Thyrotropin activates mitogen-activated protein kinase pathway in FRTL-5 by a cAMP-dependent protein kinase A-independent mechanism.

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：:Paclitaxel, a potent antitumor agent, has been shown to be lipopolysaccharide (LPS) mimetic in mice, stimulating signaling pathways and gene expression indistinguishably from LPS. In the present study, we showed the intracellular signaling pathway of paclitaxel-induced nuclear factor-kappaB (NF-kappaB) activation and ...

journal_title：Molecular pharmacology

authors： Lee M,Jeon YJ

更新日期：2001-02-01 00:00:00

abstract：:A recently isolated monoclonal antibody was found to be a potent and powerful inhibitor of the catalytic activity of rabbit brain acetylcholinesterase (AChE; acetylcholine acetylhydrolase, EC 3.1.1.7), with an IC50 of about 1 nM and a maximal inhibition of at least 90%. The antibody increased the optimal concentration...

journal_title：Molecular pharmacology

authors： Brimijoin S,Mintz KP,Prendergast FG

更新日期：1985-12-01 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：:Cardiac function is regulated by many hormones and neurotransmitters that exert their physiological effects through the activation of G protein-coupled receptors (GPCRs). Identification of new GPCRs that might display a specific pattern of expression within the heart and differentially regulate specific cardiac functi...

journal_title：Molecular pharmacology

authors： Moore-Morris T,Varrault A,Mangoni ME,Le Digarcher A,Negre V,Dantec C,Journot L,Nargeot J,Couette B

更新日期：2009-05-01 00:00:00

abstract：:AM1710 (3-(1,1-dimethyl-heptyl)-1-hydroxy-9-methoxy-benzo(c) chromen-6-one), a cannabilactone cannabinoid receptor 2 (CB2) agonist, suppresses chemotherapy-induced neuropathic pain in rodents without producing tolerance or unwanted side effects associated with CB1 receptors; however, the signaling profile of AM1710 re...

journal_title：Molecular pharmacology

authors： Li AL,Lin X,Dhopeshwarkar AS,Thomaz AC,Carey LM,Liu Y,Nikas SP,Makriyannis A,Mackie K,Hohmann AG

更新日期：2019-02-01 00:00:00

abstract：:TWIK-related K(+) 1 (TREK1) potassium channels are members of the two-pore domain potassium channel family and contribute to background potassium conductances in many cell types, where their activity can be regulated by a variety of physiologic and pharmacologic mediators. Fenamates such as FFA (flufenamic acid; 2-{[3...

journal_title：Molecular pharmacology

authors： Veale EL,Al-Moubarak E,Bajaria N,Omoto K,Cao L,Tucker SJ,Stevens EB,Mathie A

更新日期：2014-05-01 00:00:00

abstract：:The co-transfection assay is a novel functional assay using cells transiently transfected with plasmids encoding intracellular receptors and corresponding reporter genes. Using this assay, natural product extracts were tested to identify compounds that modulate intracellular receptor activity, measured as changes in r...

journal_title：Molecular pharmacology

authors： Pathirana C,Stein RB,Berger TS,Fenical W,Ianiro T,Mais DE,Torres A,Goldman ME

更新日期：1995-03-01 00:00:00

abstract：:Camptothecin (CPT) is an effective chemotherapeutic agent for treatment of patients with cancer. The mechanisms underlying CPT-mediated responses in cancer cells are not fully understood. MicroRNA (miRNA) play important roles in tumorigenesis and drug sensitivity. However, the interaction between camptothecin and miRN...

journal_title：Molecular pharmacology

authors： Zeng CW,Zhang XJ,Lin KY,Ye H,Feng SY,Zhang H,Chen YQ

更新日期：2012-04-01 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：:Heart cells in culture need no external stimulation to contract; they beat rhythmically at a rate and intensity dependent on culture conditions. These cells respond to the general anesthetic 2-bromo-2-chloro-1,1,1-trifluorethane (halothane), with a loss of beating intensity and a lessening of beating rate. Increased c...

