Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species.

abstract：:In the search for 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives, we have found 6-benzyl-1-(ethoxymethyl)-5-isopropyl-uracil (MKC-442) to be a highly potent and selective inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). The IC50 value of MKC-442 for HIV-1 RT was 8 nM....

journal_title：Molecular pharmacology

authors： Yuasa S,Sadakata Y,Takashima H,Sekiya K,Inouye N,Ubasawa M,Baba M

更新日期：1993-10-01 00:00:00

abstract：:Fusion proteins were generated between the human 5-hydroxytryptamine (5-HT)(1A) receptor and both wild-type (Cys(351)) and pertussis toxin-resistant (Gly(351) and Ile(351)) forms of G(i1). These were expressed stably. Pertussis toxin treatment substantially reduced basal high-affinity GTPase activity in clones express...

journal_title：Molecular pharmacology

authors： Kellett E,Carr IC,Milligan G

更新日期：1999-10-01 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：:The anti-human immunodeficiency virus (-HIV) nucleoside analogs azidothymidine (AZT), dideoxycytidine (ddC), dideoxyinosine (ddl), dideoxydidehydrothymidine (D4T), and dideoxydidehydrocytidine (D4C) and the anticancer drug cytosine arabinoside (AraC) were compared for their effects on the mitochondrial DNA (mtDNA) con...

journal_title：Molecular pharmacology

authors： Chen CH,Vazquez-Padua M,Cheng YC

更新日期：1991-05-01 00:00:00

abstract：:The nicotinic acetylcholine receptor (nAChR) belongs to a superfamily of pentameric ligand-gated ion channels involved in many physiologic and pathologic processes. Among nAChRs, receptors comprising the α7 subunit are unique because of their high Ca(2+) permeability and fast desensitization. nAChR agonists elicit a t...

journal_title：Molecular pharmacology

authors： Corradi J,Bouzat C

更新日期：2016-09-01 00:00:00

abstract：:The aryl hydrocarbon receptor (AHR) and its DNA binding partner, the AHR nuclear translocator (ARNT), are basic helix-loop-helix transcription factors that mediate many of the toxic and carcinogenic effects of polyhalogenated aromatic hydrocarbons. The basic regions of the AHR and ARNT contact the GCGTG recognition si...

journal_title：Molecular pharmacology

authors： Swanson HI,Yang JH

更新日期：1998-10-01 00:00:00

abstract：:The in vitro binding of [3H]LY354740, the first high affinity group II-selective metabotropic glutamate (mGlu) receptor radioligand, was characterized in rat cortical, hippocampal, and thalamic membranes as well as in rat brain sections. [3H]LY354740 binding was saturable in all regions investigated. Nonspecific bindi...

journal_title：Molecular pharmacology

authors： Schaffhauser H,Richards JG,Cartmell J,Chaboz S,Kemp JA,Klingelschmidt A,Messer J,Stadler H,Woltering T,Mutel V

更新日期：1998-02-01 00:00:00

abstract：:One-electron oxidation of several derivatives of pyrazolin-5-one, including the drug antipyrine, were studied by pulse radiolysis of aqueous solutions. All the compounds were found to be oxidized by Br2 rapidly (k approximately 3 X 10(8)-2 X 10(9) M-1 s-1) but considerably more slowly by weaker oxidants, such as perox...

journal_title：Molecular pharmacology

authors： Jovanovic SV,Neta P,Simic MG

更新日期：1985-10-01 00:00:00

abstract：:The presence and properties of the Ah receptor were examined in the guinea pig, rat, hamster, monkey, and three different strains of mice. These species and strains have demonstrated differences in sensitivity and variability of response to 2,3,7,8-tetrachlorodibenzo-p-dioxin and related compounds. All species examine...

journal_title：Molecular pharmacology

authors： Gasiewicz TA,Rucci G

更新日期：1984-07-01 00:00:00

abstract：:The therapeutic potential of antitumor drugs is seriously limited by the manifestation of cellular drug resistance. We used the budding yeast Saccharomyces cerevisiae as a model system to identify novel mechanisms of resistance to one of the most active anticancer agents, cisplatin. We pinpointed NPR2 (nitrogen permea...

