Involvement of nuclear factor kappaB in c-Myc induction by tubulin polymerization inhibitors.

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：:The effects of tournefolic acid B (TAB) and two ester derivatives, TAB methyl ester (TABM) and TAB ethyl ester (TABE), on N-methyl-D-aspartate (NMDA)-mediated excitotoxicity and the underlying mechanisms were investigated. Treatment with 50 microM NMDA elicited neuronal death by 48.7 +/- 5.1%, coinciding with the appe...

journal_title：Molecular pharmacology

authors： Wang CN,Pan HC,Lin YL,Chi CW,Shiao YJ

更新日期：2006-03-01 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：:The carbocyclic analogue of 5-nitro-2'-deoxyuridine (NO2dUrd), in which the sugar moiety is replaced by a cyclopentane ring and which was designated C-NO2dUrd, has been evaluated for its cytostatic, antimetabolic, and antitumor properties. The following findings are noted. C-NO2dUrd is about 500- to 2000-fold less inh...

journal_title：Molecular pharmacology

authors： Balzarini J,De Clercq E,Herdewijn P,Robins MJ

更新日期：1985-05-01 00:00:00

abstract：:Sulfated polymannuroguluronate (SPMG) has entered the phase II clinical trial as the first anti-AIDS drug candidate in China. Herein, we report that SPMG was effective at protecting T lymphocytes against apoptosis. Further studies indicated that SPMG significantly elevated mitochondrial membrane potential (MMP) of T c...

journal_title：Molecular pharmacology

authors： Miao B,Li J,Fu X,Gan L,Xin X,Geng M

更新日期：2005-12-01 00:00:00

abstract：:The nucleoside analog 5-azacytidine is an archetypical drug for epigenetic cancer therapy, and its clinical effectiveness has been demonstrated in the treatment of myelodysplastic syndromes (MDS) and acute myelogenous leukemia (AML). However, therapy resistance in patients with MDS/AML remains a challenging issue. Mem...

journal_title：Molecular pharmacology

authors： Hummel-Eisenbeiss J,Hascher A,Hals PA,Sandvold ML,Müller-Tidow C,Lyko F,Rius M

更新日期：2013-09-01 00:00:00

abstract：:Glioma cells with stem cell properties, termed glioma stem-like cells (GSCs), have been linked to tumor formation, maintenance, and progression and are responsible for the failure of chemotherapy and radiotherapy. Because conventional glioma treatments often fail to eliminate GSCs completely, residual surviving GSCs a...

journal_title：Molecular pharmacology

authors： Kim RK,Kim MJ,Yoon CH,Lim EJ,Yoo KC,Lee GH,Kim YH,Kim H,Jin YB,Lee YJ,Cho CG,Oh YS,Gye MC,Suh Y,Lee SJ

更新日期：2012-09-01 00:00:00

abstract：:The D2 dopamine receptor (D2R) was examined for its ability to mediate nuclear factor-kappaB (NF-kappaB) activation through G proteins. Stimulation of D2R-transfected HeLa cells with its agonist quinpirole induced the expression of a NF-kappaB luciferase reporter and formation of NF-kappaB-DNA complex. This response w...

journal_title：Molecular pharmacology

authors： Yang M,Zhang H,Voyno-Yasenetskaya T,Ye RD

更新日期：2003-08-01 00:00:00

abstract：:Direct gastric mucosal cell damage mediated by nonsteroidal anti-inflammatory drugs (NSAIDs) is involved in the formation of NSAID-induced gastric lesions. We recently suggested that this direct cytotoxicity of NSAIDs is caused by their membrane-permeabilization activity. Geranylgeranylacetone (GGA), a clinically used...

journal_title：Molecular pharmacology

authors： Ushijima H,Tanaka K,Takeda M,Katsu T,Mima S,Mizushima T

更新日期：2005-10-01 00:00:00

abstract：:Unlike the majority of G protein-coupled receptors, the prostaglandin E(2) (PGE(2)) E-prostanoid 3 (EP3) receptor binds agonist with high affinity that is insensitive to the presence of guanosine 5[prime]-O-(3-thio)triphosphate (GTPγS). We report the identification of mutations that confer GTPγS sensitivity to agonist...

journal_title：Molecular pharmacology

authors： Natarajan C,Hata AN,Hamm HE,Zent R,Breyer RM

更新日期：2013-01-01 00:00:00

abstract：:The response of myeloid leukemia cells to treatment with 1-beta-D-arabinofuranosylcytosine (ara-C) includes activation of the c-Abl protein tyrosine kinase and the stress-activated protein kinase (SAPK). The present studies demonstrate that treatment of human U-937 leukemia cells with ara-C is associated with transloc...

