Functional coupling of the beta 2-adrenoceptor to a pertussis toxin-sensitive G protein in cardiac myocytes.

abstract：:We previously described the development of genetic models to study the in vivo functions of the hepatic cytochrome P450 (P450) system, through the hepatic deletion of either cytochrome P450 oxidoreductase [POR; HRN (hepatic reductase null) line] or cytochrome b(5) [HBN (hepatic cytochrome b(5) null) line]. However, HR...

journal_title：Molecular pharmacology

authors： Henderson CJ,McLaughlin LA,Wolf CR

更新日期：2013-06-01 00:00:00

abstract：:Stimulation of beta2-adrenoceptors with the selective beta2 agonist procaterol caused a biphasic decrease in cell surface M2 muscarinic receptor number in human embryonic lung 299 cells when measured with the hydrophilic antagonist [3H]N-methylscopolamine. In contrast, total muscarinic receptor number, measured with t...

journal_title：Molecular pharmacology

authors： Rousell J,Haddad EB,Mak JC,Webb BL,Giembycz MA,Barnes PJ

更新日期：1996-04-01 00:00:00

abstract：:Ethanol-inducible CYP2E1 is an enzyme of major toxicological interest because it metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. CYP2E1 has also been implicated in alcohol liver disease because of its contribution to oxidative stress. Previously, polymorphic alleles with mutations in i...

journal_title：Molecular pharmacology

authors： Hu Y,Oscarson M,Johansson I,Yue QY,Dahl ML,Tabone M,Arincò S,Albano E,Ingelman-Sundberg M

更新日期：1997-03-01 00:00:00

abstract：:The 90-kDa heat shock family (HSP90) of protein and two-component histidine kinases, although quite distinct at the primary amino acid sequence level, share a common structural ATP-binding domain known as the Bergerat fold. The Bergerat fold is important for the ATPase activity and associated chaperone function of HSP...

journal_title：Molecular pharmacology

authors： Besant PG,Lasker MV,Bui CD,Turck CW

更新日期：2002-08-01 00:00:00

abstract：:Low-density lipoprotein (LDL) is known to be a mitogenic factor for vascular smooth muscle cells (VSMCs), fibroblasts, and endothelial cells. In the current study, we describe possible intracellular mechanisms by which LDL elicits its mitogenic effects. Stimulation of VSMCs with LDL resulted in a pertussis-toxin (PTX)...

journal_title：Molecular pharmacology

authors： Sachinidis A,Seewald S,Epping P,Seul C,Ko Y,Vetter H

更新日期：1997-09-01 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：:Aldehyde hydrogenases (ALDHs) belong to a large gene family involved in oxidation of both endogenous and exogenous compounds in mammalian tissues. Among ALDHs, the rat ALDH1A7 gene displays a curious strain dependence in phenobarbital (PB)-induced hepatic expression: the responsive RR ...

journal_title：Molecular pharmacology

authors： Touloupi K,Küblbeck J,Magklara A,Molnár F,Reinisalo M,Konstandi M,Honkakoski P,Pappas P

更新日期：2019-11-01 00:00:00

abstract：:When exposed to the beta-agonist (-)-isoproterenol, rat glioma C6 cells exhibited a time-and concentration-dependent reduction in isoproterenol responsiveness (desensitization) and a loss of beta-adrenergic receptors (down-regulation). Other agents, such as dibutyryl cyclic AMP, isobutylmethylxanthine, and cholera tox...

journal_title：Molecular pharmacology

authors： Zaremba TG,Fishman PH

更新日期：1984-09-01 00:00:00

abstract：:Anthracyclines are potent anticancer agents, but their use is limited by cardiotoxicity at high cumulative doses. The mechanisms involved in anthracycline-mediated cardiotoxicity are still poorly understood, but numerous investigations have indicated a role for iron in this process. Our previous studies using neoplast...

journal_title：Molecular pharmacology

authors： Kwok JC,Richardson DR

更新日期：2004-01-01 00:00:00

abstract：:Polyamides are a class of synthetic molecules that exhibit high-affinity, sequence-specific reversible binding in the DNA minor groove but are incapable of inducing DNA damage. In cell-free systems, polyamides have been shown to regulate gene expression by activation, repression, and antirepression. However, effective...

journal_title：Molecular pharmacology

authors： Philips BJ,Chang AY,Dervan PB,Beerman TA

更新日期：2005-03-01 00:00:00

abstract：:Typical equilibrium binding experiments cannot be quantitatively analyzed on the basis of classical mathematical equations when the receptor concentration is so high that a significant fraction of the added radioligand concentration is in the bound form. In this paper, the appropriate equations are derived and used in...

