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Publikationen

2020

Reßing N, Sönnichsen M, Osko J, Schöler A, Schliehe-Diecks J, Skerhut AJ, Borkhardt A, Hauer J, Kassack MU, Christianson DW, Bhatia S, Hansen FK. Multicomponent synthesis, binding mode and structure-activity relationships of selective histone deacetylase 6 (HDAC6) inhibitors with bifurcated capping groups. J Med Chem. 2020; doi: 10.1021/acs.jmedchem.9b01888. PMID: 32803970.

Sinatra L, Bandolik JJ, Roatsch M, Sönnichsen M, Schoeder CT, Hamacher A, Schoeler A, Borkhardt A, Meiler J, Bhatia S, Kassack MU#, Hansen FK#. #Shared senior authorship. Hydroxamic Acids Immobilized on Resins (HAIRs): A Toolbox for the Synthesis of Dual-Targeting HDAC Inhibitors and HDAC Degraders (PROTACs). Angew Chem Int Ed Engl. 2020; doi: 10.1002/anie.202006725. PMID: 32780485.

Friedrich A, Assmann AS, Schumacher L, Stuijvenberg JV, Kassack MU, Schulz WA, Roos WP, Hansen FK, Pflieger M, Kurz T, Fritz G. In Vitro Assessment of the Genotoxic Hazard of Novel Hydroxamic Acid- and Benzamide-Type Histone Deacetylase Inhibitors (HDACi). Int J Mol Sci. 2020; 21(13): E4747. doi: 10.3390/ijms21134747.

Jahn SK, Hennicke T, Kassack MU, Drews L, Reichert AS, Fritz G. Distinct influence of the anthracycline derivative doxorubicin on the differentiation efficacy of mESC-derived endothelial progenitor cells. Biochim Biophys Acta Mol Cell Res. 2020; 1867(7): 118711. doi: 10.1016/j.bbamcr.2020.118711.

Wang C, Hamacher A, Petzsch P, Köhrer K, Niegisch G, Hoffmann M, Schulz WA, and Kassack MU. Combination of Decitabine and Entinostat Synergistically Inhibits Urothelial Bladder Cancer Cells via Activation of FoxO1. Cancers. 2020; 12: 337. doi:10.3390/cancers12020337.

Krieger V, Hamacher A, Cao F, Stenzel K, Gertzen CGW, Schäker-Hübner L, Kurz T, Gohlke H, Dekker FJ, Kassack MU*, Hansen FK*. *Shared senior authorship. Synthesis of peptoid-based class I selective histone deacetylase inhibitors with chemosensitizing properties. J. Med. Chem. 2019;62(24), 11260-11279.

Asfaha Y, Schrenk C, Alves Avelar L, Lange F, Wang C, Bandolik JJ, Hamacher A, Kassack MU#, Kurz T#. #Shared senior authorship. Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells. Bioorg Med Chem. 2020; 28(1):115108. doi: 10.1016/j.bmc.2019.115108.

2019

Asfaha Y, Schrenk C, Alves Avelar L, Hamacher A, Pflieger M, Kassack MU#, Kurz T#. #Shared senior authorship. Recent advances in class IIa histone deacetylases research. Bioorg Med Chem. 2019; 27(22): 115087. doi: 10.1016/j.bmc.2019.115087.

Wang C, Engelke L, Bickel D, Hamacher A, Frank M, Proksch P, Gohlke H, Kassack MU. The tetrahydroxanthone-dimer phomoxanthone A is a strong inducer of apoptosis in cisplatin-resistant solid cancer cells. Bioorg Med Chem. 2019; 27(19): 115044. doi: 10.1016/j.bmc.2019.115044.

Pflieger M, Hamacher A, Öz T, Horstick-Muche N, Boesen B, Schrenk C, Kassack MU#, Kurz T#. #Shared senior authorship. Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. Bioorg Med Chem. 2019; 27(19): 115036.

Frank M, Hartmann R, Plenker M, Mándi A, Kurtán T, Özkaya FC, Müller WEG, Kassack MU, Hamacher A, Lin W, Liu Z, Proksch P. Brominated Azaphilones from the Sponge-Associated Fungus Penicillium canescens Strain 4.14.6a. J Nat Prod. 2019; 82(8):2159-2166. doi: 10.1021/acs.jnatprod.9b00151.

Abdel-Wahab NM, Harwoko H, Müller WEG, Hamacher A, Kassack MU, Fouad MA, Kamel MS, Lin W, Ebrahim W, Liu Z, Proksch P. Cyclic heptapeptides from the soil-derived fungus Clonostachys rosea. Bioorg Med Chem. 2019; 27(17):3954-3959. doi: 10.1016/j.bmc.2019.07.025.

Brockmann N, Sureechatchaiyan P, Müller D, Hennicke T, Hausmann R, Fritz G, Hamacher A, Kassack MU. Profiling of a suramin-derived compound library at recombinant human P2Y receptors identifies NF272 as a competitive but non-selective P2Y2 receptor antagonist. Purinergic Signalling. 2019. DOI: 10.1007/s11302-019-09663-4.

Yu H, Sperlich J, Höfert SP, Janiak C, Teusch N, Stuhldreier F, Wesselborg S, Wang C, Kassack MU, Dai H, Liu Z, Proksch P. Azaphilone pigments and macrodiolides from the coprophilous fungus Coniella fragariae. Fitoterapia. 2019. 137:104249. doi: 10.1016/j.fitote.2019.104249.

Bandolik JJ, Hamacher A, Schrenk C, Weishaupt R, and Kassack MU. Class I-Histone Deacetylase (HDAC) Inhibition is Superior to pan-HDAC Inhibition in Modulating Cisplatin Potency in High Grade Serous Ovarian Cancer Cell Lines. Int J Mol Sciences. 2019; 20(12). pii: E3052. doi: 10.3390/ijms20123052.

Rehberg N, Omeje E, Ebada SS, van Geelen L, Liu Z, Sureechatchayan P, Kassack MU, Ioerger TR, Proksch P, Kalscheuer R. 3-O-Methyl-alkylgallates inhibit fatty acid desaturation in Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2019. pii: AAC.00136-19. doi: 10.1128/AAC.00136-19.

Ariantari NP, Ancheeva E, Wang C, Mándi A, Knedel TO, Kurtán T, Chaidir C, Müller WEG, Kassack MU, Janiak C, Daletos G, Proksch P. Indole Diterpenoids from an Endophytic Penicillium sp. J Nat Prod. 2019. 82(6):1412-1423. doi: 10.1021/acs.jnatprod.8b00723.

Choi SY, Kee HJ, Sun S, Seok YM, Ryu Y, Kim GR, Kee SJ, Pflieger M, Kurz T, Kassack MU, Jeong MH. Histone deacetylase inhibitor LMK235 attenuates vascular constriction and aortic remodelling in hypertension. J Cell Mol Med. 2019. 23(4):2801-2812. doi: 10.1111/jcmm.14188.

Frank M, Özkaya FC, Müller WEG, Hamacher A, Kassack MU, Lin W, Liu Z, Proksch P. Cryptic Secondary Metabolites from the Sponge-Associated Fungus Aspergillus ochraceus. Mar Drugs. 2019;17(2). pii: E99. doi: 10.3390/md17020099.

2018

Sureechatchaiyan P, Hamacher H, Brockmann B, Stork B, Kassack MU. Adenosine enhances cisplatin sensitivity in human ovarian cancer cells. Purinergic Signalling. 2018; 14(4):395-408.

Kaletsch A, Pinkerneil M, Hoffmann MJ, Jaguva Vasudevan AA, Wang C, Hansen FK, Wiek C, Hanenberg H, Gertzen C, Gohlke H, Kassack MU, Kurz T, Schulz WA, Niegisch G. Effects of novel HDAC inhibitors on urothelial carcinoma cells. Clin Epigenetics. 2018; 10(1): 100.

Mackwitz MKW, Hamacher A, Osko JD, Held J, Schöler A, Christianson DW, Kassack MU, Hansen FK. Multicomponent Synthesis and Binding Mode of Imidazo[1,2- a]pyridine-Capped Selective HDAC6 Inhibitors. Org Lett. 2018; 20(11): 3255-3258.

Kamdem RST, Pascal W, Rehberg N, van Geelen L, Höfert SP, Knedel TO, Janiak C, Sureechatchaiyan P, Kassack MU, Lin W, Kalscheuer R, Liu Z, Proksch P. Metabolites from the endophytic fungus Cylindrocarpon sp. isolated from tropical plant Sapium ellipticum. Fitoterapia; 2018; 128:175-179.

Bhatia S, Diedrich D, Frieg B, Ahlert H, Stein S, Bopp B, Lang F, Zang T, Kröger T, Ernst T, Kögler G, Krieg A, Lüdeke S, Kunkel H, Rodrigues Moita AJ, Kassack MU, Marquardt V, Opitz FV, Oldenburg M, Remke M, Babor F, Grez M, Hochhaus A, Borkhardt A, Groth G, Nagel-Steger L, Jose J, Kurz T, Gohlke H, Hansen FK, Hauer J. Targeting HSP90 dimerization via the C terminus is effective in imatinib-resistant CML and lacks the heat shock response. Blood. 2018; 132(3):307-320.

Buß I, Hamacher A, Sarin N, Kassack MU, Kalayda GV. Relevance of copper transporter 1 and organic cation transporters 1-3 for oxaliplatin uptake and drug resistance in colorectal cancer cells. Metallomics. 2018; 10(3): 414-425.

Brychta N, Drosch M, Driemel C, Fischer JC, Neves RP, Esposito I, Knoefel W, Möhlendick B, Hille C, Stresemann A, Krahn T, Kassack MU, Stoecklein NH, von Ahsen O. Isolation of circulating tumor cells from pancreatic cancer by automated filtration. Oncotarget. 2017; 8(49): 86143-86156.

Kamdem RST, Wang H, Wafo P, Ebrahim W, Özkaya FC, Makhloufi G, Janiak C, Sureechatchaiyan P, Kassack MU, Lin W, Liu Z, Proksch P. Induction of new metabolites from the endophytic fungus Bionectria sp. through bacterial co-culture. Fitoterapia. 2018; 124: 132-136.

2017

Gohr K, Hamacher A, Engelke LH, Kassack MU. Inhibition of PI3K/Akt/mTOR overcomes cisplatin resistance in the triple negative breast cancer cell line HCC38. BMC Cancer. 2017; 17(1): 711.

