Methyl 2-cyano-3,12-dioxooleana-1,9-dien-28-oate decreases specificity protein transcription factors and inhibits pancreatic tumor growth: role of microRNA-27a.

abstract：:Angiotensin II (AII) stimulates rapid increases in cytosolic Ca2+ concentrations in Xenopus laevis oocytes after binding to specific receptors located in the surrounding follicular cells. In follicular oocytes, the peptide AII receptor antagonists saralasin (IC50 = 25 nM) and CGP 42112A (IC50 = 400 nM) were orders of ...

journal_title：Molecular pharmacology

authors： Ji H,Sandberg K,Catt KJ

更新日期：1991-02-01 00:00:00

abstract：:The heptadecapeptide orphanin FQ (OFQ) has been identified as the endogenous ligand for a G protein-coupled receptor (OFQ-R), which, despite its high degree of sequence similarity to opioid receptors, fails to bind opioid ligands. We developed two radioligands for the OFQ-R: a tritiated native OFQ peptide ([3H]OFQ) an...

journal_title：Molecular pharmacology

authors： Ardati A,Henningsen RA,Higelin J,Reinscheid RK,Civelli O,Monsma FJ Jr

更新日期：1997-05-01 00:00:00

abstract：:The cytochrome P450 26 family is believed to be responsible for all-trans-retinoic acid (atRA) metabolism and elimination in the human fetus and adults. CYP26A1 and CYP26B1 mRNA is expressed in a tissue-specific manner, and mice in which the CPY26 isoform has been knocked out show distinct malformations and lethality....

journal_title：Molecular pharmacology

authors： Tay S,Dickmann L,Dixit V,Isoherranen N

更新日期：2010-02-01 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：:[3H]P1075 binding to membrane preparations of rabbit skeletal muscle were observed in the presence of nucleotide triphosphates or diphosphates but not AMP, cAMP, adenosine, tripolyphosphate, or pyrophosphate. Nonhydrolyzable or poorly hydrolyzable ATP analogs inhibited MgATP-supported binding. The EC50 value for MgATP...

journal_title：Molecular pharmacology

authors： Dickinson KE,Bryson CC,Cohen RB,Rogers L,Green DW,Atwal KS

更新日期：1997-09-01 00:00:00

abstract：:To determine the structural basis for binding subtype selective agonists in the beta-adrenergic receptor (beta AR), we examined the interaction of the mutant beta 2AR and chimeric beta 1/beta 2AR with a selective beta 2AR agonist, TA-2005 (8-hydroxy-5-[(1R)-1-hydroxy-2-[N-[(1R)-2-(p-methoxyphenyl)-1-methyle thy l] am...

journal_title：Molecular pharmacology

authors： Kikkawa H,Isogaya M,Nagao T,Kurose H

更新日期：1998-01-01 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：:Amitriptyline is a classic tricyclic antidepressant (TCA) and has been used to treat the depression and anxiety of patients with cancer, but its relevance to cancer cell apoptosis is not known. In the present study, we demonstrated that amitriptyline inhibited cyclin D2 transactivation and displayed potential antimyel...

journal_title：Molecular pharmacology

authors： Mao X,Hou T,Cao B,Wang W,Li Z,Chen S,Fei M,Hurren R,Gronda M,Wu D,Trudel S,Schimmer AD

更新日期：2011-04-01 00:00:00

abstract：:Recent studies from our laboratory have provided evidence that multiple states of the phencyclidine (PCP) receptor exist. In addition, several compounds such as PCP and the novel anticonvulsant MK-801 were found to inhibit binding more potently in the presence of Mg2+ and L-glutamate (L-GLU) than when these agents wer...

journal_title：Molecular pharmacology

authors： Sills MA,Loo PS

更新日期：1989-07-01 00:00:00

abstract：:G protein-coupled receptors (GPCRs) contribute to the regulation of every aspect of human physiology and are therapeutic targets for the treatment of numerous diseases. As a consequence, understanding the myriad of mechanisms controlling GPCR signaling and trafficking is essential for the development of new pharmacolo...

