Expression of tandem glutathione S-transferase recombinant genes in COS cells for analysis of efficiency of protein expression and associated drug resistance.

abstract：:The anticancer agent 2-cyano-3,12-dioxooleana-1,9-dien-28-oic acid (CDDO) and its methyl ester (CDDO-Me) typically induce a broad spectrum of growth-inhibitory, proapoptotic, and antiangiogenic responses. Treatment of Panc1, Panc28, and L3.6pL pancreatic cancer cells with low micromolar concentrations of CDDO or CDDO-...

journal_title：Molecular pharmacology

authors： Jutooru I,Chadalapaka G,Abdelrahim M,Basha MR,Samudio I,Konopleva M,Andreeff M,Safe S

更新日期：2010-08-01 00:00:00

abstract：:Adenosine receptors of the A1 and A2 subtypes were characterized in membranes from DDT1 MF-2 smooth muscle cells. These cells possess a high density of A1 adenosine receptors (Bmax = 0.8-0.9 pmol/mg of protein), as measured by both agonist and antagonist radioligands. Agonists compete for [125I]N6-[2-(4-amino-3-iodoph...

journal_title：Molecular pharmacology

authors： Ramkumar V,Barrington WW,Jacobson KA,Stiles GL

更新日期：1990-02-01 00:00:00

abstract：:We describe here the cloning and characterization of a rat homolog of the chemokine receptor CXCR3. The predicted amino acid sequence of rat CXCR3 contains 367 amino acid residues, sharing 96 and 87% amino acid sequence identity to the murine and human CXCR3, respectively. Among a large panel of chemokines tested, onl...

journal_title：Molecular pharmacology

authors： Wang X,Li X,Schmidt DB,Foley JJ,Barone FC,Ames RS,Sarau HM

更新日期：2000-06-01 00:00:00

abstract：:Rat and human lung microsomal cytochrome P-450 (P-450) enzymes have been characterized with regard to their catalytic activities towards several xenobiotic chemicals, including procarcinogens, in different microsomal preparations. Rat lung microsomal P-450s were more active than the human P-450s in catalyzing most of ...

journal_title：Molecular pharmacology

authors： Shimada T,Yun CH,Yamazaki H,Gautier JC,Beaune PH,Guengerich FP

更新日期：1992-05-01 00:00:00

abstract：:Aldose reductase (AKR1B1) is a critical drug target because of its involvement in diabetic complications, inflammation, and tumorigenesis. However, to date, development of clinically useful inhibitors has been largely unsuccessful. Cyclopentenone prostaglandins (cyPGs) are reactive lipid mediators that bind covalently...

journal_title：Molecular pharmacology

authors： Díez-Dacal B,Sánchez-Gómez FJ,Sánchez-Murcia PA,Milackova I,Zimmerman T,Ballekova J,García-Martín E,Agúndez JA,Gharbi S,Gago F,Stefek M,Pérez-Sala D

更新日期：2016-01-01 00:00:00

abstract：:Cytokines are thought to cause the depression of cytochrome P-450 (CYP)-associated drug metabolism in humans during inflammation and infection. We have examined the role of five cytokines, i.e., interleukin-1 beta, interleukin-4, interleukin-6, tumor necrosis factor-alpha, and interferon-gamma, on the expression of CY...

journal_title：Molecular pharmacology

authors： Abdel-Razzak Z,Loyer P,Fautrel A,Gautier JC,Corcos L,Turlin B,Beaune P,Guillouzo A

更新日期：1993-10-01 00:00:00

abstract：:The midbrain periaqueductal gray (PAG) is involved in organizing behavioral responses to threat, stress, and pain. These PAG functions are modulated by cholinergic agents. In the present study, we examined the cholinergic modulation of synaptic transmission in the PAG using whole-cell voltage-clamp recordings from rat...

journal_title：Molecular pharmacology

authors： Lau BK,Vaughan CW

更新日期：2008-11-01 00:00:00

abstract：:The NO/cGMP signaling pathway plays a major role in the cardiovascular system, in which it is involved in the regulation of smooth muscle tone and inhibition of platelet aggregation. Under pathophysiological conditions such as endothelial dysfunction, coronary artery disease, and airway hyperreactivity, smooth muscle ...

journal_title：Molecular pharmacology

authors： Mullershausen F,Lange A,Mergia E,Friebe A,Koesling D

更新日期：2006-06-01 00:00:00

abstract：:The GABA type A receptor (GABA(A)R) is the major inhibitory receptor in the mammalian central nervous system and the target of numerous pharmaceuticals. The alpha-subunit of these pentameric Cys-loop neurotransmitter-gated ion channels contributes to the binding of both GABA and allosteric modulators such as the benzo...

