Role of mPKCI, a novel mu-opioid receptor interactive protein, in receptor desensitization, phosphorylation, and morphine-induced analgesia.

abstract：:Cholinesterase inhibitors are commonly used to improve cognition and treat psychosis and other behavioral symptoms in Alzheimer's disease, Parkinson's disease, and other neuropsychiatric conditions. However, mechanisms may exist that down-regulate the synaptic response to altered cholinergic transmission, thus limitin...

journal_title：Molecular pharmacology

authors： Volpicelli-Daley LA,Hrabovska A,Duysen EG,Ferguson SM,Blakely RD,Lockridge O,Levey AI

更新日期：2003-12-01 00:00:00

abstract：:To study the molecular pharmacology of low-voltage-activated calcium channels in biophysical detail, human medullary thyroid carcinoma (hMTC) cells were investigated using the single-channel technique. These cells had been reported to express T-type whole-cell currents and a Ca(v)3.2 (or alpha 1H) channel subunit. We ...

journal_title：Molecular pharmacology

authors： Michels G,Matthes J,Handrock R,Kuchinke U,Groner F,Cribbs LL,Pereverzev A,Schneider T,Perez-Reyes E,Herzig S

更新日期：2002-03-01 00:00:00

abstract：:Chemokine receptors belong to the class A of G protein-coupled receptors (GPCRs) and are implicated in a wide variety of physiologic functions, mostly related to the homeostasis of the immune system. Chemokine receptors are also involved in multiple pathologic processes, including immune and autoimmune diseases, as we...

journal_title：Molecular pharmacology

authors： Arimont M,Hoffmann C,de Graaf C,Leurs R

更新日期：2019-12-01 00:00:00

abstract：:High-affinity glycine transport in neurons and glial cells is a primary means of inactivating synaptic glycine. We have synthesized a potent selective inhibitor of glycine transporter 1 (GlyT1), and characterized its activity using a quail fibroblast cell line (QT6). The glycine transporters GlyT1A, GlyT1B, GlyT1C, an...

journal_title：Molecular pharmacology

authors： Atkinson BN,Bell SC,De Vivo M,Kowalski LR,Lechner SM,Ognyanov VI,Tham CS,Tsai C,Jia J,Ashton D,Klitenick MA

更新日期：2001-12-01 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：:The mammalian copper transporter 1 (CTR1) is responsible for the uptake of copper from the extracellular space. In this study, we used an isogenic pair of CTR1(+/+) and CTR1(-/-) mouse embryo fibroblasts to examine the contribution of CTR1 to the influx of cisplatin (DDP), carboplatin (CBDCA), oxaliplatin (L-OHP), and...

journal_title：Molecular pharmacology

authors： Larson CA,Blair BG,Safaei R,Howell SB

更新日期：2009-02-01 00:00:00

abstract：:The human CYP2C9 plays a crucial role in the metabolic clearance of a wide range of clinical therapeutics. The *2 allele is a prevalent genetic variation in CYP2C9 that is found in various populations. A marked reduction of catalytic activity toward many important drug substrates has been demonstrated by CYP2C9*2, whi...

journal_title：Molecular pharmacology

authors： Parikh SJ,Evans CM,Obi JO,Zhang Q,Maekawa K,Glass KC,Shah MB

更新日期：2020-11-01 00:00:00

abstract：:Bufuralol 1'-hydroxylation is a prototypical reaction catalyzed by cytochrome P450 (P450) 2D6, an enzyme known to show debrisoquine/sparteine-type genetic polymorphism in humans. In the present study we further examined the roles of several human P450 enzymes, as well as P450 2D6, in the hydroxylation of (+/-)-bufural...

journal_title：Molecular pharmacology

authors： Yamazaki H,Guo Z,Persmark M,Mimura M,Inoue K,Guengerich FP,Shimada T

更新日期：1994-09-01 00:00:00

abstract：:An alteration in the balance between a T-helper type 2 cell (Th2) response and a Th1 response may predispose to the development of bronchial asthma. Interleukin-18 (IL-18) has an ability to promote both Th1 and Th2 responses, depending on the surrounding cytokine environment. Reactive oxygen species (ROS) play a cruci...

