Herbert Waldmann

Chemical Biology

Phone:+49 (231) 133-2400



Secretary

Brigitte Rose
Phone: +49 (231) - 133 2401
Fax: +49 (231) - 133 2499

Research Interests

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 frequently in collaboration with Andrey Antonchick and Kamal Kumar. 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 List>



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.


 

 
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