journal_title：Molecular pharmacology

authors： Hanek AP,Lester HA,Dougherty DA

更新日期：2010-07-01 00:00:00

abstract：:By limiting unrestricted activation of intracellular effectors, compartmentalised signalling of cyclic nucleotides confers specificity to extracellular stimuli and is critical for the development and health of cells and organisms. Dissecting the molecular mechanisms that allow local control of cyclic nucleotide signal...

journal_title：Molecular pharmacology

authors： Schleicher K,Zaccolo M

更新日期：2020-02-28 00:00:00

abstract：:The UGT1 locus is felt to be highly conserved between species, as is evident from the characterization of the locus in rodents and humans. In rabbits, cDNAs encoding proteins homologous to human UGT1A4, UGT1A6, and UGT1A7 have previously been identified. Here we demonstrate by Southern blot analysis, using exon 1 dive...

journal_title：Molecular pharmacology

authors： Li Q,Lamb G,Tukey RH

更新日期：2000-07-01 00:00:00

abstract：:The highly conserved aspartate residue in the second transmembrane domain of G protein-coupled receptors is present in position 113 in the type 1 neurotensin receptor (NTR1) but is replaced by an Ala residue in position 79 in the type 2 neurotensin receptor (NTR2). NTR1 couples to Galphaq to stimulate phospholipase C ...

journal_title：Molecular pharmacology

authors： Martin S,Botto JM,Vincent JP,Mazella J

更新日期：1999-02-01 00:00:00

abstract：:TWIK-related K+ channel TREK1, a background leak K+ channel, has been strongly implicated as the target of several general and local anesthetics. Here, using the whole-cell and single-channel patch-clamp technique, we investigated the effect of lidocaine, a local anesthetic, on the human (h)TREK1 channel heterologousl...

journal_title：Molecular pharmacology

authors： Nayak TK,Harinath S,Nama S,Somasundaram K,Sikdar SK

更新日期：2009-10-01 00:00:00

abstract：:A human recombinant L-type Ca2+ channel (alpha1C,77) was coexpressed with the rat angiotensin AT1A receptor in Xenopus laevis oocytes. In oocytes expressing only alpha1C,77 channels, application of human angiotensin II (1-10 microM) did not affect the amplitude or kinetics of Ba2+ currents (IBa). In sharp contrast, in...

journal_title：Molecular pharmacology

authors： Oz M,Melia MT,Soldatov NM,Abernethy DR,Morad M

更新日期：1998-12-01 00:00:00

abstract：:The diphosphoinositol polyphosphates ("inositol pyrophosphates") are a specialized subgroup of the inositol phosphate signaling family. This review proposes that many of the current data concerning the metabolic turnover and biological effects of the diphosphoinositol polyphosphates are linked by a common theme: these...

journal_title：Molecular pharmacology

authors： Shears SB

更新日期：2009-08-01 00:00:00

abstract：:Guanine nucleotides have been examined as to their effects on subclass-specific excitatory amino acid receptor-ligand interactions. Guanine nucleotides selectively inhibit L-[3H]glutamate binding to the N-methyl-D-aspartate (NMDA) recognition site while showing a lesser effect on [3H]kainate, [3H]alpha-amino-3-hydroxy...

journal_title：Molecular pharmacology

authors： Monahan JB,Hood WF,Michel J,Compton RP

更新日期：1988-08-01 00:00:00

abstract：:The verapamil-like arylazide (-)-[3H]azidopamil specifically photoaffinity labeled two low molecular mass polypeptides, with apparent molecular masses of 22 and 27 kDa, in the endoplasmic reticulum of guinea pig liver, kidney, adrenal gland, and lung. It was recently shown that the 22-kDa polypeptide binds the anti-is...

journal_title：Molecular pharmacology

authors： Moebius FF,Burrows GG,Hanner M,Schmid E,Striessnig J,Glossmann H

更新日期：1993-11-01 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：:A central axiom of ligand-receptor theory is that agonists bind more tightly to active than to inactive receptors. However, measuring agonist affinity in inactive receptors is confounded by concomitant activation. We identified a cysteine substituted mutant γ-aminobutyric acid type A (GABAA) receptor with unique chara...

journal_title：Molecular pharmacology

authors： Stewart DS,Hotta M,Desai R,Forman SA

更新日期：2013-06-01 00:00:00

abstract：:Mammalian A2-adenosine receptor binding subunits (A2AR) can be visualized by covalent labeling with the photoaffinity crosslinking ligand 125I-2-[4-[2-[2-[(4-aminophenyl)methylcarbonylamino] ethylaminocarbonyl]ethyl]phenyl]ethylamino-5'-N-ethylcarboxamidoad enosine or directly with the azide derivative described in th...

