Search Results - "Zischinsky, Gunther"

A novel CDK7 inhibitor of the Pyrazolotriazine class exerts broad-spectrum antiviral activity at nanomolar concentrations by Hutterer, Corina, Eickhoff, Jan, Milbradt, Jens, Korn, Klaus, Zeitträger, Isabel, Bahsi, Hanife, Wagner, Sabrina, Zischinsky, Gunther, Wolf, Alexander, Degenhart, Carsten, Unger, Anke, Baumann, Matthias, Klebl, Bert, Marschall, Manfred

“…Protein kinases represent central and multifunctional regulators of a balanced virus-host interaction. Cyclin-dependent protein kinase 7 (CDK7) plays crucial…”
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Dual Inhibition of GSK3β and CDK5 Protects the Cytoskeleton of Neurons from Neuroinflammatory-Mediated Degeneration In Vitro and In Vivo by Reinhardt, Lydia, Kordes, Susanne, Reinhardt, Peter, Glatza, Michael, Baumann, Matthias, Drexler, Hannes C.A., Menninger, Sascha, Zischinsky, Gunther, Eickhoff, Jan, Fröb, Claudia, Bhattarai, Prabesh, Arulmozhivarman, Guruchandar, Marrone, Lara, Janosch, Antje, Adachi, Kenjiro, Stehling, Martin, Anderson, Eric N., Abo-Rady, Masin, Bickle, Marc, Pandey, Udai Bhan, Reimer, Michell M., Kizil, Caghan, Schöler, Hans R., Nussbaumer, Peter, Klebl, Bert, Sterneckert, Jared L.

“…Neuroinflammation is a hallmark of neurological disorders and is accompanied by the production of neurotoxic agents such as nitric oxide. We used stem…”
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In vivo proof-of-concept for two experimental antiviral drugs, both directed to cellular targets, using a murine cytomegalovirus model by Sonntag, Eric, Hahn, Friedrich, Bertzbach, Luca D., Seyler, Lisa, Wangen, Christina, Müller, Regina, Tannig, Pierre, Grau, Benedikt, Baumann, Matthias, Zent, Eldar, Zischinsky, Gunther, Eickhoff, Jan, Kaufer, Benedikt B., Bäuerle, Tobias, Tsogoeva, Svetlana B., Marschall, Manfred

“…Infections with the human cytomegalovirus (HCMV) cause serious medical problems including organ rejection and congenital infection. Treatment of HCMV…”
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Abstract 5936: A novel class of orally bioavailable small molecules induces potent and sustained tumor growth inhibition and T cell infiltration in various solid tumor mouse models by Gapp, Bianca, Zischinsky, Gunther, Urban, Maria, Birnbacher, Nora, Schwarzböck, Alice, Grünaug, Sabine, Gastaldi, Tommaso, Stütz, Anton, Nussbaumer, Peter, Stranner, Stefan, Buchberger, Julia, Birbach, Andreas, Schögl, Daniela, Kuttke, Mario, Dohnal, Alexander, Gugenberger, Romana

“…The introduction of targeted immunomodulating agents has transformed cancer treatment over the last decade by demonstrating unprecedented efficacy in patients…”
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Chemical Validation of DegS As a Target for the Development of Antibiotics with a Novel Mode of Action by Bongard, Jens, Schmitz, Anna Laura, Wolf, Alex, Zischinsky, Gunther, Pieren, Michel, Schellhorn, Birgit, Bravo‐Rodriguez, Kenny, Schillinger, Jasmin, Koch, Uwe, Nussbaumer, Peter, Klebl, Bert, Steinmann, Jörg, Buer, Jan, Sanchez‐Garcia, Elsa, Ehrmann, Michael, Kaiser, Markus

