Pharmacological differences between human and guinea pig histamine H1 receptors: Asn84 (2.61) as key residue within an additional binding pocket in the H1 receptor.

abstract：:Ubiquitination plays a crucial role in regulating protein turnover. Here we show that ubiquitination regulates the stability of the MDR1 gene product, P-glycoprotein, thereby affecting the functions of this membrane transporter that mediates multidrug resistance. We found that P-glycoprotein was constitutively ubiquit...

journal_title：Molecular pharmacology

authors： Zhang Z,Wu JY,Hait WN,Yang JM

更新日期：2004-09-01 00:00:00

abstract：:Inhibitors of the proteasome, a multicatalytic proteinase complex responsible for intracellular proteolysis, activate programmed cell death in part through the c-Jun-N-terminal kinase (JNK). Proteasome inhibitors also induce mitogen-activated protein kinase phosphatase-1 (MKP-1), however, which can inactivate JNK, and...

journal_title：Molecular pharmacology

authors： Small GW,Shi YY,Edmund NA,Somasundaram S,Moore DT,Orlowski RZ

更新日期：2004-12-01 00:00:00

abstract：:The selective inactivation by 17 beta-substituted steroids of rabbit and rat liver cytochromes P-450 involved in the 21-hydroxylation of progesterone has been investigated. Five derivatives each of pregnenolone and progesterone were prepared, in which the methylketo substituent of the 17 beta-position was replaced by ...

journal_title：Molecular pharmacology

authors： Halpert J,Jaw JY,Balfour C

更新日期：1989-01-01 00:00:00

abstract：:Merbarone (5-[N-phenyl carboxamido]-2-thiobarbituric acid) is an anticancer drug that inhibits the catalytic activity of DNA topoisomerase II (topo II) without damaging DNA or stabilizing DNA-topo II cleavable complexes. Although the cytotoxicity of the complex-stabilizing DNA-topo II inhibitors such as VP-16 (etoposi...

journal_title：Molecular pharmacology

authors： Khélifa T,Beck WT

更新日期：1999-03-01 00:00:00

abstract：:Labeled histidine was taken up into rat leukemic basophil 2H3 cells by a system with high affinity for histidine and then decarboxylated to form histamine. Uptake was partially inhibited and decarboxylation was completely blocked by alpha-fluoromethylhistidine (alpha-FMH) at concentrations of 10-100 microM. alpha-FMH ...

journal_title：Molecular pharmacology

authors： WoldeMussie E,Beaven MA

更新日期：1985-08-01 00:00:00

abstract：:This study demonstrates the presence of a novel endothelin (ET) receptor subtype that displays high affinity for both ETA- and ETB-selective ligands. This subtype has been identified in canine spleen membranes using ETB-selective agonists ET-3, IRL-1620, sarafotoxin 6c (S6c) as well as ETA-selective antagonists BQ123 ...

journal_title：Molecular pharmacology

authors： Nambi P,Pullen M,Kincaid J,Nuthulaganti P,Aiyar N,Brooks DP,Gellai M,Kumar C

更新日期：1997-10-01 00:00:00

abstract：:Thiopurine methyltransferase (TPMT) catalyzes the S-methylation of thiopurine drugs such as 6-mercaptopurine. Levels of TPMT activity in human tissue are controlled by a common genetic polymorphism that is an important factor responsible for individual variation in thiopurine drug toxicity and therapeutic efficacy. Ou...

journal_title：Molecular pharmacology

authors： Honchel R,Aksoy IA,Szumlanski C,Wood TC,Otterness DM,Wieben ED,Weinshilboum RM

更新日期：1993-06-01 00:00:00

abstract：:The thiazolidinediones are a class of antidiabetic compounds that increase the sensitivity of target tissues to insulin. An earlier study has shown that these compounds enhance the insulin-stimulated differentiation of 3T3-L1 cells and up-regulate expression of differentiation-dependent genes. We have observed that th...

journal_title：Molecular pharmacology

authors： Harris PK,Kletzien RF

更新日期：1994-03-01 00:00:00

abstract：:We present a mechanism for agonist-promoted alpha(2A)-adrenergic receptor (alpha(2A)-AR) activation based on structural, pharmacological, and theoretical evidence of the interactions between phenethylamine ligands and alpha(2A)-AR. In this study, we have: 1) isolated enantiomerically pure phenethylamines that differ b...

