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Hier finden Sie wissenschaftliche Publikationen aus den Fraunhofer-Instituten.
2021AGMO Inhibitor Reduces 3T3-L1 Adipogenesis
Fischer, C.; Wilken-Schmitz, A.; Hernandez-Olmos, V.; Proschak, E.; Stark, H.; Fleming, I.; Weigert, A.; Thurn, M.; Hofmann, M.; Werner, E.R.; Geisslinger, G.; Niederberger, E.; Watschinger, K.; Tegeder, I.
Journal Article
2021Combined Cardioprotective and Adipocyte Browning Effects Promoted by the Eutomer of Dual sEH/PPARγ Modulator
Hartmann, M.; Bibli, S.-I.; Tews, D.; Ni, X.; Kircher, T.; Kramer, J.S.; Kilu, W.; Heering, J.; Hernandez-Olmos, V.; Weizel, L.; Scriba, G.K.E.; Krait, S.; Knapp, S.; Chaikuad, A.; Merk, D.; Fleming, I.; Fischer-Posovszky, P.; Proschak, E.
Journal Article
2021Demonstrating Ligandability of the LC3A and LC3B Adapter Interface
Hartmann, M.; Huber, J.; Kramer, J.S.; Heering, J.; Pietsch, L.; Stark, H.; Odadzic, D.; Bischoff, I.; Fürst, R.; Schröder, M.; Akutsu, M.; Chaikuad, A.; Dötsch, V.; Knapp, S.; Biondi, R.M.; Rogov, V.V.; Proschak, E.
Journal Article
2021Structural Insights into Plasticity and Discovery of Remdesivir Metabolite GS-441524 Binding in SARS-CoV-2 Macrodomain
Ni, X.; Schröder, M.; Olieric, V.; Sharpe, M.E.; Hernandez-Olmos, V.; Proschak, E.; Merk, D.; Knapp, S.; Chaikuad, A.
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2020Computer-Aided Fragment Growing Strategies to Design Dual Inhibitors of Soluble Epoxide Hydrolase and LTA4 Hydrolase
Hefke, L.; Hiesinger, K.; Zhu, W.F.; Kramer, J.S.; Proschak, E.
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2020Design, Synthesis, and Structure - Activity Relationship Studies of Dual Inhibitors of Soluble Epoxide Hydrolase and 5-Lipoxygenase
Hiesinger, K.; Kramer, J.S.; Beyer, S.; Eckes, T.; Brunst, S.; Flauaus, C.; Wittmann, S.K.; Weizel, L.; Kaiser, A.; Kretschmer, S.B.M.; George, S.; Angioni, C.; Heering, J.; Geisslinger, G.; Schubert-Zsilavecz, M.; Schmidtko, A.; Pogoryelov, D.; Pfeilschifter, J.; Hofmann, B.; Steinhilber, D.; Schwalm, S.; Proschak, E.
Journal Article
2020Dual Farnesoid X Receptor/Soluble Epoxide Hydrolase Modulators Derived from Zafirlukast
Schierle, S.; Helmstädter, M.; Schmidt, J.; Hartmann, M.; Horz, M.; Kaiser, A.; Weizel, L.; Heitel, P.; Proschak, A.; Hernandez-Olmos, V.; Proschak, E.; Merk, D.
Journal Article
2020Dual soluble epoxide hydrolase inhibitor/PPAR-γ agonist attenuates renal fibrosis
Stavniichuk, A.; Hye Khan, M.A.; Yeboah, M.M.; Chesnik, M.A.; Jankiewicz, W.K.; Hartmann, M.; Blöcher, R.; Kircher, T.; Savchuk, O.; Proschak, E.; Imig, J.D.
Journal Article
2020The endocannabinoid anandamide has an anti-inflammatory effect on CCL2 expression in vascular smooth muscle cells
Pflüger-Müller, B.; Oo, J.A.; Heering, J.; Warwick, T.; Proschak, E.; Günther, S.; Looso, M.; Rezende, F.; Fork, C.; Geisslinger, G.; Thomas, D.; Gurke, R.; Steinhilber, D.; Schulz, M.; Leisegang, M.S.; Brandes, R.P.