journal_title：Molecular pharmacology

authors： Swillens S

更新日期：1995-06-01 00:00:00

abstract：:The renal outer medullary potassium channel (ROMK) is expressed in the kidney tubule and critically regulates sodium and potassium balance. The physiological functions of other inward rectifying K(+) (Kir) channels expressed in the nephron, such as Kir7.1, are less well understood in part due to the lack of selective ...

journal_title：Molecular pharmacology

authors： Lewis LM,Bhave G,Chauder BA,Banerjee S,Lornsen KA,Redha R,Fallen K,Lindsley CW,Weaver CD,Denton JS

更新日期：2009-11-01 00:00:00

abstract：:The incorporation of leucine into protein was studied in Ca2+-depleted and Ca2+-restored preparations of normal liver cells isolated from fed, adult male rats. Ca2+-restored cells incorporated amino acid 5-10-fold more rapidly than did Ca2+-depleted cells for incubation periods up to 1 hr. Readdition of Ca2+ at suprap...

journal_title：Molecular pharmacology

authors： Brostrom CO,Bocckino SB,Brostrom MA,Galuska EM

更新日期：1986-01-01 00:00:00

abstract：:3H-Neurokinin A (3H-NKA) with high specific activity (75 Ci/mmol) was synthesized to study NKA (NK-2)-binding sites on membrane preparations of various tissues in the rat, including brain, spinal cord, duodenum, vas deferens, and ileum. The binding capacity of 3H-NKA (0.9 nM) was very low in membrane preparations of d...

journal_title：Molecular pharmacology

authors： Bergström L,Beaujouan JC,Torrens Y,Saffroy M,Glowinski J,Lavielle S,Chassaing G,Marquet A,D'Orleans-Juste P,Dion S

更新日期：1987-12-01 00:00:00

abstract：:2',3'-Dideoxyadenosine (ddAdo) and its deamination product 2',3'-dideoxyinosine (ddIno) (didanosine) inhibit the replication and infectivity of the human immunodeficiency virus (HIV) in a number of in vitro assay systems. Early clinical studies (phase I) have indicated a role for ddIno in the treatment of patients wit...

journal_title：Molecular pharmacology

authors： Hartman NR,Ahluwalia GS,Cooney DA,Mitsuya H,Kageyama S,Fridland A,Broder S,Johns DG

更新日期：1991-07-01 00:00:00

abstract：:In cells expressing both the insulin receptor isoform A (IRA) and the insulin-like growth factor-1 receptor (IGF1R), the presence of hybrid receptors, made up of an alphabeta-IRA chain associated with an alphabeta-IGF1R chain, has been demonstrated. These heterodimers are found in normal cells, and they also seem to p...

journal_title：Molecular pharmacology

authors： Blanquart C,Gonzalez-Yanes C,Issad T

更新日期：2006-11-01 00:00:00

abstract：:Sazetidine-A has been recently proposed to be a "silent desensitizer" of alpha4beta2 nicotinic acetylcholine receptors (nAChRs), implying that it desensitizes alpha4beta2 nAChRs without first activating them. This unusual pharmacological property of sazetidine-A makes it, potentially, an excellent research tool to dis...

journal_title：Molecular pharmacology

authors： Zwart R,Carbone AL,Moroni M,Bermudez I,Mogg AJ,Folly EA,Broad LM,Williams AC,Zhang D,Ding C,Heinz BA,Sher E

更新日期：2008-06-01 00:00:00

abstract：:Leukotriene B4 (LTB4) induced rapid breakdown of prelabeled inositol phospholipids in rat peritoneal polymorphonuclear leukocytes (PMNs). Formation of [3H]inositol triphosphate ([3H]IP3) was rapid, with a peak of 250-300% of the control level, after 5-15 sec of exposure to LTB4. Accumulation of [3H]inositol bisphospha...

journal_title：Molecular pharmacology

authors： Mong S,Chi-Rosso G,Miller J,Hoffman K,Razgaitis KA,Bender P,Crooke ST

更新日期：1986-09-01 00:00:00

abstract：:Cannabinoids have been implicated in the reduction of glioma growth. The present study investigated a possible relationship between the recently shown induction of cyclooxygenase (COX)-2 expression by the endocannabinoid analog R(+)methanandamide [R(+)-MA] and its effect on the viability of H4 human neuroglioma cells....

journal_title：Molecular pharmacology

authors： Hinz B,Ramer R,Eichele K,Weinzierl U,Brune K

更新日期：2004-12-01 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：:Multidrug resistance protein (MRP) 4 transports a variety of endogenous and xenobiotic organic anions. MRP4 is widely expressed in the body and specifically localized to the renal apical proximal tubule cell membrane, where it mediates the excretion of these compounds into urine. To characterize the MRP4 substrate-bin...

