G Protein-Coupled Receptor Endocytosis Confers Uniformity in Responses to Chemically Distinct Ligands.

abstract：:Serotonin [5-hydroxytryptamine (5-HT)] receptors are distinguished pharmacologically by their characteristic affinities for agonists and antagonists. Two serotonin receptors, the 5-HT2 and 5-HT1c, share a number of pharmacologic and structural properties while differing in their affinities for certain agonists and ant...

journal_title：Molecular pharmacology

authors： Choudhary MS,Craigo S,Roth BL

更新日期：1992-10-01 00:00:00

abstract：:Tissue plasminogen activator (tPA), a serine protease, catalyzes the conversion of plasminogen to plasmin. In the present study, we investigated the role of the tPA-plasmin system in depolarization-evoked dopamine (DA) and acetylcholine (ACh) release in the nucleus accumbens (NAc) and hippocampus, respectively, of mic...

journal_title：Molecular pharmacology

authors： Ito M,Nagai T,Kamei H,Nakamichi N,Nabeshima T,Takuma K,Yamada K

更新日期：2006-11-01 00:00:00

abstract：:Lysophosphatidic acid (LPA) and sphingosine-1-phosphate (S1P) are members of the phospholipid growth factor family. A major limitation in the field to date has been a lack of receptor subtype-specific agonists and antagonists. Here, we report that dioctylglycerol pyrophosphate and dioctylphosphatidic acid are selectiv...

journal_title：Molecular pharmacology

authors： Fischer DJ,Nusser N,Virag T,Yokoyama K,Wang Da,Baker DL,Bautista D,Parrill AL,Tigyi G

更新日期：2001-10-01 00:00:00

abstract：:The levels of hepatic mRNAs for several enzymes involved in drug metabolism were measured following administration to rats of either phenobarbitone or 2-allyl-2-isopropylacetamide. There was a substantial elevation in the mRNA levels for cytochromes P450 IIB1, IIB2, and IIIA1, epoxide hydrolase, glutathione-S-transfer...

journal_title：Molecular pharmacology

authors： Srivastava G,Hansen AJ,Bawden MJ,May BK

更新日期：1990-10-01 00:00:00

abstract：:Smad4, a key transcription factor in the transforming growth factor-β signaling pathway, is involved in a variety of cell physiologic and pathologic processes. Here, we characterized megakaryocyte/platelet-specific Smad4 deficiency in mice to elucidate its effect on platelet function. We found that megakaryocyte/plate...

journal_title：Molecular pharmacology

authors： Wang Y,Jiang L,Mo X,Lan Y,Yang X,Liu X,Zhang J,Zhu L,Liu J,Wu X

更新日期：2017-09-01 00:00:00

abstract：:Cidofovir [(S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine; (S)-HPMPC] is an antiviral drug that has been approved for the treatment of cytomegalovirus retinitis in patients with AIDS. Cidofovir also possesses potent activity against human papillomavirus-induced tumors in animal models and patients. We have recent...

journal_title：Molecular pharmacology

authors： Liekens S,Gijsbers S,Vanstreels E,Daelemans D,De Clercq E,Hatse S

更新日期：2007-03-01 00:00:00

abstract：:Glyceryl trinitrate (GTN) is used in the treatment of angina pectoris and cardiac failure, but the rapid onset of GTN tolerance limits its clinical utility. Research suggests that a principal cause of tolerance is inhibition of an enzyme responsible for the production of physiologically active concentrations of NO fro...

journal_title：Molecular pharmacology

authors： DiFabio J,Ji Y,Vasiliou V,Thatcher GR,Bennett BM

更新日期：2003-11-01 00:00:00

abstract：:Tienilic acid-induced hepatitis is characterized by the presence of anti-liver and -kidney microsomal (anti-LKM2) autoantibodies in patient sera. Cytochrome P4502C9(CYP2C9), involved in the metabolism of tienilic acid, was shown to be a target for tienilic acid-reactive metabolites and for autoantibodies. To further i...

journal_title：Molecular pharmacology

authors： Lecoeur S,André C,Beaune PH

更新日期：1996-08-01 00:00:00

abstract：:Recombinant interferon-alpha (IFN) enhances the cytotoxic effects of the fluorinated pyrimidine, 5-fluorouracil (5FU), against two human colon cancer cell lines. The aspartate transcarbamylase (ATCase) inhibitor, N-(phosphonacetyl)-L-aspartate (PALA), was studied in combination with 5FU/IFN to determine whether furthe...

journal_title：Molecular pharmacology

authors： Wadler S,Mao X,Bajaj R,Hallam S,Schwartz EL

更新日期：1993-11-01 00:00:00

abstract：:K-252b, a member of the staurosporine family of protein kinase inhibitors, selectively potentiates the activation of the nerve growth factor receptor, TrkA, by a nonpreferred ligand, neurotrophin-3 (NT-3), in a variety of cell types. At higher (micromolar) concentrations of K-252b, an inhibitory effect occurs because ...

