Publications
2025
Willems S, Maksumic L, Niggenaber J, Lin TC, Schulz T, Weisner J, Sievers S, Müller MP, Summerer D, Rauh D. Advancing TET Inhibitor Development: From Structural Insights to Biological Evaluation. ACS Med Chem Lett. 2025 Apr 8;16(5):804-810. doi: 10.1021/acsmedchemlett.5c00042. PMID: 40365382;
Hoock JGF, Burhop A, Greiner LC, Schölermann B, Da Cruz Lopes Guita C, Liu J, Bag S, Pahl A, Sievers S, Scheel R, Strohmann C, Ziegler S, Grigalunas M, Waldmann H. An Indole Dearomatization Strategy for the Synthesis of Pseudo- Natural Products. Chembiochem. 2025 Apr 9:e2500182. doi: 10.1002/cbic.202500182. Epub ahead of print. PMID: 40202775.
Qiu X, Kemker C, Goebel GL, Lampe P, Wallis N, Schiller D, Bigler K, Jiang M, Sievers S, Yeo GW, Wu P. Phenylpyrazoles as Inhibitors of the m<sup>6</sup>A RNA-Binding Protein YTHDF2. JACS Au. 2025 Feb 10;5(2):618-630. doi: 10.1021/jacsau.4c00754. PMID: 40017738
Azam U, Humayun WA, Avathan Veettil AK, Liu Y, Hastürk O, Jiang M, Sievers S, Wu P, Naseer MM. Identification of 5-amino-1,3,4-thiadiazole appended isatins as bioactive small molecules with polypharmacological activities. RSC Med Chem. 2025 Jan 29. doi: 10.1039/d4md00770k. Epub ahead of print. PMID: 39990167.
Binici A, Hennes E, Koska S, Alexander Niemann J, Reich A, Pfaff C, Sievers S, Stefanie Kahnt A, Thomas D, Ziegler S, Watzl C, Waldmann H. Identification of Natural Killer Cell Enhancers Through Mimicking of the Tumor Microenvironment. Chemistry. 2025 Mar 25;31(18):e202404006. doi: 10.1002/chem.202404006. Epub 2025 Feb 28. PMID: 39932696.
Griggs SD, Piticari AS, Liver S, Arter C, Sievers S, Marsden SP, Nelson A. Phenotype-directed discovery of diverse, biologically-relevant molecular scaffolds. Chem Commun (Camb). 2025 Feb 20;61(17):3528-3531. doi: 10.1039/d4cc06605g. PMID: 39907073.
Schulz T, Gontla R, Teuber A, Beerbaum M, Fletcher BS, Mühlenberg T, Kaitsiotou H, Hardick J, Jeyakumar K, Keul M, Müller MP, Sievers S, Bauer S, Rauh D. Design, Synthesis, and SAR of Covalent KIT and PDGFRA Inhibitors─Exploring Their Potential in Targeting GIST. J Med Chem. 2025 Feb 13;68(3):3238-3259. doi: 10.1021/acs.jmedchem.4c02472. Epub 2025 Jan 22. PMID: 39841084.
Bauer LG, Ward JA, Díaz-Sáez L, Sundström Y, Tolvanen T, Alarcón Barrera JC, Kostidis S, Rogers CM, Panagakou I, Singh U, Rothweiler EM, Gonzalez Orta A, Kaniskan HÜ, Hu J, Jin J, Sievers S, Waldmann H, Giera M, Sundström M, Berg L, Huber KVM. Phenomics-Based Discovery of Novel Orthosteric Choline Kinase Inhibitors. Angew Chem Int Ed Engl. 2025 Feb 10;64(7):e202420149. doi: 10.1002/anie.202420149. Epub 2025 Jan 13. PMID: 39740997; PMCID: PMC11811597.
Jiang M, Giannino N, Goebel GL, Sievers S, Wu P. LIN28-Targeting Chromenopyrazoles and Tetrahydroquinolines Induced Cellular Morphological Changes and Showed High Biosimilarity with BRD PROTACs. ChemMedChem. 2025 Jan 2;20(1):e202400547. doi: 10.1002/cmdc.202400547. Epub 2024 Nov 12. PMID: 39353851; PMCID: PMC11694606.
