Cellular uptake of the antitumor agent Dp44mT occurs via a carrier/receptor-mediated mechanism.

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：: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：: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：:The nuclear receptor peroxisome proliferator-activated receptor (PPAR) is activated by a diverse group of acidic ligands, including many peroxisome proliferator chemicals present in the environment. Janus tyrosine kinase-signal transducer and activator of transcription (JAK-STAT) signaling is activated by multiple cyt...

journal_title：Molecular pharmacology

authors： Shipley JM,Waxman DJ

更新日期：2003-08-01 00:00:00

abstract：:A site-directed alkylating agent was used to inactivate one or more types of opioid receptor in two bioassay preparations in the presence of type-selective ligands as protectors of other opioid receptor types. Since the pharmacological potency of an agonist is decreased when the receptor type through which it acts has...

journal_title：Molecular pharmacology

authors： Goldstein A,James IF

更新日期：1984-05-01 00:00:00

abstract：:Interleukin 6 (IL-6), which is elevated in patients with congestive heart failure and acts as both a chronic marker of inflammation and an acute-phase reactant, is associated with myocardial damage. Circulating levels of arginine vasopressin (AVP) are elevated during cardiac stress and could be a factor for cardiac in...

journal_title：Molecular pharmacology

authors： Xu F,Sun S,Wang X,Ni E,Zhao L,Zhu W

更新日期：2017-09-01 00:00:00

abstract：:Chimeric receptors of the beta2-adrenergic receptor in which the extracellular loops were replaced with the corresponding amino acids of the alpha1a-adrenergic receptor were generated to measure changes in alpha1-antagonist affinity. Although no changes in alpha1-antagonist affinity were measured in the beta2/alpha1a ...

journal_title：Molecular pharmacology

authors： Zhao MM,Gaivin RJ,Perez DM

更新日期：1998-03-01 00:00:00

abstract：:The deletion of Phe-508 (DeltaPhe508) constitutes the most prevalent of a number of mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) that cause cystic fibrosis (CF). This mutation leads to CFTR misfolding and retention in the endoplasmic reticulum, as well as impaired channel activity. The b...

journal_title：Molecular pharmacology

authors： Wellhauser L,Kim Chiaw P,Pasyk S,Li C,Ramjeesingh M,Bear CE

更新日期：2009-06-01 00:00:00

abstract：:The instability of the solubilized/purified form, the lack of catalytic activity of the stabilized, macrolide-complexed form, and the compromised catalytic activity of the decomplexed form of steroid-inducible cytochrome P450IIIA1 motivated further investigations of the substrate specificity of this isozyme. A major c...

journal_title：Molecular pharmacology

authors： Namkung MJ,Yang HL,Hulla JE,Juchau MR

更新日期：1988-11-01 00:00:00

abstract：:The precise mechanism by which the cellular uptake of the endocannabinoid anandamide (AEA) occurs has been the source of much debate. In the current study, we show that neuronal differentiated CAD (dCAD) cells accumulate anandamide by a process that is inhibited in a dose-dependent manner by N-(4-hydroxyphenyl)arachid...

journal_title：Molecular pharmacology

authors： McFarland MJ,Bardell TK,Yates ML,Placzek EA,Barker EL

更新日期：2008-07-01 00:00:00

abstract：:The phenylalkylamine emopamil prevents brain damage due to experimental cerebral ischemia. Stereoselective, high affinity, binding sites for (-)-[3H]emopamil in guinea pig brain cortex and liver membranes have been proposed to mediate its antiischemic effect. Using [N-methyl-3H]LU49888 as a photoaffinity probe we now ...

journal_title：Molecular pharmacology

authors： Moebius FF,Burrows GG,Striessnig J,Glossmann H

更新日期：1993-02-01 00:00:00

abstract：:Binding of [3H](d)-N-allylnormetazocine ([3H](d)-NANM) to rat brain membranes is stereospecific, reversible, and saturable (Bmax = 260 fmol/mg of protein) and manifests moderately high affinity (Kd = 20 nM). The rank order of potency among opioidbenzomorphans and phencyclidine (PCP) analogs for competition for [3H](d)...

journal_title：Molecular pharmacology

authors： Itzhak Y,Hiller JM,Simon EJ

更新日期：1985-01-01 00:00:00

abstract：:The co-transfection assay is a novel functional assay using cells transiently transfected with plasmids encoding intracellular receptors and corresponding reporter genes. Using this assay, natural product extracts were tested to identify compounds that modulate intracellular receptor activity, measured as changes in r...

journal_title：Molecular pharmacology

authors： Pathirana C,Stein RB,Berger TS,Fenical W,Ianiro T,Mais DE,Torres A,Goldman ME

更新日期：1995-03-01 00:00:00

abstract：:Ca-dependent, K-stimulated 86Rb efflux, a measure of Ca-activated K conductance in rat brain synaptosomes, was blocked by phenothiazines and haloperidol. Micromolar concentrations of the phenothiazines, fluphenazine and trifluoperazine, and haloperidol, a non-phenothiazine antipsychotic and calmodulin antagonist, sele...

journal_title：Molecular pharmacology

authors： Benishin CG,Krueger BK,Blaustein MP

更新日期：1988-02-01 00:00:00

abstract：:G protein-coupled receptors (GPCRs) and receptor tyrosine kinases (RTKs) act in concert to regulate cell growth, proliferation, survival, and migration. Metabotropic GABAB receptor (GABABR) is the GPCR for the main inhibitory neurotransmitter GABA in the central nervous system. Increased expression of GABABR has been ...