Journal Article
2020First Structure-Activity Relationship Study of Potent BLT2 Agonists as Potential Wound-Healing Promoters
Hernandez-Olmos, V.; Heering, J.; Planz, V.; Liu, T.; Kaps, A.; Rajkumar, R.; Gramzow, M.; Kaiser, A.; Schubert-Zsilavecz, M.; Parnham, M.J.; Windbergs, M.; Steinhilber, D.; Proschak, E.
Journal Article
2020l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC are Potent Activators of PPARγ
Gellrich, L.; Heitel, P.; Heering, J.; Kilu, W.; Pollinger, J.; Goebel, T.; Kahnt, A.; Arifi, S.; Pogoda, W.; Paulke, A.; Steinhilber, D.; Proschak, E.; Wurglics, M.; Schubert-Zsilavecz, M.; Chaikuad, A.; Knapp, S.; Bischoff, I.; Fürst, R.; Merk, D.
Journal Article
2020Reversible Small Molecule Inhibitors of MAO A and MAO B with Anilide Motifs
Hagenow, J.; Hagenow, S.; Grau, K.; Khanfar, M.; Hefke, L.; Proschak, E.; Stark, H.
Journal Article
2020A Selective Modulator of Peroxisome Proliferator-Activated Receptor γ with an Unprecedented Binding Mode
Hanke, T.; Cheung, S.-Y.; Kilu, W.; Heering, J.; Ni, X.; Planz, V.; Schierle, S.; Faudone, G.; Friedrich, M.; Wanior, M.; Werz, O.; Windbergs, M.; Proschak, E.; Schubert-Zsilavecz, M.; Chaikuad, A.; Knapp, S.; Merk, D.
Journal Article
2020Soluble epoxide hydrolase inhibitors with carboranes as non-natural 3-D pharmacophores
Scholz, M.S.; Wingen, L.M.; Brunst, S.; Wittmann, S.K.; Cardoso, I.L.A.; Weizel, L.; Proschak, E.
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2020Systematic Assessment of Fragment Identification for Multitarget Drug Design
Brunst, S.; Kramer, J.S.; Kilu, W.; Heering, J.; Pollinger, J.; Hiesinger, K.; George, S.; Steinhilber, D.; Merk, D.; Proschak, E.
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2019Capillary electrophoresis‐based enzyme assays for β‐lactamase enzymes
Chen, C.; Kramer, J.S.; Brunst, S.; Proschak, E.; Scriba, G.K.E.
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2019Computer-Aided Selective Optimization of Side Activities of Talinolol
Hiesinger, K.; Kramer, J.S.; Achenbach, J.; Moser, D.; Weber, J.; Wittmann, S.K.; Morisseau, C.; Angioni, C.; Geisslinger, G.; Kahnt, A.S.; Kaiser, A.; Proschak, A.; Steinhilber, D.; Pogoryelov, D.; Wagner, K.; Hammock, B.D.; Proschak, E.
Journal Article
2019Computer-Assisted Discovery and Structural Optimization of a Novel Retinoid X Receptor Agonist Chemotype
Heitel, P.; Gellrich, L.; Kalinowsky, L.; Heering, J.; Kaiser, A.; Ohrndorf, J.; Proschak, E.; Merk, D.
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2019Development of multitarget agents possessing soluble epoxide hydrolase inhibitory activity
Hiesinger, K.; Wagner, K.M.; Hammock, B.D.; Proschak, E.; Hwang, S.H.
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2019Discovery of the First in Vivo Active Inhibitors of the Soluble Epoxide Hydrolase Phosphatase Domain
Kramer, JS.; Woltersdorf, S.; Duflot, T.; Hiesinger, K.; Lillich, FF.; Knoll, F.; Wittmann, SK.; Klingler, FM.; Brunst, S.; Chaikuad, A.; Morisseau, C.; Hammock, BD.; Buccellati, C.; Sala, A.; Rovati, GE.; Leuillier, M.; Fraineau, S.; Rondeaux, J.; Hernandez-Olmos, V.; Heering, J.; Merk, D.; Pogoryelov, D.; Steinhilber, D.; Knapp, S.; Bellien, J.; Proschak, E.