“…Despite the availability of hundreds of antibiotic drugs, infectious diseases continue to remain one of the most notorious health issues. In addition, the…”
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Design and Synthesis of a New Class of Selective Integrin α5β1 Antagonists by Stragies, Roland, Osterkamp, Frank, Zischinsky, Gunther, Vossmeyer, Doerte, Kalkhof, Holger, Reimer, Ulf, Zahn, Grit

“…Starting from the structure of integrin αvβ3 in a complex with a peptidic ligand plus SAR data on nonpeptidic ligands, we derived a new class of integrin α5β1…”
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Abstract 416: A novel non-covalent and rapidly reversible proteasome inhibitor for multiple myeloma and various solid cancers by Ahn, Won-Gyun, Jeon, Yeejin, Yang, Yeong-In, Kim, Jaeseung, Lee, Seung-Joo, Koch, Uwe, Zischinsky, Gunther, Choidas, Axel, Pasha, Ayesha, Klebl, Bert, Huber, Robert, Hamacher, Michael, Nam, Kiyean

“…The existing proteasome inhibitors, such as bortezomib and ixazomib, are effective in multiple myeloma, but have little activity against solid tumors. These…”
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Abstract 2997: Dynarrestin, a novel dynein inhibitor that does not block ciliogenesis by Baumann, Matthias, Höing, Susanne, Yeh, Ting-Yu, Martinez, Nancy, Habenberger, Peter, Kremer, Lea, Drexler, Hannes CA, Küchler, Philipp, Reinhardt, Peter, Choidas, Axel, Zischinsky, Mia-Lisa, Zischinsky, Gunther, Ketcham, Stephanie A., Wagner, Lydia, Nussbaumer, Peter, Ziegler, Slava, Klebl, Bert, Schroer, Trina, Schöler, Hans R., Waldmann, Herbert, Sterneckert, Jared L.

“…Introduction: Aberrant hedgehog (Hh) pathway activation contributes to the pathogenesis of multiple cancers. Currently available Hh pathway inhibitors target…”
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α5β1 Integrin Blockade Inhibits Lymphangiogenesis in Airway Inflammation by Okazaki, Tatsuma, Ni, Amy, Ayeni, Oluwasheyi A, Baluk, Peter, Yao, Li-Chin, Vossmeyer, Doerte, Zischinsky, Gunther, Zahn, Grit, Knolle, Jochen, Christner, Claudia, McDonald, Donald M

“…The integrin α5β1 has been previously implicated in tumor angiogenesis, but its role in the remodeling of both blood vessels and lymphatics during inflammation…”
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Abstract 695: The generation of a mono-selective CDK7 inhibitor by Eickhoff, Jan E., Zischinsky, Gunther, Choidas, Axel, Habenberger, Peter, Wolf, Alexander, Degenhardt, Carsten, Baumann, Matthias, Unger, Anke, Ghallab, Ahmad, Werchau, Doreen, Hengstler, Jan, Nussbaumer, Peter, Klebl, Bert M.

“…Cyclin-depending kinase (CDK) family members that trigger passage through the cell cycle have been considered as attractive cancer targets for at least two…”
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Discovery of orally available integrin α5β1 antagonists by Zischinsky, Gunther, Osterkamp, Frank, Vossmeyer, Doerte, Zahn, Grit, Scharn, Dirk, Zwintscher, Ariane, Stragies, Roland

“…Combining structural features of integrin α5β1 antagonists leads to the generic structure 3. The compounds expressing high integrin α5β1 binding affinities,…”
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SAR of N-phenyl piperidine based oral integrin α5β1 antagonists by Zischinsky, Gunther, Osterkamp, Frank, Vossmeyer, Doerte, Zahn, Grit, Scharn, Dirk, Zwintscher, Ariane, Stragies, Roland

“…Correlation of structural features of selected N-phenyl piperidine derivatives 3 with integrin α5β1 binding affinities and selectivities as well as…”
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SAR of N-phenyl piperidine based oral integrin a5b1 antagonists by Zischinsky, Gunther, Osterkamp, Frank, Vossmeyer, Doerte, Zahn, Grit, Scharn, Dirk, Zwintscher, Ariane, Stragies, Roland