journal_title：Molecular pharmacology

authors： Schenk PW,Brok M,Boersma AW,Brandsma JA,Den Dulk H,Burger H,Stoter G,Brouwer J,Nooter K

更新日期：2003-08-01 00:00:00

abstract：:Ligands that selectively inhibit human α3β2 and α6β2 nicotinic acetylcholine receptor (nAChRs) and not the closely related α3β4 and α6β4 subtypes are lacking. Current α-conotoxins (α-Ctxs) that discriminate among these nAChR subtypes in rat fail to discriminate among the human receptor homologs. In this study, we desc...

journal_title：Molecular pharmacology

authors： Hone AJ,McIntosh JM,Azam L,Lindstrom J,Lucero L,Whiteaker P,Passas J,Blázquez J,Albillos A

更新日期：2015-11-01 00:00:00

abstract：:Organic anion transporter-1 (OAT1) mediates the body disposition of a diverse array of clinically important drugs, including anti-HIV therapeutics, antitumor drugs, antibiotics, antihypertensives, and anti-inflammatories. Therefore, understanding the regulation of OAT1 has profound clinical significance. We previously...

journal_title：Molecular pharmacology

authors： Li S,Zhang Q,You G

更新日期：2013-07-01 00:00:00

abstract：:It is widely accepted that cAMP signaling is compartmentalized within cells. However, our knowledge of how receptors, cAMP signaling enzymes, effectors, and other key proteins form specific signaling complexes to regulate specific cell responses is limited. The multicomponent nature of these systems and the spatiotemp...

journal_title：Molecular pharmacology

authors： Johnstone TB,Agarwal SR,Harvey RD,Ostrom RS

更新日期：2018-04-01 00:00:00

abstract：:A collection of analogues of atrial natriuretic peptide (ANP) were screened for their ability to inhibit ANP-induced cGMP stimulation. The antagonists revealed through this screen are structurally related; almost all are substituted at either aspartate-13 or phenylalanine-26. This tendency is consistent throughout sev...

journal_title：Molecular pharmacology

authors： von Geldern TW,Budzik GP,Dillon TP,Holleman WH,Holst MA,Kiso Y,Novosad EI,Opgenorth TJ,Rockway TW,Thomas AM

更新日期：1990-12-01 00:00:00

abstract：:Fusion proteins between the human 5-hydroxytryptamine (5-HT)(1A) receptor and either wild type or certain pertussis toxin-resistant forms of G(o1)alpha and G(i1)alpha display constitutive GTPase activity that can be inhibited by the inverse agonist spiperone. Addition of recombinant regulator of G protein signaling (R...

journal_title：Molecular pharmacology

authors： Welsby PJ,Kellett E,Wilkinson G,Milligan G

更新日期：2002-05-01 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：:β-Adrenergic receptor blockers (β-blockers) are commonly used to treat heart failure, but the biologic mechanisms governing their efficacy are still poorly understood. The complexity of β-adrenergic signaling coupled with the influence of receptor polymorphisms makes it difficult to intuit the effect of β-blockers on ...

journal_title：Molecular pharmacology

authors： Amanfu RK,Saucerman JJ

更新日期：2014-08-01 00:00:00

abstract：:G-protein-coupled receptor activation is generally analyzed under equilibrium conditions. However, real-life receptor functions are often dependent on very short, transient stimuli that may not allow the achievement of a steady state. This is particularly true for synaptic receptors such as the α(2A)-adrenergic recept...

journal_title：Molecular pharmacology

authors： Ambrosio M,Lohse MJ

更新日期：2012-06-01 00:00:00

abstract：:The two forms of pituitary adenylate cyclase-activating polypeptide, PACAP27 and PACAP38, are two neuropeptide hormones related to the vasoactive intestinal peptide/secretin/ glucagon family of peptides. PACAP receptors that are positively coupled to adenylyl cyclase and phospholipase C have been identified in culture...

journal_title：Molecular pharmacology

authors： Cavallaro S,Copani A,D'Agata V,Musco S,Petralia S,Ventra C,Stivala F,Travali S,Canonico PL

更新日期：1996-07-01 00:00:00

abstract：:The availability of high-affinity agonists for peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta) has led to significant advances in our understanding of the functional role of PPARbeta/delta. In this study, a new PPARbeta/delta antagonist, 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethy...