Hennes E, Lucas B, Scholes NS, Cheng XF, Scott DC, Bischoff M, Reich K,Gasper R, Lucas M, Xu TT, Pulvermacher LM, Dötsch L, Imrichova H, Brause A, Naredla KR, Sievers S, Kumar K, Janning P, Gersch M, Murray PJ, Schulman BA, Winter GE, Ziegler S, Waldmann H. Identification of a Monovalent Pseudo-Natural Product Degrader Class Supercharging Degradation of IDO1 by its native E3 KLHDC3. bioRxiv [Preprint]. 2025 Jan 17:2024.07.10.602857. doi: 10.1101/2024.07.10.602857. PMID: 39026748; PMCID: PMC11257573.
2024
Rezaei Adariani S, Agne D, Koska S, Burhop A, Seitz C, Warmers J, Janning P, Metz M, Pahl A, Sievers S, Waldmann H, Ziegler S. Detection of a Mitochondrial Fragmentation and Integrated Stress Response Using the Cell Painting Assay. J Med Chem. 2024 Aug 8;67(15):13252-13270. doi: 10.1021/acs.jmedchem.4c01183. Epub 2024 Jul 17. PMID: 39018123; PMCID: PMC11320566.
Cigler M, Imrichova H, Frommelt F, Caramelle L, Depta L, Rukavina A, Kagiou C, Hannich JT, Mayor-Ruiz C, Superti-Furga G, Sievers S, Forrester A, Laraia L, Waldmann H, Winter GE. Orpinolide disrupts a leukemic dependency on cholesterol transport by inhibiting OSBP. Nat Chem Biol. 2025 Feb;21(2):193-202. doi: 10.1038/s41589-024-01614-4. Epub 2024 Jun 21. PMID: 38907113; PMCID: PMC11782089.
Goebel GL, Giannino N, Lampe P, Qiu X, Schloßhauer JL, Imig J, Sievers S, Wu P. Profiling Cellular Morphological Changes Induced by Dual-Targeting PROTACs of Aurora Kinase and RNA-Binding Protein YTHDF2. Chembiochem. 2024 Oct 1;25(19):e202400183. doi: 10.1002/cbic.202400183. Epub 2024 Jul 22. PMID: 38837838.
Patil S, Cremosnik G, Dötsch L, Flegel J, Schulte B, Maier KC, Žumer K, Cramer P, Janning P, Sievers S, Ziegler S, Waldmann H. The Pseudo-Natural Product Tafbromin Selectively Targets the TAF1 Bromodomain 2. Angew Chem Int Ed Engl. 2024 Aug 5;63(32):e202404645. doi: 10.1002/anie.202404645. Epub 2024 Jul 4. PMID: 38801173.
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. Illuminating Dark Chemical Matter Using the Cell Painting Assay. J Med Chem. 2024 Jun 13;67(11):8862-8876. doi: 10.1021/acs.jmedchem.4c00160. Epub 2024 Apr 30. PMID: 38687818
Wang L, Yilmaz F, Yildirim O, Schölermann B, Bag S, Greiner L, Pahl A, Sievers S, Scheel R, Strohmann C, Squire C, Foley DJ, Ziegler S, Grigalunas M, Waldmann H. Discovery of a Novel Pseudo-Natural Product Aurora Kinase Inhibitor Chemotype through Morphological Profiling. Adv Sci (Weinh). 2024 Jun;11(21):e2309202. doi: 10.1002/advs.202309202. Epub 2024 Apr 3. PMID: 38569218
He N, Depta L, Sievers S, Laraia L. Fluorescent probes and degraders of the sterol transport protein Aster-A. Bioorg Med Chem. 2024 Apr 1;103:117673. doi: 10.1016/j.bmc.2024.117673. Epub 2024 Mar 2. PMID: 38518734.