journal_title：Molecular pharmacology

authors： Barrington WW,Jacobson KA,Stiles GL

更新日期：1990-08-01 00:00:00

abstract：:Activation of endothelial nitric-oxide synthase (eNOS) has been shown to occur through various pathways involving increases in the cytosolic Ca(2+) concentration, activation of the phosphatidylinositol-3' kinase/Akt pathway, as well as regulation by other kinases and by protein-protein interactions. We have recently r...

journal_title：Molecular pharmacology

authors： Barsacchi R,Perrotta C,Bulotta S,Moncada S,Borgese N,Clementi E

更新日期：2003-04-01 00:00:00

abstract：:The irreversible proteolytic nature of protease-activated receptor-2 (PAR2) activation suggests that mechanism(s) responsible for termination of receptor signaling are critical determinants of the magnitude and duration of PAR2-elicited cellular responses. Rapid desensitization of activated G-protein-coupled receptors...

journal_title：Molecular pharmacology

authors： Stalheim L,Ding Y,Gullapalli A,Paing MM,Wolfe BL,Morris DR,Trejo J

更新日期：2005-01-01 00:00:00

abstract：:The aryl hydrocarbon receptor (AHR) is a ligand-activated transcription factor with constitutive activities and those induced by xenobiotic ligands, such as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD). One unexplained cellular role for the AHR is its ability to promote cell cycle progression in the absence of exogenous...

journal_title：Molecular pharmacology

authors： Barhoover MA,Hall JM,Greenlee WF,Thomas RS

更新日期：2010-02-01 00:00:00

abstract：:In the rat isolated optic nerve, nitric oxide (NO) activates soluble guanylyl cyclase (sGC), resulting in a selective accumulation of cGMP in the axons. The axons are also selectively vulnerable to NO toxicity. The experiments initially aimed to determine any causative link between these two effects. It was shown, usi...

journal_title：Molecular pharmacology

authors： Garthwaite G,Goodwin DA,Neale S,Riddall D,Garthwaite J

更新日期：2002-01-01 00:00:00

abstract：:Both in vivo and in vitro treatments with the irreversible protein-modifying reagent, N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ), were used to investigate rat striatal D1 dopamine receptor/effector interactions. Peripherally administered EEDQ markedly reduced D1 dopamine receptor binding and D1 dopamine rec...

journal_title：Molecular pharmacology

authors： Hess EJ,Battaglia G,Norman AB,Creese I

更新日期：1987-01-01 00:00:00

abstract：:bTREK-1 K(+) channels set the resting membrane potential of bovine adrenal zona fasciculata (AZF) cells and function pivotally in the physiology of cortisol secretion. Adrenocorticotropic hormone controls the function and expression of bTREK-1 channels through signaling mechanisms that may involve cAMP and downstream ...

journal_title：Molecular pharmacology

authors： Enyeart JA,Liu H,Enyeart JJ

更新日期：2010-03-01 00:00:00

abstract：:Nitric oxide (NO) possesses potent anti-inflammatory properties; however, an over-production of NO will promote inflammation and induce cell and tissue dysfunction. Thus, the ability to precisely regulate NO production could prove beneficial in controlling damage. In this study, advantage was taken of the well charact...

journal_title：Molecular pharmacology

authors： Bian K,Harari Y,Zhong M,Lai M,Castro G,Weisbrodt N,Murad F

更新日期：2001-04-01 00:00:00

abstract：:The successful synthesis of dolastatin 11, a depsipeptide originally isolated from the mollusk Dolabella auricularia, permitted us to study its effects on cells. The compound arrested cells at cytokinesis by causing a rapid and massive rearrangement of the cellular actin filament network. In a dose-and time-dependent ...

journal_title：Molecular pharmacology

authors： Bai R,Verdier-Pinard P,Gangwar S,Stessman CC,McClure KJ,Sausville EA,Pettit GR,Bates RB,Hamel E

更新日期：2001-03-01 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：:The 5'-flanking region of the mouse mu opioid receptor (MOR) gene has two promoters, referred to as distal and proximal. MOR mRNA is predominantly initiated by the proximal promoter. Previously, several important cis-elements and trans-factors have been shown to play a functional role in the proximal promoter of the M...

journal_title：Molecular pharmacology

authors： Choi HS,Hwang CK,Kim CS,Song KY,Law PY,Wei LN,Loh HH

更新日期：2005-05-01 00:00:00