journal_title：Molecular pharmacology

authors： Dunn HA,Ferguson SS

更新日期：2015-10-01 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：:Accumulated evidence suggests that dopamine and dopamine D1 agonists can activate phospholipase C in both brain and peripheral tissue. The receptor that mediates the hydrolysis of phosphoinositides has not been identified. The cloned dopamine D1A receptor that is generally thought to be linked to adenylyl cyclase, has...

journal_title：Molecular pharmacology

authors： Friedman E,Jin LQ,Cai GP,Hollon TR,Drago J,Sibley DR,Wang HY

更新日期：1997-01-01 00:00:00

abstract：:In previous studies, it was shown that the overexpression of beta2-adrenoceptor (beta2AR) in the hearts of transgenic mice (Tg) leads to agonist-independent activation of adenylate cyclase and enhanced myocardial function. Here, we measured the physical coupling of beta2AR and Gs by evaluating the coimmunoprecipitatio...

journal_title：Molecular pharmacology

authors： Gürdal H,Bond RA,Johnson MD,Friedman E,Onaran HO

更新日期：1997-08-01 00:00:00

abstract：:Aldose reductase (AKR1B1) is a critical drug target because of its involvement in diabetic complications, inflammation, and tumorigenesis. However, to date, development of clinically useful inhibitors has been largely unsuccessful. Cyclopentenone prostaglandins (cyPGs) are reactive lipid mediators that bind covalently...

journal_title：Molecular pharmacology

authors： Díez-Dacal B,Sánchez-Gómez FJ,Sánchez-Murcia PA,Milackova I,Zimmerman T,Ballekova J,García-Martín E,Agúndez JA,Gharbi S,Gago F,Stefek M,Pérez-Sala D

更新日期：2016-01-01 00:00:00

abstract：:Stimulation of alpha1-adrenoreceptors (alpha1-AR) acutely alters ion channel behavior via several signaling pathways [calcium and protein kinase C (PKC)]. Little is known about sustained alpha1-adrenergic/PKC signaling and channel regulation as may occur during cardiovascular disease states. Here we describe the effec...

journal_title：Molecular pharmacology

authors： Chen J,Chen K,Sroubek J,Wu ZY,Thomas D,Bian JS,McDonald TV

更新日期：2010-08-01 00:00:00

abstract：:The precise mechanism by which the cellular uptake of the endocannabinoid anandamide (AEA) occurs has been the source of much debate. In the current study, we show that neuronal differentiated CAD (dCAD) cells accumulate anandamide by a process that is inhibited in a dose-dependent manner by N-(4-hydroxyphenyl)arachid...

journal_title：Molecular pharmacology

authors： McFarland MJ,Bardell TK,Yates ML,Placzek EA,Barker EL

更新日期：2008-07-01 00:00:00

abstract：:Previous studies have shown that exposure of phenobarbital-pretreated rats to halothane in 10% O2 causes centrilobular necrosis, induces expression of the 72-kDa heat shock protein (HSP72), and produces several trifluoroacetylated adducts. In the present study the time course of development of the centrilobular lesion...

journal_title：Molecular pharmacology

authors： Lin WQ,van Dyke RA,Marsh HM,Trudell JR

更新日期：1994-10-01 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：:Recent years have witnessed the discovery of novel selective agonists of the M(1) muscarinic acetylcholine (ACh) receptor (mAChR). One mechanism invoked to account for the selectivity of such agents is that they interact with allosteric sites. We investigated the molecular pharmacology of two such agonists, 1-[3-(4-bu...

journal_title：Molecular pharmacology

authors： Avlani VA,Langmead CJ,Guida E,Wood MD,Tehan BG,Herdon HJ,Watson JM,Sexton PM,Christopoulos A

