Discovery of an ectopic activation site on the M(1) muscarinic receptor.

abstract：:Identifying novel mechanisms to enhance glucagon-like peptide-1 (GLP-1) receptor signaling may enable nascent medicinal chemistry strategies with the aim of developing new orally available therapeutic agents for the treatment of type 2 diabetes mellitus. Therefore, we tested the hypothesis that selectively modulating ...

journal_title：Molecular pharmacology

authors： Willard FS,Wootten D,Showalter AD,Savage EE,Ficorilli J,Farb TB,Bokvist K,Alsina-Fernandez J,Furness SG,Christopoulos A,Sexton PM,Sloop KW

更新日期：2012-12-01 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：:Corticotropin-releasing factor (CRF) receptors encoded by two distinct genes have recently been identified and termed CRF1 and CRF2. CRF and the non-mammalian-related peptide sauvagine bind to and activate CRF1 receptors with high affinity and equal potency. Although CRF is significantly weaker at the CRF2 receptor, s...

journal_title：Molecular pharmacology

authors： Grigoriadis DE,Liu XJ,Vaughn J,Palmer SF,True CD,Vale WW,Ling N,De Souza EB

更新日期：1996-09-01 00:00:00

abstract：:The endocannabinoids anandamide and 2-arachidonyl glycerol (2-AG) bind to G protein-coupled central and peripheral cannabinoid receptors CB1 and CB2, respectively. Due to the relatively high expression of the CB2 isotype on peripheral immune cells, it has been hypothesized that this receptor mediates the immunosuppres...

journal_title：Molecular pharmacology

authors： Gonsiorek W,Lunn C,Fan X,Narula S,Lundell D,Hipkin RW

更新日期：2000-05-01 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：:(6R)-5,6,7,8-Tetrahydrobiopterin (BH4), which is synthesized intracellularly from GTP, caused a concentration-dependent increase in rat pheochromocytoma (PC12) cell proliferation when added exogenously. Incubation with sepiapterin, which is converted enzymatically to BH4 within cells, also increased PC12 cell prolifer...

journal_title：Molecular pharmacology

authors： Anastasiadis PZ,States JC,Imerman BA,Louie MC,Kuhn DM,Levine RA

更新日期：1996-01-01 00:00:00

abstract：:Phosphorylation of G protein-coupled receptors (GPCRs) by GPCR kinases (GRKs) is a major mechanism of desensitization of these receptors. GPCR activation of GRKs involves an allosteric site on GRKs distinct from the catalytic site. Although recent studies have suggested an important role of the N- and C-termini and do...

journal_title：Molecular pharmacology

authors： Baameur F,Morgan DH,Yao H,Tran TM,Hammitt RA,Sabui S,McMurray JS,Lichtarge O,Clark RB

更新日期：2010-03-01 00:00:00

abstract：:Ethanol administration to rats by ethanol vapor inhalation (14 days) results in a 40-50% reduction in the level of gamma-aminobutyric acidA (GABAA) receptor alpha 1 subunit mRNAs [4.4 and 4.8 kilobases (kb)] in the cerebral cortex. The level of alpha 2 subunit mRNA (8.0 kb) was also reduced by 29%, whereas there was n...

journal_title：Molecular pharmacology

authors： Montpied P,Morrow AL,Karanian JW,Ginns EI,Martin BM,Paul SM

更新日期：1991-02-01 00:00:00

abstract：:It is widely accepted that cAMP signaling is compartmentalized within cells. However, our knowledge of how receptors, cAMP signaling enzymes, effectors, and other key proteins form specific signaling complexes to regulate specific cell responses is limited. The multicomponent nature of these systems and the spatiotemp...

journal_title：Molecular pharmacology

authors： Johnstone TB,Agarwal SR,Harvey RD,Ostrom RS

更新日期：2018-04-01 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：:The blocking effects of guanethidine on electrically induced, neurally mediated, contractions of the guinea pig vas deferens in vitro could be markedly antagonized by the bee venom polypeptide apamin (20-60 nM), by 0.1 mM methylene blue, and (less regularly) by 0.1-0.15 mM quinine, three substances known to inhibit ca...

