Intern
Institut für Pharmazie und Lebensmittelchemie

Publications

  • K. Götte, R. Dinter, L. Justen, N. Kockmann,* A. Brunschweiger,* Development of an Automatable Affinity Purification Process for DNA Encoded Chemistry. ACS Omega 2022, 7, 32, 28369–28377
     
  • S. Chines, C. Ehrt, M. Potowski, F. Biesenkamp, L. Grützbach, S. Brunner, F. van den Broek, S. Bali, K. Ickstadt, A. Brunschweiger, Navigating Chemical Reaction Space – Application to DNA-encoded Chemistry. Chem. Sci. 2022, 13, 11221-11231.
     
  • M. Potowski, V. B. K. Kunig, L. Eberlein, M. Klika Škopić, A. Vakalopoulos, S. M. Kast,* A. Brunschweiger,* Investigations into chemically stabilized four-letter DNA for DNA-encoded chemistry. Front. Chem. 2022, online, doi: 10.3389/fchem.2022.894563.
     
  • J. Bobers, L. K. Hahn, T. Averbeck, A. Brunschweiger, N. Kockmann. Reaction Optimization of a Suzuki-Miyaura Cross-Coupling using Design of Experiments. Chemie Ingenieur Technik 2022, 94, 780-785.
     
  • A. Brunschweiger, A DNA-encoded library special issue. Editorial. Bioorg. Med. Chem. 2022, 56, 116582.
     
  • M. Klika Škopić, F. Losch, A. E. McMillan, N. Willeke, M. Malenica, L. Bering, J. Bode, A. Brunschweiger,* Solid phase synthesis of DNA-tagged sp3-rich heterocycles by SnAP chemistry: Reagent-based scaffold diversity for DNA-encoded library design. Org. Lett. 2022, 24, 1383–1387.
     
  • A. L. Satz, A. Brunschweiger, M. E. Flanagan, A. Gloger, N. J. V. Hansen, L. Kuai, V. B. K. Kunig, X. Lu, D. Madsen, L. A. Marcaurelle, C. Mulrooney, G. O’Donovan, S. Sakata, J. Scheuermann. DNA-Encoded Chemical Libraries. Nat. Rev. Methods Primers 2022, 2, doi.org/10.1038/s43586-021-00084-5.
     
  • J. H. Hunter, M Potowski, H. A. Stanway-Gordon, A. Madin, G. Pairaudeau, A. Brunschweiger,* M. J. Waring,* Functional group tolerance of a micellar on-DNA Suzuki-Miyaura cross-coupling reaction for DNA-encoded library design. J. Org. Chem. 2021, 86, 17930–17935.
     
  • M. Potowski, V. B. K. Kunig, L. Eberlein, A. Vakalopoulos, S. M. Kast,* A. Brunschweiger,* Chemically stabilized DNA barcodes for DNA-encoded chemistry. Angew. Chem. Int. Ed. 2021, 60, 19744-19749.
     
  • M. Potowski, R. Lüttig, A. Vakalopoulos, A. Brunschweiger, Copper(I/II)-promoted diverse imidazo[1,2-α]pyridine synthesis on solid-phase bound DNA oligonucleotides for encoded library design. Org. Lett. 2021, 23, 5480–5484.
     
  • M. Klika Škopić, C. Gramse, R. Oliva, S. Pospich, L. Neukirch, M. Manisegaran, S. Raunser, R. Winter, R. Weberskirch,* A. Brunschweiger*, Towards DNA-Encoded Micellar Chemistry: DNA-Micelle Association and Environment Sensitivity of Catalysis. Chem. Eur. J. 2021, 27, 10048-10057. Highlighted as back cover.
     
  • V. B. K. Kunig, M. Potowski, M. Klika Škopić, A. Brunschweiger, Scanning protein surfaces with DNA-encoded libraries. Chemmedchem 2021, 16, 1048-1062. Invited review, VIP article.
     