journal_title：Molecular pharmacology

authors： Raina D,Mishra N,Kumar S,Kharbanda S,Saxena S,Kufe D

更新日期：2002-06-01 00:00:00

abstract：:G protein-coupled receptors are sensors that interact with a large variety of elements, including photons, ions, and large proteins. Not surprisingly, these receptors participate in the numerous normal physiologic processes that we refer to as health and in its perturbations that constitute disease. It has been estima...

journal_title：Molecular pharmacology

authors： Pupo AS,García-Sáinz JA

更新日期：2016-11-01 00:00:00

abstract：:The mammalian copper transporter 1 (CTR1) is responsible for the uptake of copper from the extracellular space. In this study, we used an isogenic pair of CTR1(+/+) and CTR1(-/-) mouse embryo fibroblasts to examine the contribution of CTR1 to the influx of cisplatin (DDP), carboplatin (CBDCA), oxaliplatin (L-OHP), and...

journal_title：Molecular pharmacology

authors： Larson CA,Blair BG,Safaei R,Howell SB

更新日期：2009-02-01 00:00:00

abstract：:The two G protein-coupled receptors (GPCRs) C-X-C chemokine receptor type 4 (CXCR4) and atypical chemokine receptor 3 (ACKR3) are part of the class A chemokine GPCR family and represent important drug targets for human immunodeficiency virus (HIV) infection, cancer, and inflammation diseases. CXCR4 is one of only thre...

journal_title：Molecular pharmacology

authors： Adlere I,Caspar B,Arimont M,Dekkers S,Visser K,Stuijt J,de Graaf C,Stocks M,Kellam B,Briddon S,Wijtmans M,de Esch I,Hill S,Leurs R

更新日期：2019-12-01 00:00:00

abstract：:GPR139 is an orphan G-protein-coupled receptor expressed in the central nervous system. To identify its physiologic ligand, we measured GPR139 receptor activity from recombinant cells after treatment with amino acids, orphan ligands, serum, and tissue extracts. GPR139 activity was measured using guanosine 5'-O-(3-[(35...

journal_title：Molecular pharmacology

authors： Liu C,Bonaventure P,Lee G,Nepomuceno D,Kuei C,Wu J,Li Q,Joseph V,Sutton SW,Eckert W,Yao X,Yieh L,Dvorak C,Carruthers N,Coate H,Yun S,Dugovic C,Harrington A,Lovenberg TW

更新日期：2015-11-01 00:00:00

abstract：:We cloned and expressed a human metabotropic glutamate receptor 1 alpha (HmGluR1 alpha) in a novel cell line. The human mGluR1 alpha cDNA was found to be 86% identical to rat mGluR1 alpha, and the predicted protein sequence was found to be 93% identical to rat mGluR1 alpha. We expressed HmGluR1 alpha in AV12-664, an a...

journal_title：Molecular pharmacology

authors： Desai MA,Burnett JP,Mayne NG,Schoepp DD

更新日期：1995-10-01 00:00:00

abstract：:Styrylquinoline derivatives (SQ) efficiently inhibit the 3'-processing activity of integrase (IN) with IC50 values of between 0.5 and 5 microM. We studied the mechanism of action of these compounds in vitro. First, we used steady-state fluorescence anisotropy to assay the effects of the SQ derivatives on the formation...

journal_title：Molecular pharmacology

authors： Deprez E,Barbe S,Kolaski M,Leh H,Zouhiri F,Auclair C,Brochon JC,Le Bret M,Mouscadet JF

更新日期：2004-01-01 00:00:00

abstract：:The effects of alpha 2-adrenergic receptors are usually attributed to inhibition of adenylyl cyclase through pertussis toxin-sensitive Gi coupling. In kidney distal convoluted tubule (DCT) cells, stimulation of Na+/K(+)-ATPase by alpha 2 receptors involves activation of protein kinase C (PKC). To identify the signal p...

journal_title：Molecular pharmacology

authors： Gesek FA

更新日期：1996-08-01 00:00:00

abstract：:Polycyclic aromatic hydrocarbons (PAHs) are widely distributed environmental toxicants derived from sources that include cigarette smoke, petroleum distillation, gas- and diesel-engine exhaust, and charcoal-grilled food. The gastrointestinal tract is the principal route of PAH exposures, even when inhaled. The most th...

