Slava Ziegler

Project Group Leader, Chemical Biology

Publications

2024

Patil S, Cremosnik G, Dötsch L, Flegel J, Schulte B, Maier KC, Žumer K, Cramer P, Janning P, Sievers S, Ziegler S, Waldmann H (2024). Tafbromin selectively targets the TAF1 bromodomain.​ Angew Chem Int Ed Engl 
Source

Pahl A, Liu J, Patil S, Rezaei Adariani S, Schölermann B, Warmers J, Bonowski J, Koska S, Akbulut Y, Seitz C, Sievers S, Ziegler S, Waldmann H (2024). Illuminating Dark Chemical Matter Using the Cell Painting Assay​​​​.​ J Med Chem 
Source

Wang, L.;Yilmaz, F.;Yildirim, O.;Scholermann, B.;Bag, S.;Greiner, L.;Pahl, A.;Sievers, S.;Scheel, R.;Strohmann, C.;Squire, C.;Foley, D. J.;Ziegler, S.;Grigalunas, M.; Waldmann, H., Discovery of a Novel Pseudo-Natural Product Aurora Kinase Inhibitor Chemotype through Morphological Profiling, Adv Sci (Weinh) 2024, e2309202.

Dotsch, L.;Davies, C.;Hennes, E.;Schonfeld, J.;Kumar, A.;Guita, C.;Ehrler, J. H. M.;Hiesinger, K.;Thavam, S.;Janning, P.;Sievers, S.;Knapp, S.;Proschak, E.;Ziegler, S.; Waldmann, H., Discovery of the Seh Inhibitor Epoxykynin as a Potent Kynurenine Pathway Modulator, J Med Chem 2024, 67, 4691-4706.

Bag, S.;Liu, J.;Patil, S.;Bonowski, J.;Koska, S.;Scholermann, B.;Zhang, R.;Wang, L.;Pahl, A.;Sievers, S.;Brieger, L.;Strohmann, C.;Ziegler, S.;Grigalunas, M.; Waldmann, H., A Divergent Intermediate Strategy Yields Biologically Diverse Pseudo-Natural Products, Nat Chem 2024.

2023

Xie, J.;Pahl, A.;Krzyzanowski, A.;Krupp, A.;Liu, J.;Koska, S.;Scholermann, B.;Zhang, R.;Bonowski, J.;Sievers, S.;Strohmann, C.;Ziegler, S.;Grigalunas, M.; Waldmann, H., Synthetic Matching of Complex Monoterpene Indole Alkaloid Chemical Space, Angew Chem Int Ed Engl 2023, 62, e202310222.

Liu, J.;Mallick, S.;Xie, Y.;Grassin, C.;Lucas, B.;Scholermann, B.;Pahl, A.;Scheel, R.;Strohmann, C.;Protzel, C.;Berg, T.;Merten, C.;Ziegler, S.; Waldmann, H., Morphological Profiling Identifies the Motor Protein Eg5 as Cellular Target of Spirooxindoles, Angew Chem Int Ed Engl 2023, 62, e202301955.

Corkery, D.;Ursu, A.;Lucas, B.;Grigalunas, M.;Kriegler, S.;Oliva, R.;Dec, R.;Koska, S.;Pahl, A.;Sievers, S.;Ziegler, S.;Winter, R.;Wu, Y. W.; Waldmann, H., Inducin Triggers Lc3-Lipidation and Escrt-Mediated Lysosomal Membrane Repair, Chembiochem 2023, 24, e202300579.

Pahl, A.;Liu, J.;Patil, S.;Adariani, S. R.;Schölermann, B.;Warmers, J.;Bonowski, J.;Koska, S.;Sievers, S.;Ziegler, S.; Waldmann, H., Illuminating Dark Chemical Matter Using the Cell Painting Assay, bioRxiv 2023, 2023.2005.2031.542818.