Mokhlesi A, Stuhldreier F, Wex KW, Berscheid A, Hartmann R, Rehberg N, Sureechatchaiyan P, Chaidir C, Kassack MU, Kalscheuer R, Brötz-Oesterhelt H, Wesselborg S, Stork B, Daletos G, Proksch P. Cyclic Cystine-Bridged Peptides from the Marine Sponge Clathria basilana Induce Apoptosis in Tumor Cells and Depolarize the Bacterial Cytoplasmic Membrane. J Nat Prod. 2017; 80(11): 2941-2952.

Stenzel K, Chua MJ, Duffy S, Antonova-Koch Y, Meister S, Hamacher A, Kassack MU, Winzeler E, Avery VM, Kurz T, Andrews KT, Hansen FK. Design and Synthesis of Terephthalic Acid-Based Histone Deacetylase Inhibitors with Dual-Stage Anti-Plasmodium Activity. ChemMedChem. 2017; 12(19): 1627-1636.

Stenzel K, Hamacher A, Hansen FK, Gertzen CGW, Senger J, Marquardt V, Marek L, Marek M, Romier C, Remke M, Jung M, Gohlke H, Kassack MU*, Kurz T*. *Shared senior authorship. Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. J Med Chem. 2017; 60(13): 5334-5348.

Krieger V, Hamacher A, Gertzen CGW, Senger J, Zwinderman MRH, Marek M, Romier C, Dekker FJ, Kurz T, Jung M, Gohlke H, Kassack MU, Hansen FK. Design, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups. J Med Chem. 2017; 60(13):5493-5506.

Alves Avelar LA, Held J, Engel JA, Sureechatchaiyan P, Hansen FK, Hamacher A, Kassack MU, Mordmüller B, Andrews KT, Kurz T. Design and Synthesis of Novel Anti-Plasmodial Histone Deacetylase Inhibitors Containing an Alkoxyamide Connecting Unit. Arch Pharm (Weinheim). 2017; 350(3-4): doi: 10.1002/ardp.201600347. PMID: 28317157.

Hemphill CF, Sureechatchaiyan P, Kassack MU, Orfali RS, Lin W, Daletos G, Proksch P. OSMAC approach leads to new fusarielin metabolites from Fusarium tricinctum. J Antibiot (Tokyo). 2017; doi: 10.1038/ja.2017.21. PMID: 28270687.

Li HL, Li XM, Li X, Wang CY, Liu H, Kassack MU, Meng LH, Wang BG. Antioxidant Hydroanthraquinones from the Marine Algal-Derived Endophytic Fungus Talaromyces islandicus EN-501. J Nat Prod. 2017; 80(1): 162-8.

2016

Meng LH, Wang CY, Mándi A, Li XM, Hu XY, Kassack MU, Kurtán T, Wang BG. Three Diketopiperazine Alkaloids with Spirocyclic Skeletons and One Bisthiodiketopiperazine Derivative from the Mangrove-Derived Endophytic Fungus Penicillium brocae MA-231. Org Lett. 2016; Epub ahead of print. PMID: 27723361.

Diedrich D, Moita AJR, Rüther A, Frieg B, Reiss GJ, Hoeppner A, Kurz T, Gohlke H, Lüdeke S, Kassack MU, Hansen FK. α‑Aminoxy oligopeptides: synthesis, secondary structure and cytotoxicity of a novel class of anticancer foldamers. Chemistry. 2016; 22(49): 17600-11.

Liu S, Dai H, Makhloufi G, Heering C, Janiak C, Hartmann R, Mándi A, Kurtán T, Müller WE, Kassack MU, Lin W, Liu Z, Proksch P. Cytotoxic 14-Membered Macrolides from a Mangrove-Derived Endophytic Fungus, Pestalotiopsis microspora. J Nat Prod. 2016; 79(9): 2332-40.

Meyer H, Brenner M, Höfert SP, Knedel TO, Kunz PC, Schmidt AM, Hamacher A, Kassack MU, Janiak C. Synthesis of oxime-based CO-releasing molecules, CORMs and their immobilization on maghemite nanoparticles for magnetic-field induced CO release. Dalton Trans. 2016; 45(18): 7605-15.

Hansen SV, Christiansen E, Urban C, Hudson BD, Stocker CJ, Due-Hansen ME, Wargent ET, Shimpukade B, Almeida R, Ejsing CS, Cawthorne MA, Kassack MU, Milligan G, Ulven T. Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area, and Robust in Vivo Efficacy. J Med Chem. 2016; 59(6): 2841-6.

Cui H, Goddard R, Pörschke KR, Hamacher A, Kassack MU. Bispidin-9,9-diol Analogues of Cisplatin, Carboplatin, and Oxaliplatin: Synthesis, Structures, and Cytotoxicity. Inorg Chem. 2016; 55(6): 2986-97.

Diedrich D, Hamacher A, Gertzen C, Alves Avelar LA, Reiss GJ, Kurz T, Gohlke H, Kassack MU, Hansen FK. Rational design and diversity-oriented synthesis of peptoid-based selective HDAC6 inhibitors. Chem Commun (Camb). 2016; 52(15): 3219-22.

Engelke LH, Hamacher A, Proksch P, Kassack MU. Ellagic acid and resveratrol prevent the development of cisplatin resistance in the epithelial ovarian cancer cell line A2780. J Cancer. 2016; 7(4): 353-63.

