Desensitization and trafficking of μ-opioid receptors in locus ceruleus neurons: modulation by kinases.

abstract：:The isoprenoid donor for protein geranylgeranylation reactions, geranylgeranyl diphosphate (GGDP), is the product of the enzyme GGDP synthase (GGDPS) that condenses farnesyl diphosphate (FDP) and isopentenyl pyrophosphate. GGDPS inhibition is of interest from a therapeutic perspective for multiple myeloma because we h...

journal_title：Molecular pharmacology

authors： Allen C,Kortagere S,Tong H,Matthiesen RA,Metzger JI,Wiemer DF,Holstein SA

更新日期：2017-03-01 00:00:00

abstract：:Ceramides are naturally occurring compounds recognized to mediate apoptosis. N-acylsphingosines, containing a double bond at carbons 4 and 5 of their sphingoid backbone, are thought to be the active form, because N-acylsphinganines with completely saturated sphingoid are inactive. In the present study, we synthesized ...

journal_title：Molecular pharmacology

authors： Hwang O,Kim G,Jang YJ,Kim SW,Choi G,Choi HJ,Jeon SY,Lee DG,Lee JD

更新日期：2001-05-01 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：:The 5-hydroxytryptamine3 receptor 5-HT3R has been implicated in gut and cardiac motility and in behavioral disorders. Characteristics of 5-HT3Rs appear to be heterogeneous among species, but human 5-HT3R cDNA has not been identified. We isolated a cDNA encoding 5-HT3R from human hippocampus. The mouse 5-HT3R gene has ...

journal_title：Molecular pharmacology

authors： Miyake A,Mochizuki S,Takemoto Y,Akuzawa S

更新日期：1995-09-01 00:00:00

abstract：:Prostaglandin E(2) (PGE(2)), originally discovered as a pro-inflammatory mediator, also inhibits several chemoattractant-elicited neutrophil functions, including adhesion, secretion of cytotoxic enzymes, production of superoxide anions, and chemotaxis. In this study, we have examined the effects of PGE(2) and prostagl...

journal_title：Molecular pharmacology

authors： Burelout C,Thibault N,Levasseur S,Simard S,Naccache PH,Bourgoin SG

更新日期：2004-08-01 00:00:00

abstract：:There are now several examples of single G protein-coupled receptors to which binding of specific agonists causes differential effects on the associated signaling pathways. The dopamine D(2) receptor is of special importance because the selective activation of functional pathways has been shown both in vitro and in si...

journal_title：Molecular pharmacology

authors： Gay EA,Urban JD,Nichols DE,Oxford GS,Mailman RB

更新日期：2004-07-01 00:00:00

abstract：:High expression of the aflatoxin B1 (AFB1)-8,9-epoxide-conjugating glutathione S-transferase A3 (mGSTA3) subunit in mouse liver confers intrinsic resistance to AFB1 hepatocarcinogenesis. It is not known how the gene encoding this protein is regulated. The murine mGSTA3 gene has been identified using bioinformatics. It...

journal_title：Molecular pharmacology

authors： Jowsey IR,Jiang Q,Itoh K,Yamamoto M,Hayes JD

更新日期：2003-11-01 00:00:00

abstract：:Interleukin-2 (IL-2) is an immunoregulatory cytokine whose biological effects are mediated through interaction with specific receptors on the surface of target cells. Due to its presumed role in generating a normal immune response, IL-2 is being evaluated for the treatment of a variety of tumors, in addition to infect...

journal_title：Molecular pharmacology

authors： Chang DZ,Tasayco ML,Ciardelli TL

更新日期：1995-01-01 00:00:00

abstract：:The constitutive androstane receptor (CAR) regulates mouse and human CYP2B genes through binding to the direct repeat-4 (DR4) motifs present in the phenobarbital-responsive enhancer module (PBREM). The preference of PBREM elements for nuclear receptors and the extent of cross-talk between CAR and other nuclear recepto...

journal_title：Molecular pharmacology

authors： Mäkinen J,Frank C,Jyrkkärinne J,Gynther J,Carlberg C,Honkakoski P

更新日期：2002-08-01 00:00:00

abstract：:All-trans-retinoic acid (atRA) is the active metabolite of vitamin A. atRA is also used as a drug, and synthetic atRA analogs and inhibitors of retinoic acid (RA) metabolism have been developed. The hepatic clearance of atRA is mediated primarily by CYP26A1, but design of CYP26A1 inhibitors is hindered by lack of info...