journal_title：Molecular pharmacology

authors： Lee KS,Kim SR,Park SJ,Min KH,Lee KY,Jin SM,Yoo WH,Lee YC

更新日期：2006-10-01 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：:Enzalutamide is a potent second-generation androgen receptor (AR) antagonist with activity in metastatic castrate-resistant prostate cancer (CRPC). Although enzalutamide is initially effective, disease progression inevitably ensues with the emergence of resistance. Intratumoral hypoxia is also associated with CRPC pro...

journal_title：Molecular pharmacology

authors： Fernandez EV,Reece KM,Ley AM,Troutman SM,Sissung TM,Price DK,Chau CH,Figg WD

更新日期：2015-06-01 00:00:00

abstract：:cRNAs encoding the kappa-opioid receptor and an inwardly rectifying, G protein-coupled, K+ channel were coinjected into Xenopus oocytes. The effects of kappa-opioid receptor agonists and antagonists on the membrane currents in these oocytes were studied using the two-electrode voltage-clamp technique. The kappa-opioid...

journal_title：Molecular pharmacology

authors： Ma GH,Miller RJ,Kuznetsov A,Philipson LH

更新日期：1995-05-01 00:00:00

abstract：:The MUC1 C-terminal transmembrane subunit (MUC1-C) oncoprotein is a direct activator of the canonical nuclear factor-kappaB (NF-kappaB) RelA/p65 pathway and is aberrantly expressed in human multiple myeloma cells. However, it is not known whether multiple myeloma cells are sensitive to the disruption of MUC1-C functio...

journal_title：Molecular pharmacology

authors： Yin L,Ahmad R,Kosugi M,Kufe T,Vasir B,Avigan D,Kharbanda S,Kufe D

更新日期：2010-08-01 00:00:00

abstract：:Guanine nucleotide-binding proteins (G proteins) transduce signals from agonist- and light-sensitive receptors. In the visual excitation system, the photon receptor rhodopsin is coupled to the G protein Gt (transducin). Gt is composed of alpha, beta, and gamma subunits; the alpha subunit binds guanine nucleotide, wher...

journal_title：Molecular pharmacology

authors： Halpern JL,Moss J

更新日期：1990-06-01 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：:Nefiracetam (DM-9384) is a new pyrrolidone nootropic drug being developed for the treatment of Alzheimer's type and poststroke vascular-type dementia. Because the cholinergic system plays an important role in cognitive functions and Alzheimer's disease dementia, the present study was conducted to elucidate the mechani...

journal_title：Molecular pharmacology

authors： Zhao X,Kuryatov A,Lindstrom JM,Yeh JZ,Narahashi T

更新日期：2001-04-01 00:00:00

abstract：:Because cytotoxicity by an alkylating agent such as N-methyl-N'-nitrosoguanidine is markedly increased in adenine methylase-deficient dam-3 Escherichia coli, it was of interest to assess whether mismatch repair was similarly important in the repair of DNA damage induced by cis-diamminedichloroplatinum(II) (CDDP). The ...

journal_title：Molecular pharmacology

authors： Fram RJ,Cusick PS,Wilson JM,Marinus MG

更新日期：1985-07-01 00:00:00

abstract：:Nicotine biotransformation affects the smoking habits of addicted individuals and therefore their health risk. Using an improved analytical method, we have discovered that the human UDP-glucuronosyltransferase (UGT) 2B10, a liver enzyme previously unknown to conjugate nicotine or exhibit considerable activity toward a...

journal_title：Molecular pharmacology

authors： Kaivosaari S,Toivonen P,Hesse LM,Koskinen M,Court MH,Finel M

更新日期：2007-09-01 00:00:00

abstract：:Tetrodotoxin-sensitive Na(+) currents have been extensively studied because they play a major role in neuronal firing and bursting. In this study, we showed that voltage-dependent Na(+) currents are regulated in a slow manner by oxotremorine (oxo-M) and angiotensin II in rat sympathetic neurons. We found that these cu...

