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Inhibition of inducible nitric oxide synthase in respiratory diseases

Autor: Wolf-Rüdiger Ulrich, Andreas Strub, Clemens Braun, Martin D. Lehner, Christian Hesslinger, Rainer Boer

Publikováno v: Biochemical Society Transactions. 37:886-891

Nitric oxide (NO) is a key physiological mediator and disturbed regulation of NO release is associated with the pathophysiology of almost all inflammatory diseases. A multitude of inhibitors of NOSs (nitric oxide synthases) have been developed, initi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5c57ff63daac90cd4d86f5f4162a67b7
https://doi.org/10.1042/bst0370886

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Imidazoquinolinone, Imidazopyridine, and Isoquinolindione Derivatives as Novel and Potent Inhibitors of the Poly(ADP-ribose) Polymerase (PARP): A Comparison with Standard PARP Inhibitors

Autor: Thomas Klein, Steffen Weinbrenner, Christoph Thiemermann, Alexander Bürkle, Rainer Boer, Michelle C. McDonald, Tobias Eltze, Thomas Wagner

Publikováno v: Molecular Pharmacology. 74:1587-1598

We have identified three novel structures for inhibitors of the poly(ADP-ribose) polymerase (PARP), a nuclear enzyme activated by strand breaks in DNA and implicated in DNA repair, apoptosis, organ dysfunction or necrosis. 2-[4-(5-Methyl-1H-imidazol-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a44a7f939f8b684849da141abbb84831
https://doi.org/10.1124/mol.108.048751

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BYK191023 (2-[2-(4-Methoxy-pyridin-2-yl)-ethyl]-3H-imidazo[4,5-b]pyridine) Is an NADPH- and Time-Dependent Irreversible Inhibitor of Inducible Nitric-Oxide Synthase

Autor: Mauro Tiso, Rainer Boer, Claire Kenney, Christian Hesslinger, Andreas Strub, Dennis J. Stuehr

Publikováno v: Molecular Pharmacology. 73:1244-1253

Imidazopyridine derivates were recently shown to be a novel class of selective and arginine-competitive inhibitors of inducible nitric-oxide synthase (iNOS), and 2-[2-(4-methoxypyridin-2-yl)-ethyl]-3H-imidazo[4,5-b]pyridine (BYK191023) was found to h

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7a36fa0ec5312ab8270687edb40faf41
https://doi.org/10.1124/mol.107.041319

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In Vivo Characterization of the Novel Imidazopyridine BYK191023 [2-[2-(4-Methoxy-pyridin-2-yl)-ethyl]-3H-imidazo[4,5-b]pyridine], a Potent and Highly Selective Inhibitor of Inducible Nitric-Oxide Synthase

Autor: Wolf-Rüdiger Ulrich, Rainer Boer, Andreas Strub, Degenhard Marx, Christian Hesslinger, Manfrid Eltze, Martin Lehner, Ralph T. Schermuly, Frank Schwoebel, Johannes Barsig

Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 317:181-187

Excessive release of nitric oxide from inducible nitric-oxide synthase (iNOS) has been postulated to contribute to pathology in a number of inflammatory diseases. We recently identified imidazopyridine derivatives as a novel class of potent nitricoxi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b5a19c85fb7a766f175e9daf2a300f0c
https://doi.org/10.1124/jpet.105.098673

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Characterization of the Dexniguldipine Binding Site in the Multidrug Resistance-Related Transport Protein P-Glycoprotein by Photoaffinity Labeling and Mass Spectrometry

Autor: Michael Przybylski, Thomas Denzinger, Kurt Prof Dr Klemm, S. Haas, W Ise, Volker Gekeler, Volker Dr Figala, Wolf-Rüdiger Ulrich, C Borchers, Rainer Boer

Publikováno v: Molecular Pharmacology. 61:1366-1376

Human P-glycoprotein (P-gp), an integral membrane transport protein, is responsible for the efflux of various drugs, including cytostatics from cancer cells leading to multidrug resistance. P-gp is composed of two homologous half domains, each carryi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::22d8db5c4a7374094d3fb410752de8cc
https://doi.org/10.1124/mol.61.6.1366

