The anti-yellow fever virus activity of ribavirin is independent of error-prone replication.

abstract：:There is no approved means to prevent the toxic actions of cocaine. Cocaine esterase (CocE) is found in a rhodococcal strain of bacteria that grows in the rhizosphere soil around the coca plant and has been found to hydrolyze cocaine in vitro. The esteratic activity of CocE (0.1-1.0 mg, i.v.) was characterized and con...

journal_title：Molecular pharmacology

authors： Cooper ZD,Narasimhan D,Sunahara RK,Mierzejewski P,Jutkiewicz EM,Larsen NA,Wilson IA,Landry DW,Woods JH

更新日期：2006-12-01 00:00:00

abstract：:Using cultured airway smooth muscle cells, we showed previously that the platelet-derived growth factor (PDGF) receptor uses the G-protein, G(i), to stimulate Grb-2-associated phosphoinositide 3-kinase (PI3K) activity. We also showed that this was an intermediate step in the activation of p42/p44 mitogen-activated pro...

journal_title：Molecular pharmacology

authors： Rakhit S,Pyne S,Pyne NJ

更新日期：2000-08-01 00:00:00

abstract：:Seven transmembrane G protein-coupled receptors (GPCRs) are often phosphorylated at the C terminus and on intracellular loops in response to various extracellular stimuli. Phosphorylation of GPCRs by GPCR kinases and certain other kinases can promote the recruitment of arrestin molecules. The arrestins critically regu...

journal_title：Molecular pharmacology

authors： Yang Z,Yang F,Zhang D,Liu Z,Lin A,Liu C,Xiao P,Yu X,Sun JP

更新日期：2017-09-01 00:00:00

abstract：:Aspartyl aminopeptidase (DNPEP) has been implicated in the control of angiotensin signaling and endosome trafficking, but its precise biologic roles remain incompletely defined. We performed a high-throughput screen of ∼25,000 small molecules to identify inhibitors of DNPEP for use as tools to study its biologic funct...

journal_title：Molecular pharmacology

authors： Chen Y,Tang H,Seibel W,Papoian R,Oh K,Li X,Zhang J,Golczak M,Palczewski K,Kiser PD

更新日期：2014-08-01 00:00:00

abstract：:Cocaine use poses a major health problem not only because of the dependence it causes but also because of the generation of life-threatening cardiac arrhythmias following overdose. Elucidating the molecular mechanisms of action of cocaine, therefore, remains a critical step in developing treatment for cocaine addictio...

journal_title：Molecular pharmacology

authors： Premkumar LS

更新日期：1999-12-01 00:00:00

abstract：:We describe the structural and functional features of the human alpha3 nicotinic receptor subunit promoter. A 0.35-kb region immediately upstream of the start codon was identified that when transfected in human neuroblastoma cells was able to drive the expression of the luciferase reporter gene with a strength compara...

journal_title：Molecular pharmacology

authors： Fornasari D,Battaglioli E,Flora A,Terzano S,Clementi F

更新日期：1997-02-01 00:00:00

abstract：:The firmest candidate among the transmembrane portions of the nicotinic acetylcholine receptor (AChR) to be in contact with the lipid bilayer is the fourth segment, M4. To explore the contribution of alphaM4 amino acid residues of mouse AChR to channel gating, we combined site-directed mutagenesis with single-channel ...

journal_title：Molecular pharmacology

authors： Bouzat C,Roccamo AM,Garbus I,Barrantes FJ

更新日期：1998-07-01 00:00:00

abstract：:Ethanol (ETOH) can cause apoptotic death of neurons by depleting GSH with an associated increase in oxidative stress. The current study illustrates a means to overcome this ETOH-induced neurotoxicity by enhancing GSH through boosting Nrf2, a transcription factor that controls GSH homeostasis. ETOH treatment caused a s...

journal_title：Molecular pharmacology

authors： Narasimhan M,Mahimainathan L,Rathinam ML,Riar AK,Henderson GI

更新日期：2011-12-01 00:00:00

abstract：:The CB1 cannabinoid receptor has been implicated in the regulation of bone remodeling and bone mass. A high bone mass (HBM) phenotype was reported in CB1-null mice generated on a CD1 background (CD1(CB1-/-) mice). By contrast, our preliminary studies in cb1-/- mice, backcrossed to C57BL/6J mice (C57(CB1-/-) mice), rev...

journal_title：Molecular pharmacology

authors： Tam J,Ofek O,Fride E,Ledent C,Gabet Y,Müller R,Zimmer A,Mackie K,Mechoulam R,Shohami E,Bab I

更新日期：2006-09-01 00:00:00

abstract：:Hepatocyte nuclear factor 4alpha (HNF4alpha) is a key transcription factor for the constitutive expression of cytochromes P450 (P450s) in the liver. However, human hepatoma HepG2 cells show a high level of HNF4alpha but express only marginal P450 levels. We found that the HNF4alpha-mediated P450 transcription in HepG2...

