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36 results on '"Wágner, Gábor"'

1. New Chemical Biology Tools for the Histamine Receptor Family

Author

Zheng, Yang, Wágner, Gábor, Hauwert, Niels, Ma, Xiaoyuan, Vischer, Henry F., Leurs, Rob, Geyer, Mark A., Series Editor, Marsden, Charles A., Series Editor, Ellenbroek, Bart A., Series Editor, Barnes, Thomas R. E., Series Editor, Andersen, Susan L., Series Editor, Paulus, Martin P., Series Editor, Yanai, Kazuhiko, editor, and Passani, Maria Beatrice, editor

Published
2022
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3. Discovery of 4-amino-3-arylsulfoquinolines, a novel non-acetylenic chemotype of metabotropic glutamate 5 (mGlu5) receptor negative allosteric modulators

Author

Galambos, János, Bielik, Attila, Wágner, Gábor, Domány, György, Kóti, János, Béni, Zoltán, Szigetvári, Áron, Sánta, Zsuzsanna, Orgován, Zoltán, Bobok, Amrita, Kiss, Béla, Mikó-Bakk, Mónika L., Vastag, Mónika, Sághy, Katalin, Krasavin, Mikhail, Gál, Krisztina, Greiner, István, Szombathelyi, Zsolt, and Keserű, György M.

Published
2017
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5. SAR exploration of the non‐imidazole histamine H3 receptor ligand ZEL‐H16 reveals potent inverse agonism

Author

Wágner, Gábor, primary, Mocking, Tamara A. M., additional, Ma, Xiaoyuan, additional, Slynko, Inna, additional, Da Costa Pereira, Daniel, additional, Breeuwer, Robin, additional, Rood, Niek J. N., additional, van der Horst, Cas, additional, Vischer, Henry F., additional, de Graaf, Chris, additional, de Esch, Iwan J. P., additional, Wijtmans, Maikel, additional, and Leurs, Rob, additional

Published
2022
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13. Covalent Inhibition of the Histamine H3 Receptor

Author

Wágner, Gábor, primary, Mocking, Tamara A. M., additional, Kooistra, Albert J., additional, Slynko, Inna, additional, Ábrányi-Balogh, Péter, additional, Keserű, György M., additional, Wijtmans, Maikel, additional, Vischer, Henry F., additional, de Esch, Iwan J. P., additional, and Leurs, Rob, additional

Published
2019
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14. 4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H3 Receptor Agonists with in Vivo Central Nervous System Activity

Author

Wágner, Gábor, primary, Mocking, Tamara A. M., additional, Arimont, Marta, additional, Provensi, Gustavo, additional, Rani, Barbara, additional, Silva-Marques, Bruna, additional, Latacz, Gniewomir, additional, Da Costa Pereira, Daniel, additional, Karatzidou, Christina, additional, Vischer, Henry F., additional, Wijtmans, Maikel, additional, Kieć-Kononowicz, Katarzyna, additional, de Esch, Iwan J. P., additional, and Leurs, Rob, additional

Published
2019
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21. Discovery of 4-amino-3-arylsulfoquinolines, a novel non-acetylenic chemotype of metabotropic glutamate 5 (mGlu 5 ) receptor negative allosteric modulators

Author

Galambos, János, primary, Bielik, Attila, additional, Wágner, Gábor, additional, Domány, György, additional, Kóti, János, additional, Béni, Zoltán, additional, Szigetvári, Áron, additional, Sánta, Zsuzsanna, additional, Orgován, Zoltán, additional, Bobok, Amrita, additional, Kiss, Béla, additional, Mikó-Bakk, Mónika L., additional, Vastag, Mónika, additional, Sághy, Katalin, additional, Krasavin, Mikhail, additional, Gál, Krisztina, additional, Greiner, István, additional, Szombathelyi, Zsolt, additional, and Keserű, György M., additional

Published
2017
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22. Discovery and Preclinical Characterization of 3-((4-(4-Chlorophenyl)-7-fluoroquinoline-3-yl)sulfonyl)benzonitrile, a Novel Non-acetylenic Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator for Psychiatric Indications