2015

Meyer H, Winkler F, Kunz P, Schmidt AM, Hamacher A, Kassack MU, Janiak C. Stabilizing Alginate Confinement and Polymer Coating of CO-Releasing Molecules Supported on Iron Oxide Nanoparticles To Trigger the CO Release by Magnetic Heating. Inorg Chem. 2015; 54(23): 11236-46.

Hennicke T, Nieweg K, Brockmann N, Kassack MU, Gottmann K, Fritz G. mESC-Based in vitro Differentiation Models to Study Vascular Response and Functionality Following Genotoxic Insults. Toxicol Sci. 2015; 144(1):138-50.

Khosravani F, Suvorava T, Dao VT, Brockmann N, Kocgirli O, Herbst FF, Valcaccia S, Kassack MU, Bas M, Kojda G. Stability of murine bradykinin type 2 receptor despite treatment with NO, bradykinin, icatibant, or C1-INH. Allergy. 2015; 70(3):285-94.

Bouaziz Z, Issa S, Gentili J, Gratz A, Bollacke A, Kassack M, Jose J, Herfindal L, Gausdal G, Døskeland SO, Mullié C, Sonnet P, Desgrouas C, Taudon N, Valdameri G, Di Pietro A, Baitiche M, Le Borgne M. Biologically active carbazole derivatives: focus on oxazinocarbazoles and related compounds. J Enzyme Inhib Med Chem. 2015; 30(2):180-8.

2014

Zhang Y, Lau P, Pansky A, Kassack MU, Hemmersbach R, Tobiasch E. The Influence of Simulated Microgravity on Purinergic Signaling Is Different between Individual Culture and Endothelial and Smooth Muscle Cell Coculture. BioMed Research International. 2014; Volume 2014: Article ID 413708, 11 pages.

Hansen FK, Sumanadasa SD, Stenzel K, Duffy S, Meister S, Marek L, Schmetter R, Kuna K, Hamacher A, Mordmüller B, Kassack MU, Winzeler EA, Avery VM, Andrews KT, Kurz T. Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. Eur J Med Chem. 2014; 82:204-13.

Cui H, Goddard R, Pörschke KR, Hamacher A, Kassack MU. Bispidine analogues of cisplatin, carboplatin, and oxaliplatin: synthesis, structures, and cytotoxicity. Inorg Chem. 2014; 53(7):3371-84.

Ebada SS, Fischer T, Klaßen S, Hamacher A, Roth YO, Kassack MU, Roth EH. A new cytotoxic steroid from co-fermentation of two marine alga-derived micro-organisms. Nat Prod Res. 2014; ; 28(16): 1241-5.

Ebada SS, Fischer T, Hamacher A, Du FY, Roth YO, Kassack MU, Wang BG, Roth EH. Psychrophilin E, a new cyclotripeptide, from co-fermentation of two marine alga-derived fungi of the genus Aspergillus. Nat Prod Res. 2014;28(11):776-81.

Nobbio L, Visigalli D, Mannino E, Fiorese F, Kassack MU, Sturla L, Prada V, De Flora A, Zocchi E, Bruzzone S, Schenone A. The diadenosine homodinucleotide P18 improves in vitro myelination in experimental Charcot-Marie-Tooth type 1A. J Cell Biochem. 2014; 115(1):161-7.

2013

Rönsberg D, Debbab A, Mándi A, Vasylyeva V, Böhler P, Stork B, Engelke L, Hamacher A, Sawadogo R, Diederich M, Wray V, Lin W, Kassack MU, Janiak C, Scheu S, Wesselborg S, Kurtán T, Aly AH, Proksch P. Pro-apoptotic and immunostimulatory tetrahydroxanthone dimers from the endophytic fungus Phomopsis longicolla. J Org Chem. 2013; 78(24):12409-25.

Urban C, Hamacher A, Partke HJ, Roden M, Schinner S, Christiansen E, Due-Hansen ME, Ulven T, Gohlke H, and Kassack MU. In vitro and mouse in vivo characterization of the potent free fatty acid 1 receptor agonist TUG-469. Naunyn-Schmiedeberg's Arch Pharmacol. 2013; 386(12):1021-30.

Christiansen E, Hansen SV, Urban C, Hudson BD, Wargent ET, Grundmann M, Jenkins L, Zaibi M, Stocker CJ, Ullrich S, Kostenis E, Kassack MU, Milligan G, Cawthorne MA, Ulven T. Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes. ACS Med Chem Lett. 2013; 4(5):441-445.

Marques AF, Esser D, Rosenthal PJ, Kassack MU, Lima LM. Falcipain-2 inhibition by suramin and suramin analogues. Bioorg Med Chem. 2013; 21(13):3667-73.

Ebrahim W, Aly AH, Wray V, Mándi A, Teiten MH, Gaascht F, Orlikova B, Kassack MU, Lin W, Diederich M, Kurtán T, Debbab A, Proksch P. Embellicines A and B: Absolute Configuration and NF-κB Transcriptional Inhibitory Activity. J Med Chem. 2013; 56(7):2991-9.

Christiansen E, Due-Hansen ME, Urban C, Grundmann M, Schmidt J, Hansen SV, Hudson BD, Zaibi M, Markussen SB, Hagesaether E, Milligan G, Cawthorne MA, Kostenis E, Kassack MU, Ulven T. Discovery of a potent and selective free fatty acid receptor 1 agonist with low lipophilicity and high oral bioavailability. J Med Chem. 2013; 56(3):982-92.

