Balzulat, A., Zhu, W.F., Flauaus, C., Hernandez-Olmos, V., Heering, J., Sethumadhavan, S., Dubiel, M., Frank, A., Menge, A., Hebchen, M., Metzner, K., Lu, R., Lukowski, R., Ruth, P., Knapp, S., Müller, S., Steinhilber, D., Hänelt, I., Stark, H., Proschak, E., Schmidtko, A. (2024)
Discovery of a Small Molecule Activator of Slack (Kcnt1) Potassium Channels That Significantly Reduces Scratching in Mouse Models of Histamine-Independent and Chronic Itch
Adv. Sci ePub


Li, F., Zhu, W.F., Empel, C., Datsenko, O., Kumar, A., Xu, Y., Ehrler, J.H.M., Atodiresei, I., Knapp, S., Mykhailiuk, P.K., Proschak, E., Koenigs, R.M. (2024)
Photosensitization enables Pauson-Khand-type reactions with nitrenes
Science 383, 498-503


Alcober-Boquet, L., Zang, T., Pietsch, L., Suess, E., Hartmann, M., Proschak, E., Gross, L.Z.F., Sacerdoti, M., Zeuzem, S., Rogov, V.V., Leroux, A.E., Piiper, A., Biondi, R.M. (2024)
AThe PB1 and the ZZ domain of the autophagy receptor p62/SQSTM1 regulate the interaction of p62/SQSTM1 with the autophagosome protein LC3B
Protein Sci. 33, e4840



Arifi, S., Marschner, J.A., Pollinger, J., Isigkeit, L., Heitel, P., Kaiser, A., Obeser, L., Höfner, G., Proschak, E., Knapp, S., Chaikuad, A., Heering, J., Merk, D. (2023)
Targeting the Alternative Vitamin E Metabolite Binding Site Enables Noncanonical PPARγ Modulation
J. Am. Chem. Soc.145, 14802-14810


Rotter, M.J., Zentgraf, S., Weizel, L., Frank, D., Burgers, L.D., Brunst, S., Fürst, R., Proschak, A., Wichelhaus, T.A., Proschak, E. (2023)
Integrating Siderophore Substructures in Thiol-Based Metallo-β-Lactamase Inhibitors
Molecules 28, 1984



Hufnagel, B., Zhu, W.F., Franz, H.M., Proschak, E., Hernandez-Olmos, V. (2022)
Phenolate-Induced N-O Bond Formation versus Tiemann-Type Rearrangement for the Synthesis of 3-Aminobenzisoxazoles and 2-Aminobenzoxazoles
ChemistryOpen 11, 12


Helmstädter, M., Schierle, S., Isigkeit, L., Proschak, E., Marschner, J.A., Merk, D. (2022)
Activity Screening of Fatty Acid Mimetic Drugs Identified Nuclear Receptor Agonists
Int. J. Mol. Sci. 2022 23, 10070

Ehrler, J.H.M., Brunst, S., Tjaden, A., Kilu, W., Heering, J., Hernandez-Olmos, V., Krommes, A., Kramer, J.S., Steinhilber, D., Schubert-Zsilavecz, M., Müller, S., Merk, D., Proschak, E. (2022)
Compilation and evaluation of a fatty acid mimetics screening library
Biochem. Pharmacol. 204, 115191

Brunst, S., Schönfeld, J., Breunig, P., Burgers, L.D., DeMeglio, M., Ehrler, J.H.M., Lillich, F.F., Weizel, L., Hefendehl, J.K., Fürst, R., Proschak, E., Hiesinger, K. (2022)
Designing a Small Fluorescent Inhibitor to Investigate Soluble Epoxide Hydrolase Engagement in Living Cells
ACS Med. Chem. Lett. 2022 13, 7, 1062-1067

Kaya, C., Konstantinović, J., Kany, A., Andreas, A., Kramer, J., Brunst, S., Weizel, L., Rotter, M., Frank, D., Yahiaoui, S., Müller, R., Hartmann, R., Haupenthal, J., Proschak, E., Wichelhaus, T., Hirsch, AKH. (2022)
N-Aryl mercaptopropionamides as broad-spectrum inhibitors of metallo-beta-lactamases
J. Med. Chem. 65, 5, 3913-3922

