[3H]ethylketocyclazocine binding to NCB-20 hybrid neurotumor cells.

abstract：:Molecular cloning of the alpha 2A-adrenergic receptor has shown that this receptor is a member of the gene superfamily of guanine nucleotide-binding protein (G protein)-coupled receptors. The alpha 2A-adrenergic receptor expressed in Chinese hamster ovary (CHO) cells attenuates and potentiates forskolin-stimulated cAM...

journal_title：Molecular pharmacology

authors： Wang CD,Buck MA,Fraser CM

更新日期：1991-08-01 00:00:00

abstract：:Neurotrophins are a family of secreted proteins that play an important role in the development, differentiation, and survival of neurons. Studies also suggest that aberrant neurotrophin signaling may play a role in processes underlying disease states such as schizophrenia, Alzheimer's disease, and depression. Whereas ...

journal_title：Molecular pharmacology

authors： Lewis MA,Hunihan L,Franco D,Robertson B,Palmer J,Laurent DR,Balasubramanian BN,Li Y,Westphal RS

更新日期：2006-04-01 00:00:00

abstract：:The molecular determinants of high-affinity human ether-a-go-go-related gene (HERG) potassium channel blockade by methanesulfonanilides include two aromatic residues (Phe656 and Tyr652) on the inner helices (S6) and residues on the pore helices that face into the inner cavity, but determinants for lower-affinity HERG ...

journal_title：Molecular pharmacology

authors： Witchel HJ,Dempsey CE,Sessions RB,Perry M,Milnes JT,Hancox JC,Mitcheson JS

更新日期：2004-11-01 00:00:00

abstract：:The effect of mercuric acetate on the activities of deoxyuridine triphosphate nucleotidohydrolase (dUTPase), DNA polymerase (alpha, beta), and uracil-DNA glycosylase has been studied in cultured human KB cells. There was a dose- and time-dependent inactivation of both dUTPase and DNA polymerase alpha activities by mer...

journal_title：Molecular pharmacology

authors： Williams MV,Winters T,Waddell KS

更新日期：1987-02-01 00:00:00

abstract：:Autophagy is the process by which cellular material is delivered to lysosomes for degradation and recycling. There are three different types of autophagy, but macroautophagy, which involves the formation of double membrane vesicles that engulf proteins and organelles that fuse with lysosomes, is by far the most studie...

journal_title：Molecular pharmacology

authors： Thorburn A,Thamm DH,Gustafson DL

更新日期：2014-06-01 00:00:00

abstract：:In cervical cancer, the p53 and retinoblastoma (pRb) tumor suppressor pathways are disrupted by the human papilloma virus (HPV) E6 and E7 oncoproteins, because E6 targets p53 and E7 targets pRb for rapid proteasome-mediated degradation. We have investigated whether E6 suppression with small interfering RNA (siRNA) res...

journal_title：Molecular pharmacology

authors： Tan S,Hougardy BM,Meersma GJ,Schaap B,de Vries EG,van der Zee AG,de Jong S

更新日期：2012-05-01 00:00:00

abstract：:2-Methyl-2-nitrosopropane (MNP) has long been known to undergo photochemical and thermal decomposition, generating di-tert-butyl nitroxide, in organic solvent. The present study was undertaken to demonstrate that MNP can be used as a caged-nitric oxide (NO), which can liberate NO upon illumination. Photolysis of MNP l...

journal_title：Molecular pharmacology

authors： Pou SJ,Anderson DE,Surichamorn W,Keaton LL,Tod ML

更新日期：1994-10-01 00:00:00

abstract：:The CYP2C genes are extensively regulated at the transcriptional stage. The present study shows for the first time that CYP2Cs are also regulated post-transcriptionally by microRNAs (miRNAs). By using online search engines, we found potential miRNA response elements (MREs) in the 3'-untranslated region (3'-UTR) of the...

journal_title：Molecular pharmacology

authors： Zhang SY,Surapureddi S,Coulter S,Ferguson SS,Goldstein JA

更新日期：2012-09-01 00:00:00

abstract：:The present study was conducted to establish a pharmacological method of controlling growth of vascular smooth muscle cells (VSMC) by blocking calcium entry. In cultured rat VSMC, 1 nM platelet-derived growth factor (PDGF) induced a biphasic elevation of cytoplasmic free calcium concentration, ([Ca2+]c). The second su...