Marek L, Hamacher A, Hansen FK, Kuna K, Gohlke H, Kassack MU, Kurz T. Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells. J Med Chem. 2013; 56(2):427-36.

Hausmann R, Günther J, Kless A, Kuhlmann D, Kassack MU, Bahrenberg G, Markwardt F, Schmalzing G. Salt bridge switching from Arg290/Glu167 to Arg290/ATP promotes the closed-to-open transition of the P2X2 receptor. Mol Pharmacol. 2013; 83(1):73-84.

2012

Christiansen E, Due-Hansen ME, Urban C, Grundmann M, Schröder R, Hudson B, Milligan G, Cawthorne M, Kostenis E, Kassack MU, Ulven T. Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonists: Mesylpropoxy Appendage Lowers Lipophilicity and Improves ADME Properties. J Med Chem. 2012; 55(14):6624-8.

Wollinsky B, Ludwig L, Hamacher A, Yu X, Kassack MU, Li SM. Prenylation at the indole ring leads to a significant increase of cytotoxicity of tryptophan-containing cyclic dipeptides. Bioorg Med Chem Lett. 2012; 22(12):3866-9.

Cargnelutti MT, Marques AF, Esser D, Monteiro RQ, Kassack MU, Lima LM. Allosteric activation of human α-thrombin through exosite 2 by suramin analogs. Arch Biochem Biophys. 2012; 520(1):36-41.

Zippel N, Limbach CA, Ratajskia N, Urban C, Luparello C, Pansky A, Kassack MU, Tobiasch E. Purinergic Receptors Influence the Differentiation of Human Mesenchymal Stem Cells. Stem Cells Dev. 2012; 21(6):884-900.

2011

Christiansen E, Urban C, Grundmann M, Due-Hansen ME, Hagesaether E, Schmidt J, Pardo L, Ullrich S, Kostenis E, Kassack M, Ulven T. Identification of a Potent and Selective Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist with Favorable Physicochemical and in Vitro ADME Properties. J Med Chem. 2011; 54(19):6691-703.

Wetzel C, Kunz PC, Kassack MU, Hamacher A, Böhler C, Waetjen W, Ott I, Rubbiani R, Spingler B. Gold(I) complexes of water-soluble diphos-type ligands: Synthesis, anticancer activity, apoptosis and thioredoxin reductase inhibition. Dalton Transactions. 2011; 40(36):9212-20.

Ebada SS, Schulz B, Wray V, Totzke F, Kubbutat MHG, Müller WEG, Hamacher A, Kassack MU, Lin W, Proksch P. Arthrinins A–D: Novel diterpenoids and further constituents from the sponge derived fungus Arthrinium sp. Biorg Med Chem. 2011; 19(15):4644-51.

Wolf C, Rosefort C, Fallah G, Kassack MU, Hamacher A, Bodnar M, Wang H, Illes P, Kless A, Bahrenberg G, Schmalzing G, Hausmann R. Molecular Determinants of Potent P2X2 Antagonism Identified by Functional Analysis, Mutagenesis and Homology Docking. Mol Pharmacol. 2011; 79(4):649-61.

Kornum BR, Kawashima M, Faraco J, Lin L, Rico TJ, Hesselson S, Axtell RC, Kuipers H, Weiner K, Hamacher A, Kassack MU, Han F, Knudsen S, Li J, Dong X, Winkelmann J, Plazzi G, Nevsimalova S, Hong SC, Honda Y, Honda M, Högl B, Ton TG, Montplaisir J, Bourgin P, Kemlink D, Huang YS, Warby S, Einen M, Eshragh JL, Miyagawa T, Desautels A, Ruppert E, Hesla PE, Poli F, Pizza F, Frauscher B, Jeong JH, Lee SP, Strohl KP, Longstreth WT Jr, Kvale M, Dobrovolna M, Ohayon MM, Nepom GT, Wichmann HE, Rouleau GA, Gieger C, Levinson DF, Gejman PV, Meitinger T, Peppard P, Young T, Jennum P, Steinman L, Tokunaga K, Kwok PY, Risch N, Hallmayer J, Mignot E. Common variants in P2RY11 are associated with narcolepsy. Nat Genet. 2011; 43(1):66-71.

Kunz PC, Wetzel C, Kögel S, Kassack MU, Spingler B. [(C3H4N2)2Au]Cl—a bis protic gold(I)-NHC. Dalton Transactions. 2011; 40(1):35-7.

2010

Christiansen E, Due-Hansen ME, Urban C, Merten N, Pfleiderer M, Karlsen KK, Rasmussen SS, Steensgard M, Hamacher A, Schmidt J, Drewke C, Petersen RK, Kristiansen K, Ullrich S, Kostenis E, Kassack MU, Ulven T. Structure−Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. ACS Med Chem Lett. 2010; 1(7):345-9.

Tacke R, Nguyen B, Burschka C, Lippert WP, Hamacher A, Urban C, Kassack MU. Sila-trifluperidol, a Silicon Analogue of the Dopamine (D2) Receptor Antagonist Trifluperidol: Synthesis and Pharmacological Characterization. Organometallics. 2010; 29(7):1652-60.

Meis S, Hamacher A, Hongwiset D, Marzian C, Wiese M, Eckstein N, Royer HD, Communi D, Boeynaems JM, Hausmann R, Schmalzing G, Kassack MU. NF546 [4,4'-(carbonylbis(imino-3,1-phenylene-carbonylimino-3,1‑(4-methyl-phenylene)-carbonyl-imino))-bis(1,3-xylene-a,a'-diphosphonic acid) tetrasodium salt] is the first non-nucleotide P2Y11 agonist and stimulates release of IL-8 from human monocyte-derived dendritic cells. J Pharmacol Exp Ther. 2010; 332(1):238-47.

