Herbert Waldmann

Chemical Biology

Phone:+49 (231) 133-2400



Secretary

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

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

Pahl A, Waldmann H, Kumar K. (2017). Exploring Natural Product Fragments for Drug and Probe Discovery. Chimia (Aarau)
doi: doi: 10.2533/chimia.2017.653.

Küchler P, Zimmermann G, Winzker M, Janning P, Waldmann H, Ziegler S (2017). Identification of novel PDEδ interacting proteins. Bioorg Med Chem
doi: 10.1016/j.bmc.2017.08.033.

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.

Xu H, Laraia L, Schneider L, Louven K, Strohmann C, Antonchick AP and Waldmann H (2017). Highly Enantioselective Catalytic Vinylogous Propargylation of Coumarins Yields a Novel Autophagy Inhibitor Class. Angew Chem Int Ed Engl
doi: 10.1002/anie.201706005.

Sheremet M, Kapoor S, Schröder P, Kumar K, Ziegler S and Waldmann H (2017). Natural Product Withanolide-Inspired Small molecules as Potent Inhibitors of Wnt Signaling. Chembiochem
doi: 10.1002/cbic.201700260.

Winter RHA, Dwiwedi M, Mejuch T, Waldmann H (2017). The Myristoyl Modification of c-Src Alters the Lateral Organization of Host Heterogenous Raft-like Membranes. Angew Chem Int Ed Engl
doi: 10.1002/anie.201706233.

Laraia L, Waldmann H (2017). Natural product inspired compound collections: evolutionary principle, chemical synthesis, phenotypic screening, and target identification. Drug Discov Today Technol
doi: 10.1016/j.ddtec.2017.03.003.

Plowright AT, Ottmann C, Arkin M, Auberson YP, Timmerman H, Waldmann H.(2017). Small-Molecule Inhibition of the UNC119-Cargo Interaction. Cell Chem Biol
doi: 10.1016/j.chembiol.2017.05.019.

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.

Mejuch T, Garivet G, Hofer W, Kaiser N, Fansa EK, Ehrt C, Koch O, Baumann M, Ziegler S, Wittinghofer A, Waldmann H (2017). Small-Molecule Inhibition of the UNC119-Cargo Interaction. Angew Chem Int Ed Engl
doi: 10.1002/anie.201701905.

Martín-Gago P, Fansa EK, Winzker M, Murarka S, Janning P, Schultz-Fademrecht C, Baumann M, Wittinghofer A, Waldmann H (2017). Covalent Protein Labeling at Glutamic Acids. Cell Chem Biol
doi: 10.1002/cbic.201700015.

Waldmann H, Förster T, Lopéz-Tosco S, Ziegler S, Antonchick AP (2017). Enantioselective Organocatalytic Synthesis of a Secoyohimbane-Inspired Compound Collection with Neuritogenic Activity. Chembiochem
doi: 10.1002/cbic.201700015.

Rubaiy HN, Ludlow MJ, Henrot M, Gaunt HJ, Miteva K, Cheung SY, Tanahashi Y, Hamzah N, Musialowski KE, Blythe NM, Appleby HL, Bailey MA, McKeown L, Taylor R, Foster R, Waldmann H, Nussbaumer P, Christmann M, Bon RS, Muraki K, Beech DJ (2017). Picomolar, selective and subtype specific small-molecule inhibition of TRPC1/4/5 channels. J Biol Chem
doi: 10.1074/jbc.M116.773556.

Mosalaganti S, Keller J, Altenfeld A, Winzker M, Rombaut P, Saur M, Petrovic A, Wehenkel A, Wohlgemuth S, Müller F, Maffini S, Bange T, Herzog F, Waldmann H, Raunser S & Musacchio A (2017). Structure of the RZZ complex and molecular basis of its interaction with Spindly. J Cell Bio 216(4):961-981
doi: 10.1083/jcb.201611060.

Sidarovich A, Will CL, Anokhina MM, Ceballos J, Sievers S, Agafonov DE, Samatov T, Bao P, Kastner B, Urlaub H, Waldmann H, Lührmann R (2017). Identification of a small molecule inhibitor that stalls splicing at an early step of spliceosome activation. Elife
doi: http://dx.doi.org/10.7554/eLife.23533

Waldmann H, Martinez NE, Zimmermann TJ, Goosmann C, Alexander T, Hedberg C, Ziegler S, Zychlinsky A (2017). Tetrahydroisoquinolines are Novel Inhibitors of Neutrophil Extracellular Trap (NET) Formation. Chembiochem
doi: 10.1002/cbic.201600650.

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.

Waldmann H, Valeur E, Guéret SM, Adihou H, Gopalakrishnan R, Lemurell M, Grossmann TN, Plowright AT (2017). New Modalities for Challenging Targets in Drug Discovery. Angew Chem Int Ed Engl
doi: 10.1002/anie.201611914.

Jia ZJ, