Portrait Prof. Dr. Waldmann

Herbert Waldmann

Director, Chemical Biology

News and Press Releases

Chemists climb a new path to ascend cancer’s steepest research challenges
A team of RNA scientists, chemists and cancer biologists from Florida, Dortmund and Münster have found new possibilities for targeting cancer genes’ RNA with nature-inspired compounds more
postrait Waldmann
The European Federation for Medicinal Chemistry and Chemical Biology has awarded Prof. Dr. Dr. h.c. Herbert Waldmann the „Nauta Pharmacochemistry Award in Medicinal Chemistry and Chemical Biology“  more
In search of (un)desired side effects
Morphological fingerprinting could help identify side effects and new bioactive compounds in drug discovery more
Herbert Waldmann was awarded for his outstanding achievements in the entire field of chemistry with the Liebig Medal of the German Chemical Society (GDCh). Here you can watch an interview with the laureate.

Intervierw with the Liebig Medal laureate Prof. Herbert Waldmann

Herbert Waldmann was awarded for his outstanding achievements in the entire field of chemistry with the Liebig Medal of the German Chemical Society (GDCh). Here you can watch an interview with the laureate.

Research Interests

> Department Chemical Biology

We focus on the organic chemistry-biology interface. Grounded in chem- and bioinformatic charting of biologically relevant chemical space we develop novel strategies for the synthesis of natural product (NP)-inspired compound collections and use them for the study of biological phenomena. Natural products and their structural scaffolds represent the biologically relevant and prevalidated regions of chemical structure space explored by nature. In our Biology Oriented Synthesis (BIOS) programme we have synthesized various focused NP-inspired compound collections. We employ a plethora of cell-biological, biochemical and biophysical methods to find modulators of various cellular processes. Cell-based screens are further employed to find the targets of active compounds. We are paying special attention to identifying small molecules that regulate the function and activity of Ras family GTPases.

Selected Publications

PubMed Liste>

Tong Y, Lee Y, Liu X, Childs-Disney JL, Suresh BM, Benhamou RI, Yang C, Li W, Costales MG, Haniff HS, Sievers S, Abegg D, Wegner T, Paulisch TO, Lekah E, Grefe M, Crynen G, Van Meter M, Wang T, Gibaut QMR, Cleveland JL, Adibekian A, Glorius F, Waldmann H, Disney MD (2023). Programming inactive RNA-binding small molecules into bioactive degraders. Nature

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.

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.

Grigalunas M, Burhop A, Zinken S, Pahl A, Gally JM, Wild N, Mantel Y, Sievers S, Foley DJ, Scheel R, Strohmann C, Antonchick AP, Waldmann H (2021). Natural product fragment combination to performance-diverse pseudo-natural products. Nat Commun.

Liu J, Cremosnik GS, Otte F, Pahl A, Sievers S, Strohmann C, Waldmann H (2021). Design, synthesis and biological evaluation of chemically and biologically diverse pyrroquinoline pseudo natural products Angew Chem Int Ed Engl.

Guéret SM, Thavam S, Carbajo RJ, Potowski M, Larsson N, Dahl G, Grossmann T, Plowright AT, Valeur E, Lemruell M and Waldmann H (2020). Macrocyclic Modalities Combining Peptide Epitopes and Natural Product Fragments. J Am Chem Soc.  

Karageorgis G, Foley DJ, Laraia L and Waldmann H (2020). Synthesis of Indomorphan Pseudo Natural Product Inhibitors of Glucose Transporters GLUT-1 and -3. Nat Chem 
doi: 10.1038/s41557-019-0411-x

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.

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

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

Lee YC, Kumar K, Waldmann H (2017). Ligand-directed Divergent Synthesis of Carbo- and Heterocyclic Ring Systems. Angew Chem Int Ed Engl
doi: 10.1002/anie.201710247.

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.

Robke L, Laraia L, Carnero Corrales MA, Konstantinidis G, Muroi M, Richters A, Winzker M, Engbring T, Tomassi S, Watanabe N, Osada H, Rauh D, Waldmann H, Wu Y, Engel J. (2017). Small-Molecule Inhibition of the UNC119-Cargo Interaction. Angew Chem Int Ed Engl
doi: 10.1002/anie.201703738.

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.

Martín-Gago P, Fansa EK, Klein CH, Murarka S, Janning P, Schürmann M, Metz M, Ismail S, Schultz-Fademrecht C, Baumann M, Bastiaens PI, Wittinghofer A, Waldmann H (2017). A PDE6δ-KRas Inhibitor Chemotype with up to Seven H-Bonds and Picomolar Affinity that Prevents Efficient Inhibitor Release by Arl2. Angew Chem Int Ed Engl
doi: 10.1002/anie.201610957.

Xu H, Golz C, Strohmann C, Antonchick AP & Waldmann H (2016). Enantiodivergent Combination of Natural Product Scaffolds Enabled by Catalytic Enantioselective Cycloaddition. Angew Chem Int Ed Engl 55(27):7761-5.
doi: 10.1002/anie.201602084.

Qian Y, Schürmann M, Janning P, Hedberg C & Waldmann H (2016). Activity-Based Proteome Profiling Probes Based on Woodward's Reagent K with Distinct Target Selectivity. Angew Chem Int Ed Engl 55(27):7766-71.
doi: 10.1002/anie.201602666.

Papke B, Murarka S, Vogel HA, Martín-Gago P, Kovacevic M, Truxius DC, Fansa EK, Ismail S, Zimmermann G, Heinelt K, Schultz-Fademrecht C, Al Saabi A, Baumann M, Nussbaumer P, Wittinghofer A, Waldmann H, Bastiaens PI (2016). Identification of pyrazolopyridazinones as PDEδ inhibitors. Nat Commun 7:11360.
doi: 10.1038/ncomms11360.

Ursu A, Illich DJ, Takemoto Y, Porfetye AT, Zhang M, Brockmeyer A, Janning P, Watanabe N, Osada H, Vetter IR, Ziegler S, Schöler HR & Waldmann H (2016). Epiblastin A Induces Reprogramming of Epiblast Stem Cells Into Embryonic Stem Cells by Inhibition of Casein Kinase 1. Cell Chem Biol 23(4):494-507.
doi: 10.1016/j.chembiol.2016.02.015.

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.

Švenda 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.

Vidadala SR, Golz C, Strohmann C, Daniliuc CG & Waldmann H (2015). Highly enantioselective intramolecular 1,3-dipolar cycloaddition: a route to piperidino-pyrrolizidines. Angew Chem Int Ed Engl 54(2):651-655.
doi: 10.1002/anie.201409942.

Eschenbrenner-Lux V, Küchler 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.

Spiegel J, Cromm PM, Itzen A, Goody RS, Grossmann TN & Waldmann H (2014). Direct Targeting of Rab-GTPase–Effector Interactions. Angew Chem Int Ed Engl 53(9):2498-2503.
doi: 10.1002/anie.201308568.

Go to Editor View