journal_title：Molecular pharmacology

authors： Palkar PS,Borland MG,Naruhn S,Ferry CH,Lee C,Sk UH,Sharma AK,Amin S,Murray IA,Anderson CR,Perdew GH,Gonzalez FJ,Müller R,Peters JM

更新日期：2010-09-01 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：:The effect of cyanomorpholinyldoxorubicin, morpholinyldoxorubicin, doxorubicin, and Actinomycin D were studied on purified mouse leukemia (L1210) DNA topoisomerases I and II. DNA unwinding and cross-linking were also studied. It was found that 1) morpholinyldoxorubicin, cyanomorpholinyldoxorubicin, and Actinomycin D (...

journal_title：Molecular pharmacology

authors： Wassermann K,Markovits J,Jaxel C,Capranico G,Kohn KW,Pommier Y

更新日期：1990-07-01 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：:Platelet-activating factor (PAF) receptor-coupled activation of phosphoinositide-specific phospholipase C (PLC) was studied in platelets that were made refractory, by short-term pretreatments, to either PAF or thrombin. Generation of [3H]inositol triphosphate ( [3H]IP3) was monitored specifically for this purpose. [3H...

journal_title：Molecular pharmacology

authors： Morrison WJ,Shukla SD

更新日期：1988-01-01 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, inositol hexakisphosphate (phytic acid) was shown to bind to photoreceptor arrestin and block its interaction with rhodopsin. Such an interaction might predict that inositol polyphosphates could alter G protein-coupled receptor desensitization. To investigate the possible roles of higher inositol polyphospha...

journal_title：Molecular pharmacology

authors： Sasakawa N,Ferguson JE,Sharif M,Hanley MR

更新日期：1994-08-01 00:00:00

abstract：:The mechanisms underlying mastoparan-induced elevation of the intracellular free calcium concentration ([Ca2+]i) were investigated in the insulin-secreting cell lines RINm5F and HIT. In both cell types, micromolar concentrations of mastoparan induced a prompt increase of [Ca2+]i, measured as an increase in fura-2 fluo...

journal_title：Molecular pharmacology

authors： Eddlestone GT,Komatsu M,Shen L,Sharp GW

更新日期：1995-04-01 00:00:00

abstract：:We have previously identified allosteric modulators of the cannabinoid CB(1) receptor (Org 27569, PSNCBAM-1) that display a contradictory pharmacological profile: increasing the specific binding of the CB(1) receptor agonist [(3)H]CP55940 but producing a decrease in CB(1) receptor agonist efficacy. Here we investigate...

journal_title：Molecular pharmacology

authors： Baillie GL,Horswill JG,Anavi-Goffer S,Reggio PH,Bolognini D,Abood ME,McAllister S,Strange PG,Stephens GJ,Pertwee RG,Ross RA

更新日期：2013-02-01 00:00:00

abstract：:The phosphorylation of μ-opioid receptors (MOPRs) by G protein-coupled receptor kinases (GRKs), followed by arrestin binding, is thought to be a key pathway leading to desensitization and internalization. The present study used the combination of intracellular and whole-cell recordings from rats and mice, as well as l...

journal_title：Molecular pharmacology

authors： Arttamangkul S,Lau EK,Lu HW,Williams JT

更新日期：2012-03-01 00:00:00

abstract：:We have studied the mechanism of action of Arg(*)-Arg-Nal(2)-Cys(1x)-Tyr-Gln-Lys-(d-Pro)-Pro-Tyr-Arg-Cit-Cys(1x)-Arg-Gly-(d-Pro)(*) (POL3026), a novel specific beta-hairpin mimetic CXC chemokine receptor (CXCR)4 antagonist. POL3026 specifically blocked the binding of anti-CXCR4 monoclonal antibody 12G5 and the intrace...

journal_title：Molecular pharmacology

authors： Moncunill G,Armand-Ugón M,Clotet-Codina I,Pauls E,Ballana E,Llano A,Romagnoli B,Vrijbloed JW,Gombert FO,Clotet B,De Marco S,Esté JA

更新日期：2008-04-01 00:00:00