journal_title：Molecular pharmacology

authors： Nyrönen T,Pihlavisto M,Peltonen JM,Hoffrén AM,Varis M,Salminen T,Wurster S,Marjamäki A,Kanerva L,Katainen E,Laaksonen L,Savola JM,Scheinin M,Johnson MS

更新日期：2001-05-01 00:00:00

abstract：:Recently we demonstrated that the effects of beta 2-adrenoceptor (AR) stimulation to augment Ca2+ current (ICa), cytosolic Ca2+ (Cai) transients, and contractility in rat ventricular myocytes are largely dissociated from its effect to increase cellular cAMP levels. This result suggested that beta 2ARs might be coupled...

journal_title：Molecular pharmacology

authors： Xiao RP,Ji X,Lakatta EG

更新日期：1995-02-01 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：:The retinoid-related orphan receptors (RORs) and liver X receptors (LXRs) were postulated to have distinct functions. RORs play a role in tissue development and circadian rhythm, whereas LXRs are sterol sensors that affect lipid homeostasis. In this study, we revealed a novel function of RORalpha (NR1F1) in regulating...

journal_title：Molecular pharmacology

authors： Wada T,Kang HS,Angers M,Gong H,Bhatia S,Khadem S,Ren S,Ellis E,Strom SC,Jetten AM,Xie W

更新日期：2008-03-01 00:00:00

abstract：:Mouse embryonic spinal cord neurons in culture exhibit spontaneous calcium oscillations from day in vitro (DIV) 6 through DIV 10. Such spontaneous activity in developing spinal cord contributes to maturation of synapses and development of pattern-generating circuits. Here we demonstrate that these calcium oscillations...

journal_title：Molecular pharmacology

authors： Kelamangalath L,Dravid SM,George J,Aldrich JV,Murray TF

更新日期：2011-06-01 00:00:00

abstract：:The nuclear pregnane X receptor (PXR) and constitutive androstane receptor (CAR) play central roles in protecting the body against environmental chemicals (xenobiotics). PXR and CAR are activated by a wide range of xenobiotics and regulate cytochrome P450 and other genes whose products are involved in the detoxificati...

journal_title：Molecular pharmacology

authors： Maglich JM,Stoltz CM,Goodwin B,Hawkins-Brown D,Moore JT,Kliewer SA

更新日期：2002-09-01 00:00:00

abstract：:The N-methyl-D-aspartate (NMDA)-sensitive glutamate receptors are known to be inhibited by 3-amino-1-hydroxy-2-pyrrolidone (HA-966) and 7-chlorokynurenic acid (Cl-KYN), which act at the glycine-regulated allosteric modulatory center. In this work we show that, in synaptic membranes prepared from rat brain, Cl-KYN and ...

journal_title：Molecular pharmacology

authors： Danysz W,Fadda E,Wroblewski JT,Costa E

更新日期：1989-12-01 00:00:00

abstract：:Cell-penetrating peptides are amphipathic or cationic oligopeptides able to transport covalently attached cargoes across cell membranes. Peptide aptamers are polypeptide fragments of endogenous proteins that mimic and thus perturb interactions with other cellular proteins. Combining aptamer and CPP technology can gene...

journal_title：Molecular pharmacology

authors： Eiden LE

更新日期：2005-04-01 00:00:00

abstract：:1-[6-[[(17beta)-3-methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrrole-2,5-dione (U73122) is widely used to inhibit phospholipase C (PLC)-mediated signaling, but we and others have also reported a PLC-independent block of Kir3 channels in native cells. To elaborate on this major side effect, we examined the acti...

journal_title：Molecular pharmacology

authors： Klose A,Huth T,Alzheimer C

更新日期：2008-11-01 00:00:00

abstract：:alpha2-Adrenergic receptor (alpha(2)-AR) activation in the pregnant rat myometrium at midterm potentiates beta(2)-AR stimulation of adenylyl cyclase (AC) via Gbetagamma regulation of the type II isoform of adenylyl cyclase. However, at term, alpha(2)-AR activation inhibits beta(2)-AR stimulation of AC. This phenomenon...

journal_title：Molecular pharmacology

authors： Limon-Boulez I,Bouet-Alard R,Gettys TW,Lanier SM,Maltier JP,Legrand C

更新日期：2001-02-01 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：:Beta-L-dioxolane-cytidine (L-OddC, BCH-4556, Troxacitabine), a novel L-configuration deoxycytidine analog, is under phase III clinical trial for cancer treatment. We showed that human apurinic/apyrimidinic endonuclease (APE-1) has exonuclease activity for preferentially removing L-OddC and other L-configuration nucleo...

