Transcriptional Regulation of Human Cytosolic Sulfotransferase 1C3 by Peroxisome Proliferator-Activated Receptor γ in LS180 Human Colorectal Adenocarcinoma Cells.

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：: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：:Tumor cell resistance to anthracyclines and epipodophyllotoxins can be due to reduced drug accumulation and/or alterations in the activity of topoisomerase II (TOPO II). HL-60 cells selected in 0.05 micrograms/ml doxorubicin (DOX) are 10-fold and > 20-fold resistant to DOX and etoposide (VP-16), respectively. The accu...

journal_title：Molecular pharmacology

authors： Ganapathi R,Constantinou A,Kamath N,Dubyak G,Grabowski D,Krivacic K

更新日期：1996-08-01 00:00:00

abstract：:Previous studies revealed that phenylhistamines and histaprodifens possess higher potency and affinity at guinea pig histamine H(1)-receptor (gpH(1)R) than at human histamine H(1)-receptor (hH(1)R). However, we recently identified an imidazolylpropylguanidine [N(1)-(3-cyclohexylbutanoyl)-N(2)-[3-(1H-imidazol-4-yl)-pro...

journal_title：Molecular pharmacology

authors： Strasser A,Wittmann HJ,Kunze M,Elz S,Seifert R

更新日期：2009-03-01 00:00:00

abstract：:The activities of phosphorylase kinase and myosin light-chain kinase are regulated by Ca2+ binding to calmodulin. However, differences in the activation properties of the purified enzymes are apparent, since calmodulin binds to phosphorylase kinase in the absence of Ca2+ whereas prior formation of a Ca2+ . calmodulin ...

journal_title：Molecular pharmacology

authors： Silver PJ,Stull JT

更新日期：1983-05-01 00:00:00

abstract：:Valproic acid (VPA) is an effective antiepileptic drug with an additional activity for the treatment of bipolar disorder. It has been assumed that both activities arise from a common target. At the molecular level, VPA targets a number of distinct proteins that are involved in signal transduction. VPA inhibition of in...

journal_title：Molecular pharmacology

authors： Shimshoni JA,Dalton EC,Jenkins A,Eyal S,Ewan K,Williams RS,Pessah N,Yagen B,Harwood AJ,Bialer M

更新日期：2007-03-01 00:00:00

abstract：:15-Deoxy-Delta(12,14)-prostaglandin J(2) (15d-PGJ(2)) is a cyclopentenonic prostaglandin endowed with powerful anti-inflammatory activities, as shown in animal models of inflammatory/autoimmune diseases, where pharmacological administration of this prostanoid can ameliorate inflammation and local tissue damage via act...

journal_title：Molecular pharmacology

authors： Fionda C,Nappi F,Piccoli M,Frati L,Santoni A,Cippitelli M

更新日期：2007-11-01 00:00:00

abstract：:Vesnarinone, a cardiotonic agent, blocks I(Kr) and, unlike other I(Kr) blockers, produces a frequency-dependent prolongation of action potential duration (APD). To elucidate the mechanisms, we studied the effects of vesnarinone on HERG, the cloned human I(Kr) channel, heterologously expressed in Xenopus laevis oocytes...

journal_title：Molecular pharmacology

authors： Kamiya K,Mitcheson JS,Yasui K,Kodama I,Sanguinetti MC

更新日期：2001-08-01 00:00:00

abstract：:(6R)-5,6,7,8-Tetrahydrobiopterin (BH4), which is synthesized intracellularly from GTP, caused a concentration-dependent increase in rat pheochromocytoma (PC12) cell proliferation when added exogenously. Incubation with sepiapterin, which is converted enzymatically to BH4 within cells, also increased PC12 cell prolifer...

journal_title：Molecular pharmacology

authors： Anastasiadis PZ,States JC,Imerman BA,Louie MC,Kuhn DM,Levine RA

更新日期：1996-01-01 00:00:00

abstract：:Polycyclic aromatic hydrocarbons (PAHs) are widely distributed environmental toxicants derived from sources that include cigarette smoke, petroleum distillation, gas- and diesel-engine exhaust, and charcoal-grilled food. The gastrointestinal tract is the principal route of PAH exposures, even when inhaled. The most th...

journal_title：Molecular pharmacology

authors： Shi Z,Dragin N,Gálvez-Peralta M,Jorge-Nebert LF,Miller ML,Wang B,Nebert DW