2009

Kunz PC, Kassack MU, Hamacher A, and Spingler B. Imidazole-based phosphane gold(I) complexes as potential agents for cancer treatment: synthesis, structural studies and antitumor activity. Dalton Trans. 2009; 37:7741-7.

Eckstein N, Servan K, Hildebrandt B, Pölitz A, von Jonquíeres G, Wolf-Kümmeth S, Napierski I, Hamacher A, Kassack MU, Budczies J, Beier M, Dietel M, Royer-Pokora B, Denkert C, Royer HD. Hyperactivation of the insulin-like growth factor receptor 1 signaling pathway is an essential event for cisplatin resistance of ovarian cancer cells. Cancer Res. 2009; 69(7): 2996-3003.

2008

Parai MK, Shagufta, Srivastava AK, Kassack M, Panda G. An unexpected reaction of phosphorous tribromide on chromanone, thiochromanone, 3,4-dihydro-2H-benzo[b]thiepin-5-one, 3,4-dihydro-2Hbenzo[b]oxepin-5-one and tetralone derived allylic alcohols: a case study. Tetrahedron. 2008; 64: 9962-76.

Christiansen E, Urban C, Merten N, Liebscher K, Karlsen KK, Hamacher A, Spinrath A, Bond AD, Drewke C, Ullrich S, Kassack MU, Kostenis E, Ulven T. Discovery of Potent and Selective Agonists for the Free Fatty Acid Receptor 1 (FFA1/GPR40), a Potential Target for the Treatment of Type II Diabetes. J Med Chem. 2008; 51(22): 7061–4

Magnone M, Basile G, Bruzzese D, Guida L, Signorello MG, Parakkottil Chothi M, Bruzzone S, Millo E, Qi AD, Nicholas RA, Kassack MU, Leoncini G, Zocchi E. Adenylic dinucleotides produced by CD38 are negative endogenous modulators of platelet aggregation. J Biol Chem. 2008; 283(36): 24460-8.

Gosepath EM, Eckstein N, Hamacher A, Servan K, von Jonquieres G, Lage H, Györffy B, Royer HD, Kassack MU. Acquired cisplatin resistance in the head-neck cancer cell line Cal27 is associated with decreased DKK1 expression and can partially be reversed by overexpression of DKK1. Int J Cancer. 2008; 123(9): 2013-9.

Ecke D, Hanck T, Tulapurkar M, Schafer R, Kassack M, Stricker R, Reiser G. Hetero-oligomerization of the P2Y11 and P2Y1 receptor controls receptor internalization and ligand selectivity of the P2Y11 receptor. Biochem J. 2008; 409(1): 107-16.

Eckstein N, Servan K, Girard L, Cai D, von Jonquieres G, Jaehde U, Kassack MU, Gazdar AF, Minna JD, Royer HD. EGFR-pathway analysis identifies amphiregulin as a key factor for cisplatin resistance of  human breast cancer cells. J Biol Chem. 2008; 283(2):739-50.

Tacke R, Popp F, Müller B, Theis B, Burschka C, Hamacher A, Kassack MU, Schepmann D, Wünsch B, Jurva U, Wellner E. Sila-Haloperidol, a Silicon Analogue of the Dopamine (D(2)) Receptor Antagonist Haloperidol: Synthesis, Pharmacological Properties, and Metabolic Fate. ChemMedChem. 2008; 3(1):152-164.

Moreschi I, Bruzzone S, Bodrato N, Usai C, Guida L, Nicholas RA, Kassack MU, Zocchi E, and De Flora A. NAADP+ is an agonist of the human P2Y11 purinergic receptor. Cell Calcium. 2008; 43(4):344-55.

2007

Vaughan KR, Stokes L, Prince LR, Marriott HM, Meis S, Kassack MU, Bingle CD, Sabroe I, Surprenant A, Whyte MK. Inhibition of Neutrophil Apoptosis by ATP Is Mediated by the P2Y11 Receptor. J Immunol. 2007; 179(12):8544-53.

Greve H, Meis S, Kassack MU, Kehraus S, Krick A, Wright AD, König GM. New Iantherans from the Marine Sponge Ianthella quadrangulata: Novel Agonists of the P2Y11 Receptor. J Med Chem. 2007; 50(23):5600-7.

Mueller H, Klinkhammer W, Globisch C, Kassack MU, Pajeva IK, Wiese M. New functional assay of P-glycoprotein activity using Hoechst 33342. Bioorg Med Chem. 2007; 15(23):7470-9.

Trapp J, Meier R, Hongwiset D, Kassack MU, Sippl W, Jung M. Structure activity studies on suramin analogues as inhibitors of NAD+-dependent histone diacetylases (sirtuins). ChemMedChem. 2007; 2(10):1419-31.

Zisowsky J, Koegel S, Leyers S, Devarakonda K, Kassack MU, Osmak M, Jaehde U. Relevance of drug uptake and efflux for cisplatin sensitivity of tumor cells. Biochem Pharmacol. 2007; 73(2):298-307.

