Publication

2022

   

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.; accepted

 

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.; accepted

 

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 ; accepted

2021

   

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.
   

2020

2019

2018

2017

2016

2015

2014

2013

 

2012

2011


2010

2009

2008

2007