Dötsch L, Davies C, Hennes E, Schönfeld J, Kumar A, Guita CDCL, Ehrler JHM,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 Mar 28;67(6):4691-4706. doi: 10.1021/acs.jmedchem.3c02245. Epub 2024 Mar 12. PMID: 38470246
Pahl I, Pahl A, Hauk A, Budde D, Sievers S, Fruth L, Menzel R. Assessing biologic/toxicologic effects of extractables from plastic contact materials for advanced therapy manufacturing using cell painting assay and cytotoxicity screening. Sci Rep. 2024 Mar 11;14(1):5933. doi: 10.1038/s41598-024-55952-3. PMID: 38467674
Mühlenberg T, Falkenhorst J, Schulz T, Fletcher BS, Teuber A, Krzeciesa D, Klooster I, Lundberg M, Wilson L, Lategahn J, von Mehren M, Grunewald S, Tüns AI, Wardelmann E, Sicklick JK, Brahmi M, Serrano C, Schildhaus HU, Sievers S, Treckmann J, Heinrich MC, Raut CP, Ou WB, Marino-Enriquez A, George S, Rauh D, Fletcher JA, Bauer S. KIT ATP-Binding Pocket/Activation Loop Mutations in GI Stromal Tumor: Emerging Mechanisms of Kinase Inhibitor Escape. J Clin Oncol. 2024 Apr 20;42(12):1439-1449. doi: 10.1200/JCO.23.01197. Epub 2024 Feb 26. PMID: 38408285
Bag S, Liu J, Patil S, Bonowski J, Koska S, Schölermann 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 Jun;16(6):945-958. doi: 10.1038/s41557-024-01458-4. Epub 2024 Feb 16. PMID: 38365941
2023
Xie J, et al. Synthetic Matching of Complex Monoterpene Indole Alkaloid Chemical Space. Angew Chem Int Ed Engl. 2023:e202310222. Epub 2023/10/11. doi: 10.1002/anie.202310222. PubMed PMID: 37818743.
Whitmarsh-Everiss T, et al. Identification of biologically diverse tetrahydronaphtalen-2-ols through the synthesis and phenotypic profiling of chemically diverse, estradiol-inspired compounds. Chembiochem. 2023. Epub 2023/01/04. doi: 10.1002/cbic.202200555. PubMed PMID: 36594441.
Tong Y, et al. Programming inactive RNA-binding small molecules into bioactive degraders. Nature. 2023;618(7963):169-79. Epub 2023/05/25. doi: 10.1038/s41586-023-06091-8. PubMed PMID: 37225982.
Shamloo S, et al. Integrative CRISPR Activation and Small Molecule Inhibitor Screening for lncRNA Mediating BRAF Inhibitor Resistance in Melanoma. Biomedicines. 2023;11(7). Epub 2023/07/29. doi: 10.3390/biomedicines11072054. PubMed PMID: 37509693.
Riege D, et al. Identification of Maleimide-Fused Carbazoles as Novel Noncanonical Bone Morphogenetic Protein Synergizers ACS Pharmacol Transl Sci. 2023;6(8):1207-20. Epub 2023/08/17. doi: 10.1021/acsptsci.3c00103. PubMed PMID: 37588754.
Pahl A, et al. Morphological subprofile analysis for bioactivity annotation of small molecules. Cell Chem Biol. 2023;30(7):839-53 e7. Epub 2023/06/30. doi: 10.1016/j.chembiol.2023.06.003. PubMed PMID: 37385259.
Okolo EA, et al. Scaffold Remodelling of Diazaspirotricycles Enables Synthesis of Diverse sp(3) -Rich Compounds With Distinct Phenotypic Effects. Chemistry. 2023;29(26):e202203992. Epub 2023/02/02. doi: 10.1002/chem.202203992. PubMed PMID: 36722618.
Liu J, et al. A highly enantioselective intramolecular 1,3-dipolar cycloaddition yields novel pseudo-natural product inhibitors of the Hedgehog signalling pathway. Chem Sci. 2023;14(29):7936-43. Epub 2023/07/28. doi: 10.1039/d3sc01240a. PubMed PMID: 37502335.
Liu J, et al. Morphological Profiling Identifies the Motor Protein Eg5 as Cellular Target of Spirooxindoles. Angew Chem Int Ed Engl. 2023;62(21):e202301955. Epub 2023/03/18. doi: 10.1002/anie.202301955. PubMed PMID: 36929571.
Krzyzanowski A, et al. Spacial Score horizontal line A Comprehensive Topological Indicator for Small-Molecule Complexity. J Med Chem. 2023;66(18):12739-50. Epub 2023/08/31. doi: 10.1021/acs.jmedchem.3c00689. PubMed PMID: 37651653.