Journal Article
2019Gliotoxin from Aspergillus fumigatus Abrogates Leukotriene B4 Formation through Inhibition of Leukotriene A4 Hydrolase
König, S.; Pace, S.; Pein, H.; Heinekamp, T.; Kramer, J.; Romp, E.; Straßburger, M.; Troisi, F.; Proschak, A.; Dworschak, J.; Scherlach, K.; Rossi, A.; Sautebin, L.; Haeggström, J.Z.; Hertweck, C.; Brakhage, A.A.; Gerstmeier, J.; Proschak, E.; Werz, O.
Journal Article
2019Identification of the novel class D β-lactamase OXA-679 involved in carbapenem resistance in Acinetobacter calcoaceticus
Tietgen, M.; Kramer, J.S.; Brunst, S.; Djahanschiri, B.; Wohra, S.; Higgins, P.G.; Weidensdorfer, M.; Riedel-Christ, S.; Pos, K.M.; Gonzaga, A.; Steglich, M.; Nübel, U.; Ebersberger, I.; Proschak, E.; Göttig, S.
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2019Polypharmacology by Design: A Medicinal Chemist’s Perspective on Multitargeting Compounds
Proschak, E.; Stark, H.; Merk, D.
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2019Structure optimization of a new class of PPARγ antagonists
Hernandez-Olmos, V.; Knape, T.; Heering, J.; Knethen, A. von; Kilu, W.; Kaiser, A.; Wurglics, M.; Helmstadter, M.; Merk, D.; Schubert-Zsilavecz, M.; Parnham, M.J.; Steinhilber, D.; Proschak, E.
Journal Article
2019Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation
Pollinger, J.; Gellrich, L.; Schierle, S.; Kilu, W.; Schmidt, J.; Kalinowsky, L.; Ohrndorf, J.; Kaiser, A.; Heering, J.; Proschak, E.; Merk, D.
Journal Article
2019Zafirlukast Is a Dual Modulator of Human Soluble Epoxide Hydrolase and Peroxisome Proliferator-Activated Receptor γ
Göbel, T.; Diehl, O.; Heering, J.; Merk, D.; Angioni, C.; Wittmann, S.K.; Buscato, E. la; Kottke, R.; Weizel, L.; Schader, T.; Maier, T.J.; Geisslinger, G.; Schubert-Zsilavecz, M.; Steinhilber, D.; Proschak, E.; Kahnt, A.S.
Journal Article
2018Boosting Anti-Inflammatory Potency of Zafirlukast by Designed Polypharmacology
Schierle, S.; Flauaus, C.; Heitel, P.; Willems, S.; Schmidt, J.; Kaiser, A.; Weizel, L.; Goebel, T.; Kahnt, A.S.; Geisslinger, G.; Steinhilber, D.; Wurglics, M.; Rovati, G.E.; Schmidtko, A.; Proschak, E.; Merk, D.
Journal Article
2018Challenges in the Development of a Thiol-Based Broad-Spectrum Inhibitor for Metallo-β-Lactamases
Büttner, D.; Kramer, J.S.; Klingler, F.-M.; Wittmann, S.K.; Hartmann, M.R.; Kurz, C.G.; Kohnhäuser, D.; Weizel, L.; Brüggerhoff, A.; Frank, D.; Steinhilber, D.; Wichelhaus, T.A.; Pogoryelov, D.; Proschak, E.
Journal Article
2018A coupled fluorescence-based assay for the detection of protein arginine N-methyltransferase 6 (PRMT6) enzymatic activity
Kramer, J.; Désor, V.; Brunst, S.; Wittmann, S.K.; Lausen, J.; Heering, J.; Proschak, A.; Proschak, E.