journal_title：Molecular pharmacology

authors： Shi Z,Dragin N,Gálvez-Peralta M,Jorge-Nebert LF,Miller ML,Wang B,Nebert DW

更新日期：2010-07-01 00:00:00

abstract：:[3H]-d-cis-Diltiazem binds to canine cardiac sarcolemma in a specific, saturable, and reversible manner with a KD = 58.0 +/- 9.5 nM and a receptor site density (maximum binding) of 2.19 +/- 0.24 pmol/mg of protein. Bepridil and verapamil, Ca2+ channel inhibitors, can completely inhibit this binding at nM concentration...

journal_title：Molecular pharmacology

authors： Balwierczak JL,Johnson CL,Schwartz A

更新日期：1987-02-01 00:00:00

abstract：:The effect of breast cancer resistance protein (Bcrp/Abcg2) on the disposition of the phytoestrogens daidzein, genistein, and coumestrol was investigated using Bcrp(-/-) mice. Expression of the genes for either mouse Bcrp or human BCRP in MDCK II cells induced apically directed transport of the three phytoestrogens, w...

journal_title：Molecular pharmacology

authors： Enokizono J,Kusuhara H,Sugiyama Y

更新日期：2007-10-01 00:00:00

abstract：:The chemotherapeutic anthracycline metabolite doxorubicinol (doxOL) has been shown to interact with and disrupt the function of the cardiac ryanodine receptor Ca2+ release channel (RyR2) in the sarcoplasmic reticulum (SR) membrane and the SR Ca2+ binding protein calsequestrin 2 (CSQ2). Normal increases in RyR2 activit...

journal_title：Molecular pharmacology

authors： Hanna AD,Lam A,Thekkedam C,Willemse H,Dulhunty AF,Beard NA

更新日期：2017-11-01 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：:Many human cancers show constitutive or amplified expression of the transcriptional regulator and oncoprotein Myc, making Myc a potential target for therapeutic intervention. Here we report the down-regulation of Myc activity by reducing the availability of Max, the essential dimerization partner of Myc. Max is expres...

journal_title：Molecular pharmacology

authors： Jiang H,Bower KE,Beuscher AE 4th,Zhou B,Bobkov AA,Olson AJ,Vogt PK

更新日期：2009-09-01 00:00:00

abstract：:Neuronal cell degeneration was studied in vitro in primary rat brain neuronal cultures grown in serum-free, chemically defined, CDM R12 medium, by measuring lactate dehydrogenase (LDH) released in the culture medium. A Ca2+-dependent neuronal cell degeneration was observed after prolonged and transient exposure 30 mic...

journal_title：Molecular pharmacology

authors： Pauwels PJ,Van Assouw HP,Leysen JE,Janssen PA

更新日期：1989-10-01 00:00:00

abstract：:Autophagy is the process by which cellular material is delivered to lysosomes for degradation and recycling. There are three different types of autophagy, but macroautophagy, which involves the formation of double membrane vesicles that engulf proteins and organelles that fuse with lysosomes, is by far the most studie...

journal_title：Molecular pharmacology

authors： Thorburn A,Thamm DH,Gustafson DL

更新日期：2014-06-01 00:00:00

abstract：:In previous studies, we have shown that mouse RAW 264.7 macrophages possess pyrimidinoceptors, coupled to a phosphoinositide-specific phospholipase C, with a higher specificity for UTP than for ATP. In the current study, we explored the mechanism involved in the UTP-induced intracellular acidification seen in this cel...

journal_title：Molecular pharmacology

authors： Lin WW,Chang SH,Wu ML

更新日期：1998-02-01 00:00:00

abstract：:Anthracyclines are effective anticancer agents. However, their use is limited by cardiotoxicity, an effect linked to their ability to chelate iron and to perturb iron metabolism (Mol Pharmacol 68:261-271, 2005). These effects on iron-trafficking remain poorly understood, but they are important to decipher because trea...

journal_title：Molecular pharmacology

authors： Xu X,Sutak R,Richardson DR

更新日期：2008-03-01 00:00:00

abstract：:The subunit composition and pharmacological regulation of rat neuronal nicotinic cholinergic receptors were assessed. Specific immunoprecipitation was determined in solubilized rat brain homogenates using [3H]cytisine, a high affinity agonist at nicotinic receptors, in conjunction with polyclonal antisera generated ag...

journal_title：Molecular pharmacology

authors： Flores CM,Rogers SW,Pabreza LA,Wolfe BB,Kellar KJ

更新日期：1992-01-01 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