Search Results - "Dove, Stefan"

International Union of Basic and Clinical Pharmacology. CI. Structures and Small Molecule Modulators of Mammalian Adenylyl Cyclases by Dessauer, Carmen W, Watts, Val J, Ostrom, Rennolds S, Conti, Marco, Dove, Stefan, Seifert, Roland

“…Adenylyl cyclases (ACs) generate the second messenger cAMP from ATP. Mammalian cells express nine transmembrane AC (mAC) isoforms (AC1-9) and a soluble AC…”
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The extracellular loop 2 (ECL2) of the human histamine H4 receptor substantially contributes to ligand binding and constitutive activity by Wifling, David, Bernhardt, Günther, Dove, Stefan, Buschauer, Armin

“…In contrast to the corresponding mouse and rat orthologs, the human histamine H4 receptor (hH4R) shows extraordinarily high constitutive activity. In the…”
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Functional selectivity of GPCR ligand stereoisomers: new pharmacological opportunities by Seifert, Roland, Dove, Stefan

“…It is now well established that any given ligand for a G-protein-couple receptor (GPCR) does not simply possess a single defined efficacy. Rather, a ligand…”
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Paradoxical stimulatory effects of the "standard" histamine H4-receptor antagonist JNJ7777120: the H4 receptor joins the club of 7 transmembrane domain receptors exhibiting functional selectivity by Seifert, Roland, Schneider, Erich H, Dove, Stefan, Brunskole, Irena, Neumann, Detlef, Strasser, Andrea, Buschauer, Armin

“…The histamine H(4) receptor (H(4)R) is expressed in several cell types of the immune system and is assumed to play an important pro-inflammatory role in…”
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Synthesis and Structure−Activity Relationships of Cyanoguanidine-Type and Structurally Related Histamine H4 Receptor Agonists by Igel, Patrick, Geyer, Roland, Strasser, Andrea, Dove, Stefan, Seifert, Roland, Buschauer, Armin

“…Recently, we identified high-affinity human histamine H3 (hH3R) and H4 receptor (hH4R) ligands among a series of NG-acylated imidazolylpropylguanidines, which…”
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Expression and functional properties of canine, rat, and murine histamine H4 receptors in Sf9 insect cells by Schnell, David, Brunskole, Irena, Ladova, Katerina, Schneider, Erich H., Igel, Patrick, Dove, Stefan, Buschauer, Armin, Seifert, Roland

“…The histamine H 4 receptor (H 4 R) is expressed on cells of the immune system including eosinophils, dendritic cells, and T cells and plays an important role…”
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Structure-bias relationships for fenoterol stereoisomers in six molecular and cellular assays at the β2-adrenoceptor by Reinartz, Michael T., Kälble, Solveig, Littmann, Timo, Ozawa, Takeaki, Dove, Stefan, Kaever, Volkhard, Wainer, Irving W., Seifert, Roland

“…Functional selectivity is well established as an underlying concept of ligand-specific signaling via G protein-coupled receptors (GPCRs). Functionally,…”
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Constitutive activity and ligand selectivity of human, guinea pig, rat, and canine histamine H2 receptors by Preuss, Hendrik, Ghorai, Prasanta, Kraus, Anja, Dove, Stefan, Buschauer, Armin, Seifert, Roland

“…Previous studies revealed pharmacological differences between human and guinea pig histamine H(2) receptors (H(2)Rs) with respect to the interaction with…”
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Different Roles of N-Terminal and C-Terminal Domains in Calmodulin for Activation of Bacillus anthracis Edema Factor by Lübker, Carolin, Dove, Stefan, Tang, Wei-Jen, Urbauer, Ramona J Bieber, Moskovitz, Jackob, Urbauer, Jeffrey L, Seifert, Roland

“…Bacillus anthracis adenylyl cyclase toxin edema factor (EF) is one component of the anthrax toxin and is essential for establishing anthrax disease. EF…”
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Molecular analysis of the interaction of Bordetella pertussis adenylyl cyclase with fluorescent nucleotides by Göttle, Martin, Dove, Stefan, Steindel, Phillip, Shen, Yuequan, Tang, Wei-Jen, Geduhn, Jens, König, Burkhard, Seifert, Roland