journal_title：Molecular pharmacology

authors： Lam W,Park SY,Leung CH,Cheng YC

更新日期：2006-05-01 00:00:00

abstract：:Multidrug resistance-associated protein 1 (Mrp1; Abcc1) is expressed in sarcolemma of murine heart, where it probably protects the cardiomyocyte by mediating efflux of endo- and xenobiotics. We used doxorubicin (DOX), a chemotherapeutic drug known to induce oxidative stress and thereby cardiac injury, as a model cardi...

journal_title：Molecular pharmacology

authors： Jungsuwadee P,Nithipongvanitch R,Chen Y,Oberley TD,Butterfield DA,St Clair DK,Vore M

更新日期：2009-05-01 00:00:00

abstract：:A1 adenosine receptors in bovine cerebral cortex have been solubilized and subjected to sedimentation analysis using sucrose density gradient centrifugation. Because the receptors bound both agonists and antagonists with high affinity after solubilization, receptors labeled with an agonist or an antagonist radioligand...

journal_title：Molecular pharmacology

authors： Leung E,Green RD

更新日期：1989-09-01 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：:Multiple lines of evidence indicate that the platinum-containing cancer drugs enter cells, are distributed to various subcellular compartments, and are exported from cells via transporters that evolved to manage copper homeostasis. The cytotoxicity of the platinum drugs is directly related to how much drug enters the ...

journal_title：Molecular pharmacology

authors： Howell SB,Safaei R,Larson CA,Sailor MJ

更新日期：2010-06-01 00:00:00

abstract：:A series of aminotriarylmethane dyes were examined for binding to the nicotinic acetylcholine receptor (AChR) from Torpedo californica. Several compounds were found to bind to the noncompetitive antagonist site of the AChR as demonstrated by inhibition of [3H]phencyclidine binding; apparent KD values ranged from 50 nM...

journal_title：Molecular pharmacology

authors： Lurtz MM,Pedersen SE

更新日期：1999-01-01 00:00:00

abstract：:Acute cannabidiol treatment of mice inactivated hepatic microsomal cytochrome P-450IIIA (P-450IIIA) and markedly inhibited in vitro cannabinoid metabolism. Antibodies raised against purified P-450IIIA inhibited the microsomal formation of quantitatively minor cannabinoid metabolites but had no effect on the major meta...

journal_title：Molecular pharmacology

authors： Bornheim LM,Correia MA

更新日期：1991-08-01 00:00:00

abstract：:The effects of saturating concentrations of DDT [1,1,1-trichloro-2,2-bis(p-chlorophenyl)ethane] and the pyrethroid insecticides cismethrin and deltamethrin on alkaloid-dependent activation of the voltage-sensitive sodium channel were studied using measurements of 22Na+ uptake into mouse brain synaptosomes. In survey e...

journal_title：Molecular pharmacology

authors： Bloomquist JR,Soderlund DM

更新日期：1988-05-01 00:00:00

abstract：:Exposure to hepatitis C virus (HCV) can lead to the development of cirrhosis and hepatocellular carcinoma. To examine the effects of long-term HCV infection on hepatic cytochrome P450 1A1 (CYP1A1) expression and function, we used a human hepatoma cell line expressing the HCV subgenomic replicon (Huh.8) to evaluate CYP...

journal_title：Molecular pharmacology

authors： Anderson GR,Hasan A,Yin H,Qadri I,Quattrochi LC

更新日期：2006-09-01 00:00:00

abstract：:Our laboratory recently isolated and sequenced cDNAs encoding the microsomal flavin-containing monooxygenases (FMOs) from rabbit liver and rabbit lung. As a first step in understanding the molecular bases for the catalytic and physical differences between these enzymes, we have expressed them in COS-1 cells and compar...

journal_title：Molecular pharmacology

authors： Lawton MP,Kronbach T,Johnson EF,Philpot RM

更新日期：1991-11-01 00:00:00

abstract：:Potassium channels play fundamental roles in physiology. Chemically diverse drugs bind in the pore region of K+ channels. Here, we homology-modeled voltage- and Ca2+-gated K+ channel BK and voltage-gated Kv1.3 using the X-ray structures of MthK and Kv1.2, respectively, and simulated the binding of d-tubocurarine in th...

journal_title：Molecular pharmacology

authors： Rossokhin A,Teodorescu G,Grissmer S,Zhorov BS

更新日期：2006-04-01 00:00:00