journal_title：Molecular pharmacology

authors： Stutzin A,Paravic F,Ormenño G,Orrego F

更新日期：1983-03-01 00:00:00

abstract：:Inhibition of multidrug resistance protein 1 (MRP1) mediated cytostatic drug efflux might be useful in the treatment of drug resistant tumors. Because the glutathione (GSH) conjugate of ethacrynic acid (EA), GS-EA, is a good substrate of MRP1, GS-EA derivatives are expected to be good inhibitors of MRP1. To study stru...

journal_title：Molecular pharmacology

authors： Burg D,Wielinga P,Zelcer N,Saeki T,Mulder GJ,Borst P

更新日期：2002-11-01 00:00:00

abstract：:Adult guinea pig hippocampal membranes contain two 5-hydroxytryptamine (5-HT) receptors positively coupled with an adenylate cyclase. One is a typical 5-HT1A receptor and the second is a nonclassical 5-HT receptor that we previously proposed to call 5-HT4. Here, we show that 4-amino-5-chlor-2-methoxy-benzamide derivat...

journal_title：Molecular pharmacology

authors： Bockaert J,Sebben M,Dumuis A

更新日期：1990-03-01 00:00:00

abstract：:Of four monoclonal antibodies to purified rat liver cytochrome P450s, including those from 3-methylcholanthrene-, phenobarbital-, ethanol-, and pregnenolone-16-alpha-carbonitrile-treated rats, only the monoclonal antibody against pregnenolone-16-alpha-carbonitrile-inducible P450 immunodetected proteins in chicken live...

journal_title：Molecular pharmacology

authors： Lorr NA,Bloom SE,Park SS,Gelboin HV,Miller H,Friedman FK

更新日期：1989-05-01 00:00:00

abstract：:Several lines of evidence suggest that G-protein-coupled receptors can adopt different active conformations, but their direct demonstration in intact cells is still missing. Using a fluorescence resonance energy transfer (FRET)-based approach we studied conformational changes in alpha(2A)-adrenergic receptors in intac...

journal_title：Molecular pharmacology

authors： Zürn A,Zabel U,Vilardaga JP,Schindelin H,Lohse MJ,Hoffmann C

更新日期：2009-03-01 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：:UDP-glucuronosyltransferase (UGT) 1A1 glucuronidates endogenous metabolites, such as bilirubin, and exogenous substances, and plays a critical role in their detoxification and excretion. In a previous article, we described the phenobarbital response activity to a 290-base pair (bp) distal enhancer sequence (-3499/-321...

journal_title：Molecular pharmacology

authors： Sugatani J,Nishitani S,Yamakawa K,Yoshinari K,Sueyoshi T,Negishi M,Miwa M

更新日期：2005-03-01 00:00:00

abstract：:Mitsuya and Broder [Proc. Natl. Acad. Sci. USA 83:1911-1915 (1986)] demonstrated that every purine (adenosine, guanosine, and inosine) and pyrimidine (cytidine and thymidine) nucleoside containing the 2',3'-dideoxyribose configuration, when evaluated against human immunodeficiency virus (HIV) in vitro, significantly s...

journal_title：Molecular pharmacology

authors： Hao Z,Cooney DA,Hartman NR,Perno CF,Fridland A,DeVico AL,Sarngadharan MG,Broder S,Johns DG

更新日期：1988-10-01 00:00:00

abstract：:In cervical cancer, the p53 and retinoblastoma (pRb) tumor suppressor pathways are disrupted by the human papilloma virus (HPV) E6 and E7 oncoproteins, because E6 targets p53 and E7 targets pRb for rapid proteasome-mediated degradation. We have investigated whether E6 suppression with small interfering RNA (siRNA) res...

journal_title：Molecular pharmacology

authors： Tan S,Hougardy BM,Meersma GJ,Schaap B,de Vries EG,van der Zee AG,de Jong S