  • V. B. K. Kunig, M. Potowski, M. Akbarzadeh, M. Klika Škopić, D. dos Santos Smith, L. Arendt, I. Dormuth, H. Adihou, B. Andlovic, H. Karatas, S. Shaabani, T. Zarganes-Tzitzikas, C. G. Neochoritis, R. Zhang, M. Groves, S. M. Guéret, C. Ottmann, J. Rahnenführer, R. Fried, A. Dömling, A. Brunschweiger, TEAD-YAP interaction inhibitors and MDM2 binders from DNA-encoded indole-focused Ugi-peptidomimetics. Angew. Chem. Int. Ed. 2020, 59, 20338-20342. VIP article.
     
  • Highlighted by ChemistryViews: www.chemistryviews.org/details/ezine/11258967/ DNA-Encoded_Combinatorial_Synthesis.html
     
  • K. Götte, S. Chines, A. Brunschweiger, Reaction Development for DNA-Encoded Library Technology: From Evolution to Revolution? Tetrahedron Lett. 2020, 61, 151889. Invited Digest.
     
  • M. Potowski, R. Esken, A. Brunschweiger, Translation of the copper/bipyridine-promoted Petasis reaction to solid phase-coupled DNA for encoded library synthesis. Bioorg. Med. Chem. 2020, 28, 115441.
     
  • D. Kögel, B. Linder, A. Brunschweiger, S. Chines, C. Behl, At the Crossroads of Apoptosis and Autophagy: Multiple Roles of the Co-Chaperone BAG3 in Stress and Therapy Resistance of Cancer. Cells. 2020, 9, 574.
     
  • J. Bobers, M. Klika Škopić, R. Dinter, P. Sakthithasan, L. Neukirch, C. Gramse, R. Weberskirch, A. Brunschweiger,* N. Kockmann,* Design of an Automated Reagent-Dispensing System for Reaction Screening and Validation with DNA-tagged Substrates. ACS Comb. Sci. 2020, 22, 101-108.
     
  • M. Potowski, F. Losch, E. Wünnemann, J. K. Dahmen, S. Chines, A. Brunschweiger, Screening of metal ions and organocatalysts on solid support-coupled DNA oligonucleotides guides design of DNA-encoded reactions. Chem. Sci. 2019, 10, 10481-10492. Highlighted on back inside cover.
     
  • V. Kunig, C. Ehrt, A. Dömling, A. Brunschweiger, Isocyanide Multicomponent Reactions on Solid-Phase-Coupled DNA Oligonucleotides for Encoded Library Synthesis. Org. Lett., 2019, 21, 7238-7243.
     
  • M. Klika Škopić, K. Götte, C. Gramse, M. Dieter, S. Pospich, S. Raunser, R. Weberskirch,* A. Brunschweiger,* Micellar Brønsted Acid-Mediated Synthesis of DNA-Tagged Heterocycles. J. Am. Chem. Soc. 2019, 141, 10546-10555.
     
  • M. Potowski, V. Kunig, F. Losch, A. Brunschweiger, Synthesis of DNA-coupled isoquinolones and pyrrolidines by solid phase ytterbium- and silver-mediated imine chemistry. Med. Chem. Commun. 2019, 10, 1082-1093. Highlighted on front cover
     
  • V. Kunig, M. Potowski, A. Gohla, A. Brunschweiger, DNA-encoded libraries – an efficient small molecule discovery technology for the biomedical sciences. Biol. Chem. 2018, 399, 691-710.
     
  • P. Koch, A. Brunschweiger, V. Namasivayam, S. Ullrich, A. Maruca, B. Lazzaretto, P. Küppers, S. Hinz, J. Hockemeyer, M. Wiese, S. Alcaro, K. Kiec-Kononowiz, C. E. Müller, Probing substituents in the 1- and 3-position: Tetrahydropyrazino-annelated water-soluble xanthine derivatives as multi-target drugs with potent adenosine receptor antagonistic activity. Front. Chem. 2018, doi: 10.3389/fchem.2018.00206.
     
  • M. Klika Škopić, S. Willems, B. Wagner, J. Schieven, N. Krause, A. Brunschweiger, Exploration of a Au(I)-mediated three-component reaction for the synthesis of DNA-tagged highly substituted spiroheterocycles. Org. Biomol. Chem. 2017, 15, 8648-8654.
     
