Agonist-promoted Lys63-linked polyubiquitination of the human kappa-opioid receptor is involved in receptor down-regulation.

abstract：:A novel cloned polymorphism of the human concentrative nucleoside transporter hCNT3 was described and functionally characterized. This variant consists of a T/C transition leading to the substitution of cysteine 602 by an arginine residue in the core of transmembrane domain 13. The resulting hCNT3(C602R) protein has t...

journal_title：Molecular pharmacology

authors： Errasti-Murugarren E,Cano-Soldado P,Pastor-Anglada M,Casado FJ

更新日期：2008-02-01 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：:The 90-kDa heat shock family (HSP90) of protein and two-component histidine kinases, although quite distinct at the primary amino acid sequence level, share a common structural ATP-binding domain known as the Bergerat fold. The Bergerat fold is important for the ATPase activity and associated chaperone function of HSP...

journal_title：Molecular pharmacology

authors： Besant PG,Lasker MV,Bui CD,Turck CW

更新日期：2002-08-01 00:00:00

abstract：:The nicotinic acetylcholine receptor (nAChR) belongs to a superfamily of pentameric ligand-gated ion channels involved in many physiologic and pathologic processes. Among nAChRs, receptors comprising the α7 subunit are unique because of their high Ca(2+) permeability and fast desensitization. nAChR agonists elicit a t...

journal_title：Molecular pharmacology

authors： Corradi J,Bouzat C

更新日期：2016-09-01 00:00:00

abstract：:The ability of dopamine agonists and antagonists to compete with [3H]spiperone binding to rat striatal membrane preparations at 4, 15, 26, and 37 degrees varied markedly with temperature. Dopamine and the dopamine agonist 2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene hydrobromide (ADTN) were more potent at lower...

journal_title：Molecular pharmacology

authors： Kilpatrick GJ,el Tayar N,Van de Waterbeemd H,Jenner P,Testa B,Marsden CD

更新日期：1986-09-01 00:00:00

abstract：:The exofacial part of transmembrane domain 5 (TMD 5) of the cationic amine-binding subclass of 7-transmembrane receptors is thought to be important in binding the side chain of the agonist. Residues Ile-188 through Ala-196 in TMD 5 of the M(1) muscarinic acetylcholine receptor (mAChR) have been studied by Cys- and Ala...

journal_title：Molecular pharmacology

authors： Allman K,Page KM,Curtis CA,Hulme EC

更新日期：2000-07-01 00:00:00

abstract：:Valproic acid (VPA) is a widely used antiepileptic agent that is undergoing clinical evaluation for anticancer therapy. We assessed the effects of VPA on angiogenesis in vitro and in vivo. In human umbilical vein endothelial cells, therapeutically relevant concentrations of VPA (0.25 to 1 mM) inhibited proliferation, ...

journal_title：Molecular pharmacology

authors： Michaelis M,Michaelis UR,Fleming I,Suhan T,Cinatl J,Blaheta RA,Hoffmann K,Kotchetkov R,Busse R,Nau H,Cinatl J Jr

更新日期：2004-03-01 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：:In vivo administration of the porphyrogenic agent allylisopropylacetamide (AIA) to phenobarbital-pretreated rats results in marked loss of hepatic cytochrome P-450 content. Using isozyme-selective functional markers, we now show that such loss reflects inactivation of several phenobarbital-inducible and constitutive i...

journal_title：Molecular pharmacology

authors： Bornheim LM,Underwood MC,Caldera P,Rettie AE,Trager WF,Wrighton SA,Correia MA

更新日期：1987-08-01 00:00:00

abstract：:Organic anion transporting polypeptides (Oatp) mediate the transport of a wide variety of amphipathic organic substrates. Rat Oatp1b2 and human OATP1B3 are members of a liver-specific subfamily of Oatps/OATPs. We investigated whether prolactin (PRL) and growth hormone (GH) regulated Oatp1b2 and OATP1B3 gene expression...

journal_title：Molecular pharmacology

authors： Wood M,Ananthanarayanan M,Jones B,Wooton-Kee R,Hoffman T,Suchy FJ,Vore M

更新日期：2005-07-01 00:00:00

abstract：:Cytotoxic effects of quinones are thought to be mediated by redox cycles between quinones and quinols whereby reactive oxygen species are generated. The role of glucuronidation in preventing these toxic redox cycles was investigated by using benzo(a)pyrene-3,6-quinone and isolated rat hepatocytes or Reuber hepatoma ce...

journal_title：Molecular pharmacology

authors： Lilienblum W,Bock-Hennig BS,Bock KW

更新日期：1985-04-01 00:00:00

abstract：:AM1710 (3-(1,1-dimethyl-heptyl)-1-hydroxy-9-methoxy-benzo(c) chromen-6-one), a cannabilactone cannabinoid receptor 2 (CB2) agonist, suppresses chemotherapy-induced neuropathic pain in rodents without producing tolerance or unwanted side effects associated with CB1 receptors; however, the signaling profile of AM1710 re...

