To content

Publications

2022

44. 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, accepted.

43. 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

42. 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.

41. Jens Bobers, Lisa Katharina Hahn, Tobias Averbeck, Andreas Brunschweiger, Norbert Kockmann
Reaction Optimization of a Suzuki-Miyaura Cross-Coupling using Design of Experiments
Chemie Ingenieur Technik

40. 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, accepted.

39. A. Brunschweiger,
A DNA-encoded library special issue. Editorial.
Bioorg. Med. Chem. 2022, 56, 116582.

38. 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, accepted

2021

37. 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.

36. 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.

35. 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

34. M. Potowski, V. B. K. Kunig, L. Eberlein, A. Vakalopoulos, S. M. Kast,* 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.

33. V. B. K. Kunig, M. Potowski, M. Klika Škopić, A. Brunschweiger,
"Scanning protein surface with DNA-encoded libraries."
Chemmedchem 202116, 1048-1062. Invited review, VIP article.

2020

32. 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.
The TEAD-YAP-inhibitors (Angew. Chem. Int. Ed. 2020) have been highlighted in ChemistryViews.

31. K. Götte, S. Chines, A. Brunschweiger
"Reaction Development for DNA-Encoded Library Technology: From Evolution to Revolution?"
Tet. Lett., 2020, 61, 151889. Invited Digest Article by Tetrahedron Letters.

30. 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.

29. 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.

28. J. Bobers, M. Klika Škopic, 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.

2019

27. 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.

26. V. B. K. 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.

25. M. Klika Škopic, 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, 26, 10546-10555.

24. M. Potowski, V. B. K. 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 as front cover

2018

23. 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.

22. V. B. K. 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.

2017

21. M. Klika Škopic, 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.

20. 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.

19. M. Klika Škopic, 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

2016

18. M. Klika Škopic, 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.

17. H. Salamon, M. Klika S?kopic´, K. Jung, O. Bugain, A. Brunschweiger,*
"Chemical biology probes from advanced DNA-encoded libraries."
ACS Chem. Biol. 2016, 19, 296-307.

16. 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

15. 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.

2015

14. 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

2014

13. 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.

12. 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.

2013

11. P. Koch, R. Akkari, A. Brunschweiger, T. Borrmann, M. Schlenk, P. Küppers, M. Köse, H. Radjainia, J. Hockemeyer, A. Drabczynska, K. Kiec-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.

10. U. Pradère, A. Brunschweiger, L. F. Gebert, M. Lucic, M. Roos M, J. Hall,
"Chemical Synthesis of Mono- and Bis-Labeled Pre-MicroRNAs."
Angew. Chem. Int. Ed. Engl. 2013, 52, 12028-12032.

9. 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.

2012

8. A. Brunschweiger, J. Hall,
"A decade of the human genome sequence – how does the medicinal chemist benefit?"
ChemMedChem. 2012, 7, 194-203.

7. F. E. Loughlin, L. F. Gebert, H. Towbin, A. Brunschweiger, J. Hall, H. 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.

6. P. Ripphausen, M. Freundlieb, A. Brunschweiger, H. Zimmermann, C. E. Müller, J. Bajorath,
"Identification of first-in-class inhibitors of ecto-5´-nucleotidaseJ."
Med. Chem. 2012, 55, 6576-81.

2008

5. 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.

2006

4. A. Brunschweiger and C. E. Müller,
"Medizinische Chemie der Diuretika."
Pharmazie in Unserer Zeit 2006, 35, 310-320.

3. A. Brunschweiger, J. Iqbal, A. Scheiff, M. N. Munkonda, J. Sévigny, A. F. Knowles, C. E. Müller,
"Synthesis and structure-activity relationships of 5'-substituted uridine and adenosine derivatives as ectonucleotidase inhibitors."
Abstract in: Purinergic Signalling 2006, 2, 170.

2. A. Brunschweiger and C. E. Müller,
"P2 Receptors activated by uracil nucleotides – an update."
Curr. Med. Chem. 2006, 12, 325-348.

2001

1. A. Brunschweiger and D. Heber,
"Two Approaches to α,α-bis-Mannich Salts of N-monosubstituted Amides."
Tet. Lett. 2001, 42, 2653-2656.