Pahl A, Schölermann B, Rusch M, Dow M, Hedberg C, Nelson A, Sievers S, Waldmann H, Ziegler S (2023). Morphological Subprofile Analysis for Bioactivity Annotation of Small Molecules. bioRxiv
Source

2022

Flegel J, Shaaban S, Jia ZJ, Schulte B, Lian Y, Krzyzanowski A, Metz M, Schneidewind T, Wesseler F, Flegel A, Reich A, Brause A, Xue G, Zhang M, Dötsch L, Stender ID, Hoffmann JE, Scheel R, Janning P, Rastinejad F, Schade D, Strohmann C, Antonchick AP, Sievers S, Moura-Alves P, Ziegler S, Waldmann H (2022). The Highly Potent AhR Agonist Picoberin Modulates Hh-Dependent Osteoblast Differentiation. J Med Chem
Source

Schölermann B, Bonowski J, Grigalunas M, Burhop A, Xie Y, Hoock JGF, Liu J, Dow M, Nelson A, Nowak C, Pahl A, Sievers S, Ziegler S (2022). Identification of Dihydroorotate Dehydrogenase Inhibitors Using the Cell Painting Assay. Chembiochem.
Source

Grigalunas M, Patil S, Krzyzanowski A, Pahl A, Flegel J, Schölermann B, Xie J, Sievers S, Ziegler S, Waldmann H (2022). Unprecedented Combination of Polyketide Natural Product Fragments Identifies the New Hedgehog Signaling Pathway Inhibitor Grismonone. Chemistry
Source

Davies C, Dötsch L, Ciulla MG, Hennes E, Yoshida K, Gasper R, Scheel R, Sievers S, Strohmann C, Kumar K, Ziegler S, Waldmann H (2022). Identification of a Novel Pseudo-Natural Product Type IV IDO1 Inhibitor Chemotype. Angew Chem Int Ed Engl.
Source

Akbarzadeh M, Flegel J, Patil S, Shang E, Narayan R, Buchholzer M, Jasemi NSK, Grigalunas M, Krzyzanowski A, Abegg D, Shuster A, Potowski M, Karatas H, Karageorgis G, Mosaddeghzadeh N, Zischinsky ML, Merten C, Golz C, Brieger L, Strohmann C, Antonchick AP, Janning P, Adibekian A, Goody RS, Ahmadian MR, Ziegler S, Waldmann H (2022). The Pseudo-Natural Product Rhonin Targets RHOGDI. Angew Chem Int Ed Engl.

2021

Akbarzadeh M, Deipenwisch I, Schoelermann B, Pahl A, Sievers S, Ziegler S, Waldmann H.(2021). Morphological profiling by means of the Cell Painting assay enables identification of tubulin-targeting compounds. Cell Chem Biol.
Source

Schneidewind T, Brause A, Schölermann B, Sievers S, Pahl A, Sankar MG, Winzker M, Janning P, Kumar K, Ziegler S, Waldmann H (2021). Combined morphological and proteome profiling reveals target-independent impairment of cholesterol homeostasis. Cell Chem Biol.
Source

Ziegler S, Sievers S, Waldmann H. (2021). Morphological profiling of small molecules. Cell Chem Biol.
Source

Hennes E, Lampe P, Dötsch L, Bruning N, Pulvermacher LM, Sievers S, Ziegler S, Waldmann H (2021). Cell-Based Identification of New IDO1 Modulator Chemotypes Angew Chem Int Ed Engl.
Source

Wilke J, Kawamura T, Xu H, Brause A, Friese A, Metz M, Schepmann D, Wünsch B, Artacho-Cordón A, Nieto FR, Watanabe N, Osada H, Ziegler S, Waldmann H (2021). Discovery of a σ1 receptor antagonist by combination of unbiased cell painting and thermal proteome profiling Cell Chem Biol.
Source

2020

Furuta T, Mizukami Y, Asano L, Kotake K, Ziegler S, Yoshida H, Watanabe M, Sato SI, Waldmann H, Nishikawa M, Uesugi M. (2020). Nutrient-Based Chemical Library as a Source of Energy Metabolism Modulators. ACS Chem Biol  
doi: 10.1021/acschembio.0c00532

Schneidewind T, Brause A, Pahl A, Burhop A, Mejuch T, Sievers S, Waldmann H, Ziegler S (2020). Morphological Profiling Enables the Identification of Common Mode of Action for Small Molecules With Different Targets. ChemBioChem  
doi: 10.1002/cbic.202000381

