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

Mach ma – Andreas Brunschweiger. A feature produced by DSW21, published on YouTube: https://www.youtube.com/watch?v=8KvfHLOV1j8

Picture credits