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2018Discovery of polar spirocyclic orally bioavailable urea inhibitors of soluble epoxide hydrolase
Lukin, A.; Kramer, J.; Hartmann, M.; Weizel, L.; Hernandez-Olmos, V.; Falahati, K.; Burghardt, I.; Kalinchenkova, N.; Bagnyukova, D.; Zhurilo, N.; Rautio, J.; Forsberg, M.; Ihalainen, J.; Auriola, S.; Leppänen, J.; Konstantinov, I.; Pogoryelov, D.; Proschak, E.; Dar'in, D.; Krasavin, M.
Journal Article
2018Drug-Mediated Intracellular Donation of Nitric Oxide Potently Inhibits 5-Lipoxygenase
Roos, J.; Peters, M.; Maucher, I.V.; Kühn, B.; Fettel, J.; Hellmuth, N.; Brat, C.; Sommer, B.; Urbschat, A.; Piesche, M.; Vogel, A.; Proschak, E.; Blöcher, R.; Buscató, E.; Häfner, A.-K.; Matrone, C.; Werz, O.; Heidler, J.; Wittig, I.; Angioni, C.; Geisslinger, G.; Parnham, M.J.; Zacharowski, K.; Steinhilber, D.; Maier, T.J.
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2018Two-pronged approach to anti-inflammatory therapy through the modulation of the arachidonic acid cascade
Sala, A.; Proschak, E.; Steinhilber, D.; Rovati, G.E.
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2018Urate transporter inhibitor lesinurad is a selective peroxisome proliferator-activated receptor gamma modulator (sPPARγM) in vitro
Heitel, P.; Gellrich, L.; Heering, J.; Goebel, T.; Kahnt, A.; Proschak, E.; Schubert-Zsilavecz, M.; Merk, D.
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2018Urate transporter inhibitor lesinurad is a selective peroxisome proliferator-activated receptor gamma modulator (sPPARγM) in vitro
Heitel, P.; Gellrich, L.; Heering, J.; Goebel, T.; Kahnt, A.; Proschak, E.; Schubert-Zsilavecz, M.; Merk, D.
Journal Article
2017Camptothecin and its analog SN-38, the active metabolite of irinotecan, inhibit binding of the transcriptional regulator and oncoprotein FUBP1 to its DNA target sequence FUSE
Hosseini, S.K.; Kolterer, S.; Steiner, M.; Manstein, V. von; Gerlach, K.; Trojan, J.; Waidmann, O.; Zeuzem, S.; Schulze, J.O.; Hahn, S.; Steinhilber, D.; Gatterdam, V.; Tampé, R.; Biondi, R.M.; Proschak, E.; Zörnig, M.
Journal Article
2017Design, Synthesis and Cellular Characterization of a Dual Inhibitor of 5-Lipoxygenase and Soluble Epoxide Hydrolase
Meirer, K.; Glatzel, D.; Kretschmer, S.; Wittmann, S.K.; Hartmann, M.; Blöcher, R.; Angioni, C.; Geisslinger, G.; Steinhilber, D.; Hofmann, B.; Fürst, R.; Proschak, E.
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2017DrugBank screening revealed alitretinoin and bexarotene as liver X receptor modulators
Heitel, P.; Achenbach, J.; Moser, D.; Proschak, E.; Merk, D.
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2017A dual modulator of farnesoid X receptor and soluble epoxide hydrolase to counter nonalcoholic steatohepatitis
Schmidt, J.; Rotter, M.; Weiser, T.; Wittmann, S.; Weizel, L.; Kaiser, A.; Heering, J.; Goebel, T.; Angioni, C.; Wurglics, M.; Paulke, A.; Geisslinger, G.; Kahnt, A.; Steinhilber, D.; Proschak, E.; Merk, D.
Journal Article
2017Multitarget‐Directed Ligands Combining Cholinesterase and Monoamine Oxidase Inhibition with Histamine H3R Antagonism for Neurodegenerative Diseases
Bautista‐Aguilera, O.M.; Hagenow, S.; Palomino‐Antolin, A.; Farré‐Alins, V.; Ismaili, L.; Joffrin, P.-L.; Jimeno, M.L.; Soukup, O.; Janočková, J.; Kalinowsky, L.; Proschak, E.; Iriepa, I.; Moraleda, I.; Schwed, J.S.; Martínez, A.R.; López‐Muñoz, F.; Chioua, M.; Egea, J.; Ramsay, R.R.; Marco‐Contelles, J.; Stark, H.