journal_title：Molecular pharmacology

authors： El-Sheikh AA,van den Heuvel JJ,Krieger E,Russel FG,Koenderink JB

更新日期：2008-10-01 00:00:00

abstract：:Adenine-uridine rich elements (AREs) play an important role in modulating mRNA stability, being the target site of many ARE-binding proteins (AUBPs) that are involved in the decay process. Three 26-mer 2'-O-methyl oligoribonucleotides (ORNs) homologous to the core region of ARE of bcl2 mRNA have been studied for decoy...

journal_title：Molecular pharmacology

authors： Bevilacqua A,Ghisolfi L,Franzi S,Maresca G,Gherzi R,Capaccioli S,Nicolin A,Canti G

更新日期：2007-02-01 00:00:00

abstract：:Bryostatin 1 and phorbol-12-myristate-13-acetate (PMA) are both potent activators of protein kinase C (PKC), although in primary mouse keratinocytes bryostatin 1 does not induce differentiation and blocks PMA-induced differentiation. We report here that in primary mouse keratinocytes PMA caused translocation of PKC-ep...

journal_title：Molecular pharmacology

authors： Szallasi Z,Denning MF,Smith CB,Dlugosz AA,Yuspa SH,Pettit GR,Blumberg PM

更新日期：1994-11-01 00:00:00

abstract：:In order to elucidate the key atoms and/or stereostructures necessary for the inhibitory emergence of aldose reductase, crystal structure determinations were carried out for 11 oxazolecarbamate analogues, which have similar chemical and physicochemical properties but different inhibitory activities. The molecular conf...

journal_title：Molecular pharmacology

authors： Ishida T,In Y,Ohishi H,Yamamoto D,Inoue M,Tanaka C,Ueno Y,Ohmomo Y,Kanda N,Tanaka A

更新日期：1988-09-01 00:00:00

abstract：:The alpha2-adrenergic receptors (alpha2-ARs) mediate signals to intracellular second messengers via guanine nucleotide binding proteins. Three human genes encoding alpha2-AR subtypes (alpha2A, alpha2B, alpha2C) have been cloned. Several chemical compounds display subtype differences in their binding and/or functional ...

journal_title：Molecular pharmacology

authors： Marjamaki A,Pihlavisto M,Cockcroft V,Heinonen P,Savola JM,Scheinin M

更新日期：1998-03-01 00:00:00

abstract：:The transient receptor potential cation channel subfamily V member 1 (TRPV1) is known as a thermosensor and integrator of inflammation-induced hyperalgesia. TRPV1 is expressed in a subpopulation of primary afferent neurons that express several different neurotransmitters. The role of the TRPV1 channel in the developme...

journal_title：Molecular pharmacology

authors： Rogoz K,Andersen HH,Kullander K,Lagerström MC

更新日期：2014-02-01 00:00:00

abstract：:The insecticide imidacloprid and structurally related neonicotinoids act selectively on insect nicotinic acetylcholine receptors (nAChRs). To investigate the mechanism of neonicotinoid selectivity, we have examined the effects of mutations to basic amino acid residues in loop D of the nAChR acetylcholine (ACh) binding...

journal_title：Molecular pharmacology

authors： Shimomura M,Yokota M,Ihara M,Akamatsu M,Sattelle DB,Matsuda K

更新日期：2006-10-01 00:00:00

abstract：:Compound BM5 [N-methyl-N(1-methyl-4-pyrrolidino-2-butynyl) acetamide] has previously been described as an agonist at postsynaptic muscarinic receptors and as an antagonist at presynaptic receptors. In the current work, we studied the ability of this compound to selectively stimulate phosphoinositide (PI) turnover in C...

journal_title：Molecular pharmacology

authors： Baumgold J,Drobnick A

更新日期：1989-09-01 00:00:00

abstract：:Anaplastic thyroid carcinoma (ATC) is among the most aggressive malignancies known and is characterized with rapid growth, early invasion, and complete refractoriness to current therapies. Here we report that triptolide, a small molecule from a Chinese herb, could potently inhibit proliferation in vitro, angiogenesis ...

journal_title：Molecular pharmacology

authors： Zhu W,Ou Y,Li Y,Xiao R,Shu M,Zhou Y,Xie J,He S,Qiu P,Yan G

更新日期：2009-04-01 00:00:00

abstract：:NAD(P):quinone acceptor oxidoreductase (quinone reductase) (DT-diaphorase, EC 1.6.99.2) is involved in the process of reductive activation of cytotoxic antitumor quinones and nitrobenzenes. In this study, we initially examined the relative abilities of mouse, rat, and human quinone reductases to reduce two prodrugs, C...

journal_title：Molecular pharmacology

authors： Chen S,Knox R,Lewis AD,Friedlos F,Workman P,Deng PS,Fung M,Ebenstein D,Wu K,Tsai TM

更新日期：1995-05-01 00:00:00