Corkery D, et al. Inducin Triggers LC3-Lipidation and ESCRT-Mediated Lysosomal Membrane Repair. Chembiochem. 2023:e202300579. Epub 2023/10/23. doi: 10.1002/cbic.202300579. PubMed PMID: 37869939.
Buhrmann M, et al. Fragtory: Pharmacophore-Focused Design, Synthesis, and Evaluation of an sp(3)-Enriched Fragment Library. J Med Chem. 2023;66(9):6297-314. Epub 2023/05/02. doi: 10.1021/acs.jmedchem.3c00187. PubMed PMID: 37130057.
Aoyama H, et al. Collective Synthesis of Sarpagine and Macroline Alkaloid-Inspired Compounds. Chemistry. 2023:e202303027. Epub 2023/09/27. doi: 10.1002/chem.202303027. PubMed PMID: 37755456.
2022
Wesseler F, et al. Phenotypic Discovery of Triazolo[1,5-c]quinazolines as a First-In-Class Bone Morphogenetic Protein Amplifier Chemotype. J Med Chem. 2022;65(22):15263-81. Epub 2022/11/09. doi: 10.1021/acs.jmedchem.2c01199. PubMed PMID: 36346705.
Scholermann B, et al. Identification of Dihydroorotate Dehydrogenase Inhibitors Using the Cell Painting Assay. Chembiochem. 2022;23(22):e202200475. Epub 2022/09/23. doi: 10.1002/cbic.202200475. PubMed PMID: 36134475.
Flegel J, et al. The Highly Potent AhR Agonist Picoberin Modulates Hh-Dependent Osteoblast Differentiation. J Med Chem. 2022;65(24):16268-89. Epub 2022/12/03. doi: 10.1021/acs.jmedchem.2c00956. PubMed PMID: 36459434
Wesseler, F. et al. Probing Embryonic Development Enables the Discovery of Unique Small-Molecule Bone Morphogenetic Protein Potentiators. J Med Chem 65, 3978-3990, doi:10.1021/acs.jmedchem.1c01800 (2022).
Niggemeyer, G. et al. Synthesis of 20-Membered Macrocyclic Pseudo-Natural Products Yields Inducers of LC3 Lipidation. Angew Chem Int Ed Engl 61, e202114328, doi:10.1002/anie.202114328 (2022).
Hwang, J. et al. Synthesis and evaluation of RNase L-binding 2-aminothiophenes as anticancer agents. Bioorg Med Chem 58, 116653, doi:10.1016/j.bmc.2022.116653 (2022).
Heinrich, S., Grote, M., Sievers, S., Kushnir, S. & Schulz, F. Polyether Cyclization Cascade Alterations in Response to Monensin Polyketide Synthase Mutations. Chembiochem 23, e202100584, doi:10.1002/cbic.202100584 (2022).
Grigalunas, M. et al. Unprecedented Combination of Polyketide Natural Product Fragments Identifies the New Hedgehog Signaling Pathway Inhibitor Grismonone. Chemistry, e202202164, doi:10.1002/chem.202202164 (2022).
Davies, C. et al. Identification of a Novel Pseudo-Natural Product Type IV IDO1 Inhibitor Chemotype. Angew Chem Int Ed Engl 61, e202209374, doi:10.1002/anie.202209374 (2022).
Carrillo Garcia, C. et al. High-Throughput Screening Platform in Postnatal Heart Cells and Chemical Probe Toolbox to Assess Cardiomyocyte Proliferation. J Med Chem 65, 1505-1524, doi:10.1021/acs.jmedchem.1c01173 (2022).
Borgelt, L. et al. Small-molecule screening of ribonuclease L binders for RNA degradation. Biomed Pharmacother 154, 113589, doi:10.1016/j.biopha.2022.113589 (2022).
Akbarzadeh, M. et al. The Pseudo-Natural Product Rhonin Targets RHOGDI. Angew Chem Int Ed Engl 61, e202115193, doi:10.1002/anie.202115193 (2022).
Akbarzadeh, M. et al. Morphological profiling by means of the Cell Painting assay enables identification of tubulin-targeting compounds. Cell Chem Biol 29, 1053-1064 e1053, doi:10.1016/j.chembiol.2021.12.009 (2022).
2021
Ziegler, S., Sievers, S. & Waldmann, H. Morphological profiling of small molecules. Cell Chem Biol 28, 300-319, doi:10.1016/j.chembiol.2021.02.012 (2021).