  • M. Menzi, B. Wild, U. Pradère, A. L. Malinowska, A. Brunschweiger, H. L. Lightfoot, J. Hall, Towards improved oligonucleotide therapeutics through faster target binding kinetics. Chem. Eur. J. 2017, 23, 14221-14230.
  • M. Klika Škopić, H. Salamon, O. Bugain, K. Jung, A. Gohla, L. J. Doetsch, D. dos Santos, A. Bhat, B. Wagner, A. Brunschweiger, Acid- and Au(I)-mediated synthesis of hexathymidine-DNA-heterocycle chimeras, an efficient entry to DNA-encoded libraries inspired by drug structures. Chem. Sci. 2017, 8, 3356-3361. Highlighted as inside front cover.
     
  • M. Klika Škopić, O. Bugain, K. Jung, S. Onstein, S. Brandherm, T. Kalliokoski, A. Brunschweiger, Design and synthesis of DNA-encoded libraries based on a benzodiazepine and a pyrazolopyrimidine scaffold. Med. Chem. Commun. 2016, 7, 1957-1965.
     
  • A. Brunschweiger,* L. F. Gebert*, M. Lucic, U. Pradère, H. Jahns, J. Hunziker, J. Hall, Site-specific conjugation of drug-like fragments to anti-miRNA oligonucleotides demonstrates pros and cons of targeting miRNAs in RISC. Chem. Commun. 2016, 52, 156-159. *joint first authors
     
  • H. Salamon, M. Klika Škopić, K. Jung, O. Bugain, A. Brunschweiger, Chemical biology probes from advanced DNA-encoded libraries. ACS Chem. Biol. 2016, 19, 296-307.
     
  • A. Brunschweiger, P. Koch, M. Schlenk, R. M, Radjainia, P. Küppers, S. Hinz, F. Pineda, M. Wiese, J. Hockemeyer, J. Heer, F. Denonne, C. E. Müller, 8-Substituted 1,3-dimethyltetrahydropyrazino[2,1-f]purinediones: Water-soluble adenosine receptor antagonists and monoamine oxidase B inhibitors. Bioorg. Med. Chem. 2016, 24, 5462-5480.
  • J. Imig,* A. Brunschweiger,* A. Brümmer, B. Guennewig, N. Mittal, S. Kishore, P. Tsikrika, A. P. Gerber, M. Zavolan, J. Hall, MiR-CLIP capture of a miRNA targetome uncovers a lincRNA H19-miR-106a interaction. Nat. Chem. Biol. 2015, 11, 107-114. *joint first authors
     
  • A. Brunschweiger, P. Koch, M. Schlenk, F. Pineda, P. Küppers, S. Hinz, M. Köse, S. Ullrich, J. Hockemeyer, M. Wiese, J. Heer, C. E. Müller, 8-​Benzyltetrahydropyrazino[2,​1-​f]​purinediones: water-​soluble tricyclic xanthine derivatives as multitarget drugs for neurodegenerative diseases. Chemmedchem 2014, 9, 1704-1724.
  • A. Brunschweiger, Report from the Third Annual Symposium of the RIKEN-Max Planck Joint Research Center for Systems Chemical Biology. ACS Chem. Biol. 2014, 9, 1649-1652.
  • U. Pradère, A. Brunschweiger, L. F. Gebert, M. Lucic, M. Roos, J. Hall, Chemical synthesis of mono- and bis-labeled pre-microRNAs. Angew. Chem. Int. Ed. Engl. 2013, 52, 12028-12032.
  • P. Koch, R. Akkari, A. Brunschweiger, T. Borrmann, M. Schlenk, P. Küppers, M. Köse, H. Radjainia, J. Hockemeyer, A. Drabczyńska, K. Kieć-Kononowicz, C. E. Müller, 1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases. Bioorg. Med. Chem. 2013, 21, 7435-7452.
     