journal_title：Molecular pharmacology

authors： Thatcher JE,Buttrick B,Shaffer SA,Shimshoni JA,Goodlett DR,Nelson WL,Isoherranen N

更新日期：2011-08-01 00:00:00

abstract：:When expressed via an inducible promoter in human embryonic kidney 293 cells, the rat Mas-related gene D (rMrgD) receptor responded to beta-alanine but not L-alanine by elevating intracellular [Ca(2+)], stimulating phosphorylation of the mitogenactivated protein kinases known as extracellular signal-regulated kinase (...

journal_title：Molecular pharmacology

authors： Milasta S,Pediani J,Appelbe S,Trim S,Wyatt M,Cox P,Fidock M,Milligan G

更新日期：2006-02-01 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：:Studies of the biochemical mechanisms evoked by conventional treatments for neoplastic diseases point to apoptosis as a key process for elimination of unwanted cells. Although the pathways through which chemotherapeutics promote cell death remain largely unknown, caspase proteases play a central role in the induction ...

journal_title：Molecular pharmacology

authors： Benjamin CW,Hiebsch RR,Jones DA

更新日期：1998-03-01 00:00:00

abstract：:The N-methyl-D-aspartate (NMDA) receptor is believed to play a major role in learning and in excitotoxic neuronal damage associated with stroke and epilepsy. Pregnenolone sulfate, a neurosteroid, specifically enhances NMDA-gated currents in spinal cord neurons, while inhibiting receptors for the inhibitory amino acids...

journal_title：Molecular pharmacology

authors： Wu FS,Gibbs TT,Farb DH

更新日期：1991-09-01 00:00:00

abstract：:Tetradecyl 2,3-dihydroxybenzoate (ABG-001) is a lead compound derived from neuritogenic gentisides. In the present study, we investigated the mechanism by which ABG-001 induces neurite outgrowth in a rat adrenal pheochromocytoma cell line (PC12). Inhibitors of insulin-like growth factor 1 (IGF-1) receptor, phosphatidy...

journal_title：Molecular pharmacology

authors： Tang R,Gao L,Kawatani M,Chen J,Cao X,Osada H,Xiang L,Qi J

更新日期：2015-08-01 00:00:00

abstract：:The binding of [3H]quinuclidinyl benzilate ([3H]QNB) to cardiac muscarinic receptors was inhibited not only by classical muscarinic antagonists but also by nicotinic blocking agents and inhibitors of acetylcholinesterase. Gallamine, pancuronium, ambenonium, and decamethonium were the most potent of these agents examin...

journal_title：Molecular pharmacology

authors： Dunlap J,Brown JH

更新日期：1983-07-01 00:00:00

abstract：:Seven transmembrane G protein-coupled receptors (GPCRs) are often phosphorylated at the C terminus and on intracellular loops in response to various extracellular stimuli. Phosphorylation of GPCRs by GPCR kinases and certain other kinases can promote the recruitment of arrestin molecules. The arrestins critically regu...

journal_title：Molecular pharmacology

authors： Yang Z,Yang F,Zhang D,Liu Z,Lin A,Liu C,Xiao P,Yu X,Sun JP

更新日期：2017-09-01 00:00:00

abstract：:Tumor suppressor gene BRCA1 is frequently mutated in familial breast and ovarian cancer. BRCA1 plays pivotal roles in maintaining genomic stability by interacting with numerous proteins in cell cycle control and DNA repair. Irofulven (6-hydroxymethylacylfulvene, HMAF, MGI 114, NSC 683863) is one of a new class of anti...

journal_title：Molecular pharmacology

authors： Wiltshire T,Senft J,Wang Y,Konat GW,Wenger SL,Reed E,Wang W

更新日期：2007-04-01 00:00:00

abstract：:The structure-activity relationships for vasoactive intestinal peptide (VIP) receptor binding were studied using N-terminally modified VIP analogs. VIP fragments, and VIP receptor antagonists. Tissue sources included bovine coronary artery, rat mesenteric artery, rat pituitary, rat brain synaptosomes, and rat liver. E...