Wilke, J. et al. Discovery of a sigma1 receptor antagonist by combination of unbiased cell painting and thermal proteome profiling. Cell Chem Biol 28, 848-854 e845, doi:10.1016/j.chembiol.2021.01.009 (2021).
Spinck, M. et al. Discovery of Dihydro-1,4-Benzoxazine Carboxamides as Potent and Highly Selective Inhibitors of Sirtuin-1. J Med Chem 64, 5838-5849, doi:10.1021/acs.jmedchem.1c00017 (2021).
Schneidewind, T. et al. Combined morphological and proteome profiling reveals target-independent impairment of cholesterol homeostasis. Cell Chem Biol 28, 1780-1794 e1785, doi:10.1016/j.chembiol.2021.06.003 (2021).
Liu, J. et al. Combination of Pseudo-Natural Product Design and Formal Natural Product Ring Distortion Yields Stereochemically and Biologically Diverse Pseudo-Sesquiterpenoid Alkaloids. Angew Chem Int Ed Engl 60, 21384-21395, doi:10.1002/anie.202106654 (2021).
Liu, J. et al. Design, Synthesis, and Biological Evaluation of Chemically and Biologically Diverse Pyrroquinoline Pseudo Natural Products. Angew Chem Int Ed Engl 60, 4648-4656, doi:10.1002/anie.202013731 (2021).
Hennes, E. et al. Cell-Based Identification of New IDO1 Modulator Chemotypes. Angew Chem Int Ed Engl 60, 9869-9874, doi:10.1002/anie.202016004 (2021).
Grigalunas, M. et al. Natural product fragment combination to performance-diverse pseudo-natural products. Nat Commun 12, 1883, doi:10.1038/s41467-021-22174-4 (2021).
Carnero Corrales, M. A. et al. Thermal proteome profiling identifies the membrane-bound purinergic receptor P2X4 as a target of the autophagy inhibitor indophagolin. Cell Chem Biol 28, 1750-1757 e1755, doi:10.1016/j.chembiol.2021.02.017 (2021).
Burhop, A. et al. Synthesis of Indofulvin Pseudo-Natural Products Yields a New Autophagy Inhibitor Chemotype. Adv Sci (Weinh) 8, e2102042, doi:10.1002/advs.202102042 (2021).
Borgelt, L. et al. Trisubstituted Pyrrolinones as Small-Molecule Inhibitors Disrupting the Protein-RNA Interaction of LIN28 and Let-7. ACS Med Chem Lett 12, 893-898, doi:10.1021/acsmedchemlett.0c00546 (2021).
2020
Schneidewind, T. et al. Morphological Profiling Identifies a Common Mode of Action for Small Molecules with Different Targets. Chembiochem 21, 3197-3207, doi:10.1002/cbic.202000381 (2020).
Laraia, L. et al. Image-Based Morphological Profiling Identifies a Lysosomotropic, Iron-Sequestering Autophagy Inhibitor. Angew Chem Int Ed Engl 59, 5721-5729, doi:10.1002/anie.201913712 (2020).
Karatas, H. et al. Discovery of Covalent Inhibitors Targeting the Transcriptional Enhanced Associate Domain Central Pocket. J Med Chem 63, 11972-11989, doi:10.1021/acs.jmedchem.0c01275 (2020).
Foley, D. J. et al. Phenotyping Reveals Targets of a Pseudo-Natural-Product Autophagy Inhibitor. Angew Chem Int Ed Engl 59, 12470-12476, doi:10.1002/anie.202000364 (2020).
2019
Zimmermann, S. et al. A Scaffold-Diversity Synthesis of Biologically Intriguing Cyclic Sulfonamides. Chemistry 25, 15498-15503, doi:10.1002/chem.201904175 (2019).
Schneidewind, T. et al. The Pseudo Natural Product Myokinasib Is a Myosin Light Chain Kinase 1 Inhibitor with Unprecedented Chemotype. Cell Chem Biol 26, 512-523 e515, doi:10.1016/j.chembiol.2018.11.014 (2019).
Reckzeh, E. S. et al. Inhibition of Glucose Transporters and Glutaminase Synergistically Impairs Tumor Cell Growth. Cell Chem Biol 26, 1214-1228 e1225, doi:10.1016/j.chembiol.2019.06.005 (2019).
