Stabilization of cellular mRNAs and up-regulation of proteins by oligoribonucleotides homologous to the Bcl2 adenine-uridine rich element motif.

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：:Avermectins are a family of potent broad-spectrum anthelmintic compounds, which bind with high affinity to membranes isolated from the free-living nematode Caenorhabditis elegans. Binding of avermectins is thought to modulate chloride channel activity, but the exact mechanism for anthelmintic activity remains to be de...

journal_title：Molecular pharmacology

authors： Arena JP,Liu KK,Paress PS,Cully DF

更新日期：1991-09-01 00:00:00

abstract：:The neuropeptides vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase-activating peptide (PACAP) and their class II G protein-coupled receptors VPAC(1), VPAC(2), and PAC(1) play important roles in human physiology. No small molecule modulator has ever been reported for the VIP/PACAP receptors, and ther...

journal_title：Molecular pharmacology

authors： Chu A,Caldwell JS,Chen YA

更新日期：2010-01-01 00:00:00

abstract：:Bufuralol 1'-hydroxylation is a prototypical reaction catalyzed by cytochrome P450 (P450) 2D6, an enzyme known to show debrisoquine/sparteine-type genetic polymorphism in humans. In the present study we further examined the roles of several human P450 enzymes, as well as P450 2D6, in the hydroxylation of (+/-)-bufural...

journal_title：Molecular pharmacology

authors： Yamazaki H,Guo Z,Persmark M,Mimura M,Inoue K,Guengerich FP,Shimada T

更新日期：1994-09-01 00:00:00

abstract：:The ligand specificity of rat adenohypophyseal vasopressin receptors was directly compared to that of peripheral receptors of the V1 and V2 types. For this purpose a series of 15 recently designed vasopressin antagonists was used. The affinities of these antagonists for rat adenohypophyseal membranes were deduced from...

journal_title：Molecular pharmacology

authors： Jard S,Gaillard RC,Guillon G,Marie J,Schoenenberg P,Muller AF,Manning M,Sawyer WH

更新日期：1986-08-01 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：:The effects of interleukin (IL)-1 beta, IL-4, IL-6, tumor necrosis factor (TNF)-alpha, interferon (IFN)-alpha, IFN-gamma, and transforming growth factor (TGF)-beta 1 on cytochrome P-450 (CYP) 1A expression and polycyclic aromatic hydrocarbon (PAH)-mediated induction in primary human hepatocyte cultures were determined...

journal_title：Molecular pharmacology

authors： Abdel-Razzak Z,Corcos L,Fautrel A,Campion JP,Guillouzo A

更新日期：1994-12-01 00:00:00

abstract：:We examined the effects on allosteric modulation and ligand binding of the mutation of amino acid residues of the human A(3) adenosine receptor (A(3)AR) that are hypothesized to be near one of three loci: the putative sodium binding site, the putative ligand binding site, and the DRY motif in transmembrane helical dom...

journal_title：Molecular pharmacology

authors： Gao ZG,Kim SK,Gross AS,Chen A,Blaustein JB,Jacobson KA

更新日期：2003-05-01 00:00:00

abstract：:The highly conserved Arg in the so-called DRY motif (Asp-Arg-Tyr) at the intracellular end of transmembrane helix 3 is in general considered as an essential residue for G protein coupling in rhodopsin-like seven transmembrane (7TM) receptors. In the open reading frame 74 (ORF74) receptor encoded by equine herpesvirus ...

journal_title：Molecular pharmacology

authors： Rosenkilde MM,Kledal TN,Schwartz TW

更新日期：2005-07-01 00:00:00

abstract：:For a series of antitumor-active 5-substituted 9-aminoacridine-4-carboxamide topoisomerase II poisons, we have used X-ray crystallography and stopped-flow spectrophotometry to explore relationships between DNA binding kinetics, biological activity, and the structures of their DNA complexes. The structure of 5-F-9-amin...