Heering, J., Hernandez-Olmos, V., Ildefeld, N., Liu, T., Kaiser, A., Naeem, Z., Frömel, T., Fleming, I., Steinhilber, S., Proschak, E. (2022)
Development and characterization of a fluorescent ligand for Leukotriene B4 receptor 2 in cells and tissues
J. Med. Chem.65, 3; 2023-2034

Seredinski, S., Boos, F., Günther, S., Oo, J.A., Warwick, T., Izquierdo Ponce, J., Lillich, F., Proschak, E., Knapp, S., Gilsbach, R., Pflüger-Müller, B., Brandes, R.P., Leisegang, M.S. (2022)
DNA topoisomerase inhibition with the HIF inhibitor Acriflavine promotes the transcription of lncRNAs in endothelial cells.
Mol. Ther. Nucleic Acids27; 1023-1035

Willems, S., Müller, M., Ohrndorf, J., Heering, J., Proschak, E., Merk, D. (2022)
Scaffold hopping from amodiaquine to novel Nurr1 agonist chemotypes via microscale analogue libraries, ChemMedChem 2022, 17, e2022000

Zhu, W. F., Krämer, A., Knapp, S., Proschak, E., Hernandez-Olmos, V. (2022)
Cascade Synthesis of Kinase-Privileged 3-Aminoindazoles via Intramolecular N-N Bond Formation
J. Org. Chem. 2022, 87, 5, 3856–3862


Mastromarino, M., Niso, M., Abate, C., Proschak, E., Dubiel, M., Stark, H., Castro, M., Lacivita, E., Leopoldo, M. (2022)
Design and Synthesis of Arylpiperazine Serotonergic/Dopaminergic Ligands with Neuroprotective Properties.
Molecules 2022 Feb; 27(4): 1297



Luciano, V. Langer, J., Proschak, E., Knapp, S., Marschalek, R., Heering, J. (2021)
Closantel is an allosteric inhibitor of human Taspase1
iScience 2424; 103524


Kaya, C., Konstantinović, J., Kany, A., Andreas, A., Kramer, J., Brunst, S., Weizel, L., Rotter, M., Frank, D., Yahiaoui, S., Müller, R., Hartmann, R., Haupenthal, J., Proschak, E., Wichelhaus, T., Hirsch, AKH. (2022)
N-Aryl mercaptopropionamides as broad-spectrum inhibitors of metallo-beta-lactamases
J. Med. Chem.12; 1698

Lillich, F.F., Willems, S., Ni, X., Borkowsky, C., Kilu, W., Brodsky, M., Kramer, J.S., Brunst, S., Hernandez-Olmos, V., Heering, J., Schierle, S., Kestner, R.I., Mayser, F.M., Helmstädter, M., Göbel, T., Weizel, L., Namgaladze, D., Kaiser, A., Steinhilber, D., Pfeilschifter, W., Kahnt, A.S., Proschak, A., Chaikuad, A., Knapp, S., Merk, D., Proschak E. (2021)
Structure-based design of dual partial peroxisome proliferator activated receptor agonists/ soluble epoxide hydrolase inhibitors
J. Med. Chem.64; 17259-17276.

Proschak, A., Martinelli, G., Frank, D., Rotter, M.J., Brunst, S., Weizel, L., Burgers, L.D., Fürst, R., Proschak, E., Sosič, I., Gobec, S., Wichelhaus, T.A. (2021)
Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases.
Eur. J. Med. Chem.228;113975


Imig, J.D., Merk, D., Proschak, E. (2021)
Multi-Target Drugs for Kidney Diseases.
Kidney360 2; 1645-1653.

Yahiaoui, S., Voos, K., Haupenthal, J., Wichelhaus, T.A., Frank, D., Weizel, L., Rotter, M., Brunst, S., Kramer, J.S., Proschak, E., Ducho, C., Hirsch, A.K.H. (2021)
N-Aryl mercaptoacetamides as potential multi-target inhibitors of metallo-β-lactamases (MBLs) and the virulence factor LasB from Pseudomonas aeruginosa
RCS Med. Chem12; 1698-1708.

Hernandez-Olmos, V., Heering, J., Bischoff-Kont, I., Kaps, A., Rajkumar, R., Liu, T., F rst, R., Steinhilber, D., Proschak, E. (2021)
Discovery of Irbesartan Derivatives as BLT2 Agonists by Virtual Screening.
ACS Med. Chem. Lett.12; 1261-1266.