Pobbati, A. V. et al. Identification of Quinolinols as Activators of TEAD-Dependent Transcription. ACS Chem Biol 14, 2909-2921, doi:10.1021/acschembio.9b00786 (2019).
Pahl, A. & Sievers, S. The Cell Painting Assay as a Screening Tool for the Discovery of Bioactivities in New Chemical Matter. Methods Mol Biol 1888, 115-126, doi:10.1007/978-1-4939-8891-4_6 (2019).
Nemec, V. et al. 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 58, 1062-1066, doi:10.1002/anie.201810312 (2019).
Li, H. et al. Enantioselective Formal C(sp(3) )-H Bond Activation in the Synthesis of Bioactive Spiropyrazolone Derivatives. Angew Chem Int Ed Engl 58, 307-311, doi:10.1002/anie.201811041 (2019).
Laraia, L. et al. The cholesterol transfer protein GRAMD1A regulates autophagosome biogenesis. Nat Chem Biol 15, 710-720, doi:10.1038/s41589-019-0307-5 (2019).
Kremer, L. et al. Discovery of the Hedgehog Pathway Inhibitor Pipinib that Targets PI4KIIIss. Angew Chem Int Ed Engl 58, 16617-16628, doi:10.1002/anie.201907632 (2019).
Konstantinidis, G., Sievers, S. & Wu, Y. W. Identification of Novel Autophagy Inhibitors via Cell-Based High-Content Screening. Methods Mol Biol 1854, 187-195, doi:10.1007/7651_2018_125 (2019).
Kaiser, N., Corkery, D., Wu, Y., Laraia, L. & Waldmann, H. Modulation of autophagy by the novel mitochondrial complex I inhibitor Authipyrin. Bioorg Med Chem 27, 2444-2448, doi:10.1016/j.bmc.2019.02.028 (2019).
Garivet, G. et al. Small-Molecule Inhibition of the UNC-Src Interaction Impairs Dynamic Src Localization in Cells. Cell Chem Biol 26, 842-851 e847, doi:10.1016/j.chembiol.2019.02.019 (2019).
Friese, A. et al. Chemical Genetics Reveals a Role of dCTP Pyrophosphatase 1 in Wnt Signaling. Angew Chem Int Ed Engl 58, 13009-13013, doi:10.1002/anie.201905977 (2019).
Christoforow, A. et al. Design, Synthesis, and Phenotypic Profiling of Pyrano-Furo-Pyridone Pseudo Natural Products. Angew Chem Int Ed Engl 58, 14715-14723, doi:10.1002/anie.201907853 (2019).
Ceballos, J. et al. Synthesis of Indomorphan Pseudo-Natural Product Inhibitors of Glucose Transporters GLUT-1 and -3. Angew Chem Int Ed Engl 58, 17016-17025, doi:10.1002/anie.201909518 (2019).
2018
Wilke, J. et al. Identification of cytotoxic, glutathione-reactive moieties inducing accumulation of reactive oxygen species via glutathione depletion. Bioorg Med Chem 26, 1453-1461, doi:10.1016/j.bmc.2017.11.009 (2018).
Spinck, M., Ecke, M., Sievers, S. & Neumann, H. Highly Sensitive Lysine Deacetylase Assay Based on Acetylated Firefly Luciferase. Biochemistry 57, 3552-3555, doi:10.1021/acs.biochem.8b00483 (2018).
Shan, G. et al. C-H Bond Activation for the Synthesis of Heterocyclic Atropisomers Yields Hedgehog Pathway Inhibitors. Angew Chem Int Ed Engl 57, 14250-14254, doi:10.1002/anie.201809680 (2018).
Robke, L. et al. Discovery of the novel autophagy inhibitor aumitin that targets mitochondrial complex I. Chem Sci 9, 3014-3022, doi:10.1039/c7sc05040b (2018).
Klein, A. S. et al. Preparation of Cyclic Prodiginines by Mutasynthesis in Pseudomonas putida KT2440. Chembiochem 19, 1545-1552, doi:10.1002/cbic.201800154 (2018).
Karageorgis, G. et al. Chromopynones are pseudo natural product glucose uptake inhibitors targeting glucose transporters GLUT-1 and -3. Nat Chem 10, 1103-1111, doi:10.1038/s41557-018-0132-6 (2018).