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In vitro and in vivo uroselectivity of B8805-033, an antagonist with high affinity at prostatic α 1A - vs. α 1B - and α 1D -adrenoceptors

Autor: Rodolfo Testa, Karl Sanders, Rainer Boer, Norbert Kolassa, Wolf-Rüdiger Ulrich, Peter Hein, Manfrid Eltze, Martin C. Michel

Publikováno v: Naunyn-Schmiedeberg's Archives of Pharmacology. 363:649-662

We have investigated the pharmacological properties of B8805-033 [(+/-)- 1,3,5-trimethyl-6-[[3-[4-((2,3-dihydro-2-hydroxymethyl)-1,4-benzodioxin-5-yl)-1-piperazinyl]propyl] amino]-2,4(1H,3H)-pyrimidinedione], a new alpha1A-adrenoceptor (AR) selective

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4864eea16cbea494f8eb96d061eab388
https://doi.org/10.1007/s002100100413

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The Inhibitory Potency and Selectivity of Arginine Substrate Site Nitric-Oxide Synthase Inhibitors Is Solely Determined by Their Affinity toward the Different Isoenzymes

Autor: Berit Mirau, Thomas Klein, Ilka Baur, Rainer Boer, S. Haas, Wolf-Rüdiger Ulrich

Publikováno v: Molecular Pharmacology. 58:1026-1034

We have investigated various nitric oxide (NO) synthase inhibitors for their affinity and selectivity toward the three human isoenzymes in radioligand binding experiments. Therefore, we developed the new radioligand [(3)H]2-amino-4-picoline to measur

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0e82bf7018107768842e5b2edbdce753
https://doi.org/10.1124/mol.58.5.1026

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Rhodamine 123 efflux modulation in the presence of low or high serum from CD56+ hematopoietic cells or CD34+ leukemic blasts by B9309-068, a newly designed pyridine derivative

Autor: Wolf-Rüdiger Ulrich, Volker Gekeler, Dietrich Niethammer, Frank Buchholz, James F. Beck, Rainer Boer, Karl Sanders

Publikováno v: Cancer Letters. 129:157-163

The newly designed pyridine derivative B9309-068 and a series of structurally different compounds were tested for their ability to modulate rhodamine 123 (RHO) efflux from CD56+ hematopoietic cells in the presence of either 10% fetal calf serum or un

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::27c8543af978a450782541a060b380c7
https://doi.org/10.1016/s0304-3835(98)00094-9

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Effects of the selective bisindolylmaleimide protein kinase C inhibitor GF 109203X on P-glycoprotein-mediated multidrug resistance

Autor: I. Utz, Kurt Prof Dr Klemm, C. Schachtele, Florian Überall, Volker Gekeler, Rainer Boer, Johann Hofmann, W Ise, C Schubert, H. Grunicke, K.H. Sanders

Publikováno v: British Journal of Cancer

Inhibition of protein kinase C (PKC) is discussed as a new approach for overcoming multidrug resistance (MDR) in cancer chemotherapy. For evaluation of this concept we applied the bisindolylmaleimide GF 109203X, which shows a highly selective inhibit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2a8869fdbf4f5de792bb23c285f53518
https://doi.org/10.1038/bjc.1996.454

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Modulation of P-glycoprotein mediated drug accumulation in multidrug resistant CCRF VCR-1000 cells by chemosensitisers

Autor: W. Ise, W.-R. Ulrich, P. Zimmermann, S. Haas, Volker Gekeler, A. Schödl, Rainer Boer

Publikováno v: European Journal of Cancer. 32:857-861

P-glycoprotein (PGP) mediated transport of cytostatic drugs out of resistant cancer cells is a major cause of experimental and probably also of clinical multidrug resistance, which often leads to treatment failure during chemotherapy. The broad subst

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d648b6937533edd0cd58a728293da961
https://doi.org/10.1016/0959-8049(95)00661-3

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