journal_title：Molecular pharmacology

authors： Pollack S,Young L,Bilsland J,Wilkie N,Ellis S,Hefti F,Broughton H,Harper S

更新日期：1999-07-01 00:00:00

abstract：:Circular RNAs (circRNAs) are a distinct category of single-stranded, covalently closed RNAs formed by backsplicing. The functions of circRNAs are incompletely known and are under active investigation. Here, we report that in addition to traditional linear mRNAs (linRNA), mouse, rat, and human opioid receptor genes gen...

journal_title：Molecular pharmacology

authors： Irie T,Shum R,Deni I,Hunkele A,Le Rouzic V,Xu J,Wilson R,Fischer GW,Pasternak GW,Pan YX

更新日期：2019-08-01 00:00:00

abstract：:Adaptive changes in gene expression are thought to contribute to dependence, addiction and other behavioral responses to chronic ethanol abuse. DNA array studies provide a nonbiased detection of networks of gene expression changes, allowing insight into functional consequences and mechanisms of such molecular response...

journal_title：Molecular pharmacology

authors： Thibault C,Lai C,Wilke N,Duong B,Olive MF,Rahman S,Dong H,Hodge CW,Lockhart DJ,Miles MF

更新日期：2000-12-01 00:00:00

abstract：:Low-density lipoprotein (LDL) is known to be a mitogenic factor for vascular smooth muscle cells (VSMCs), fibroblasts, and endothelial cells. In the current study, we describe possible intracellular mechanisms by which LDL elicits its mitogenic effects. Stimulation of VSMCs with LDL resulted in a pertussis-toxin (PTX)...

journal_title：Molecular pharmacology

authors： Sachinidis A,Seewald S,Epping P,Seul C,Ko Y,Vetter H

更新日期：1997-09-01 00:00:00

abstract：:Up-regulation of fractalkine is involved in vascular and tissue damage in inflammatory conditions. Resveratrol has been shown to have anti-inflammatory, antioxidant, and antitumor activities. Its regulatory effects on expression of fractalkine in vascular endothelial cells and fractalkine receptor CX3CR1 in monocytes ...

journal_title：Molecular pharmacology

authors： Moon SO,Kim W,Sung MJ,Lee S,Kang KP,Kim DH,Lee SY,So JN,Park SK

更新日期：2006-07-01 00:00:00

abstract：:The local anesthetic-like Na+ channel-blocking drug [3H]PD85639 [alpha-([4-3H]phenyl)-N-[3-(2,6-dimethyl-1-piperizinyl)-alpha-prop yl] [4-3H]benzeneacetamide] binds specifically to receptor sites on Na+ channels in intact synaptosomes and synaptosomal membranes, purified and reconstituted Na+ channels, and type IIA Na...

journal_title：Molecular pharmacology

authors： Thomsen W,Hays SJ,Hicks JL,Schwarz RD,Catterall WA

更新日期：1993-06-01 00:00:00

abstract：:In rat pancreatic zymogen granules (ZG), an ATP-sensitive K(+) conductance and a Cl(-) conductance have been characterized that are inversely regulated by an approximately 65-kDa multidrug resistance P-glycoprotein (mdr1) gene product. In search of a label for purification of this protein, we found that the dihydropyr...

journal_title：Molecular pharmacology

authors： Braun M,Thévenod F

更新日期：2000-02-01 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：:Corticotropin-releasing factor (CRF) receptors encoded by two distinct genes have recently been identified and termed CRF1 and CRF2. CRF and the non-mammalian-related peptide sauvagine bind to and activate CRF1 receptors with high affinity and equal potency. Although CRF is significantly weaker at the CRF2 receptor, s...

journal_title：Molecular pharmacology

authors： Grigoriadis DE,Liu XJ,Vaughn J,Palmer SF,True CD,Vale WW,Ling N,De Souza EB

更新日期：1996-09-01 00:00:00

abstract：:5-Hydroxytryptamine3 (5-HT3) receptors are ligand-gated ion channels that mediate neurotransmission by serotonin in the central nervous system. Pharmacological inhibition of 5-HT3 receptor activity has therapeutic potential in several psychiatric diseases, including depression and anxiety. The recently approved multim...

journal_title：Molecular pharmacology

authors： Ladefoged LK,Munro L,Pedersen AJ,Lummis SCR,Bang-Andersen B,Balle T,Schiøtt B,Kristensen AS

更新日期：2018-12-01 00:00:00

abstract：:We have previously reported that, depending on the dose, nitric oxide (NO)-generating agents exert a dual facilitatory and inhibitory action on glutamatergic transmission on the rostral ventrolateral medulla (RVLM) neurons. The molecular mechanisms underlying the NO-mediated synaptic inhibition have not yet been defin...