Kawamura T, Futamura Y, Shang E, Muroi M, Janning P, Ueno M, Wilke J, Takeda S, Kondoh Y, Ziegler S, Watanabe N, Waldmann H, Osada H. S (2020). Discovery of small-molecule modulator of heterotrimeric Gi-protein by integrated phenotypic profiling and chemical proteomics.. Biosci Biotechnol Biochem.  
Source

2019

Winzker M, Friese A, Koch U, Janning P, Ziegler S. Waldmann H (2019). Development of a PDEδ targeting PROTAC that impairs lipid metabolism. Angew Chem Int Ed Engl
doi: 10.1002/anie.201913904.

Ceballos J, Schwalfenberg M, Karageorgis G, Reckzeh ES, Sievers S, Ostermann C, Pahl A, Sellstedt M, Nowacki J, Carnero Corrales M, Wilke J, Laraia L, Tschapalda K, Metz M, Sehr DA, Brand S, Winklhofer K, Janning P, Ziegler S, Waldmann H (2019). Synthesis of Indomorphan Pseudo Natural Product Inhibitors of Glucose Transporters GLUT-1 and -3. Angew Chem Int Ed Engl
doi: 10.1002/anie.201909518.

Kremer L, Hennes E, Brause A, Ursu A, Robke L, Matsubayashi HT, Nihongaki Y, Flegel J, Mejdrová I, Eickhoff J, Baumann M, Nencka R, Janning P, Kordes S, Schöler HR, Sterneckert J, Inoue T, Ziegler S, Waldmann H (2019). Discovery of the Hedgehog Pathway Inhibitor Pipinib that Targets PI4KIIIß. Angew Chem Int Ed Engl
doi: 10.1002/anie.201907632.

Furuta T, Mizukami Y, Asano L, Kotake K, Ziegler S, Yoshida H, Watanabe M, Sato SI, Waldmann H, Nishikawa M, Uesugi M. (2019). Nutrient-Based Chemical Library as a Source of Energy Metabolism Modulators. ACS Chem Biol.
doi: 10.1021/acschembio.9b00444.

Reckzeh ES, Karageorgis G, Schwalfenberg M, Ceballos J, Nowacki J, Stroet MCM, Binici A, Knauer L, Brand S, Choidas A, Strohmann C, ZieglerS, Waldmann H (2019). Inhibition of Glucose Transporters and Glutaminase Synergistically Impairs Tumor Cell Growth Cell Chemical Biology
https://doi.org/10.1016/j.chembiol.2019.06.005

Laraia L, Friese A, Corkery Dp, Konstantinidis G, Erwin N, Hofer W, Karatas H, Klewer L, Brockmeyer A, Metz M, Schölermann B, Dwivedi M, Li L, Rios-Munoz P, Köhn M, Winter R, Vetter IR, Ziegler S, Janning P, Wu YW and Waldmann H (2019). The cholesterol transfer protein GRAMD1A regulates autophagosome biogenesis Nat Chem Biol
doi.org/10.1038/s41589-019-0307-5

Förster T, Shang E, Shimizu K, Sanada E, Schölermann B, Huebecker M, Hahne G, Lopez-Alberca AP, Janning P, Watanabe N, Sievers S, Giordanetto F, Shimizu T, Ziegler S, Osada H, Waldmann H (2019). 2‐Sulfonylpyrimidines Target the Kinesin HSET via Cysteine Alkylation Eur Joc
doi: https://doi.org/10.1002/ejoc.201900586

Friese A, Kapoor S, Schneidewind T, Vidadala SR, Sardana J, Brause A, Förster T, Bischoff M, Wagner J, Janning P, Ziegler S, Waldmann H (2019). Chemical genetics reveals a role of dCTP pyrophosphatase 1 in Wnt signaling. Angew Chem Int Ed Engl
doi: 10.1002/anie.201905977.

