Molecular pharmacology

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Metformin prevents hyperglycaemia-associated, oxidative stress-induced vascular endothelial dysfunction: essential role for the orphan nuclear receptor, Nr4a1 (Nur77). 2021
Knockdown of Long Noncoding RNAs Hepatocyte Nuclear Factor 1α Antisense RNA 1 and Hepatocyte Nuclear Factor 4α Antisense RNA 1 Alters Susceptibility of Acetaminophen-Induced Cytotoxicity in HepaRG Cells.. 97. 2020
Carboxylic Acid Derivatives of Amlexanox Display Enhanced Potency toward TBK1 and IKKε and Reveal Mechanisms for Selective Inhibition.. 94. 2018
A Transcriptional Regulatory Network Containing Nuclear Receptors and Long Noncoding RNAs Controls Basal and Drug-Induced Expression of Cytochrome P450s in HepaRG Cells.. 94. 2018
Arsenic Attenuates GLI Signaling, Increasing or Decreasing its Transcriptional Program in a Context-Dependent Manner.. 89. 2015
(4-(Bis(4-fluorophenyl)methyl)piperazin-1-yl)(cyclohexyl)methanone hydrochloride (LDK1229): a new cannabinoid CB1 receptor inverse agonist from the class of benzhydryl piperazine analogs.. 87. 2014
Sequential cytoprotective responses to Sigma1 ligand-induced endoplasmic reticulum stress.. 84. 2013
Hydrogen sulfide as an allosteric modulator of ATP-sensitive potassium channels in colonic inflammation.. 83. 2012
Novel transcriptome profiling analyses demonstrate that selective peroxisome proliferator-activated receptor γ (PPARγ) modulators display attenuated and selective gene regulatory activity in comparison with PPARγ full agonists.. 82. 2012
A dynamic model of membrane-bound phospholipase Cβ2 activation by Gβγ subunits.. 80. 2011
Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity.. 78. 2010
A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning.. 76. 2009
NHERF1 regulates parathyroid hormone receptor desensitization: interference with beta-arrestin binding.. 75. 2009
A juxtamembrane mutation in the N terminus of the dopamine transporter induces preference for an inward-facing conformation.. 75. 2008
90-kDa heat shock protein inhibition abrogates the topoisomerase I poison-induced G2/M checkpoint in p53-null tumor cells by depleting Chk1 and Wee1.. 75. 2008
Structural basis for ether-a-go-go-related gene K+ channel subtype-dependent activation by niflumic acid.. 73. 2008
Agonist-specific regulation of mu-opioid receptor desensitization and recovery from desensitization.. 73. 2008
Molecular mechanisms underlying the synergistic interaction of erlotinib, an epidermal growth factor receptor tyrosine kinase inhibitor, with the multitargeted antifolate pemetrexed in non-small-cell lung cancer cells.. 73. 2008
The differential interactions of peroxisome proliferator-activated receptor gamma ligands with Tyr473 is a physical basis for their unique biological activities.. 73. 2007
Substance P neurokinin 1 receptor activation within the dorsal raphe nucleus controls serotonin release in the mouse frontal cortex.. 72. 2007
Molecular interaction of a potent nonpeptide agonist with the chemokine receptor CCR8.. 72. 2007
Activation of the CXCR3 chemokine receptor through anchoring of a small molecule chelator ligand between TM-III, -IV, and -VI.. 71. 2006
2,3-butanedione monoxime affects cystic fibrosis transmembrane conductance regulator channel function through phosphorylation-dependent and phosphorylation-independent mechanisms: the role of bilayer material properties.. 70. 2006
Pharmacological inhibition of histone deacetylases by suberoylanilide hydroxamic acid specifically alters gene expression and reduces ischemic injury in the mouse brain.. 70. 2006
Inhibition of in vivo glioma growth and invasion by peroxisome proliferator-activated receptor gamma agonist treatment.. 70. 2006
A comprehensive structure-based alignment of prokaryotic and eukaryotic neurotransmitter/Na+ symporters (NSS) aids in the use of the LeuT structure to probe NSS structure and function.. 70. 2006
Identification of tubulin as the molecular target of proapoptotic pyrrolo-1,5-benzoxazepines.. 70. 2006
Capsaicin regulates voltage-dependent sodium channels by altering lipid bilayer elasticity.. 68. 2005
Kahalalide F induces necrosis-like cell death that involves depletion of ErbB3 and inhibition of Akt signaling.. 68. 2005
The general anesthetic isoflurane depresses synaptic vesicle exocytosis.. 67. 2005
Transfected beta3- but not beta2-adrenergic receptors regulate cystic fibrosis transmembrane conductance regulator activity via a new pathway involving the mitogen-activated protein kinases extracellular signal-regulated kinases.. 67. 2004
Certain 1,4-disubstituted aromatic piperidines and piperazines with extreme selectivity for the dopamine D4 receptor interact with a common receptor microdomain.. 66. 2004
Isoflurane and propofol inhibit voltage-gated sodium channels in isolated rat neurohypophysial nerve terminals.. 64. 2003
Anthracycline-induced suppression of GATA-4 transcription factor: implication in the regulation of cardiac myocyte apoptosis.. 63. 2003
Norepinephrine release from the ischemic heart is greatly enhanced in mice lacking histamine H3 receptors.. 63. 2003
Molecular basis of partial agonism: orientation of indoleamine ligands in the binding pocket of the human serotonin 5-HT2A receptor determines relative efficacy.. 63. 2003
Discovery of novel targets of quinoline drugs in the human purine binding proteome.. 62. 2002
Molecular requisites for drug binding to muscle CLC-1 and renal CLC-K channel revealed by the use of phenoxy-alkyl derivatives of 2-(p-chlorophenoxy)propionic acid.. 62. 2002