Helmstädter, M., Kaiser, A., Brunst, S., Schmidt, J., Ronchetti, R., Weizel, L., Proschak, E., Merk, D. (2021)
Second-Generation Dual FXR/sEH Modulators with Optimized Pharmacokinetics
J. Med. Chem64; 9525-9536.

Krasavin,M., Zhukovsky, D., Solovyev, I., Barkhatova, D., Dar’in, D., Frank, D., Martinelli, G., Weizel, L., Proschak, A., Rotter, M., Kramer, J.S., Brunst, S., Wichelhaus, T.A., Proschak, E. (2021)
Rh(II)-Catalyzed De-symmetrization of Ethane-1,2-dithiol and Propane-1,3-dithiol Yields Metallo-beta-lactamase Inhibitors
ChemMedChem16; 1-9.


Kilu, W., Merck, D., Steinhilber, D., Proschak, E., Heering, J. (2021)
Heterodimer formation with retinoic acid receptor RXRα modulates coactivator recruitment by peroxisome proliferator-activated receptor PPARγ
Journal of Biological Chemistry.


Lillich, F., Imig, J.D., Proschak, E. (2021)
Multi-target approaches in metabolic syndrome.
Front. Pharmacol. 11; 554961.

Hiesinger, K., Darìn, D., Proschak, E., Krasavin, M. (2021)
Spirocyclic Scaffolds in Medicinal Chemistry.
J. Med. Chem. 64; 150-183.


Fischer, C., Willken-Schmitz, A., Hernandez-Olmos, V., Proschak, E., Stark, H., Fleming, E., Weigert, A., Thurn, M., Hofmann, M., Werner, E.R., Geisslinger, G., Niederberger, E., Watschinger, K., Tegeder, I
AGMO inhibitor reduces 3T3-L1 adipogenesis
Cells10; 1081.

Schierle, S., Brunst, S., Helmstädter, M., Ebert, R., Kramer, J.S., Steinhilber, D., Proschak, E., Merk, D. (2021)
Development and in vitro profiling of dual FXR/LTA4H modulators
ChemMedChem16; 2366-2374.

Schierle, S.; Chaikuad, A., Lillich, F., Ni, X., Woltersdorf, S., Schallmayer, E., Renelt, B., Ronchetti, R., Knapp, S., Proschak, E., Merk, D. (2021)
Oxaprozin analogues as selective RXR agonists with superior properties and pharmacokinetics
J. Med. Chem64; 5123-5136.

Helmstädter, M., Schmidt, J., Kaiser, A., Weizel, L., Proschak, E., Merk, D. (2021)
Differential therapeutic effects of FXR activation, sEH inhibition and dual FXR/sEH modulation in NASH in diet-induced obese mice
ACS Pharmacol. Transl. Sci4; 966-979.

Ni, X., Schröder, M., Olieric, V., Sharpe, M.E., Hernandez-Olmos, V., Proschak, E., Merk, D., Knapp, S., Chaikuad, A. (2021)
Structural insights into plasticity and discovery of remdesivir metabolite GS-441524 binding in SARS-CoV-2 macrodomain
ACS Med. Chem. Lett.12; 603-609.

Hartmann, M., Huber, J., Kramer, J.S., Heering, J., Pietsch, L., Stark, L., Odadzic, D., Bischoff, I., Fürst, R., Schroder, M., Akutsu, M., Chaikuad, A., Dotsch, V., Knapp, S., Biondi, R.M., Rogov, V.V., Proschak, E. (2021)
Demonstrating Ligandability of the LC3A and LC3B Adapter Interface.
J. Med. Chem. 64; 3720-3746.

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. (2021)
Combined Cardioprotective and Adipocyte Browning Effects Promoted by the Eutomer of Dual sEH/PPARγ Modulator
J. Med. Chem. 64; 2815-2828.

Brunst, S., Kramer, J.S., Kilu, W., Heering, J., Pollinger, J., Hiesinger, K., George, S., Steinhilber, D., Merk, D., Proschak, E. (2021)
Systematic assessment of fragment identification for multi‐target drug design.
ChemMedChem. 16; 1088-1092.