2006

Moreschi I, Bruzzone S, Nicholas RA, Fruscione F, Sturla L, Benvenuto F, Usai C, Meis S, Kassack MU, Zocchi E, De Flora A. Extracellular NAD+ is an agonist of the human P2Y11 purinergic receptor in human granulocytes. J Biol Chem. 2006; 281(42):31419-29.

Hamacher A, Weigt M, Wiese M, Hoefgen B, Lehmann J, Kassack MU. Dibenzazecine compounds with a novel dopamine/5HT2A receptor profile and 3D-QSAR analysis. BMC Pharmacology. 2006, 6(1):11.

Hausmann R, Rettinger J, Gerevich Z, Meis S, Kassack MU, Illes P, Lambrecht G, Schmalzing G. The suramin analog 4,4',4'',4'''-(carbonylbis(imino-5,1,3-benzenetriylbis (carbonylimino)))tetra-kis-benzenesulfonic acid (NF110) potently blocks P2X3 receptors: subtype selectivity is determined by location of sulfonic acid groups. Mol Pharmacol. 2006; 69(6):2058-67.

Hoefgen B, Decker M, Mohr P, Schramm AM, Rostom SAF, El-Subbagh H, Schweikert PM, Rudolf DR, Kassack MU, Lehmann J. Dopamine/Serotonin Receptor Ligands, Part X1: SAR studies on azecine type dopamine receptor ligands by functional screening at human cloned D1, D2L and D5 receptors with a microplate reader based calcium assay lead to a novel potent D1/D5 selective antagonist. J Med Chem. 2006; 49(2):760-9.

2005

Jekerle V, Kassack MU, Reilly RM, Wiese M, Piquette-Miller M. Functional comparison of single- and double-stranded mdr1 antisense oligodeoxynucleotides in human ovarian cancer cell lines. J Pharm Pharm Sci. 2005; 8(3):516-27.

Kassack MU, Stratenschulte C. Expression profile of copper transporters in sensitive and cisplatin/Oxaliplatin-resistant tumor cell lines. Int J Clin Pharmacol Therapeutics. 2005; 43(12):597-8.

Gosepath EM, Weykam S, Wiese M, Kassack MU. Identification of new genes involved in cisplatin resistance and their expression profile in 18 human tumor cell lines. Int J Clin Pharmacol Therapeutics. 2005; 43(12):579-80.

Ullmann H, Meis S, Hongwiset D, Marzian C, Wiese M, Nickel P, Communi D, Boeynaems JM, Wolf C, Hausmann R, Schmalzing G, Kassack MU. Synthesis and structure-activity relationships of suramin-derived P2Y11 receptor antagonists with nanomolar potency. J Med Chem. 2005; 48:7040-8.

Nunziante M, Kehler C, Maas E, Kassack MU, Groschup M, Schätzl HM. Charged bipolar suramin derivatives induce aggregation of the prion protein at the cell surface and inhibit PrPSc replication. J Cell Science. 2005; 118(21):4959-73.

Horner S, Menke K, Hildebrandt C, Kassack MU, Nickel P, Ullmann H, Mahaut-Smith MP, Lambrecht G. The novel suramin analogue NF864 selectively blocks P2X(1) receptors in human platelets with potency in the low nanomolar range. Naunyn Schmiedebergs Arch Pharmacol. 2005; 372(1):1-13.

Wolner I, Kassack MU, Ullmann H, Karel A, Hohenegger M. Use-dependent inhibition of the skeletal muscle ryanodine receptor by the suramin analogue NF676. Br J Pharmacol. 2005; 146(4):525-33.

Hechler B, Magnenat S, Zighetti ML, Kassack MU, Ullmann H, Cazenave JP, Evans R, Cattaneo M, Gachet C. Inhibition of platelet functions and thrombosis through selective or non selective inhibition of the platelet P2 receptors with increasing doses of NF449. J Pharmacol Exp Ther. 2005; 314(1):232-243.

Rettinger J, Braun K, Hochmann H, Kassack MU, Ullmann H, Nickel P, Schmalzing G, Lambrecht G. Profiling at recombinant homomeric and heteromeric rat P2X receptors identifies the suramin analogue NF449 as a highly potent P2X1 receptor antagonist. Neuropharmacology. 2005; 48(3):461-8.

2004

Gosepath EM, Weykam S, Gruenewald E, Ko Y, Wiese M, Kassack MU. Differential gene expression studies in cisplatin-sensitive versus cisplatin-resistant human cancer cell lines. Int J Clin Pharmacol Therapeutics. 2004; 42(11):637-9.

Müller H, Klinkhammer W, Kassack MU, Eckstein N, Wiese M. Novel modulators to overcome P-glycoprotein-mediated multidrug resistance in tumor cells. Int J Clin Pharmacol Therapeutics. 2004; 42(11):644-5.

Tacke R, Heinrich T, Bertermann R, Burschka C, Hamacher A, and Kassack MU. Sila-haloperidol: A Silicon Analogue of the Dopamine (D2) Receptor Antagonist Haloperidol. Organometallics. 2004; 23(19):4468-77.

Müller H, Kassack MU, Wiese M. Comparison of the Usefulness of the MTT-, ATP-, and Calcein-Assays to Predict the Potency of Cytotoxic Agents in Various Human Cancer Cell Lines. J Biomol Screen. 2004; 9(6):506-15.

