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Articles by Herbert Waldmann
Orpinolide disrupts a leukemic dependency on cholesterol transport by inhibiting OSBP - Nature Chemical Biology
Abstract Metabolic alterations in cancer precipitate in associated dependencies that can be therapeutically exploited. To meet this goal, natural product-inspired small molecules can provide a resource of invaluable chemotypes. Here, we identify orpinolide, a synthetic withanolide analog with pronounced antileukemic properties, via orthogonal chemical screening.
Restriction of Glycolysis Increases Serial Killing Capacity of Natural Killer Cells
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Programming inactive RNA-binding small molecules into bioactive degraders - Nature
Abstract Target occupancy is often insufficient to elicit biological activity, particularly for RNA, compounded by the longstanding challenges surrounding the molecular recognition of RNA structures by small molecules. Here we studied molecular recognition patterns between a natural-product-inspired small-molecule collection and three-dimensionally folded RNA structures. Mapping these interaction landscapes across the human transcriptome defined structure–activity relationships.
Ketones as strategic building blocks for the synthesis of natural product-inspired compounds
Ketones as strategic building blocks for the synthesis of natural product-inspired compounds Daniel J. Foley *ab and Herbert Waldmann *bc Abstract Natural product-inspired compound collections serve as excellent sources for the identification of new bioactive compounds to treat disease. However, such compounds must necessarily be more structurally-enriched than traditional screening compounds, therefore inventive synthetic strategies and reliable methods are needed to prepare them.
Chemical Evolution of Natural Product Structure
Introduction The importance of small molecules that can perturb biological systems in a controlled fashion is underpinned by their successful applications in chemical biology (1) and medicine. (2) Nevertheless, the continued exploration of biologically relevant chemical space for the discovery of new small molecules remains an essential task for the better understanding of biological processes and for the advancement of therapeutics.
The Pseudo‐Natural Product Rhonin Targets RHOGDI
Research Article Herbert Waldmann, Corresponding Author Herbert Waldmann herbert.waldmann@mpi-dortmund.mpg.de brigitte.rose@mpi-dortmund.mpg.de Max-Planck-Institute of Molecular Physiology: Max-Planck-Institut fur molekulare Physiologie, Chemical Biology, Otto-Hahn-Str.
Morphological profiling of small molecules
Adams C.L. Kutsyy V. Coleman D.A. Cong G. Crompton A.M. Elias K.A. Oestreicher D.R. Trautman J.K. Vaisberg E. Compound classification using image-based cellular phenotypes. Methods Enzymol. 2006; 14: 440-468 Awale M. Reymond J.L. Web-based tools for polypharmacology prediction. Methods Mol. Biol. 2019; 1888: 255-272 Betge J. Rindtorff N. Sauer J. Rauscher B. Dingert C. Gaitantzi H. Herweck F. Miersch T. Valentini E. Hauber V. et al. Multiparametric phenotyping of compound effects on patient derived organoids.
Phenotyping reveals the targets of a pseudo‐natural product autophagy inhibitor
Research Article Herbert Waldmann Corresponding Author E-mail address: herbert.waldmann@mpi-dortmund.mpg.de E-mail address: brigitte.rose@mpi-dortmund.mpg.de Max-Planck-Institut für Molekulare Physiologie, Chemische Biologie, Otto-Hahn-Str.
Principle and design of pseudo-natural products
Abstract Natural products (NPs) are a significant source of inspiration towards the discovery of new bioactive compounds based on novel molecular scaffolds. However, there are currently only a small number of guiding synthetic strategies available to generate novel NP-inspired scaffolds, limiting both the number and types of compounds accessible.
Development of a PDEδ targeting PROTAC that impairs lipid metabolism
Communication Herbert Waldmann Corresponding Author E-mail address: herbert.waldmann@mpi-dortmund.mpg.de E-mail address: brigitte.rose@mpi-dortmund.mpg.de Max-Planck-Institut für Molekulare Physiologie, Chemische Biologie, Otto-Hahn-Str. 11, 44227 Dortmund, GERMANY Search for more papers by this author PDF PDF Share Abstract The prenyl‐protein chaperone PDEδ modulates the localization of lipidated proteins in the cell, but current knowledge about its biological function is limited.
Image‐based morphological profiling identifies a lysosomotropic, iron‐sequestering autophagy inhibitor
Abstract Graphical abstract Chemical proteomics is widely applied in small molecule target identification. However, in general it does not identify non‐protein small molecule targets, and thus, alternative methods for target identification are in high demand. We report the discovery of the autophagy inhibitor autoquin, and the identification of its molecular mode of action using image‐based morphological profiling in the cell painting assay.
Synthesis of Indomorphan Pseudo Natural Product Inhibitors of Glucose Transporters GLUT‐1 and ‐3 - Waldmann - - Angewandte Chemie International Edition - Wiley Online Library
Research Article Synthesis of Indomorphan Pseudo Natural Product Inhibitors of Glucose Transporters GLUT‐1 and ‐3 Herbert Waldmann Corresponding Author E-mail address: herbert.waldmann@mpi-dortmund.mpg.de E-mail address: brigitte.rose@mpi-dortmund.mpg.de Max-Planck-Institut für Molekulare Physiologie, Chemische Biologie, Otto-Hahn-Str.