Author

Galambos, János, primary, Bielik, Attila, additional, Krasavin, Mikhail, additional, Orgován, Zoltán, additional, Domány, György, additional, Nógrádi, Katalin, additional, Wágner, Gábor, additional, Balogh, György T., additional, Béni, Zoltán, additional, Kóti, János, additional, Szakács, Zoltán, additional, Bobok, Amrita, additional, Kolok, Sándor, additional, Mikó-Bakk, Mónika L., additional, Vastag, Mónika, additional, Sághy, Katalin, additional, Laszy, Judit, additional, Halász, Attila Sándor, additional, Balázs, Ottilia, additional, Gál, Krisztina, additional, Greiner, István, additional, Szombathelyi, Zsolt, additional, and Keserű, György M., additional

Published
2017
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25. 4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H3Receptor Agonists with in Vivo Central Nervous System Activity

Author

Wágner, Gábor, Mocking, Tamara A. M., Arimont, Marta, Provensi, Gustavo, Rani, Barbara, Silva-Marques, Bruna, Latacz, Gniewomir, Da Costa Pereira, Daniel, Karatzidou, Christina, Vischer, Henry F., Wijtmans, Maikel, Kieć-Kononowicz, Katarzyna, de Esch, Iwan J. P., and Leurs, Rob

Abstract

Despite the high diversity of histamine H3receptor (H3R) antagonist/inverse agonist structures, partial or full H3R agonists have typically been imidazole derivatives. An in-house screening campaign intriguingly afforded the non-imidazole 4-(3-azetidin-1-yl)pyrimidin-2-amine 11bas a partial H3R agonist. Here, the design, synthesis, and structure–activity relationships of 11banalogues are described. This series yields several non-imidazole full agonists with potencies varying with the alkyl substitution pattern on the basic amine following the in vitro evaluation of H3R agonism using a cyclic adenosine monophosphate response element-luciferase reporter gene assay. The key compound VUF16839 (14d) combines nanomolar on-target activity (pKi= 8.5, pEC50= 9.5) with weak activity on cytochrome P450 enzymes and good metabolic stability. The proposed H3R binding mode of 14dindicates key interactions similar to those attained by histamine. In vivo evaluation of 14din a social recognition test in mice revealed an amnesic effect at 5 mg/kg intraperitoneally. The excellent in vitro and in vivo pharmacological profiles and the non-imidazole structure of 14dmake it a promising tool compound in H3R research.

Published
2019
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26. Thieno[2,3- b ]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: Lead optimization

Author

Nógrádi, Katalin, primary, Wágner, Gábor, additional, Domány, György, additional, Bobok, Amrita, additional, Magdó, Ildikó, additional, Kolok, Sándor, additional, Mikó-Bakk, Mónika L., additional, Vastag, Mónika, additional, Sághy, Katalin, additional, Gyertyán, István, additional, Kóti, János, additional, Gál, Krisztina, additional, Farkas, Sándor, additional, Keserű, György M., additional, Greiner, István, additional, and Szombathelyi, Zsolt, additional

Published
2015
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27. Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists

Author

Galambos, János, Wágner, Gábor, Nógrádi, Katalin, Bielik, Attila, Molnár, László, Bobok, Amrita, Horváth, Attila, Kiss, Béla, Kolok, Sándor, Nagy, József, Kurkó, Dalma, Bakk, Mónika L., Vastag, Mónika, Sághy, Katalin, Gyertyán, István, Gál, Krisztina, Greiner, István, Szombathelyi, Zsolt, Keserű, György M., and Domány, György

Published
2010
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30. Corrigendum to “Hit-to-lead optimization of disubstituted oxadiazoles and tetrazoles as mGluR5 NAMs” [Bioorg. Med. Chem. Lett. 20 (2010) 3737–3741]

Author

Wágner, Gábor, primary, Wéber, Csaba, additional, Nyéki, Olga, additional, Nógrádi, Katalin, additional, Bielik, Attila, additional, Molnár, László, additional, Bobok, Amrita, additional, Horváth, Attila, additional, Kiss, Béla, additional, Kolok, Sándor, additional, Nagy, József, additional, Kurkó, Dalma, additional, Gál, Krisztina, additional, Greiner, István, additional, Szombathelyi, Zsolt, additional, Keserű, György M., additional, and Domány, György, additional

Published
2011
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34. Combined Enhancement of Microtubule Assembly and Glucose Metabolism in Neuronal Systems in Vitro:Decreased Sensitivity to Copper Toxicity

Author

Liliom, Károly, Wágner, Gábor, Kovács, János, Comin, Begoña, Cascante, Marta, Orosz, Ferenc, and Ovádi, Judit