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2017Nonacidic Farnesoid X Receptor Modulators
Flesch, D.; Cheung, S.Y.; Schmidt, J.; Gabler, M.; Heitel, P.; Kramer, J.; Kaiser, A.; Hartmann, M.; Lindner, M.; Lüddens-Dämgen, K.; Heering, J.; Lamers, C.; Lüddens, H.; Wurglics, M.; Proschak, E.; Schubert-Zsilavecz, M.; Merk, D.
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2017Opportunities and Challenges for Fatty Acid Mimetics in Drug Discovery
Proschak, E.; Heitel, P.; Kalinowsky, L.; Merk, D.
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2016Bacterial Expression and HTS Assessment of Soluble Epoxide Hydrolase Phosphatase
Klingler, F.-M.; Wolf, M.; Wittmann, S.; Gribbon, P.; Proschak, E.
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2016N-Benzylbenzamides: A novel merged scaffold for orally available dual soluble epoxide hydrolase/peroxisome proliferator-activated receptor gamma modulators
Blöcher, R.; Lamers, C.; Wittmann, S.K.; Merk, D.; Hartmann, M.; Weizel, L.; Diehl, O.; Brüggerhoff, A.; Boss, M.; Kaiser, A.; Schader, T.; Gobel, T.; Grundmann, M.; Angioni, C.; Heering, J.; Geisslinger, G.; Wurglics, M.; Kostenis, E.; Brüne, B.; Steinhilber, D.; Schubert-Zsilavecz, M.; Kahnt, A.S.; Proschak, E.
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2016Thermodynamic properties of leukotriene A4 hydrolase inhibitors
Wittmann, S.K.; Kalinowsky, L.; Kramer, J.S.; Bloecher, R.; Knapp, S.; Steinhilber, D.; Pogoryelov, D.; Proschak, E.; Heering, J.
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2015Identification and characterisation of a prototype for a new class of competitive PPAR gamma antagonists
Knape, T.; Flesch, D.; Kuchler, L.; Sha, L.K.; Giegerich, A.K.; Labocha, S.; Ferreirós, N.; Schmid, T.; Wurglics, M.; Schubert-Zsilavecz, M.; Proschak, E.; Brüne, B.; Parnham, M.J.; Knethen, A. von
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2015Lipoxin and resolvin biosynthesis is dependent on 5-lipoxygenase activating protein
Lehmann, C.; Homann, J.; Ball, A.-K.; Blöcher, R.; Kleinschmidt, T.K.; Basavarajappa, D.; Angioni, C.; Ferreirós, N.; Häfner, A.-K.; Radmark, O.; Proschak, E.; Haeggström, J.Z.; Geisslinger, G.; Parnham, M.J.; Steinhilber, D.; Kahnt, A.S.
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2015MTTB: A new pharmacological concept for sepsis
Knape, T.; Flesch, D.; Kuchler, L.; Sha, L.K.; Giegerich, A.K.; Nova, N.V.; Labocha, S.; Ferreiros, N.; Schmid, T.; Wacker, M.; Wurglics, M.; Zsilavecz, S.; Proschak, E.; Brune, B.; Parnham, M.J.; Knethen, A. von
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2013Exploring the Chemical Space of Multitarget Ligands Using Aligned Self-Organizing Maps
Aschenbach, J.; Klingler, F.M.; Blöcher, R.; Moser, D.; Häfner, A.K.; Rödl, C.B.; Kretschmer, S.; Krüger, B.; Löhr, F.; Stark, H.; Hofmann, B.; Steinhilber, D.; Proschak, E.
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2013Synthesis and pharmacological characterization of benzenesulfonamides as dual species inhibitors of human and murine mPGES-1
Hanke, T.; Rörsch, F.; Thieme, T.; Ferreiros, N.; Schneider, G.; Geisslinger, G.; Proschak, E.; Grösch, S.; Schubert-Zsilavecz, M.
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