Jia, Z. J. et al. Catalytic Enantioselective Synthesis of a Pyrrolizidine-Alkaloid-Inspired Compound Collection with Antiplasmodial Activity. J Org Chem 83, 7033-7041, doi:10.1021/acs.joc.7b03202 (2018).
Brand, S. et al. Combined Proteomic and In Silico Target Identification Reveal a Role for 5-Lipoxygenase in Developmental Signaling Pathways. Cell Chem Biol 25, 1095-1106 e1023, doi:10.1016/j.chembiol.2018.05.016 (2018).
2017
Xu, H. et al. Highly Enantioselective Catalytic Vinylogous Propargylation of Coumarins Yields a Class of Autophagy Inhibitors. Angew Chem Int Ed Engl 56, 11232-11236, doi:10.1002/anie.201706005 (2017).
Sidarovich, A. et al. Identification of a small molecule inhibitor that stalls splicing at an early step of spliceosome activation. Elife 6, doi:10.7554/eLife.23533 (2017).
Sheremet, M. et al. Small Molecules Inspired by the Natural Product Withanolides as Potent Inhibitors of Wnt Signaling. Chembiochem 18, 1797-1806, doi:10.1002/cbic.201700260 (2017).
Robke, L. et al. Phenotypic Identification of a Novel Autophagy Inhibitor Chemotype Targeting Lipid Kinase VPS34. Angew Chem Int Ed Engl 56, 8153-8157, doi:10.1002/anie.201703738 (2017).
Mejuch, T. et al. Small-Molecule Inhibition of the UNC119-Cargo Interaction. Angew Chem Int Ed Engl 56, 6181-6186, doi:10.1002/anie.201701905 (2017).
Martinez, N. E. et al. Tetrahydroisoquinolines: New Inhibitors of Neutrophil Extracellular Trap (NET) Formation. Chembiochem 18, 888-893, doi:10.1002/cbic.201600650 (2017).
Laraia, L. et al. Discovery of Novel Cinchona-Alkaloid-Inspired Oxazatwistane Autophagy Inhibitors. Angew Chem Int Ed Engl 56, 2145-2150, doi:10.1002/anie.201611670 (2017).
Kremer, L. et al. Discovery of a Novel Inhibitor of the Hedgehog Signaling Pathway through Cell-based Compound Discovery and Target Prediction. Angew Chem Int Ed Engl 56, 13021-13025, doi:10.1002/anie.201707394 (2017).
Klein, A. S. et al. New Prodigiosin Derivatives Obtained by Mutasynthesis in Pseudomonas putida. ACS Synth Biol 6, 1757-1765, doi:10.1021/acssynbio.7b00099 (2017).
Grassle, S. et al. Synthesis and Investigation of S-Substituted 2-Mercaptobenzoimidazoles as Inhibitors of Hedgehog Signaling. ACS Med Chem Lett 8, 931-935, doi:10.1021/acsmedchemlett.7b00100 (2017).
2016
Forster, T., Lopez-Tosco, S., Ziegler, S., Antonchick, A. P. & Waldmann, H. Enantioselective Organocatalytic Synthesis of a Secoyohimbane-Inspired Compound Collection with Neuritogenic Activity. Chembiochem 18, 1098-1108, doi:10.1002/cbic.201700015 (2017).
Ursu, A. et al. Epiblastin A Induces Reprogramming of Epiblast Stem Cells Into Embryonic Stem Cells by Inhibition of Casein Kinase 1. Cell Chem Biol 23, 494-507, doi:10.1016/j.chembiol.2016.02.015 (2016).
Sellstedt, M., Schwalfenberg, M., Ziegler, S., Antonchick, A. P. & Waldmann, H. Trienamine catalyzed asymmetric synthesis and biological investigation of a cytochalasin B-inspired compound collection. Org Biomol Chem 14, 50-54, doi:10.1039/c5ob02272j (2016).
Schroder, P., Bauer, J. O., Strohmann, C., Kumar, K. & Waldmann, H. Synthesis of an Iridoid-Inspired Compound Collection and Discovery of Autophagy Inhibitors. J Org Chem 81, 10242-10255, doi:10.1021/acs.joc.6b01185 (2016).
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