journal_title：Molecular pharmacology

authors： Martínez-Jiménez CP,Castell JV,Gómez-Lechón MJ,Jover R

更新日期：2006-11-01 00:00:00

abstract：:To identify novel factors or mechanisms that are important for the resistance of tissues to chemical toxicity, we have determined the mechanisms underlying the previously observed increases in resistance to acetaminophen (APAP) toxicity in the lateral nasal gland (LNG) of the male Cyp2g1-null/Cyp2a5-low mouse. Initial...

journal_title：Molecular pharmacology

authors： Zhou X,Wei Y,Xie F,Laukaitis CM,Karn RC,Kluetzman K,Gu J,Zhang QY,Roberts DW,Ding X

更新日期：2011-04-01 00:00:00

abstract：:We have investigated the effect of chronic flurazepam HCl treatment on the gamma-aminobutyric acid (GABA)A receptor complex in cultured mammalian cortical neurons. Chronic flurazepam (1-5 microM, for 1-10 days) treatment did not produce any changes in the morphological appearance or the cell protein content of cortica...

journal_title：Molecular pharmacology

authors： Hu XJ,Ticku MK

更新日期：1994-04-01 00:00:00

abstract：:Prostate cancer is a highly heterogenous disease in which a patient-tailored care program is much desired. Central to this goal is the development of novel targeted pharmacological interventions. To develop these treatment strategies, an understanding of the integration of cellular pathways involved in both tumorigene...

journal_title：Molecular pharmacology

authors： Assinder SJ,Dong Q,Mangs H,Richardson DR

更新日期：2009-03-01 00:00:00

abstract：:The recent molecular cloning of the genes encoding three somatostatin (SRIF) receptor subtypes has allowed for the individual expression of these receptors in mammalian cells and characterization of their respective pharmacological profiles. In the present study, we have investigated the affinities of a battery of SRI...

journal_title：Molecular pharmacology

authors： Raynor K,Murphy WA,Coy DH,Taylor JE,Moreau JP,Yasuda K,Bell GI,Reisine T

更新日期：1993-06-01 00:00:00

abstract：:We investigated the mechanisms of MDR1 gene activation by CCAAT/enhancer binding protein beta (C/EBPbeta, or nuclear factor for interleukin 6) in human cancer cells. Transfection of the breast cancer cell line MCF-7 and its doxorubicin-selected variant MCF-7/ADR by either C/EBPbeta or C/EBPbeta-LIP (a dominant-negativ...

journal_title：Molecular pharmacology

authors： Chen KG,Sale S,Tan T,Ermoian RP,Sikic BI

更新日期：2004-04-01 00:00:00

abstract：:The decrease in mu-opioid receptor activity after chronic agonist exposure (1 microM [D-Ala(2),N-MePhe(4),Gly-ol(5)]-enkephalin) is largely due to kinase-mediated phosphorylation of intracellular receptor domains. We have recently shown that the substitution of two putative Ca(2+)/calmodulin-dependent protein kinase I...

journal_title：Molecular pharmacology

authors： Koch T,Kroslak T,Averbeck M,Mayer P,Schröder H,Raulf E,Höllt V

更新日期：2000-08-01 00:00:00

abstract：:It is established that agmatine, an endogenously formed decarboxylated arginine, is a weak competitive inhibitor of neuronal nitric-oxide synthase (nNOS) with an apparent Ki value of 660 microM [Biochem J 316:247-249, 1996]. Although agmatine is known to bind to alpha-adrenergic and imidazoline receptors, it has been ...

journal_title：Molecular pharmacology

authors： Demady DR,Jianmongkol S,Vuletich JL,Bender AT,Osawa Y

更新日期：2001-01-01 00:00:00

abstract：:The aim of this study was to create and characterize constitutively active mutant (CAM) histamine H(1) receptors (H(1)R) using random mutagenesis methods to further investigate the activation process of the rhodopsin-like family of G protein-coupled receptors (GPCRs). This approach identified position 6.40 in TM 6 as ...

journal_title：Molecular pharmacology

authors： Bakker RA,Jongejan A,Sansuk K,Hacksell U,Timmerman H,Brann MR,Weiner DM,Pardo L,Leurs R

更新日期：2008-01-01 00:00:00

abstract：:All-trans-retinoic acid (atRA) is the active metabolite of vitamin A. atRA is also used as a drug, and synthetic atRA analogs and inhibitors of retinoic acid (RA) metabolism have been developed. The hepatic clearance of atRA is mediated primarily by CYP26A1, but design of CYP26A1 inhibitors is hindered by lack of info...

journal_title：Molecular pharmacology

authors： Thatcher JE,Buttrick B,Shaffer SA,Shimshoni JA,Goodlett DR,Nelson WL,Isoherranen N