journal_title：Molecular pharmacology

authors： Nie L,Mogami H,Kanzaki M,Shibata H,Kojima I

更新日期：1996-10-01 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：:The renal outer medullary potassium channel (ROMK) is expressed in the kidney tubule and critically regulates sodium and potassium balance. The physiological functions of other inward rectifying K(+) (Kir) channels expressed in the nephron, such as Kir7.1, are less well understood in part due to the lack of selective ...

journal_title：Molecular pharmacology

authors： Lewis LM,Bhave G,Chauder BA,Banerjee S,Lornsen KA,Redha R,Fallen K,Lindsley CW,Weaver CD,Denton JS

更新日期：2009-11-01 00:00:00

abstract：:Cell-penetrating peptides are amphipathic or cationic oligopeptides able to transport covalently attached cargoes across cell membranes. Peptide aptamers are polypeptide fragments of endogenous proteins that mimic and thus perturb interactions with other cellular proteins. Combining aptamer and CPP technology can gene...

journal_title：Molecular pharmacology

authors： Eiden LE

更新日期：2005-04-01 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：: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

abstract：:We have studied the mechanism of action of Arg(*)-Arg-Nal(2)-Cys(1x)-Tyr-Gln-Lys-(d-Pro)-Pro-Tyr-Arg-Cit-Cys(1x)-Arg-Gly-(d-Pro)(*) (POL3026), a novel specific beta-hairpin mimetic CXC chemokine receptor (CXCR)4 antagonist. POL3026 specifically blocked the binding of anti-CXCR4 monoclonal antibody 12G5 and the intrace...

journal_title：Molecular pharmacology

authors： Moncunill G,Armand-Ugón M,Clotet-Codina I,Pauls E,Ballana E,Llano A,Romagnoli B,Vrijbloed JW,Gombert FO,Clotet B,De Marco S,Esté JA

更新日期：2008-04-01 00:00:00

abstract：:Seven transmembrane G protein-coupled receptors (GPCRs) are often phosphorylated at the C terminus and on intracellular loops in response to various extracellular stimuli. Phosphorylation of GPCRs by GPCR kinases and certain other kinases can promote the recruitment of arrestin molecules. The arrestins critically regu...

journal_title：Molecular pharmacology

authors： Yang Z,Yang F,Zhang D,Liu Z,Lin A,Liu C,Xiao P,Yu X,Sun JP

更新日期：2017-09-01 00:00:00

abstract：:Very few antagonists have been identified for the human pregnane X receptor (PXR). These molecules may be of use for modulating the effects of therapeutic drugs, which are potent agonists for this receptor (e.g., some anticancer compounds and macrolide antibiotics), with subsequent effects on transcriptional regulatio...

journal_title：Molecular pharmacology

authors： Ekins S,Kholodovych V,Ai N,Sinz M,Gal J,Gera L,Welsh WJ,Bachmann K,Mani S

更新日期：2008-09-01 00:00:00

abstract：:Retroviral integrases are essential for viral replication and represent an attractive chemotherapeutic target. In the current study, we demonstrated the activity of micromolar concentrations of dinucleotides against human immunodeficiency virus type 1 (HIV-1), HIV type 2 (HIV-2), simian immunodeficiency virus, and fel...

journal_title：Molecular pharmacology

authors： Mazumder A,Uchida H,Neamati N,Sunder S,Jaworska-Maslanka M,Wickstrom E,Zeng F,Jones RA,Mandes RF,Chenault HK,Pommier Y

更新日期：1997-04-01 00:00:00

abstract：:Two different mechanisms leading to increased current have been described for the small-molecule human ether-à-go-go-related gene (herg) activator NS1643 [1,3-bis-(2-hydroxy-5-trifluoromethylphenyl)-urea]. On herg1a channels expressed in Xenopus laevis oocytes, it mainly acts via attenuation of inactivation and for ra...

journal_title：Molecular pharmacology

authors： Schuster AM,Glassmeier G,Bauer CK

更新日期：2011-11-01 00:00:00

abstract：:G protein-coupled receptor (GPCR) kinases (GRKs) play a key role in terminating signals initiated by agonist-bound GPCRs. However, chronic stimulation of GPCRs, such as that which occurs during heart failure, leads to the overexpression of GRKs and maladaptive downregulation of GPCRs on the cell surface. We previously...

journal_title：Molecular pharmacology

authors： Bouley RA,Weinberg ZY,Waldschmidt HV,Yen YC,Larsen SD,Puthenveedu MA,Tesmer JJG

更新日期：2020-06-01 00:00:00

abstract：:Nafazatrom, an antithrombotic and antimetastatic agent containing a pyrazolone functionality, is a reducing substrate for the peroxidase activity of prostaglandin H (PGH) synthase. Nafazatrom inhibits the hydroperoxide-dependent oxidation of phenylbutazone, stimulates the reduction of 15-hydroperoxy-5,8,11,13-eicosate...