Kassack MU, Braun K, Ganso M, Ullmann H, Nickel P, Böing B, Müller G, Lambrecht G. Structure-activity relationships of analogues of NF449 confirm NF449 as the most potent and selective known P2X1 receptor antagonist. Eur J Med Chem. 2004; 39(4):345-57.

McCain DF, Wu L, Nickel P, Kassack MU, Kreimeyer A, Gagliardi A, Collins DC, Zhang ZY. Suramin derivatives as inhibitors and activators of protein-tyrosine phosphatases. J Biol Chem. 2004; 279(15):14713-25.

2003

Zisowsky J, Becker A, Weykam S, Kassack M, Jaehde U. Assessment of platinum sensitivity in human tumor cells. Int J Clin Pharmacol Therapeutics. 2003; 41: 612-3.

Hülsmann M, Nickel P, Kassack M, Schmalzing G, Lambrecht G, Markwardt F. NF449, a novel picomolar potency antagonist at human P2X1 receptors. Eur J Pharmacol. 2003; 470:1-7.

Tammler U, Quillan JM, Lehmann J, Sadée W, Kassack MU. Design, synthesis, and biological evaluation of non-peptidic ligands at the Xenopus laevis skin-melanocortin receptor. Eur J Med Chem. 2003; 38:481-93.

2002

Kassack MU. Quantitative Comparison of Functional Screening by Measuring Intracellular Ca2+ with Radioligand Binding at Recombinant Human Dopamine Receptors. AAPS PharmSci. 2002; 4(4): article 31 (http://www.aapspharmsci.org).

Kassack MU, Höfgen B, Decker M, Eckstein N, Lehmann J. Pharmacological characterization of the benz[d]indolo[2,3-g]azecine LE300, a novel type of a nanomolar dopamine receptor antagonist. Naunyn Schmiedebergs Arch Pharmacol. 2002; 366:543-50.

Abadi AH, Lankow S, Hoefgen B, Decker M, Kassack MU, Lehmann J. Dopamine/Serotonin Receptor Ligands, Part III [1]: Synthesis and Biological Activities of 7,7´-Alkylene-bis-6,7,8,9,14,15-hexahydro-5H-benz[d]indolo[2,3-g]azecines - Application of the Bivalent Ligand Approach to a Novel Type of Dopamine Receptor Antagonist. Arch Pharm Pharm Med Chem. 2002; 335(8):367-73.

Kassack MU, Hoefgen B, Lehmann J, Eckstein N, Quillan JM, Sadée W. Functional screening of G-protein coupled receptors by measuring intracellular calcium with a fluorescence microplate reader. J Biomol Screen. 2002; 7(3):233-46.

Mahboobi S, Teller S, Pongratz H, Hufsky H, Sellmer A, Botzki A, Uecker A, Beckers T, Baasner S, Schachtele C, Uberall F, Kassack MU, Dove S, Bohmer FD. Bis(1H-2-indolyl)methanones as a novel class of inhibitors of the platelet-derived growth factor receptor kinase. J Med Chem. 2002; 45(5):1002-18.

Kudlacek O, Waldhoer M, Kassack MU, Nickel P, Salmi JAI, Freissmuth M, Nanoff C. Biased inhibition by a suramin analogue of A1-adenosine receptor/G protein coupling in fused receptor/G protein tandems: the A1-adenosine receptor is predominantly coupled to Goa in human brain. Naunyn Schmiedebergs Arch Pharmacol. 2002; 365(1):8-16.

2001 und früher

Braun K, Rettinger J, Ganso M, Kassack M, Hildebrandt C, Ullmann H, Nickel P, Schmalzing G, Lambrecht G. NF449: a subnanomolar potency antagonist at recombinant rat P2X1 receptors. Naunyn Schmiedebergs Arch Pharmacol. 2001; 364(3):285-90.

Kassack MU, Högger P, Gschwend DA, Kameyama K, Haga T, Graul RC, Sadée W. Molecular Modeling of G-protein Coupled Receptor Kinase 2: Docking and Biochemical Evaluation of Inhibitors. AAPS Pharmsci. 2000; 2(1): article 2 (http://www.aapspharmsci.org/).

Klinger M, Freissmuth M, Nickel P, Stabler-Schwarzbart M, Kassack M, Suko J, Hohenegger M. Suramin and suramin analogs activate skeletal muscle ryanodine receptor via a calmodulin binding site. Mol Pharmacol. 1999; 55(3):462-472.

Kreimeyer A, Muller G, Kassack M, Nickel P, Gagliardi AR. Suramin analogues with a 2-phenylbenzimidazole moiety as partial structure; potential anti HIV- and angiostatic drugs, 2: Sulfanilic acid-, benzenedisulfonic acid-, and naphthalenetrisulfonic acid analogues. Arch Pharm Pharm Med Chem. 1998; 331(3):97-103.

Gagliardi AR, Kassack M, Kreimeyer A, Muller G, Nickel P, Collins DC. Antiangiogenic and antiproliferative activity of suramin analogues. Cancer Chemother Pharmacol. 1998; 41(2):117-124.

Kassack M, Nickel P. Rapid, highly sensitive gradient narrow-bore high-performance liquid chromatographic determination of suramin and its analogues. J Chromatogr B Biomed Appl. 1996; 686(2):275-284.

Kassack M, Nickel P. Stability of suramin in aqueous solution; possible implications for the search for suramin metabolites in patients. Arch Pharm Pharm Med Chem. 1996; 329(5):225-228.

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