更新日期：2010-07-01 00:00:00

abstract：:In the present study we have investigated the capacity of various compounds sterically related to indolo[3,2-b]carbazole to inhibit specific 2,3,7,8-tetrachloro[1,6-3H]dibenzo-p-dioxin binding in rat liver cytosol, as analyzed by electrofocusing in polyacrylamide gels. When the two nitrogen atoms of indolo[3,2-b]carba...

journal_title：Molecular pharmacology

authors： Gillner M,Bergman J,Cambillau C,Alexandersson M,Fernström B,Gustafsson JA

更新日期：1993-08-01 00:00:00

abstract：:Nod2 is an intracellular pattern recognition receptor that detects a conserved moiety of bacterial peptidoglycan and subsequently activates proinflammatory signaling pathways. Mutations in Nod2 have been implicated to be linked to inflammatory granulomatous disorders, such as Crohn's disease and Blau syndrome. Many ph...

journal_title：Molecular pharmacology

authors： Huang S,Zhao L,Kim K,Lee DS,Hwang DH

更新日期：2008-07-01 00:00:00

abstract：:A fusion protein consisting of the endothelin B (ET(B)) receptor and the enhanced green fluorescent protein (EGFP) in conjunction with Cyanin3- or fluorescein-conjugated endothelin 1 (Cy3-ET1, Fluo-ET1) was used to investigate the ligand-mediated internalization of the ET(B) receptor. The ET(B) receptor and the ET(B)/...

journal_title：Molecular pharmacology

authors： Oksche A,Boese G,Horstmeyer A,Furkert J,Beyermann M,Bienert M,Rosenthal W

更新日期：2000-06-01 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：:Poly(A)+ RNA from mammalian retina expresses bicuculline/baclofen-insensitive gamma-aminobutyric acid (GABA) receptors in Xenopus oocytes with properties similar to those of homooligomeric GABA rho 1 receptors. The pharmacological profile of these rho-like receptors was extended by measuring sensitivities to various G...

journal_title：Molecular pharmacology

authors： Woodward RM,Polenzani L,Miledi R

更新日期：1993-04-01 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 have identified alpha 2-adrenergic receptors on human erythroleukemia (HEL) cells, a suspension-grown cell line related to human platelets. properties of receptors were assessed in intact cells by binding of the antagonist [3H]yohimbine and by inhibition of cAMP accumulation. [3H]Yohimbine labeled 5900 +/- 2100 rec...

journal_title：Molecular pharmacology

authors： McKernan RM,Howard MJ,Motulsky HJ,Insel PA

更新日期：1987-08-01 00:00:00

abstract：:We cloned and expressed a human metabotropic glutamate receptor 1 alpha (HmGluR1 alpha) in a novel cell line. The human mGluR1 alpha cDNA was found to be 86% identical to rat mGluR1 alpha, and the predicted protein sequence was found to be 93% identical to rat mGluR1 alpha. We expressed HmGluR1 alpha in AV12-664, an a...

journal_title：Molecular pharmacology

authors： Desai MA,Burnett JP,Mayne NG,Schoepp DD

更新日期：1995-10-01 00:00:00

abstract：:Endothelin (ET) receptors are present in pituitary cells and stimulate hormone release through the phosphoinositide/Ca2+ signaling system. In pituitary cell suspensions, ET caused [Ca2+]i elevations of much higher amplitudes than those induced by other vasoactive hormones, including angiotensin II, vasopressin, and no...

journal_title：Molecular pharmacology

authors： Stojilković SS,Iida T,Merelli F,Catt KJ

更新日期：1991-06-01 00:00:00

abstract：:To study behavior of activated G(alpha)(s) in living cells, green fluorescent protein (GFP) was inserted within the internal amino acid sequence of G(alpha)(s) to generate a G(alpha)(s)-GFP fusion protein. The fusion protein maintained a bright green fluorescence and was identified by immunoblotting with antibodies ag...

journal_title：Molecular pharmacology

authors： Yu JZ,Rasenick MM

更新日期：2002-02-01 00:00:00

abstract：:Receptors have well-conserved regions that are recognized and activated by hormones and neurotransmitters. Most drugs bind to these sites and mimic or block the action of the native ligands. Using a high-throughput functional screen, we identified a potent and selective M(1) muscarinic receptor agonist from a novel st...

journal_title：Molecular pharmacology

authors： Spalding TA,Trotter C,Skjaerbaek N,Messier TL,Currier EA,Burstein ES,Li D,Hacksell U,Brann MR