更新日期：2010-07-01 00:00:00

abstract：:Two forms of the multisubunit gamma-aminobutyric acid (GABA)A receptor were expressed in Xenopus oocytes by injecting mRNA encoding the bovine GABAA receptor subunit cDNAs for alpha 1 beta 1 gamma 2L and alpha 3 beta 1 gamma 2L. The properties of these two combinations were examined by electrophysiological recording o...

journal_title：Molecular pharmacology

authors： Wafford KA,Whiting PJ,Kemp JA

更新日期：1993-02-01 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：:Hepatic very-low-density lipoprotein particles (VLDL) containing full-length apolipoprotein B100 are metabolized in the blood stream to low-density lipoprotein (LDL) particles, whose elevated levels increase the risk of atherosclerosis. Statins and bile-acid sequestrants are effective LDL-lowering therapies for many p...

journal_title：Molecular pharmacology

authors： Yang Y,Ballatori N,Smith HC

更新日期：2002-02-01 00:00:00

abstract：:The relationship between receptor number and agonist-induced intracellular responses has been well studied in receptors coupled to adenylate cyclase; however, for receptors coupled to phospholipase C (PLC), very little is known about the effect of receptor number on receptor-mediated processes. To explore this issue, ...

journal_title：Molecular pharmacology

authors： Tsuda T,Kusui T,Hou W,Benya RV,Akeson MA,Kroog GS,Battey JF,Jensen RT

更新日期：1997-05-01 00:00:00

abstract：:It has been suggested that the teratogenic effects of the antiepileptic drug valproic acid (VPA) is reflected in vitro by the differentiation of F9 cells, activation of peroxisome proliferator-activated receptor delta (PPARdelta), and inhibition of histone deacetylases (HDACs). The aim of this study was to identify ge...

journal_title：Molecular pharmacology

authors： Lampen A,Grimaldi PA,Nau H

更新日期：2005-07-01 00:00:00

abstract：:CaV2.3 subunits are expressed in neuronal and neuroendocrine cells where they are believed to form native R-type Ca2+ channels. Although R-type currents are involved in triggering neurotransmitter and hormone secretion, little is known about their modulation. Previous studies have shown that muscarinic acetylcholine r...

journal_title：Molecular pharmacology

authors： Bannister RA,Melliti K,Adams BA

更新日期：2004-02-01 00:00:00

abstract：:The Gαi/o-coupled dopamine D2-like receptor family comprises three subtypes: the D2 receptor (D2R), with short and long isoform variants (D2SR and D2LR), D3 receptor (D3R), and D4 receptor (D4R), with several polymorphic variants. The common overlap of norepinephrine innervation and D2-like receptor expression pattern...

journal_title：Molecular pharmacology

authors： Sánchez-Soto M,Bonifazi A,Cai NS,Ellenberger MP,Newman AH,Ferré S,Yano H

更新日期：2016-04-01 00:00:00

abstract：:A functional interaction between peroxisome proliferator-activated receptor alpha (PPARalpha) and components of the circadian clock has been suggested, but whether these transcriptional factors interact to regulate the expression of their target genes remains obscure. Here we used a PPARalpha ligand, bezafibrate, to s...

journal_title：Molecular pharmacology

authors： Oishi K,Koyanagi S,Matsunaga N,Kadota K,Ikeda E,Hayashida S,Kuramoto Y,Shimeno H,Soeda S,Ohdo S

更新日期：2010-07-01 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：:The effect of mercuric acetate on the activities of deoxyuridine triphosphate nucleotidohydrolase (dUTPase), DNA polymerase (alpha, beta), and uracil-DNA glycosylase has been studied in cultured human KB cells. There was a dose- and time-dependent inactivation of both dUTPase and DNA polymerase alpha activities by mer...

journal_title：Molecular pharmacology

authors： Williams MV,Winters T,Waddell KS

更新日期：1987-02-01 00:00:00