journal_title：Molecular pharmacology

authors： Huang CC,Chan SH,Hsu KS

更新日期：2004-09-01 00:00:00

abstract：:The aim of this study was to use pharmacological inhibition of protein kinase A and mutation of potential protein kinase A phosphorylation sites to determine the role of protein kinase A-catalyzed phosphorylation of the dopamine D(1) receptor in agonist-stimulated desensitization and internalization of the receptor. T...

journal_title：Molecular pharmacology

authors： Mason JN,Kozell LB,Neve KA

更新日期：2002-04-01 00:00:00

abstract：:We examined the subtype-selective binding site of the beta-adrenergic receptors (betaARs). The beta(1)/beta(2)-chimeric receptors showed the importance of the second and seventh transmembrane domains (TM2 and TM7) of the beta(2)AR for the binding of the beta(2)-selective agonists such as formoterol and procaterol. Ala...

journal_title：Molecular pharmacology

authors： Isogaya M,Sugimoto Y,Tanimura R,Tanaka R,Kikkawa H,Nagao T,Kurose H

更新日期：1999-11-01 00:00:00

abstract：:Previously, we showed that the human kappa-opioid receptor (hkor) stably expressed in Chinese hamster ovary (CHO) cells underwent down-regulation after prolonged U50,488H treatment. In the present study, we determined the mechanisms underlying this process. U50, 488H caused a significant down-regulation of the hkor, a...

journal_title：Molecular pharmacology

authors： Li JG,Benovic JL,Liu-Chen LY

更新日期：2000-10-01 00:00:00

abstract：:Metallothioneins (MTs) are low molecular weight, thiol-rich, metal-binding proteins. Auranofin (AF) is a gold compound active in the treatment of rheumatoid arthritis. The effects of AF on regulation of MT gene expression in Chinese hamster ovary cells were studied. AF-resistant cells accumulated substantial amounts o...

journal_title：Molecular pharmacology

authors： Monia BP,Butt TR,Mirabelli CK,Ecker DJ,Sternberg E,Crooke ST

更新日期：1987-01-01 00:00:00

abstract：:A family of five cholinergic muscarinic receptor genes (m1, m2, m3, m4, and m5) has recently been identified and cloned. In order to investigate the pharmacological properties of the individual muscarinic receptors, we have transfected each of these genes into Chinese hamster ovary cells (CHO-K1) and have established ...

journal_title：Molecular pharmacology

authors： Buckley NJ,Bonner TI,Buckley CM,Brann MR

更新日期：1989-04-01 00:00:00

abstract：:Previously, we reported the presence of dual promoters, referred to as distal (DP) and proximal, with a negative regulatory element between them in the mouse mu-opioid receptor (mor) gene. Here we have identified a positive regulatory element influencing mor DP transcription, which contains multiple consensus binding ...

journal_title：Molecular pharmacology

authors： Im HJ,Smirnov D,Yuhi T,Raghavan S,Olsson JE,Muscat GE,Koopman P,Loh HH

更新日期：2001-06-01 00:00:00

abstract：:Peroxisome proliferator-activated receptor δ (PPARδ) has been implicated in vascular pathophysiology. However, its functions in atherogenic changes of the vascular wall have not been fully elucidated. PPARδ activated by GW501516 (2-[2-methyl-4-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]methylsulfanyl]ph...

journal_title：Molecular pharmacology

authors： Hwang JS,Ham SA,Yoo T,Lee WJ,Paek KS,Lee CH,Seo HG

更新日期：2016-11-01 00:00:00

abstract：:Several structurally related series of folate analogs were studied as substrates for mouse liver folylpolyglutamate synthetase (FPGS). A comparison of the kinetics of the interaction of this enzyme with folate analogs that contained the quinazoline ring in place of the pteridine ring with those of the analogous pterid...

journal_title：Molecular pharmacology

authors： Moran RG,Colman PD,Jones TR

更新日期：1989-11-01 00:00:00

abstract：:The peroxisome proliferator-activated receptors (PPARs) represent pharmacological target molecules to improve insulin resistance in type 2 diabetes mellitus. Here we assessed a functional connection between pharmacological activation of PPAR and vascular endothelial growth factor (VEGF) expression in keratinocytes and...

journal_title：Molecular pharmacology

authors： Schiefelbein D,Seitz O,Goren I,Dissmann JP,Schmidt H,Bachmann M,Sader R,Geisslinger G,Pfeilschifter J,Frank S

更新日期：2008-10-01 00:00:00

abstract：:The bile salt export pump (BSEP/ABCB11) transports bile salts from hepatocytes into bile canaliculi. Its malfunction is associated with severe liver disease. One reason for functional impairment of BSEP is systemic administration of drugs, which as a side effect inhibit the transporter. Therefore, drug candidates are ...

journal_title：Molecular pharmacology

authors： Sohail MI,Schmid D,Wlcek K,Spork M,Szakács G,Trauner M,Stockner T,Chiba P

更新日期：2017-10-01 00:00:00