  • M. A. Rebhan, A. Brunschweiger, J. Hall, Measurement by SPR of very low dissociation rates: Oxidation-mediated loss of biotin-streptavidin affinity. Chembiochem 2013, 14, 2091-2094.
     
  • A. Brunschweiger and J. Hall, A decade of the human genome sequence – how does the medicinal chemist benefit? ChemMedChem 2012, 7, 194-203.
     
  • F. E. Loughlin, L. F. Gebert, H. Towbin, A. Brunschweiger, J. Hall, F. H.-T. Allain, Structural basis of pre-let-7 miRNA recognition by the zinc knuckles of pluripotency factor Lin28. Nat. Struct. Mol. Biol. 2012, 19, 84-89.
     
  • P. Ripphausen, M. Freundlieb, A. Brunschweiger, H. Zimmermann, C. E. Müller, J. Bajorath, Identification of first-in-class inhibitors of ecto-5´-nucleotidase. J. Med. Chem. 2012, 55, 6576-81.
     
  • A. Brunschweiger, J. Iqbal, F. Umbach, A. B. Scheiff, M. N. Munkonda, J. Sévigny, A. F. Knowles, C. E. Müller, Selective nucleoside triphosphate di­phos­pho­­hydro­lase-2 (NTPDase2) inhibitors: nucleotide mimetics derived from uridine-5’-car­box­amide. J. Med. Chem. 2008, 51, 4518-4528.
     
  • A. Brunschweiger, C. E. Müller, Medizinische Chemie der Diuretika. Pharmazie in Unserer Zeit 2006, 35, 310-320.
     
  • A. Brunschweiger, C. E. Müller, P2 Receptors activated by uracil nucleotides – an update. Curr. Med. Chem. 2006, 12, 325-348.
     
  • A. Brunschweiger, D. Heber, Two approaches to α,α-bis-Mannich salts of N-monosubstituted amides. Tet. Lett. 2001, 42, 2653-2656.

  • S. Willems and A. Brunschweiger, DNA-encoded isocyanide multicomponent reactions. In Science of Synthesis. Thieme Verlag, Submitted.
     
  • E. Detta, A. Brunschweiger, J. Scheuermann, Barcoding strategies for DNA-encoded library synthesis. In DNA-encoded Libraries, a volume of Topics in Medicinal Chemistry.  Submitted.
     
  • M. Klika Škopić, D. dos Santos, A. Gohla, A. Brunschweiger, Initiating DNA-encoded library synthesis with a hexathymidine DNA oligonucleotide. In Methods in Molecular Biology, Springer, New York, United States of America. Accepted. 
     
  • A. Brunschweiger, Wahrheit oder Pflicht: Herausforderungen für die moderne Wissenschaft – ein Fazit; und Pharmaforschung im Spannungsfeld zwischen Grundlagenforschung, gesellschaftlichen Erwartungen und wirtschaftlichem Interesse, (2017) Klartext-Verlag: Essen.
     
  • A. Brunschweiger and J. Hall, Medicinal Chemistry in the Context of the Human Genome. In Personalized Medicine, (2013) Wiley-VCH Verlag GmbH & Co. KGaA: Weinheim. Chapter 13.

  • M. Klika Škopić, V. Kunig, M. Potowski, A. Brunschweiger, DNA-ENCODED CHEMICAL LIBRARY, USE THEREOF, AND METHOD TO SYNTHESIZE THE LIBRARY, submitted.
     
  • A. Bhat, M. Klika Škopić, A. Brunschweiger, R. Weberskirch, Method for the synthesis of DNA conjugates by micellar catalysis, 2018, PCT/EP2018/053650.
     
  • A. Brunschweiger, N. Krause, A. Antonchick, M. Klika Škopić, H. Salamon, K. Jung, O. Bugain, B. Wagner, DNA-encoded chemical library, use thereof and method to synthesize the library. 2016, PCT/EP2016/081845.
     
  • C. E. Müller, A. Brunschweiger, J. Iqbal, Preparation of nucleotide mimetics as ectonucleotidase inhibitors. WO2007135195 A1