“…Recently, a new class of selective integrin a5b1inhibitors consisting of a heterocyclic based scaffold was published. Herein the SAR and pharmacokinetic…”
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Discovery of orally available integrin a5b1 antagonists by Zischinsky, Gunther, Osterkamp, Frank, Vossmeyer, Doerte, Zahn, Grit, Scharn, Dirk, Zwintscher, Ariane, Stragies, Roland

“…Previous research within our laboratories identified the 3-hydroxypyrrolidine scaffold 1 as a new and selective integrin a5b1 inhibitor class which was…”
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Novel small molecule bradykinin B 1 receptor antagonists. Part 1: Benzamides and semicarbazides by Schaudt, Marco, Locardi, Elsa, Zischinsky, Gunther, Stragies, Roland, Pfeifer, Jochen R., Gibson, Christoph, Scharn, Dirk, Richter, Uwe, Kalkhof, Holger, Dinkel, Klaus, Schnatbaum, Karsten

“…Benzamides and semicarbazides are introduced as new classes of bradykinin B 1 receptor antagonists. The best compounds feature excellent pharmacokinetic…”
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Novel small molecule bradykinin B 1 receptor antagonists. Part 2: 5-membered diaminoheterocycles by Zischinsky, Gunther, Stragies, Roland, Schaudt, Marco, Pfeifer, Jochen R., Gibson, Christoph, Locardi, Elsa, Scharn, Dirk, Richter, Uwe, Kalkhof, Holger, Dinkel, Klaus, Schnatbaum, Karsten

“…New bradykinin B1 receptor antagonists based on 5-membered diaminoheterocycles with nanomolar activity are presented. Efforts to find new bradykinin B 1…”
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Novel small molecule bradykinin B 1 receptor antagonists. Part 3: Hydroxyurea derivatives by Schnatbaum, Karsten, Schaudt, Marco, Stragies, Roland, Pfeifer, Jochen R., Gibson, Christoph, Locardi, Elsa, Scharn, Dirk, Richter, Uwe, Kalkhof, Holger, Dinkel, Klaus, Zischinsky, Gunther

“…Hydroxy urea analogues have been developed as a new class of bradykinin B1 receptor antagonists. Systematic optimization led to the identification of several…”
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Design and synthesis of a new class of selective integrin alpha5beta1 antagonists by Stragies, Roland, Osterkamp, Frank, Zischinsky, Gunther, Vossmeyer, Doerte, Kalkhof, Holger, Reimer, Ulf, Zahn, Grit

“…Starting from the structure of integrin alphavbeta3 in a complex with a peptidic ligand plus SAR data on nonpeptidic ligands, we derived a new class of…”
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Novel small molecule bradykinin B sub(1) receptor antagonists. Part 1: Benzamides and semicarbazides by Schaudt, Marco, Locardi, Elsa, Zischinsky, Gunther, Stragies, Roland, Pfeifer, Jochen R, Gibson, Christoph, Scharn, Dirk, Richter, Uwe, Kalkhof, Holger, Dinkel, Klaus, Schnatbaum, Karsten

“…The synthesis and SAR of two series of bradykinin B sub(1) receptor antagonists is described. The benzamide moiety proved to be a suitable replacement for the…”
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Novel small molecule bradykinin B sub(1) receptor antagonists. Part 2: 5-membered diaminoheterocycles by Zischinsky, Gunther, Stragies, Roland, Schaudt, Marco, Pfeifer, Jochen R, Gibson, Christoph, Locardi, Elsa, Scharn, Dirk, Richter, Uwe, Kalkhof, Holger, Dinkel, Klaus, Schnatbaum, Karsten

“…Efforts to find new bradykinin B sub(1) receptor antagonists identified 2-aminobenzimidazole as a novel core. Subsequent transformation into five-membered…”
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