Publications

2022

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).

Papke, B. et al. Identification of pyrazolopyridazinones as PDEdelta inhibitors. Nat Commun 7, 11360, doi:10.1038/ncomms11360 (2016).

Kotzner, L. et al. The Organocatalytic Approach to Enantiopure 2H- and 3H-Pyrroles: Inhibitors of the Hedgehog Signaling Pathway. Angew Chem Int Ed Engl 55, 7693-7697, doi:10.1002/anie.201602932 (2016).

Jaiswal, M. et al. Novel Biochemical and Structural Insights into the Interaction of Myristoylated Cargo with Unc119 Protein and Their Release by Arl2/3. J Biol Chem 291, 20766-20778, doi:10.1074/jbc.M116.741827 (2016).

 

2015

Illich, D. J. et al. Distinct Signaling Requirements for the Establishment of ESC Pluripotency in Late-Stage EpiSCs. Cell Rep 15, 787-800, doi:10.1016/j.celrep.2016.03.073 (2016).

Vendrell-Navarro, G. et al. Positional Scanning Synthesis of a Peptoid Library Yields New Inducers of Apoptosis that Target Karyopherins and Tubulin. Chembiochem 16, 1580-1587, doi:10.1002/cbic.201500169 (2015).

Svenda, J. et al. Biology-oriented synthesis of a withanolide-inspired compound collection reveals novel modulators of hedgehog signaling. Angew Chem Int Ed Engl 54, 5596-5602, doi:10.1002/anie.201500112 (2015).

Schroder, P. et al. Neuritogenic militarinone-inspired 4-hydroxypyridones target the stress pathway kinase MAP4K4. Angew Chem Int Ed Engl 54, 12398-12403, doi:10.1002/anie.201501515 (2015).

Samanta, R. et al. Oxidative regioselective amination of chromones exposes potent inhibitors of the hedgehog signaling pathway. Chem Commun (Camb) 51, 925-928, doi:10.1039/c4cc08376h (2015).

Hackl, M. W. et al. Phenyl Esters Are Potent Inhibitors of Caseinolytic Protease P and Reveal a Stereogenic Switch for Deoligomerization. J Am Chem Soc 137, 8475-8483, doi:10.1021/jacs.5b03084 (2015).

Gilleron, J. et al. Identification of siRNA delivery enhancers by a chemical library screen. Nucleic Acids Res 43, 7984-8001, doi:10.1093/nar/gkv762 (2015).

Arndt, H. D. et al. Divergent solid-phase synthesis of natural product-inspired bipartite cyclodepsipeptides: total synthesis of seragamide A. Chemistry 21, 5311-5316, doi:10.1002/chem.201500368 (2015).

Zimmermann, G. et al. Structure guided design and kinetic analysis of highly potent benzimidazole inhibitors targeting the PDEdelta prenyl binding site. J Med Chem 57, 5435-5448, doi:10.1021/jm500632s (2014).

Eschenbrenner-Lux, V., Kumar, K. & Waldmann, H. The asymmetric hetero-Diels-Alder reaction in the syntheses of biologically relevant compounds. Angew Chem Int Ed Engl 53, 11146-11157, doi:10.1002/anie.201404094 (2014).

Zimmermann, T. J. et al. Biology-oriented synthesis of a tetrahydroisoquinoline-based compound collection targeting microtubule polymerization. Chembiochem 14, 295-300, doi:10.1002/cbic.201200711 (2013).

Zimmermann, G. et al. Small molecule inhibition of the KRAS-PDEdelta interaction impairs oncogenic KRAS signalling. Nature 497, 638-642, doi:10.1038/nature12205 (2013).

Takayama, H. et al. 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, 12404-12408, doi:10.1002/anie.201306948 (2013).

Narayan, R., Bauer, J. O., Strohmann, C., Antonchick, A. P. & Waldmann, H. Catalytic enantioselective synthesis of functionalized tropanes reveals novel inhibitors of hedgehog signaling. Angew Chem Int Ed Engl 52, 12892-12896, doi:10.1002/anie.201307392 (2013).

Antonchick, A. P. et al. Highly enantioselective catalytic synthesis of neurite growth-promoting secoyohimbanes. Chem Biol 20, 500-509, doi:10.1016/j.chembiol.2013.03.011 (2013).

Samatov, T. R. et al. Psoromic acid derivatives: a new family of small-molecule pre-mRNA splicing inhibitors discovered by a stage-specific high-throughput in vitro splicing assay. Chembiochem 13, 640-644, doi:10.1002/cbic.201100790 (2012).