journal_title：Molecular pharmacology

authors： Marnett LJ,Siedlik PH,Ochs RC,Pagels WR,Das M,Honn KV,Warnock RH,Tainer BE,Eling TE

更新日期：1984-09-01 00:00:00

abstract：:The firmest candidate among the transmembrane portions of the nicotinic acetylcholine receptor (AChR) to be in contact with the lipid bilayer is the fourth segment, M4. To explore the contribution of alphaM4 amino acid residues of mouse AChR to channel gating, we combined site-directed mutagenesis with single-channel ...

journal_title：Molecular pharmacology

authors： Bouzat C,Roccamo AM,Garbus I,Barrantes FJ

更新日期：1998-07-01 00:00:00

abstract：:Ligands that selectively inhibit human α3β2 and α6β2 nicotinic acetylcholine receptor (nAChRs) and not the closely related α3β4 and α6β4 subtypes are lacking. Current α-conotoxins (α-Ctxs) that discriminate among these nAChR subtypes in rat fail to discriminate among the human receptor homologs. In this study, we desc...

journal_title：Molecular pharmacology

authors： Hone AJ,McIntosh JM,Azam L,Lindstrom J,Lucero L,Whiteaker P,Passas J,Blázquez J,Albillos A

更新日期：2015-11-01 00:00:00

abstract：:In an attempt to better understand the role of the cyclohexene ring (ring A) in the biochemical and pharmacological properties of anthracyclines related to doxorubicin and daunorubicin, we investigated the effects of introduction of a fluorine atom at position 8 of idarubicin (4-demethoxydaunorubicin) on drug molecula...

journal_title：Molecular pharmacology

authors： Animati F,Arcamone F,Bigioni M,Capranico G,Caserini C,De Cesare M,Lombardi P,Pratesi G,Salvatore C,Supino R,Zunino F

更新日期：1996-09-01 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 aryl hydrocarbon receptor (AhR) is a transcriptional enhancer that is activated by the binding of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) and related toxic xenobiotics, as well as some naturally occurring compounds. Ligand binding initiates 1) dissociation of the ligand-bound monomeric AhR from the ligand-unocc...

journal_title：Molecular pharmacology

authors： Henry EC,Rucci G,Gasiewicz TA

更新日期：1994-12-01 00:00:00

abstract：:Microinjection, but not extracellular application, of cytidine-5'-diphosphate-D-glucose (CDPG) has been shown to elicit Ca(2+)-dependent currents in Xenopus laevis oocytes. These responses were comparable to those of inositol-1,4,5-trisphosphate (InsP3) in being both rapid and dose dependent. For example, maximal ampl...

journal_title：Molecular pharmacology

authors： Kim HY,Thomas D,Hanley MR

更新日期：1996-02-01 00:00:00

abstract：:The aliphatic adenine analogues, D-eritadenine, L-eritadenine, L-threoeritadenine, and 9-(S)-(2,3-dihydroxypropyl)adenine [(S)DHPA] function as inhibitors/inactivators of purified S-adenosylhomocysteine (AdoHcy) hydrolase, but these compounds did not induce reduction of enzyme-bound NAD+. D-Eritadenine, L-eritadenine,...

journal_title：Molecular pharmacology

authors： Schanche JS,Schanche T,Ueland PM,Holý A,Votruba I

更新日期：1984-11-01 00:00:00

abstract：:The in vitro binding of [3H]LY354740, the first high affinity group II-selective metabotropic glutamate (mGlu) receptor radioligand, was characterized in rat cortical, hippocampal, and thalamic membranes as well as in rat brain sections. [3H]LY354740 binding was saturable in all regions investigated. Nonspecific bindi...

journal_title：Molecular pharmacology

authors： Schaffhauser H,Richards JG,Cartmell J,Chaboz S,Kemp JA,Klingelschmidt A,Messer J,Stadler H,Woltering T,Mutel V

更新日期：1998-02-01 00:00:00

abstract：:Thiourea, phenylthiourea, and methimazole perfused into rat liver stimulated the biliary efflux of GSSG without affecting the excretion of GSH into either the bile or the caval perfusate. The thiocarbamide moiety appears essential, since perfusion with urea, phenylurea, or N-methylimidazole did not stimulate GSSG rele...

journal_title：Molecular pharmacology

authors： Krieter PA,Ziegler DM,Hill KE,Burk RF

更新日期：1984-07-01 00:00:00