Schneidewind T, Kapoor S, Garivet G, Karageorgis G, Narayan R, Vendrell-Navarro G, Antonchick AP, Ziegler S, Waldmann H(2019). The Pseudo Natural Product Myokinasib Is a Myosin Light Chain Kinase 1 Inhibitor with Unprecedented Chemotype. Cell Chem Biol
doi: 10.1016/j.chembiol.2018.11.014.

2018

Němec V, Hylsová M, Maier L, Flegel J, Sievers S, Ziegler S, Schroeder M, Berger BT, Chaikuad A, Valčíková B, Uldrijan S, Drápela S, Souček K, Waldmann H, Knapp S, Paruch K (2018). Furo[3,2-b]pyridine: A Privileged Scaffold for Highly Selective Kinase Inhibitors and Effective Modulators of the Hedgehog Pathway. Angew Chem Int Ed Engl
doi: 10.1002/anie.201810312.

Li H, Gontla R, Flegel J, Merten C, Ziegler S, Antonchick AP, Waldmann H (2018). Enantioselective Formal C(sp3 )-H Bond Activation in the Synthesis of Bioactive Spiropyrazolone Derivatives. Angew Chem Int Ed Engl
doi: 10.1002/anie.201811041.

Shan G, Flegel J, Li H, Merten C, Ziegler S, Antonchick AP Waldmann H (2018). C-H Bond Activation for the Synthesis of Heterocyclic Atropisomers Yields Hedgehog Pathway Inhibitors. Angew Chem Int Ed Engl
doi: 10.1002/anie.201809680.

Karageorgis G, Reckzeh ES, Ceballos J, Schwalfenberg M, Sievers S, Ostermann C, Pahl A, Ziegler S, Waldmann H (2018). Chromopynones are pseudo natural product glucose uptake inhibitors targeting glucose transporters GLUT-1 and -3. Nat Chem
doi: 10.1038/s41557-018-0132-6.

Brand S, Roy S, Schröder P, Rathmer B, Roos J, Kapoor S, Patil S, Pommerenke C, Maier T, Janning P, Eberth S, Steinhilber D, Schade D, Schneider G, Kumar K, Ziegler S, Waldmann H (2018). Combined proteomic and in silico target identification reveal a role for 5-Lipoxygenase in developmental signaling pathways. Cell Chem Bio
doi: https://doi.org/10.1016/j.chembiol.2018.05.016

Höing S, Yeh TY, Baumann M, Martinez NE, Habenberger P, Kremer L, Drexler HCA, Küchler P, Reinhardt P, Choidas A, Zischinsky ML, Zischinsky G, Nandini S, Ledray AP, Ketcham SA, Reinhardt L, Abo-Rady M, Glatza M, King SJ, Nussbaumer P, Ziegler S, Klebl B, Schroer TA, Schöler HR, Waldmann H, Sterneckert J. (2018). Dynarrestin, a Novel Inhibitor of Cytoplasmic Dynein. Cell Chem Biol. 25(4):357-369
doi: 10.1016/j.chembiol.2017.12.014.

2017

Pries V, Nöcker C, Khan D, Johnen P, Hong Z, Tripathi A, Keller AL, Fitz M, Perruccio F, Filipuzzi I, Thavam S, Aust T, Riedl R, Ziegler S, Bono F, Schaaf G, Bankaitis VA, Waldmann H, Hoepfner D. (2017). Target Identification and Mechanism of Action of Picolinamide and Benzamide Chemotypes with Antifungal Properties. Cell Chem Biol 2451-9456(17)30434-8
doi: 10.1016/j.chembiol.2017.12.007.

Wilke J, Kawamura T, Watanabe N, Osada H, Ziegler S, Waldmann H. (2017). Identification of cytotoxic, glutathione-reactive moieties inducing accumulation of reactive oxygen species via glutathione depletion. Bioorg Med CHem
doi: 10.1016/j.bmc.2017.11.009.

Küchler P, Zimmermann G, Winzker M, Janning P, Waldmann H, Ziegler S (2017). Identification of novel PDEδ interacting proteins. Bioorg Med Chem
doi: 10.1016/j.bmc.2017.08.033.