更新日期：2011-08-01 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：:Equilibrative nucleoside transporters (ENTs) 1 and 2 facilitate nucleoside transport across the blood-testis barrier (BTB). Improving drug entry into the testes with drugs that use endogenous transport pathways may lead to more effective treatments for diseases within the reproductive tract. In this study, CRISPR/CRIS...

journal_title：Molecular pharmacology

authors： Miller SR,Zhang X,Hau RK,Jilek JL,Jennings EQ,Galligan JJ,Foil DH,Zorn KM,Ekins S,Wright SH,Cherrington NJ

更新日期：2021-02-01 00:00:00

abstract：:A Walker 256 rat carcinoma cell line (WR) has been shown to be resistant to a broad spectrum of bifunctional nitrogen mustards (NM) in cell culture. The parent cell line (WS) from which the WR cells were selected retains marked sensitivity to this class of drugs. Karyotype analysis showed that the parent WS had a chro...

journal_title：Molecular pharmacology

authors： Tew KD,Wang AL

更新日期：1982-05-01 00:00:00

abstract：:C57BL/6J (C57) and DBA/JBOMf (DBA) mice were used to study the role of adipose tissue as a modifier of tissue distribution, biological effects, and elimination of a lipophilic foreign chemical, 2,4,5,2',4',5'-hexachlorobiphenyl (HCB). As an indication of biological potency of the model compound, the activities of hepa...

journal_title：Molecular pharmacology

authors： Ahotupa M,Mäntylä E

更新日期：1983-11-01 00:00:00

abstract：:Cardiac-directed expression of AC6 has pronounced favorable effects on cardiac function possibly not linked with cAMP production. To determine rigorously whether cAMP generation is required for the beneficial effects of increased AC6 expression, we generated a catalytically inactive AC6 mutant (AC6mut) that has marked...

journal_title：Molecular pharmacology

authors： Gao MH,Tang T,Lai NC,Miyanohara A,Guo T,Tang R,Firth AL,Yuan JX,Hammond HK

更新日期：2011-03-01 00:00:00

abstract：:Thromboxane A2 stimulation of smooth muscle cells contributes to the development of vascular lesions after percutaneous transluminal coronary angioplasty. In view of this, we examined the signaling pathways stimulated by a thromboxane receptor agonist, U-46619, in cultures of rat aortic smooth muscle cells. Treatment ...

journal_title：Molecular pharmacology

authors： Jones DA,Benjamin CW,Linseman DA

更新日期：1995-11-01 00:00:00

abstract：:Voltage-gated sodium channels are inhibited by many local anesthetics, antiarrhythmics, and antiepileptic drugs. The local anesthetic lidocaine appears to be able to access its binding site in the sodium channel only from the membrane phase or from the internal face of the channel. In contrast, the antiepileptic drug ...

journal_title：Molecular pharmacology

authors： Jo S,Bean BP

更新日期：2014-02-01 00:00:00

abstract：:Maurotoxin (MTX) is a potent blocker of human voltage-activated Kv1.2 and intermediate-conductance calcium-activated potassium channels, hIKCa1. Because its blocking affinity on both channels is similar, although the pore region of these channels show only few conserved amino acids, we aimed to characterize the bindin...

journal_title：Molecular pharmacology

authors： Visan V,Fajloun Z,Sabatier JM,Grissmer S

更新日期：2004-11-01 00:00:00

abstract：:The anti-arrhythmic quinidine has been reported to be a competitive inhibitor of the catalytic activities of human liver P-450DB, including sparteine delta 2-oxidation and bufuralol 1'-hydroxylation, and we confirmed the observation that submicromolar concentrations are strongly inhibitory. Human liver microsomes oxid...

journal_title：Molecular pharmacology

authors： Guengerich FP,Müller-Enoch D,Blair IA

更新日期：1986-09-01 00:00:00

abstract：:We have investigated various nitric oxide (NO) synthase inhibitors for their affinity and selectivity toward the three human isoenzymes in radioligand binding experiments. Therefore, we developed the new radioligand [(3)H]2-amino-4-picoline to measure binding of these compounds to the three human NO synthase (NOS) iso...

journal_title：Molecular pharmacology

authors： Boer R,Ulrich WR,Klein T,Mirau B,Haas S,Baur I

更新日期：2000-11-01 00:00:00

abstract：:The ligand recognition site of A2a-adenosine receptors in rabbit striatal membranes was probed using non-site-directed labeling reagents and specific affinity labels. Exposure of membranes to diethylpyrocarbonate at a concentration of 2.5 mM, followed by washing, was found to inhibit the binding of [3H]CGS 21680 and [...

journal_title：Molecular pharmacology

authors： Jacobson KA,Stiles GL,Ji XD

更新日期：1992-07-01 00:00:00