Discovery of the Hedgehog Pathway Inhibitor Pipinib that Targets PI4KIIIß - Waldmann - - Angewandte Chemie International Edition - Wiley Online Library
Research Article Discovery of the Hedgehog Pathway Inhibitor Pipinib that Targets PI4KIIIß Herbert Waldmann Corresponding Author E-mail address: herbert.waldmann@mpi-dortmund.mpg.de E-mail address: brigitte.rose@mpi-dortmund.mpg.de Max-Planck-Institut für Molekulare Physiologie, Chemische Biologie, Otto-Hahn-Str.
Design, Synthesis and Phenotypic Profiling of Pyrano‐Furo‐Pyridone Pseudo Natural Products - Waldmann - - Angewandte Chemie International Edition - Wiley Online Library
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Chemical genetics reveals a role of dCTP pyrophosphatase 1 in Wnt signaling
Communication Chemical genetics reveals a role of dCTP pyrophosphatase 1 in Wnt signaling Herbert Waldmann Corresponding Author E-mail address: herbert.waldmann@mpi-dortmund.mpg.de E-mail address: brigitte.rose@mpi-dortmund.mpg.de Max-Planck-Institut für Molekulare Physiologie, Chemische Biologie, Otto-Hahn-Str.
Enantioselective Formal C(sp3)‐H Bond Activation in the Synthesis of Bioactive Spiropyrazolone Derivatives
As a service to our authors and readers, this journal provides supporting information supplied by the authors. Such materials are peer reviewed and may be re‐organized for online delivery, but are not copy‐edited or typeset. Technical support issues arising from supporting information (other than missing files) should be addressed to the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors.
C‐H Bond Activation for the Synthesis of Heterocyclic Atropisomers Yields Hedgehog Pathway Inhibitors
As a service to our authors and readers, this journal provides supporting information supplied by the authors. Such materials are peer reviewed and may be re‐organized for online delivery, but are not copy‐edited or typeset. Technical support issues arising from supporting information (other than missing files) should be addressed to the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors.
C‐H Bond Activation for the Synthesis of Heterocyclic Atropisomers Yields Hedgehog Pathway Inhibitors
As a service to our authors and readers, this journal provides supporting information supplied by the authors. Such materials are peer reviewed and may be re‐organized for online delivery, but are not copy‐edited or typeset. Technical support issues arising from supporting information (other than missing files) should be addressed to the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors.
Ligand‐Directed Divergent Synthesis of Carbo‐ and Heterocyclic Ring Systems
Chemical tools that enable a catalytic reaction to selectively and efficiently yield different products will allow charting of wider chemical space. In ligand‐directed divergent synthesis, a common mode of catalysis is modulated by employing different ligands for catalytic organometallic complexes to transform either common substrates or common reactive intermediates into distinct molecular scaffolds.
Ligand‐Directed Divergent Synthesis of Carbo‐ and Heterocyclic Ring Systems
Chemical tools that enable a catalytic reaction to selectively and efficiently yield different products will allow charting of wider chemical space. In ligand‐directed divergent synthesis, a common mode of catalysis is modulated by employing different ligands for catalytic organometallic complexes to transform either common substrates or common reactive intermediates into distinct molecular scaffolds.
Bioactive Compound Collections: From Design to Target Identification
The research summarized in this review has implications for two of the UN's sustainable development goals (SDGs). The development of new and improved strategies for obtaining bioactive small molecules will have a significant impact on good health and well-being (UN SDG 3). Because the development of a hit compound to a drug typically falls in the remit of a pharmaceutical company, the research also contributes to industry, innovation, and infrastructure (UN SDG 9).
Enantioselective Synthesis of the Spiro-Tropanyl Oxindole Scaffold Through Bimetallic Relay Catalysis
Spiro-tropanyl oxindole alkaloids like alstonisine and chitosenine are endowed with multiple bioactivites. We report the first enantioselective synthesis of the spiro-tropanyl oxindole scaffold by means of a bimetallic relay catalysis strategy.
Ligand-directed Divergent Synthesis of Carbo- and Heterocyclic Ring Systems
Chemical tools that enable a catalytic reaction to selectively and efficiently yield different products will allow charting wider chemical space. In ligand directed divergent synthesis, a common mode of catalysis is modulated by employing different ligands of catalytic organometallic complexes to transform common substrates or common reactive intermediates into distinct molecular scaffolds.
Discovery of a Novel Inhibitor of the Hedgehog Signaling Pathway through Cell-based Compound Discovery and Target Prediction
Cell-based assays enable monitoring of small-molecule bioactivity in a target-agnostic manner and help uncover new biological mechanisms. Subsequent identification and validation of the small-molecule targets, typically employing proteomics techniques, is very challenging and limited, in particular if the targets are membrane proteins.
Small-Molecule Target Engagement in Cells
Approaches that Require Modification of Both the Small Molecule and the Target Protein Approaches that Require Modification of the Small Molecule An approach that Requires Modification of the Protein Thermally induced unfolding of a purified protein can be followed by differential static light scattering or differential scanning fluorometry and often results in a sigmoidal melting curve, which enables the determination of a distinct melting temperature (Tm).
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