“…The calmodulin (CaM)-dependent adenylyl cyclase (AC) toxin from Bordetella pertussis (CyaA) substantially contributes to the pathogenesis of whooping cough…”
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Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor by Seifert, Roland, Wenzel-Seifert, Katharina, Burckstummer, Tilmann, Pertz, Heinz H, Schunack, Walter, Dove, Stefan, Buschauer, Armin, Elz, Sigurd

“…Species isoforms of histamine H2-, H3-, and H4-receptors differ in their pharmacological properties. The study aim was to dissect differences between the human…”
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The Bivalent Ligand Approach Leads to Highly Potent and Selective Acylguanidine-Type Histamine H2 Receptor Agonists by Birnkammer, Tobias, Spickenreither, Anja, Brunskole, Irena, Lopuch, Miroslaw, Kagermeier, Nicole, Bernhardt, Günther, Dove, Stefan, Seifert, Roland, Elz, Sigurd, Buschauer, Armin

“…Bivalent histamine H2 receptor (H2R) agonists were synthesized by connecting pharmacophoric 3-(2-amino-4-methylthiazol-5-yl)-, 3-(2-aminothiazol-5-yl)-,…”
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Mutations of Cys-17 and Ala-271 in the human histamine H2 receptor determine the species selectivity of guanidine-type agonists and increase constitutive activity by Preuss, Hendrik, Ghorai, Prasanta, Kraus, Anja, Dove, Stefan, Buschauer, Armin, Seifert, Roland

“…In a steady-state GTPase activity assay, N-[3-(1H-imidazol-4-yl)propyl)]guanidines and N(G)-acylated derivatives are more potent and efficacious at fusion…”
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Structure-activity relationships of histamine H2 receptor ligands by Dove, Stefan, Elz, Sigurd, Seifert, Roland, Buschauer, Armin

“…Recent research on histamine H2 receptor agonists was focused on quantitative structure-activity relationships and receptor models explaining the activity of…”
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Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[ b]furan-2-yl)methanones by Mahboobi, Siavosh, Uecker, Andrea, Cénac, Christophe, Sellmer, Andreas, Eichhorn, Emerich, Elz, Sigurd, Böhmer, Frank-D., Dove, Stefan

“…Disubstituted bisbenzofuranylmethanones were found to inhibit PDGFR and/or FLT3 autophosphorylation. Modeling studies suggest that conformational adaptation…”
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A Single Amino Acid Exchange Inverts Susceptibility of Related Receptor Tyrosine Kinases for the ATP Site Inhibitor STI-571 by Böhmer, Frank D, Karagyozov, Luchezar, Uecker, Andrea, Serve, Hubert, Botzki, Alexander, Mahboobi, Siavosh, Dove, Stefan

“…The tyrosine kinase inhibitor STI-571 potently blocks BCR-Abl, platelet-derived growth factor (PDGF) α- and β-receptors, and c-Kit kinase activity. Flt3, a…”
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Inhibitors of Bacillus anthracis edema factor by SEIFERT, Roland, DOVE, Stefan

“…Edema factor (EF) is a calmodulin (CaM)-activated adenylyl cyclase (AC) toxin from Bacillus anthracis that contributes to anthrax pathogenesis. Anthrax is an…”
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Multivariate analysis of hydrophobic descriptors by Dove, Stefan

“…Multivariate approaches like principal component analysis (PCA) are powerful tools to investigate hydrophobic descriptors and to discriminate between intrinsic…”
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Mammalian Nucleotidyl Cyclases and Their Nucleotide Binding Sites by Dove, Stefan

“…Mammalian membranous and soluble adenylyl cyclases (mAC, sAC) and soluble guanylyl cyclases (sGC) generate cAMP and cGMP from ATP and GTP, respectively, as…”
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NG‐Acylated Aminothiazolylpropylguanidines as Potent and Selective Histamine H2 Receptor Agonists by Kraus, Anja, Ghorai, Prasanta, Birnkammer, Tobias, Schnell, David, Elz, Sigurd, Seifert, Roland, Dove, Stefan, Bernhardt, Günther, Buschauer, Armin

“…Bioisosteric replacement of the guanidino group in arpromidine‐like histamine H2 receptor (H2R) agonists by an acylguanidine moiety is useful for obtaining…”
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