Abstract

Brain cell-free extract greatly stimulates the polymerization rate of purified tubulin with a reduction of the nucleation period and without a significant alteration of the final assembly state. This effect is mimicked by neuroblastoma extract at 10-fold lower extract concentration, but not by excess muscle extract. Copper inhibits microtubule assembly in vitrobut in the presence of brain extract the copper effect is suspended. Electron microscopic images showed that intact microtubules are formed and decorated by cytosolic proteins in the absence and presence of copper, while the copper alone induces the formation of S-shaped sheets and oligomeric threads. The flux of triosephosphate formation from glucose is enhanced by microtubules in brain extract, but not in muscle extract. Copper inhibits the glycolytic flux; however, the presence of microtubules not only suspends the inhibition by copper but the activation of glycolysis by microtubules is also preserved. We conclude that the organization of neuronal proteins modifies both the rates of microtubule assembly and glycolysis, and reduces their sensitivities against the inhibition caused by copper.

Published
1999
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35. SAR exploration of the non-imidazole histamine H 3 receptor ligand ZEL-H16 reveals potent inverse agonism.

Author

Wágner G, Mocking TAM, Ma X, Slynko I, Da Costa Pereira D, Breeuwer R, Rood NJN, van der Horst C, Vischer HF, de Graaf C, de Esch IJP, Wijtmans M, and Leurs R

Subjects
Drug Inverse Agonism, Ligands, Histamine Agonists pharmacology, Histamine Agonists chemistry, Structure-Activity Relationship, Receptors, Histamine, Histamine, Receptors, Histamine H3
Abstract

Histamine H 3 receptor (H 3 R) agonists without an imidazole moiety remain very scarce. Of these, ZEL-H16 (1) has been reported previously as a high-affinity non-imidazole H 3 R (partial) agonist. Our structure-activity relationship analysis using derivatives of 1 identified both basic moieties as key interaction motifs and the distance of these from the central core as a determinant for H 3 R affinity. However, in spite of the reported H 3 R (partial) agonism, in our hands, 1 acts as an inverse agonist for Gα i signaling in a CRE-luciferase reporter gene assay and using an H 3 R conformational sensor. Inverse agonism was also observed for all of the synthesized derivatives of 1. Docking studies and molecular dynamics simulations suggest ionic interactions/hydrogen bonds to H 3 R residues D114 3.32 and E206 5.46 as essential interaction points., (© 2022 The Authors. Archiv der Pharmazie published by Wiley-VCH GmbH on behalf of Deutsche Pharmazeutische Gesellschaft.)

Published
2023
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36. 4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H 3 Receptor Agonists with in Vivo Central Nervous System Activity.

Author

Wágner G, Mocking TAM, Arimont M, Provensi G, Rani B, Silva-Marques B, Latacz G, Da Costa Pereira D, Karatzidou C, Vischer HF, Wijtmans M, Kieć-Kononowicz K, de Esch IJP, and Leurs R

Subjects
Amines chemistry, Animals, Behavior, Animal drug effects, HEK293 Cells, Histamine Agonists chemistry, Humans, Memory drug effects, Mice, Molecular Docking Simulation, Molecular Structure, Protein Binding, Protein Conformation, Social Behavior, Amines chemical synthesis, Amines pharmacology, Histamine Agonists chemical synthesis, Histamine Agonists pharmacology
Abstract

Despite the high diversity of histamine H 3 receptor (H 3 R) antagonist/inverse agonist structures, partial or full H 3 R agonists have typically been imidazole derivatives. An in-house screening campaign intriguingly afforded the non-imidazole 4-(3-azetidin-1-yl)pyrimidin-2-amine 11b as a partial H 3 R agonist. Here, the design, synthesis, and structure-activity relationships of 11b analogues are described. This series yields several non-imidazole full agonists with potencies varying with the alkyl substitution pattern on the basic amine following the in vitro evaluation of H 3 R agonism using a cyclic adenosine monophosphate response element-luciferase reporter gene assay. The key compound VUF16839 ( 14d ) combines nanomolar on-target activity (p K i = 8.5, pEC 50 = 9.5) with weak activity on cytochrome P450 enzymes and good metabolic stability. The proposed H 3 R binding mode of 14d indicates key interactions similar to those attained by histamine. In vivo evaluation of 14d in a social recognition test in mice revealed an amnesic effect at 5 mg/kg intraperitoneally. The excellent in vitro and in vivo pharmacological profiles and the non-imidazole structure of 14d make it a promising tool compound in H 3 R research.

Published
2019
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