journal_title：Molecular pharmacology

authors： Xia S,He C,Zhu Y,Wang S,Li H,Zhang Z,Jiang X,Liu J

更新日期：2017-09-01 00:00:00

abstract：:Activation of muscarinic cholinergic receptors of 1321N1 human astrocytoma cells attenuates cyclic AMP accumulation. This effect results from an activation of phosphodiesterase with no direct inhibition of adenylate cyclase activity. In spite of this lack of coupling of muscarinic receptors to adenylate cyclase, guani...

journal_title：Molecular pharmacology

authors： Evans T,Martin MW,Hughes AR,Harden TK

更新日期：1985-01-01 00:00:00

abstract：:Binding equilibria of 12 nonsteroidal, anti-inflammatory substances, salicylic acid, diflunisal, phenylbutazone, azapropazone, fenbufen, biphenylacetic acid, naproxen, flurbiprofen, ibuprofin, diclofenac, indomethacin, and benoxaprofen, to defatted human serum albumin has been investigated at 37 degrees, pH 7.4, in a ...

journal_title：Molecular pharmacology

authors： Honoré B,Brodersen R

更新日期：1984-01-01 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：:beta-arrestins have been shown to play important roles in regulation of signaling and desensitization of opioid receptors in many in vivo studies. The current study was carried out to measure the direct interaction of beta-arrestins with two functional intracellular domains, the third intracellular loop (I3L) and the ...

journal_title：Molecular pharmacology

authors： Cen B,Xiong Y,Ma L,Pei G

更新日期：2001-04-01 00:00:00

abstract：:Tumor necrosis factor α (TNFα) plays a vital role in cancer progression as it is associated with inflammation and promotion of cancer angiogenesis and metastasis. The effects of TNFα are mediated by its downstream target, the oncogene lysine-rich CEACAM1 coisolated protein (LYRIC, also known as metadherin or astrocyte...

journal_title：Molecular pharmacology

authors： Xi R,Pun IH,Menezes SV,Fouani L,Kalinowski DS,Huang ML,Zhang X,Richardson DR,Kovacevic Z

更新日期：2017-05-01 00:00:00

abstract：:High-throughput screening has led to the identification of small-molecule blockers of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel, but the structural basis of blocker binding remains to be defined. We developed molecular models of the CFTR channel on the basis of homology to the bac...

journal_title：Molecular pharmacology

authors： Norimatsu Y,Ivetac A,Alexander C,O'Donnell N,Frye L,Sansom MS,Dawson DC

更新日期：2012-12-01 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：: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：:Large-conductance Ca(2+)-activated K(+) (BK(Ca)) channels play an important role in the regulation of cell physiology in a wide variety of excitable and nonexcitable tissues. Filamin A is a conserved and ubiquitous actin-binding protein that forms perpendicular actin cross-links and contributes to changes in cell shap...

journal_title：Molecular pharmacology

authors： Kim EY,Ridgway LD,Dryer SE

更新日期：2007-09-01 00:00:00

abstract：:The isoprenoid donor for protein geranylgeranylation reactions, geranylgeranyl diphosphate (GGDP), is the product of the enzyme GGDP synthase (GGDPS) that condenses farnesyl diphosphate (FDP) and isopentenyl pyrophosphate. GGDPS inhibition is of interest from a therapeutic perspective for multiple myeloma because we h...

journal_title：Molecular pharmacology

authors： Allen C,Kortagere S,Tong H,Matthiesen RA,Metzger JI,Wiemer DF,Holstein SA

更新日期：2017-03-01 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：:Dietary lipids and fat-soluble micronutrients are solubilized in mixed micelles and absorbed in the small intestine. Based on an assumption that cholesterol and other fat-soluble molecules share a number of transport mechanisms and the fact that Niemann-Pick C1-like 1 (NPC1L1) is critical for intestinal cholesterol ab...

journal_title：Molecular pharmacology

authors： Narushima K,Takada T,Yamanashi Y,Suzuki H

更新日期：2008-07-01 00:00:00

abstract：:Human and bovine dopamine transporters (DAT) demonstrate discrete functional differences in dopamine (DA), 1-methyl-4-phenylpyridium (MPP(+)) transport, and cocaine analog binding. In a previous study, the functional analyses on the chimeras of human and bovine DAT have revealed that the region from residues 133 throu...

journal_title：Molecular pharmacology

authors： Lee SH,Chang MY,Lee KH,Park BS,Lee YS,Chin HR,Lee YS

更新日期：2000-05-01 00:00:00

abstract：:The human dopamine and norepinephrine transporters (hDAT and hNET, respectively) control neurotransmitter levels within the synaptic cleft and are the site of action for amphetamine (AMPH) and cocaine. We investigated the role of a threonine residue within the highly conserved and putative phosphorylation sequence RET...

journal_title：Molecular pharmacology

authors： Guptaroy B,Fraser R,Desai A,Zhang M,Gnegy ME

更新日期：2011-03-01 00:00:00

abstract：:The rat mu-opioid receptor clone in which novel exon 5 was found in the place of exon 4 (MOR-1B) was one of the first MOR-1 variants described. We now have identified the mouse homolog of the rat MOR-1B as well as four additional variants derived from splicing from exon 3 into different sites within exon 5. The sequen...

journal_title：Molecular pharmacology

authors： Pan YX,Xu J,Bolan E,Moskowitz HS,Xu M,Pasternak GW

更新日期：2005-09-01 00:00:00