Kremer L, Schultz-Fademrecht C, Baumann M, Habenberger P, Choidas A, Klebl B, Kordes S, Schöler HJ, Sterneckert J, Ziegler S, Schneider G., Waldmann H (2017). Discovery of a Novel Hedgehog Signaling Pathway Inhibitor by Cell-based Compound Discovery and Target Prediction. Angew Chem Int Ed Engl
doi: 10.1002/anie.201707394.

Sheremet M, Kapoor S, Schröder P, Kumar K, Ziegler S and Waldmann H (2017). Natural Product Withanolide-Inspired Small molecules as Potent Inhibitors of Wnt Signaling. Chembiochem
doi: 10.1002/cbic.201700260.

Mejuch T, Garivet G, Hofer W, Kaiser N, Fansa EK, Ehrt C, Koch O, Baumann M, Ziegler S, Wittinghofer A, Waldmann H (2017). Phenotypic Identification of a Novel Autophagy Inhibitor Chemotype Targeting Lipid Kinase VPS34. Angew Chem Int Ed Engl 
doi: 10.1002/anie.201703738.

Waldmann H, Förster T, Lopéz-Tosco S, Ziegler S, Antonchick AP (2017). Enantioselective Organocatalytic Synthesis of a Secoyohimbane-Inspired Compound Collection with Neuritogenic Activity. Chembiochem
doi: 10.1002/cbic.201700015.

Waldmann H, Martinez NE, Zimmermann TJ, Goosmann C, Alexander T, Hedberg C, Ziegler S, Zychlinsky A (2017). Tetrahydroisoquinolines are Novel Inhibitors of Neutrophil Extracellular Trap (NET) Formation. Chembiochem
doi: 10.1002/cbic.201600650.

Lee YC, Patil S, Golz C, Strohmann C, Ziegler S, Kumar K, Waldmann H (2017). A ligand-directed divergent catalytic approach to establish structural and functional scaffold diversity. Nat Commun 8:14043
doi: 10.1038/ncomms14043.

2016

2015

Schröder P, Förster T, Kleine S, Becker C, Richters A, Ziegler S, Rauh D, Kumar K & Waldmann H (2015) Neuritogenic militarinone-inspired 4-hydroxypyridones target the stress pathway kinase MAP4K4. Angew Chem Int Ed Engl 54(42):12398-12403.
doi: 10.1002/anie.201501515.

Vendrell-Navarro G, R a F, Bujons J, Brockmeyer A, Janning P, Ziegler S, Messeguer A, Waldmann H (2015). Positional Scanning Synthesis of a Peptoid Library Yields New Inducers of Apoptosis that Target Karyopherins and Tubulin. Chembiochem 16(11):1580-7.
doi: 10.1002/cbic.201500169.

Svenda J, Sheremet M, Kremer L, Maier L, Bauer JO, Strohmann C, Ziegler S, Kumar K & Waldmann H (2015). Biology-oriented synthesis of a withanolide-inspired compound collection reveals novel modulators of hedgehog signaling. Angew Chem Int Ed Engl 54(19):5596-5602
doi: 10.1002/anie.201409942.

Akbulut Y, Gaunt HJ, Muraki K, Ludlow MJ, Amer MS, Bruns A, Vasudev NS, Radtke L, Willot M, Hahn S, Seitz T, Ziegler S, Christmann M, Beech DJ & Waldmann H (2015). (-)-Englerin A is a potent and selective activator of TRPC4 and TRPC5 calcium channels. Angew Chem Int Ed Engl 54(12):3787-3791.
doi: 10.1002/anie.201411511.

Vendrell-Navarro G, Brockmeyer A, Waldmann H, Janning P, Ziegler S (2015). Identification of the targets of biologically active small molecules using quantitative proteomics. Methods Mol Biol 1263:263-86.
doi: 10.1007/978-1-4939-2269-7_21.

2014

Tran TT, Gerding-Reimers C, Schölermann B, Stanitzki B, Henkel T, Waldmann H, Ziegler S (2014). Podoverine A--a novel microtubule destabilizing natural product from the Podophyllum species. Bioorg Med Chem 22(18):5110-6.
doi: 10.1016/j.bmc.2014.01.039.