journal_title：Molecular pharmacology

authors： Adams A,Guss JM,Collyer CA,Denny WA,Prakash AS,Wakelin LP

更新日期：2000-09-01 00:00:00

abstract：:alpha-Amidation is essential for the function of many peptides in intercellular communication. This C-terminal modification is mediated in a two-step process by the hydroxylase and lyase activities of the bifunctional enzyme, peptidylglycine alpha-amidating monooxygenase (PAM). The first step, catalyzed by peptidylgly...

journal_title：Molecular pharmacology

authors： Driscoll WJ,Mueller SA,Eipper BA,Mueller GP

更新日期：1999-06-01 00:00:00

abstract：:Adult guinea pig hippocampal membranes contain two 5-hydroxytryptamine (5-HT) receptors positively coupled with an adenylate cyclase. One is a typical 5-HT1A receptor and the second is a nonclassical 5-HT receptor that we previously proposed to call 5-HT4. Here, we show that 4-amino-5-chlor-2-methoxy-benzamide derivat...

journal_title：Molecular pharmacology

authors： Bockaert J,Sebben M,Dumuis A

更新日期：1990-03-01 00:00:00

abstract：:We have identified four new mu-opiod receptor (MOR)-1 exons, indicating that the gene now contains at least nine exons spanning more than 200 kilobases. Replacement of exon 4 by combinations of the new exons yields three new receptors. When expressed in Chinese hamster ovary cells, all three variants displayed high af...

journal_title：Molecular pharmacology

authors： Pan YX,Xu J,Bolan E,Abbadie C,Chang A,Zuckerman A,Rossi G,Pasternak GW

更新日期：1999-08-01 00:00:00

abstract：:Although much has been learned about the mechanisms of ligand selectivity between different opioid receptor subtypes, little is known about the common opioid binding pocket shared by all opioid receptors. The recently discovered orphanin system offers a good opportunity to study the mechanisms involved in the binding ...

journal_title：Molecular pharmacology

authors： Meng F,Ueda Y,Hoversten MT,Taylor LP,Reinscheid RK,Monsma FJ,Watson SJ,Civelli O,Akil H

更新日期：1998-04-01 00:00:00

abstract：:The gamma-aminobutyric acid-A (GABA(A)) receptor complex is allosterically modulated by a variety of substances, some of clinical importance. Barbiturates and neurosteroids augment GABA-currents and also directly gate the channel. A variety of gamma-butyrolactone analogues also modulate GABA-induced currents, with som...

journal_title：Molecular pharmacology

authors： Williams KL,Tucker JB,White G,Weiss DS,Ferrendelli JA,Covey DF,Krause JE,Rothman SM

更新日期：1997-07-01 00:00:00

abstract：:ATP-sensitive K(+) channels are closed by the hypoglycemic sulfonylureas like glibenclamide (GBC) and activated by a class of vasorelaxant compounds, the K(+) channel openers. These channels are octamers of Kir6.x and sulfonylurea receptor (SUR) subunits with 4:4 stoichiometry. The properties of the opener-sensitive K...

journal_title：Molecular pharmacology

authors： Russ U,Hambrock A,Artunc F,Löffler-Walz C,Horio Y,Kurachi Y,Quast U

更新日期：1999-11-01 00:00:00

abstract：:The human monoamine oxidase (MAO) B plays a major role in the degradation of biogenic and dietary amines such as phenylethylamine, benzylamine, dopamine, and tyramine. We previously showed that the -246/-99 MAO B promoter region exhibited the highest activity and contained two clusters of overlapping Sp1 sites, a CACC...

journal_title：Molecular pharmacology

authors： Wong WK,Chen K,Shih JC

更新日期：2001-04-01 00:00:00

abstract：:The ubiquitously expressed nitric oxide (NO) receptor soluble guanylate cyclase (sGC) plays a key role in signal transduction. Binding of NO to the N-terminal prosthetic heme moiety of sGC results in approximately 200-fold activation of the enzyme and an increased conversion of GTP into the second messenger cGMP. sGC ...