更新日期：2012-05-01 00:00:00

abstract：:Histone deacetylase inhibitors (HDACi), which have emerged as a new class of anticancer agents, act by modulating expression of genes controlling apoptosis or cell proliferation. Here, we compared the effect of HDACi on transcriptional activation by estrogen or glucocorticoid receptors (ER and GR, respectively), two m...

journal_title：Molecular pharmacology

authors： Rocha W,Sanchez R,Deschênes J,Auger A,Hébert E,White JH,Mader S

更新日期：2005-12-01 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

abstract：:This study describes experiments investigating the mechanism of activation of A1 adenosine receptors. Isolated rat fat cells were used as a cellular model. The A1 receptors of these cells were covalently labeled with the agonist photoaffinity label R-2-azido-N6-p-hydroxyphenylisopropyladenosine. The covalent incorpora...

journal_title：Molecular pharmacology

authors： Lohse MJ,Klotz KN,Schwabe U

更新日期：1986-10-01 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 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：:Notch-1 (Notch) is a cell surface receptor that regulates cell-fate decisions in the developing nervous system, and it may also have roles in synaptic plasticity in the adult brain. Binding of its ligands results in the proteolytic cleavage of Notch by the γ-secretase enzyme complex, thereby causing the release of a N...

journal_title：Molecular pharmacology

authors： Arumugam TV,Cheng YL,Choi Y,Choi YH,Yang S,Yun YK,Park JS,Yang DK,Thundyil J,Gelderblom M,Karamyan VT,Tang SC,Chan SL,Magnus T,Sobey CG,Jo DG

更新日期：2011-07-01 00:00:00

abstract：:A UDP-glucuronosyltransferase (UDPGT) isoenzyme capable of morphine glucuronidation has been purified to apparent homogeneity and partially characterized from hepatic microsomes of female Wistar rats which have low 3 alpha-hydroxysteroid UDPGT. A rapid and sensitive assay was developed to quantify morphine glucuronide...

journal_title：Molecular pharmacology

authors： Puig JF,Tephly TR

更新日期：1986-12-01 00:00:00

abstract：:Two peptides, which have no significant homology with known protein structures, were obtained by microsequencing of a mu-opioid binding protein purified to homogeneity from bovine striatal membranes. Polyclonal antibodies generated against portions of these peptides immunoprecipitated up to 65% of radiolabeled purifie...

journal_title：Molecular pharmacology

authors： Gioannini TL,Yao YH,Hiller JM,Taylor LP,Simon EJ

更新日期：1993-10-01 00:00:00

abstract：:Activation of alpha 1-adrenergic receptors (alpha 1-AR) increases Na+/H+ exchange (NHE) in proximal tubule. NHE mediates the majority of active Na+ absorption in the proximal tubule. Three alpha 1-AR subtypes have been detected in kidney by molecular and binding techniques. We detected message for all three alpha 1-AR...

journal_title：Molecular pharmacology

authors： Liu F,Nesbitt T,Drezner MK,Friedman PA,Gesek FA

更新日期：1997-12-01 00:00:00

abstract：:We demonstrated previously that nonsteroidal anti-inflammatory drugs (NSAIDs) increased p27(Kip1) by inhibiting protein degradation to suppress the proliferation of human lung cancer cells. In this study, we elucidate the molecular mechanism by which NSAIDs modulate p27(Kip1) proteolysis. Immunoblotting and in vitro u...

journal_title：Molecular pharmacology

authors： Huang YC,Chuang LY,Hung WC

更新日期：2002-12-01 00:00:00

abstract：:Herein we provide evidence for the coexpression of two distinct prostacyclin (PGI(2)) receptors (IP) on BEAS-2B human airway epithelial cells. IP receptor heterogeneity initially was suggested by the finding that the rank orders of potency of PGI(2) and three structurally similar analogs [taprostene, iloprost, 15-deox...

journal_title：Molecular pharmacology

authors： Wilson SM,Sheddan NA,Newton R,Giembycz MA

更新日期：2011-03-01 00:00:00