journal_title：Molecular pharmacology

authors： Li AL,Lin X,Dhopeshwarkar AS,Thomaz AC,Carey LM,Liu Y,Nikas SP,Makriyannis A,Mackie K,Hohmann AG

更新日期：2019-02-01 00:00:00

abstract：:A series of isoflavone and tyrphostin compounds were found to inhibit the degradation of cAMP by several cyclic nucleotide phosphodiesterase (PDE) isozymes. Specific hydroxyl groups on the isoflavone structure were critical for PDE isozyme-selective inhibition. Replacement of the C-7 hydroxyl group of the isoflavone w...

journal_title：Molecular pharmacology

authors： Nichols MR,Morimoto BH

更新日期：2000-04-01 00:00:00

abstract：:We identified a novel azaindole derivative, L-750,667, that has high affinity (Ki = 0.51 nM) and >2000-fold selectivity for D4 dopamine receptors compared with its activity at D2 and D3 dopamine receptors. L-750,667 had little affinity for rat D1/D5 dopamine receptors, sigma binding sites, or 5-hydroxytryptamine1A or ...

journal_title：Molecular pharmacology

authors： Patel S,Patel S,Marwood R,Emms F,Marston D,Leeson PD,Curtis NR,Kulagowski JJ,Freedman SB

更新日期：1996-12-01 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：:The effects of alpha 2-adrenergic receptors are usually attributed to inhibition of adenylyl cyclase through pertussis toxin-sensitive Gi coupling. In kidney distal convoluted tubule (DCT) cells, stimulation of Na+/K(+)-ATPase by alpha 2 receptors involves activation of protein kinase C (PKC). To identify the signal p...

journal_title：Molecular pharmacology

authors： Gesek FA

更新日期：1996-08-01 00:00:00

abstract：:In the last years, reactive oxygen species (ROS) have been proposed as mediators of proliferative/hypertrophic responses to angiotensin II (Ang II), both in vivo and in vitro. However, the hypothesis that the Ang II-dependent cell contraction could be mediated by ROS, particularly H2O2, has not been tested. Present ex...

journal_title：Molecular pharmacology

authors： Torrecillas G,Boyano-Adánez MC,Medina J,Parra T,Griera M,López-Ongil S,Arilla E,Rodríguez-Puyol M,Rodríguez-Puyol D

更新日期：2001-01-01 00:00:00

abstract：:Recently, several classes of compounds have been shown to be potent, selective, and specific inhibitors of human immunodeficiency virus type 1 replication in vitro. These include the tetrahydroimidazo[4,5,1-jk][1,4]-benzodiazepin-2(1H)-one and -thione (TIBO) and the 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (H...

journal_title：Molecular pharmacology

authors： Debyser Z,Pauwels R,Baba M,Desmyter J,De Clercq E

更新日期：1992-05-01 00:00:00

abstract：:Intermediate-conductance (KCa3.1) and small-conductance (KCa2) calcium-activated K+ channels are gated by calcium binding to calmodulin (CaM) molecules associated with the calmodulin-binding domain (CaM-BD) of these channels. The existing KCa activators, such as naphtho[1,2-d]thiazol-2-ylamine (SKA-31), 6,7-dichloro-1...

journal_title：Molecular pharmacology

authors： Brown BM,Shim H,Zhang M,Yarov-Yarovoy V,Wulff H

更新日期：2017-10-01 00:00:00

abstract：:We have synthesized and characterized a high-affinity alpha 1-adrenergic receptor probe, 4-amino-6,7-dimethoxy-2[4'- [5"(3"'-125I-iodo-4"'-aminophenyl)pentanoyl]-1'-piperazinyl] quinazoline (125I-A55453). This ligand binds reversibly to rat hepatic plasma membranes with high affinity (KD = 77 +/- 6 pM), and it labels ...

journal_title：Molecular pharmacology

authors： Dickinson KE,Leeb-Lundberg LM,Heald SL,Wikberg JE,DeBernardis JF,Caron MG,Lefkowitz RJ

更新日期：1984-09-01 00:00:00

abstract：:In this work, we evaluate the structural differences of transmembrane helix 3 in rhodopsin and the 5-hydroxytryptamine 1A (5-HT1A) receptor caused by their different amino acid sequence. Molecular dynamics simulations of helix 3 in the 5-HT1A receptor tends to bend toward helix 5, in sharp contrast to helix 3 in rhodo...

journal_title：Molecular pharmacology

authors： López-Rodríguez ML,Vicente B,Deupi X,Barrondo S,Olivella M,Morcillo MJ,Behamú B,Ballesteros JA,Sallés J,Pardo L