journal_title：Molecular pharmacology

authors： Puente EI,De la Cruz L,Arenas I,Elias-Viñas D,Garcia DE

更新日期：2016-04-01 00:00:00

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：:Cadmium is a dangerous metal distributed widely in the environment. Members of our laboratory recently identified the ZIP8 transporter protein, encoded by the mouse Slc39a8 gene, to be responsible for genetic differences in response to cadmium damage of the testis. Stable retroviral infection of the ZIP8 cDNA in mouse...

journal_title：Molecular pharmacology

authors： He L,Girijashanker K,Dalton TP,Reed J,Li H,Soleimani M,Nebert DW

更新日期：2006-07-01 00:00:00

abstract：:This study assessed how conformational information encoded by ligand binding to δ-opioid receptors (DORs) is transmitted to Kir3.1/Kir3.2 channels. Human embryonic kidney 293 cells were transfected with bioluminescence resonance energy transfer (BRET) donor/acceptor pairs that allowed us to evaluate independently reci...

journal_title：Molecular pharmacology

authors： Richard-Lalonde M,Nagi K,Audet N,Sleno R,Amraei M,Hogue M,Balboni G,Schiller PW,Bouvier M,Hébert TE,Pineyro G

更新日期：2013-02-01 00:00:00

abstract：:The dissociation constants (Kd values) of substance P (SP), physalaemin, kassinin, and SP analogues acting on SP receptors in guinea pig ileal longitudinal muscle strips were determined by the pharmacological procedures of Furchgott [Adv. Drug Res. 3:21-55 (1966)]. This method involves analysis of the concentration-re...

journal_title：Molecular pharmacology

authors： Lin CW,Musacchio JM

更新日期：1983-05-01 00:00:00

abstract：:The dopamine D3 receptor, although structurally similar to the dopamine D2 receptor, has 100-fold higher affinity for agonists such as dopamine and quinpirole, when these receptors are expressed in 293 cells. Additionally, the D3 receptor has generally lower affinity for several antagonists than does the D2 receptor. ...

journal_title：Molecular pharmacology

authors： Robinson SW,Jarvie KR,Caron MG

更新日期：1994-08-01 00:00:00

abstract：:Caveolins have been recognized over the past few decades as key regulators of cell physiology. They are ubiquitously expressed and regulate a number of processes that ultimately impact efficiency of cellular processes. Though not critical to life, they are central to stress adaptation in a number of organs. The follow...

journal_title：Molecular pharmacology

authors： Schilling JM,Head BP,Patel HH

更新日期：2018-04-01 00:00:00

abstract：:The beta 3-adrenergic receptor (beta 3AR) is a member of the super-family of G protein-coupled receptors that are characterized by seven putative transmembrane helices connected by hydrophilic loops. The mechanism by which the activated beta ARs transmit the signals across the plasma membrane involves the stimulation ...

journal_title：Molecular pharmacology

authors： Guan XM,Amend A,Strader CD

更新日期：1995-09-01 00:00:00

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：:The expression and molecular regulation of the cytochrome P450IA (P450IA) gene subfamily have been examined in rat hepatic tissue after treatment with pyridine. The microsomal ethoxyresorufin O-deethylase activity, which has been shown to be specific for the P450IA subfamily, was increased approximately 2- and 3.5-fol...

journal_title：Molecular pharmacology

authors： Kim SG,Reddy SL,States JC,Novak RF

更新日期：1991-07-01 00:00:00

abstract：:Resveratrol (RES), a natural plant polyphenol, has gained interest as a nontoxic chemopreventive agent capable of inducing tumor cell death in a variety of cancer types. However, the early molecular mechanisms of RES-induced apoptosis are not well defined. Using the human breast cancer cell lines MDA-MB-231 and MCF-7,...

journal_title：Molecular pharmacology

authors： Sareen D,Darjatmoko SR,Albert DM,Polans AS

更新日期：2007-12-01 00:00:00

abstract：:Many human cancers show constitutive or amplified expression of the transcriptional regulator and oncoprotein Myc, making Myc a potential target for therapeutic intervention. Here we report the down-regulation of Myc activity by reducing the availability of Max, the essential dimerization partner of Myc. Max is expres...

journal_title：Molecular pharmacology

authors： Jiang H,Bower KE,Beuscher AE 4th,Zhou B,Bobkov AA,Olson AJ,Vogt PK

更新日期：2009-09-01 00:00:00