sites that are associated with an inner mitochondrial membrane anion channel. These mitochondrial Ca2+ antagonist receptors can be solubilized with digitonin and partially purified [as assessed by postreversible (+/-)-[3H]nitrendipine binding] using ion exchange ch...

journal_title：Molecular pharmacology

authors： Zernig G

更新日期：1992-12-01 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：: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：:The bisdioxopiperazines such as (+)-(S)-4,4'-propylenedi-2,6-piperazinedione (dexrazoxane; ICRF-187), 1,2-bis(3,5-dioxopiperazin-1-yl)ethane (ICRF-154), and 4,4'-(1,2-dimethyl-1,2-ethanediyl)bis-2,6-piperazinedione (ICRF-193) are agents that inhibit eukaryotic topoisomerase II, whereas their ring-opened hydrolysis pro...

journal_title：Molecular pharmacology

authors： Grauslund M,Thougaard AV,Füchtbauer A,Hofland KF,Hjorth PH,Jensen PB,Sehested M,Füchtbauer EM,Jensen LH

更新日期：2007-10-01 00:00:00

abstract：:Undesired block of human ERG1 potassium channels is the basis for cardiac side effects of many different types of drugs. Therefore, it is important to know exactly why some drugs particularly bind to these channels with high affinity. Upon expression in mammalian cells and Xenopus laevis oocytes, we investigated the i...

journal_title：Molecular pharmacology

authors： Gessner G,Zacharias M,Bechstedt S,Schönherr R,Heinemann SH

更新日期：2004-05-01 00:00:00

abstract：:The dopamine (DA) transporter (DAT) mediates the removal of released DA. DAT is the major molecular target responsible for the rewarding properties and abuse potential of the psychostimulant amphetamine (AMPH). AMPH has been shown to reduce the number of DATs at the cell surface, and this AMPH-induced cell surface DAT...

journal_title：Molecular pharmacology

authors： Kahlig KM,Lute BJ,Wei Y,Loland CJ,Gether U,Javitch JA,Galli A

更新日期：2006-08-01 00:00:00

abstract：:NAD(P):quinone acceptor oxidoreductase (quinone reductase) (DT-diaphorase, EC 1.6.99.2) is involved in the process of reductive activation of cytotoxic antitumor quinones and nitrobenzenes. In this study, we initially examined the relative abilities of mouse, rat, and human quinone reductases to reduce two prodrugs, C...

journal_title：Molecular pharmacology

authors： Chen S,Knox R,Lewis AD,Friedlos F,Workman P,Deng PS,Fung M,Ebenstein D,Wu K,Tsai TM

更新日期：1995-05-01 00:00:00

abstract：:We studied the ability of norepinephrine to stimulate [3H]inositol trisphosphate production and calcium mobilization in rat-1 fibroblasts stably expressing the cloned alpha 1-adrenergic subtypes and their sensitivity to phorbol-12-myristate-13-acetate (PMA). It was observed that the three subtypes were able to activat...

journal_title：Molecular pharmacology

authors： Vázquez-Prado J,García-Sáinz JA

更新日期：1996-07-01 00:00:00

abstract：:The level of cellular ceramide, an apoptotic rheostat, is increased by sphingomyelinase or de novo synthesis. The expression of the glutathione S-transferase (GST) gene, whose induction accounts for cell viability, is regulated by activation of CCAAT/enhancer binding protein-beta (C/EBPbeta) and NF-E2-related factor-2...

journal_title：Molecular pharmacology

authors： Park IN,Cho IJ,Kim SG

更新日期：2004-06-01 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：:Glucose utilization in isolated islets of Langerhans of the rat was determined by measuring the conversion of [5-3H]glucose (10 mM) to 3H2O. The alpha 2-adrenoceptor agonists clonidine, epinephrine, and norepinephrine in the presence of the alpha 1-adrenoceptor antagonist prazosin and the beta-adrenoceptor antagonist ...

journal_title：Molecular pharmacology

authors： Laychock SG

更新日期：1987-08-01 00:00:00