journal_title：Molecular pharmacology

authors： Malinconico SM,Hartzell CR,McCarl RL

更新日期：1983-03-01 00:00:00

abstract：:DNA topoisomerases are the molecular targets of a range of anticancer and antimicrobial therapeutics. Many of these drugs act by converting their target enzyme to a DNA-damaging agent through the trapping of the covalent enzyme/DNA intermediate. This drug-mediated trapping of the intermediate is reversible, and the le...

journal_title：Molecular pharmacology

authors： Nitiss JL,Wang JC

更新日期：1996-11-01 00:00:00

abstract：:Previous studies have demonstrated that the quinone group may play an important role in modulating the alkylating activity of quinone alkylating agents. Introduction of a quinone moiety markedly increased the alkylating activity and cytotoxic activity of the model quinone alkylating agents benzoquinone mustard and ben...

journal_title：Molecular pharmacology

authors： Begleiter A,Leith MK,Pan SS

更新日期：1991-09-01 00:00:00

abstract：:MicroRNAs (miRNAs) have emerged as a novel class of endogenous, small, noncoding RNAs that negatively regulate gene expression via degradation or translational inhibition of their target mRNAs. Over 700 miRNAs have been identified and sequenced in humans, and the number of miRNA genes is estimated at more than 1000. I...

journal_title：Molecular pharmacology

authors： Kukreja RC,Yin C,Salloum FN

更新日期：2011-10-01 00:00:00

abstract：:Pregnanolone [5 beta-pregnan-3 alpha-ol-20-one (5 beta 3 alpha)] and allopregnanolone [5 alpha-pregnan-3 alpha-ol-20-one (5 alpha 3 alpha)] are neuroactive steroids that are reduced metabolites of progesterone. Both 5 beta 3 alpha and 5 alpha 3 alpha are potent positive modulators of the gamma-aminobutyric acid respon...

journal_title：Molecular pharmacology

authors： Friedman L,Gibbs TT,Farb DH

更新日期：1993-07-01 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：:Cells of the murine neuroblastoma clone N1E-115 possess muscarinic receptors that influence the intracellular level of cyclic nucleotides. The stimulation of [3H]cyclic GMP levels occurs only with intact cells and has an EC50 near the "low-affinity" agonist equilibrium dissociation constant (KL) determined by radiolig...

journal_title：Molecular pharmacology

authors： McKinney M,Stenstrom S,Richelson E

更新日期：1984-09-01 00:00:00

abstract：:Tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione (TIBO) derivatives (e.g., R82150) are potent, human immunodeficiency virus-1 (HIV-1)-specific, inhibitors of reverse transcriptase (RT) that are undergoing initial evaluation in clinical trials. Because HIV-1 has become resistant to other RT inhibitor...

journal_title：Molecular pharmacology

authors： Mellors JW,Im GJ,Tramontano E,Winkler SR,Medina DJ,Dutschman GE,Bazmi HZ,Piras G,Gonzalez CJ,Cheng YC

更新日期：1993-01-01 00:00:00

abstract：:Acute desensitization of mu opioid receptors is thought to be an initial step in the development of tolerance to opioids. Given the resistance of the respiratory system to develop tolerance, desensitization of neurons in the Kölliker-Fuse (KF), a key area in the respiratory circuit, was examined. The activation of G p...

journal_title：Molecular pharmacology

authors： Levitt ES,Williams JT

更新日期：2018-01-01 00:00:00

abstract：:Ribavirin used in therapies against hepatitis C virus (HCV) is potentially efficient against other viruses but presents a high cytotoxicity. Several ribavirin triphosphate analogs modified on the ribose moiety were synthesized and tested in vitro on the RNA polymerases of HCV, phage T7, and HIV-1 reverse transcriptase...

journal_title：Molecular pharmacology

authors： Gallois-Montbrun S,Chen Y,Dutartre H,Sophys M,Morera S,Guerreiro C,Schneider B,Mulard L,Janin J,Veron M,Deville-Bonne D,Canard B

更新日期：2003-03-01 00:00:00

abstract：:A quantum chemical study of adenosine, formycin, and their 2-NH2 and 2-F derivatives is performed. The tautomerism of neutral and protonated species as well as the protonation of adenosine, formycin, and their derivatives are theoretically studied using semiempirical MNDO and AM1, as well as ab initio STO-3G methods. ...