journal_title：Molecular pharmacology

authors： Rorstad OP,Wanke I,Coy DH,Fournier A,Huang M

更新日期：1990-06-01 00:00:00

abstract：:beta-arrestins have been shown to play important roles in regulation of signaling and desensitization of opioid receptors in many in vivo studies. The current study was carried out to measure the direct interaction of beta-arrestins with two functional intracellular domains, the third intracellular loop (I3L) and the ...

journal_title：Molecular pharmacology

authors： Cen B,Xiong Y,Ma L,Pei G

更新日期：2001-04-01 00:00:00

abstract：:The molecular determinants of high-affinity human ether-a-go-go-related gene (HERG) potassium channel blockade by methanesulfonanilides include two aromatic residues (Phe656 and Tyr652) on the inner helices (S6) and residues on the pore helices that face into the inner cavity, but determinants for lower-affinity HERG ...

journal_title：Molecular pharmacology

authors： Witchel HJ,Dempsey CE,Sessions RB,Perry M,Milnes JT,Hancox JC,Mitcheson JS

更新日期：2004-11-01 00:00:00

abstract：:We have found that stypoldione, a bright red o-quinone isolated from the brown alga Stypopodium zonale, inhibits the division of sea urchin embryos in a concentration-dependent manner (IC50 approximately 2.5 X 10(-6) M). Although previous studies have shown this marine natural product to inhibit beef brain microtubule...

journal_title：Molecular pharmacology

authors： White SJ,Jacobs RS

更新日期：1983-11-01 00:00:00

abstract：:Prostate cancer is a highly heterogenous disease in which a patient-tailored care program is much desired. Central to this goal is the development of novel targeted pharmacological interventions. To develop these treatment strategies, an understanding of the integration of cellular pathways involved in both tumorigene...

journal_title：Molecular pharmacology

authors： Assinder SJ,Dong Q,Mangs H,Richardson DR

更新日期：2009-03-01 00:00:00

abstract：:Acetylsalicylic acid (aspirin) is a cyclooxygenase (COX) inhibitor, yet some of its therapeutic effects are thought to derive from mechanisms unrelated to prostaglandin synthesis inhibition. In human intestinal myofibroblasts, aspirin, at therapeutic doses, had the unexpected effect of inducing prolonged COX-2 express...

journal_title：Molecular pharmacology

authors： Mifflin RC,Saada JI,Di Mari JF,Valentich JD,Adegboyega PA,Powell DW

更新日期：2004-02-01 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：:It is established that agmatine, an endogenously formed decarboxylated arginine, is a weak competitive inhibitor of neuronal nitric-oxide synthase (nNOS) with an apparent Ki value of 660 microM [Biochem J 316:247-249, 1996]. Although agmatine is known to bind to alpha-adrenergic and imidazoline receptors, it has been ...

journal_title：Molecular pharmacology

authors： Demady DR,Jianmongkol S,Vuletich JL,Bender AT,Osawa Y

更新日期：2001-01-01 00:00:00

abstract：:Formyl peptide receptor (FPR) and formyl peptide receptor like 1 (FPRL1) play important roles in inflammation and immunity. Stimulation of FPR and FPRL1 initiates a cascade of signaling events, leading to activation of various phagocyte responses, including chemotaxis, superoxide generation, and exocytosis. Trp-Lys-Ty...

journal_title：Molecular pharmacology

authors： Bae YS,Song JY,Kim Y,He R,Ye RD,Kwak JY,Suh PG,Ryu SH

更新日期：2003-10-01 00:00:00

abstract：:It has long been believed that the cortical actin cytoskeleton plays an important role in regulating the secretion of hormones and neurotransmitters. In this study, we investigated the control of actin dynamics in primary neuroendocrine cells and determined the relationship of actin dynamics to various components of t...

journal_title：Molecular pharmacology

authors： Bittner MA,Holz RW

更新日期：2005-04-01 00:00:00

abstract：:The cDNA for the rat alpha 1c-adrenergic receptor (AR) has been cloned using a probe derived from the bovine alpha 1c-AR sequence. Clone rB7a has a 2.6-kilobase insert with a 1390-base pair open reading frame and encodes a receptor of 466 amino acids. The cloned receptor has 91% amino acid identity with the bovine alp...

journal_title：Molecular pharmacology

authors： Laz TM,Forray C,Smith KE,Bard JA,Vaysse PJ,Branchek TA,Weinshank RL

更新日期：1994-09-01 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