Complex intracellular messenger pathways regulate one type of neuronal alpha-bungarotoxin-resistant nicotinic acetylcholine receptors expressed in insect neurosecretory cells (dorsal unpaired median neurons).. 60. 2001
Decoy oligodeoxynucleotide characterization of transcription factors controlling endothelin-B receptor expression in vascular smooth muscle cells.. 58. 2000
Pharmacological characterization of chloride channels belonging to the ClC family by the use of chiral clofibric acid derivatives.. 58. 2000
Antisense inhibition of 5-hydroxytryptamine2a receptor induces an antidepressant-like effect in mice.. 52. 1997
The microtubule-stabilizing agent discodermolide competitively inhibits the binding of paclitaxel (Taxol) to tubulin polymers, enhances tubulin nucleation reactions more potently than paclitaxel, and inhibits the growth of paclitaxel-resistant cells.. 52. 1997
Effects of adenophostin-A and inositol-1,4,5-trisphosphate on Cl- currents in Xenopus laevis oocytes.. 51. 1997
Internal trafficking and surface mobility of a functionally intact beta2-adrenergic receptor-green fluorescent protein conjugate.. 51. 1997
Contribution of a helix 5 locus to selectivity of hallucinogenic and nonhallucinogenic ligands for the human 5-hydroxytryptamine2A and 5-hydroxytryptamine2C receptors: direct and indirect effects on ligand affinity mediated by the same locus.. 50. 1996
Transcriptional regulation of secretogranin II and chromogranin B by cyclic AMP in a rat pheochromocytoma cell line.. 46. 1994
Enzymatic conversion of retinaldehyde to retinoic acid by cloned murine cytosolic and mitochondrial aldehyde dehydrogenases.. 46. 1994
Antagonist-mediated down-regulation of 5-hydroxytryptamine type 2 receptor gene expression: modulation of transcription.. 45. 1994
Expression of thyrotropin-releasing hormone receptors by adenovirus-mediated gene transfer reveals that thyrotropin-releasing hormone desensitization is cell specific.. 45. 1994
A reciprocal mutation supports helix 2 and helix 7 proximity in the gonadotropin-releasing hormone receptor.. 45. 1994
2,3,7,8-tetrachlorodibenzo-p-dioxin increases cardiac myocyte intracellular calcium and progressively impairs ventricular contractile responses to isoproterenol and to calcium in chick embryo hearts.. 44. 1993
Metrazole induces the sequential activation of c-fos, proenkephalin, and tyrosine hydroxylase gene expression in the rat adrenal gland: modulation by glucocorticoid and adrenocorticotropic hormone.. 44. 1993
Transsynaptic activity regulates proenkephalin and tyrosine hydroxylase gene expression and the response to reserpine in the hamster adrenal.. 40. 1991
Sodium channel comodification with full activator reveals veratridine reaction dynamics.. 37. 1990
Interaction between DPI 201-106 enantiomers at the cardiac sodium channel.. 37. 1990
A metactoid sensitization model to describe multiple receptors linked to a common response: application to histamine receptors coupled to [3H]cyclic AMP accumulation in guinea pig cortex.. 35. 1989
A molecular model for activation of a 5-hydroxytryptamine receptor.. 32. 1987
Molecular determinants for recognition of triazole and tetrazole analogs of histamine at H2-receptors.. 31. 1987
Pharmacological characterization of two 5-hydroxytryptamine receptors coupled to adenylate cyclase in guinea pig hippocampal membranes.. 31. 1987
Theoretical studies on the activation mechanism of the histamine H2-receptor: the proton transfer between histamine and a receptor model.. 29. 1986
Site of action of phencyclidine. IV. Interaction of phencyclidine and its analogues on ionic channels of the electrically excitable membrane and nicotinic receptor: implications for behavioral effects.. 21. 1982
The influence of organometals on heme metabolism. In vivo and in vitro studies with organotins.. 21. 1982
[13C]NMR chemical shifts and calculated electronic structures of serotonin congeners: relation to biological activity.. 16. 1979
Studies on histamine H2 receptors coupled to cardiac adenylate cyclase. Blockade by H2 and H1 receptor antagonists.. 16. 1979
Structure and function of snake venom curarimimetic neurotoxins.. 14. 1978
Tautomerism and the receptor action of histamine: a mechanistic model.. 12. 1976
A theoretical and experimental study of the semirigid cholinergic agonist 3-acetoxyquinuclidine.. 11. 1975
Regulation of dopamine synthesis in rat brain striatal synaptosomes.. 11. 1975
Psychotomimetic drugs as anticholinergic agents. II. Quantum-mechanical study of molecular interaction potentials of 1-cyclohexylpiperidine derivatives with the cholinergic receptor.. 9. 1973
Effect of p-chlorophenylalanine on hydroxylation of tryptophan in pineal and brain of rats.. 8. 1972
Regulation of adrenal phenylethanolamine N-methyltransferase activity in three inbred mouse strains.. 8. 1972
The enzymatic formation of methanol from S-adenosylmethionine by various tissues of the rat.. 8. 1972
Interaction of cytochrome P-450 with antibodies raised against a solubilized P-450 preparation from hepatic microsomes.. 7. 1971
The metabolism of aminopyrine in chick embryo hepatic cell culture: effects of competitive substrates and carbon monoxide.. 7. 1971
Preparation and properties of a solubilized form of cytochrome P-450 from chick embryo liver microsomes.. 7. 1971
Ouabain-dependent incorporation of 32P from p-nitrophenyl phosphate into a microsomal phosphatase.. 6. 1970
Kinetics of oligomycin inhibition of sodium- and potassium-activated adenosine triphosphatase from beef brain.. 4. 1968

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Molecular pharmacology Journal

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