journal_title：Molecular pharmacology

authors： Orozco M,Canela EI,Franco R

更新日期：1989-02-01 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：:The antiherpetic agent (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) was found to be an efficient substrate for recombinant Drosophila melanogaster-deoxyribonucleoside kinase with a K(m) of 4.5 microM and a V(max) of 400 nmol/microg protein/h compared with 1.3 microM and 62.5 nmol/microg protein/h, respectively, for the...

journal_title：Molecular pharmacology

authors： Balzarini J,Degrève B,Hatse S,De Clercq E,Breuer M,Johansson M,Huybrechts R,Karlsson A

更新日期：2000-04-01 00:00:00

abstract：:Retina from 1-day-old chicks is a valuable tissue model for studying neuronal nicotinic receptors because it expresses a large number of the developmentally regulated high affinity [(3)H]epibatidine labeled nicotinic receptors. Most of these receptors contain the beta4 subunit associated with different alpha subunits....

journal_title：Molecular pharmacology

authors： Barabino B,Vailati S,Moretti M,McIntosh JM,Longhi R,Clementi F,Gotti C

更新日期：2001-06-01 00:00:00

abstract：:Comparative molecular field analysis (CoMFA) predicts that the large electrostatic field around the phosphate groups of ATP plays a crucial role in stabilizing the open state of the cardiac ryanodine receptor (RyR) channel. We therefore investigated the effects of adenosine-5'-(beta,gamma-methylenetriphosphate) (AMP-P...

journal_title：Molecular pharmacology

authors： Chan WM,Welch W,Sitsapesan R

更新日期：2003-01-01 00:00:00

abstract：:Studies in vertebrate neuromuscular synapses have revealed previously that ATP, via P2Y receptors, plays a critical role in regulating postsynaptic gene expressions. An equivalent regulatory role of ATP and its P2Y receptors would not necessarily be expected for the very different situation of the brain synapses, but ...

journal_title：Molecular pharmacology

authors： Siow NL,Choi RC,Xie HQ,Kong LW,Chu GK,Chan GK,Simon J,Barnard EA,Tsim KW

更新日期：2010-12-01 00:00:00

abstract：:Cytokines are thought to cause the depression of cytochrome P-450 (CYP)-associated drug metabolism in humans during inflammation and infection. We have examined the role of five cytokines, i.e., interleukin-1 beta, interleukin-4, interleukin-6, tumor necrosis factor-alpha, and interferon-gamma, on the expression of CY...

journal_title：Molecular pharmacology

authors： Abdel-Razzak Z,Loyer P,Fautrel A,Gautier JC,Corcos L,Turlin B,Beaune P,Guillouzo A

更新日期：1993-10-01 00:00:00

abstract：:The Notch family consists of four highly conserved transmembrane receptors. The release of the active intracellular domain requires the enzymatic activity of γ-secretase. Notch is involved in embryonic development and in many physiologic processes of normal cells, in which it regulates growth, apoptosis, and different...

journal_title：Molecular pharmacology

authors： Gharaibeh L,Elmadany N,Alwosaibai K,Alshaer W

更新日期：2020-11-01 00:00:00

abstract：:The nucleoside analogue, 3-deazaadenosine (c3-Ado), serves both as a substrate and as an inhibitor of S-adenosylhomocysteine (AdoHcy) hydrolase, and the ability of this compound to induce accumulation of intracellular AdoHcy and S-3-deazaadenosylhomocysteine (c3-AdoHcy) in various cells and species has been widely doc...

journal_title：Molecular pharmacology

authors： Svardal A,Djurhuus R,Ueland PM

更新日期：1986-08-01 00:00:00

abstract：:Classical chemoattractant receptors are of fundamental importance to immune responses. The two major roles of such receptors are the modulation of chemotaxis and the generation of reactive oxygen species. The formyl peptide receptor-like 1 (FPRL1) can be stimulated by two different ligands, Trp-Lys-Tyr-Met-Val-Met-CON...

journal_title：Molecular pharmacology

authors： Bae YS,Park JC,He R,Ye RD,Kwak JY,Suh PG,Ho Ryu S

更新日期：2003-09-01 00:00:00