更新日期：2002-07-01 00:00:00

abstract：:In GH3 pituitary cell homogenates, acetylcholine (ACh) (IC50 200 nM) inhibits adenylate cyclase [ATP pyrophosphate-lyase (cyclizing), EC 4.6.1.1] activity in a concentration- and GTP-dependent manner. Maximal inhibition was obtained with 10 microM ACh and corresponded to approximately a 50% decrease in basal enzyme ac...

journal_title：Molecular pharmacology

authors： Onali P,Eva C,Olianas MC,Schwartz JP,Costa E

更新日期：1983-09-01 00:00:00

abstract：:Niflumic acid [2-((3-(trifluoromethyl)phenyl)amino)-3-pyridinecarboxylic acid, NFA] is a nonsteroidal anti-inflammatory drug that also blocks or modulates the gating of a wide spectrum of ion channels. Here we investigated the mechanism of channel activation by NFA on ether-a-go-go-related gene (ERG) K(+) channel subt...

journal_title：Molecular pharmacology

authors： Fernandez D,Sargent J,Sachse FB,Sanguinetti MC

更新日期：2008-04-01 00:00:00

abstract：:In Rat-1 fibroblasts, endothelin-1 and a protein kinase C-stimulating phorbol ester stimulated extracellular signal-regulated kinase (ERK), whereas phenylephrine, acting at stably transfected human alpha1A-adrenoceptors, inhibited basal and endothelin-1- and phorbol ester-stimulated ERK. On the other hand, phenylephri...

journal_title：Molecular pharmacology

authors： Alexandrov A,Keffel S,Goepel M,Michel MC

更新日期：1998-11-01 00:00:00

abstract：:Isoproterenol increases and decreases contractile force at low and high concentrations, respectively, through beta(2)-adrenoceptors overexpressed in transgenic mouse heart (TG4), consistent with activation of both G(s) and G(i) proteins. Using TG4 hearts, we demonstrated that epinephrine behaves like isoproterenol, bu...

journal_title：Molecular pharmacology

authors： Heubach JF,Ravens U,Kaumann AJ

更新日期：2004-05-01 00:00:00

abstract：:The constitutive androstane receptor (CAR) and the pregnane X receptor (PXR) play a major part in the control of drug metabolism and transport. We have previously shown that PXR and CAR expression is controlled by the glucocorticoid receptor (GR) and proposed the existence of a signal transmission cascade GR-(PXR/CAR)...

journal_title：Molecular pharmacology

authors： Duret C,Daujat-Chavanieu M,Pascussi JM,Pichard-Garcia L,Balaguer P,Fabre JM,Vilarem MJ,Maurel P,Gerbal-Chaloin S

更新日期：2006-07-01 00:00:00

abstract：:DNA topoisomerases are the molecular targets of a range of anticancer and antimicrobial therapeutics. Many of these drugs act by converting their target enzyme to a DNA-damaging agent through the trapping of the covalent enzyme/DNA intermediate. This drug-mediated trapping of the intermediate is reversible, and the le...

journal_title：Molecular pharmacology

authors： Nitiss JL,Wang JC

更新日期：1996-11-01 00:00:00

abstract：:Na+-d-glucose cotransporter 1 (SGLT1) is rate-limiting for glucose absorption in the small intestine. Shortly after intake of glucose-rich food, SGLT1 abundance in the luminal membrane of the small intestine is increased. This upregulation occurs via glucose-induced acceleration of the release of SGLT1-containing vesi...

journal_title：Molecular pharmacology

authors： Chintalapati C,Keller T,Mueller TD,Gorboulev V,Schäfer N,Zilkowski I,Veyhl-Wichmann M,Geiger D,Groll J,Koepsell H

更新日期：2016-11-01 00:00:00

abstract：:The effects of the non-tumor-promoting protein kinase C (PKC) activator bryostatin 1 and the PKC inhibitors staurosporine and UCN-01 were examined with respect to modulation of 1-[beta-D-arabinofuranosyl]cytosine (ara-C)-induced apoptosis in human myeloid leukemia cells (HL-60) overexpressing the antiapoptotic protein...

journal_title：Molecular pharmacology

authors： Wang S,Vrana JA,Bartimole TM,Freemerman AJ,Jarvis WD,Kramer LB,Krystal G,Dent P,Grant S

更新日期：1997-12-01 00:00:00

abstract：:We examined the role of putative trafficking sequences in two GABA(A) receptor subunits: α4 and δ. These subunits assemble with a β subunit to form a subtype of GABA(A) receptor involved in generating the "tonic" outward current. Both α4 and δ subunits contain dibasic retention motifs in homologous positions. When bas...

journal_title：Molecular pharmacology

authors： Bracamontes JR,Li P,Akk G,Steinbach JH

更新日期：2014-07-01 00:00:00