journal_title：Molecular pharmacology

authors： Rothkegel C,Schmidt PM,Atkins DJ,Hoffmann LS,Schmidt HH,Schröder H,Stasch JP

更新日期：2007-11-01 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：:The interaction between two nonhomologous K+ channel toxins, Tityus serrulatus (scorpion) toxin tityustoxin-K alpha (TsTX-K alpha) and Dendroaspis angusticeps (snake) toxin dendrotoxin (alpha-DTX), was investigated on K+ currents in B82 fibroblast cells transformed to express the Kv1.2 K+ channel. As demonstrated prev...

journal_title：Molecular pharmacology

authors： Werkman TR,Gustafson TA,Rogowski RS,Blaustein MP,Rogawski MA

更新日期：1993-08-01 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：:A functional interaction between peroxisome proliferator-activated receptor alpha (PPARalpha) and components of the circadian clock has been suggested, but whether these transcriptional factors interact to regulate the expression of their target genes remains obscure. Here we used a PPARalpha ligand, bezafibrate, to s...

journal_title：Molecular pharmacology

authors： Oishi K,Koyanagi S,Matsunaga N,Kadota K,Ikeda E,Hayashida S,Kuramoto Y,Shimeno H,Soeda S,Ohdo S

更新日期：2010-07-01 00:00:00

abstract：:This study identifies signaling pathways activated by the beta(2)-/beta(3)-adrenoceptor (AR) agonist zinterol, the selective beta(3)-AR agonist L755507, and the selective beta(3)-AR antagonist L748337 in CHO-K1 cells expressing human beta(3)-adrenoceptors. Zinterol and L755507 caused a robust concentration-dependent i...

journal_title：Molecular pharmacology

authors： Sato M,Hutchinson DS,Evans BA,Summers RJ

更新日期：2008-11-01 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：:Thrombin, the key effector protease of the coagulation cascade, drives fibrin deposition and activates human platelets through protease-activated receptor-1 (PAR1). These processes are critical to the progression of thrombotic diseases. Thrombin is the main target of anticoagulant therapy, and major efforts have led t...

journal_title：Molecular pharmacology

authors： Chen B,Soto AG,Coronel LJ,Goss A,van Ryn J,Trejo J

更新日期：2015-07-01 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：:The regulation of the cellular distribution and intracellular signaling properties of the alpha(1B)- and alpha(1D)- adrenoceptor (alpha(1)-AR) subtypes was examined in stably transfected Rat 1 fibroblasts. In unstimulated cells, alpha(1B)-AR expression was noted primarily on the cell surface. Treatment with phenylephr...

journal_title：Molecular pharmacology

authors： McCune DF,Edelmann SE,Olges JR,Post GR,Waldrop BA,Waugh DJ,Perez DM,Piascik MT

更新日期：2000-04-01 00:00:00

abstract：:Diarylsulfonylurea (DSU) antitumor agents represent a new class of oncolytic compounds with an unknown, potentially novel, mechanism of action. At high concentrations of several of these agents, cytotoxicity appears to be a consequence of uncoupling of mitochondria. However, the mechanism of action at pharmacologicall...

journal_title：Molecular pharmacology

authors： Sosinski J,Thakar JH,Germain GS,Dias P,Harwood FC,Kuttesch JF,Houghton PJ

更新日期：1994-05-01 00:00:00

abstract：:Arrestins mediate G protein-coupled receptor desensitization, internalization, and signaling. Dopamine D(2) and D(3) receptors have similar structures but distinct characteristics of interaction with arrestins. The goals of this study were to compare arrestin-binding determinants in D(2) and D(3) receptors other than ...

journal_title：Molecular pharmacology

authors： Lan H,Liu Y,Bell MI,Gurevich VV,Neve KA

更新日期：2009-01-01 00:00:00