更新日期：2002-06-01 00:00:00

abstract：:α-Conotoxins are subtype-selective nicotinic acetylcholine receptor (nAChR) antagonists. Although potent α3β2 nAChR-selective α-conotoxins have been identified, currently characterized α-conotoxins show no or only weak affinity for α4β2 nAChRs, which are, besides α7 receptors, the most abundant nAChRs in the mammalian...

journal_title：Molecular pharmacology

authors： Beissner M,Dutertre S,Schemm R,Danker T,Sporning A,Grubmüller H,Nicke A

更新日期：2012-10-01 00:00:00

abstract：:The availability of high-affinity agonists for peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta) has led to significant advances in our understanding of the functional role of PPARbeta/delta. In this study, a new PPARbeta/delta antagonist, 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethy...

journal_title：Molecular pharmacology

authors： Palkar PS,Borland MG,Naruhn S,Ferry CH,Lee C,Sk UH,Sharma AK,Amin S,Murray IA,Anderson CR,Perdew GH,Gonzalez FJ,Müller R,Peters JM

更新日期：2010-09-01 00:00:00

abstract：:Westernization of dietary habits increases lipid intake and is responsible for increased numbers of patients with atherosclerotic diseases. Niemann-Pick C1-Like 1 (NPC1L1)-a cholesterol importer-plays a crucial role in dietary cholesterol absorption in the intestine and is closely associated with several lipid-related...

journal_title：Molecular pharmacology

authors： Yamamoto H,Yamanashi Y,Takada T,Mu S,Tanaka Y,Komine T,Suzuki H

更新日期：2019-07-01 00:00:00

abstract：:Two human ovarian cancer cell lines were established from a patient before (PEO1) and after (PEO4) the onset of resistance to 5-fluorouracil (5-FU)/cisplatin-based chemotherapy. Using growth inhibition assays, we determined that the PEO4 line was almost 5-fold more resistant to 5-FU than the PEO1 line. The addition of...

journal_title：Molecular pharmacology

authors： Chu E,Lai GM,Zinn S,Allegra CJ

更新日期：1990-09-01 00:00:00

abstract：:The benzomorphan opiate, (-)N-allynormetazocine [(-)ANMC, (-)SKF10047], has been shown previously to bind two distinct sites on acetylcholine receptor (AChR)-rich membranes from Torpedo electroplaque. The low affinity site seems to correspond to the site for noncompetitive blockers on the AChR. The high affinity site,...

journal_title：Molecular pharmacology

authors： Coleman BA,Michel L,Oswald R

更新日期：1987-10-01 00:00:00

abstract：:Depolarization-induced 86Rb efflux, an index of K+ efflux, was developed by using mammalian cultured spinal cord neurons to study the effect of gamma aminobutyric acid (GABAB) receptor activation on Ca2(+)-activated K(+)-channels. The Ca2(+)-activated 86Rb efflux was obtained by using two methods. The first method uti...

journal_title：Molecular pharmacology

authors： Kamatchi GL,Ticku MK

更新日期：1990-09-01 00:00:00

abstract：:Thymidine phosphorylase (TPase) is one of the key enzymes involved in the pyrimidine nucleoside salvage pathway. However, TPase also stimulates angiogenesis, and its expression correlates well with microvessel density and metastasis in a variety of human tumors. We have shown recently that 5'-O-trityl-inosine (KIN59) ...

journal_title：Molecular pharmacology

authors： Liekens S,Bronckaers A,Hernández AI,Priego EM,Casanova E,Camarasa MJ,Pérez-Pérez MJ,Balzarini J

更新日期：2006-08-01 00:00:00

abstract：:Noscapine, a microtubule-interfering agent, has been shown to arrest mitosis, to induce apoptosis, and to have potent antitumor activity. We report herein that two brominated derivatives of noscapine, 5-bromonoscapine (5-Br-nosc) and reduced 5-bromonoscapine (Rd 5-Br-nosc), have higher tubulin binding activity than no...

journal_title：Molecular pharmacology

authors： Zhou J,Gupta K,Aggarwal S,Aneja R,Chandra R,Panda D,Joshi HC

更新日期：2003-04-01 00:00:00

abstract：:Cells of the murine neuroblastoma clone N1E-115 possess muscarinic receptors that influence the intracellular level of cyclic nucleotides. The stimulation of [3H]cyclic GMP levels occurs only with intact cells and has an EC50 near the "low-affinity" agonist equilibrium dissociation constant (KL) determined by radiolig...

journal_title：Molecular pharmacology

authors： McKinney M,Stenstrom S,Richelson E

更新日期：1984-09-01 00:00:00