Eschenbrenner-Lux V, K chler P, Ziegler S, Kumar K & Waldmann H (2014). An enantioselective inverse-electron-demand imino Diels-Alder reaction. Angew Chem Int Ed Engl 53(8):2134-2137.
doi: 10.1002/anie.201309022.

2013

Takayama H, Jia ZJ, Kremer L, Bauer JO, Strohmann C, Ziegler S, Antonchick AP, Waldmann H (2013). Discovery of inhibitors of the Wnt and Hedgehog signaling pathways through the catalytic enantioselective synthesis of an iridoid-inspired compound collection. Angew Chem Int Ed Engl 52(47):12404-8.
doi: 10.1002/anie.201306948.

Ziegler S, Pries V, Hedberg C, Waldmann H (2013). Target identification for small bioactive molecules: finding the needle in the haystack. Angew Chem Int Ed Engl 52(10):2744-92.
doi: 10.1002/anie.201208749.

Zimmermann TJ, Roy S, Martinez NE, Ziegler S, Hedberg C, Waldmann H (2013). Biology-oriented synthesis of a tetrahydroisoquinoline-based compound collection targeting microtubule polymerization. Chembiochem 14(3):295-300.
doi: 10.1002/cbic.201200711.

Voigt T, Gerding-Reimers C, Ngoc Tran TT, Bergmann S, Lachance H, Schölermann B, Brockmeyer A, Janning P, Ziegler S, Waldmann H (2013). A natural product inspired tetrahydropyran collection yields mitosis modulators that synergistically target CSE1L and tubulin. Angew Chem Int Ed Engl 52(1):410-4.
doi: 10.1002/anie.20120572.

2012

Matcha K, Madduri AV, Roy S, Ziegler S, Waldmann H, Hirsch AK, Minnaard AJ (2012). Total synthesis of (-)-doliculide, structure-activity relationship studies and its binding to F-actin. Chembiochem 13(17):2537-48.
doi: 10.1002/cbic.201200512.

2011

Dückert H, Pries V, Khedkar V, Menninger S, Bruss H, Bird AW, Maliga Z, Brockmeyer A, Janning P, Hyman A, Grimme S, Schürmann M, Preut H, Hübel K, Ziegler S, Kumar K, Waldmann H (2011). Natural product-inspired cascade synthesis yields modulators of centrosome integrity. Nat Chem Biol 8(2):179-84.
doi: 10.1038/nchembio.758.

Radtke L, Willot M, Sun H, Ziegler S, Sauerland S, Strohmann C, Fr hlich R, Habenberger P, Waldmann H, Christmann M (2011). Total synthesis and biological evaluation of (-)-englerin A and B: synthesis of analogues with improved activity profile. Angew Chem Int Ed Engl 50(17):3998-4002.
doi: 10.1002/anie.201007790.

before 2011

Antonchick AP, Gerding-Reimers C, Catarinella M, Schürmann M, Preut H, Ziegler S, Rauh D, Waldmann H (2010). Highly enantioselective synthesis and cellular evaluation of spirooxindoles inspired by natural products. Nat Chem 50(17):3998-4002.
doi: 10.1038/nchem.730

Röhrs S, Kutzner N, Vlad A, Grunwald T, Ziegler S, Müller O Ziegler S, Rauh D, Waldmann H (2009). Chronological expression of Wnt target genes Ccnd1, Myc, Cdkn1a, Tfrc, Plf1 and Ramp3 Cell Biol Int 50(17):3998-4002.
doi: 10.1016/j.cellbi.2009.01.016

Ziegler S, Röhrs S, Tickenbrock L, Langerak A, Chu ST, Feldmann I, Jakubowski N, Müller O (2007). Lipocalin 24p3 is regulated by the Wnt pathway independent of regulation by iron Cell Biol Int 50(17):3998-4002.
doi: 10.1016/j.cancergencyto.2006.11.004

Ziegler S, Röhrs S, Tickenbrock L, Möröy T, Klein-Hitpass L, Vetter IR, Müller O. (2005). Novel target genes of the Wnt pathway and statistical insights into Wnt target promoter regulation. FEBS J. 50(17):3998-4002.
doi: 10.1111/j.1742-4658.2005.04581.x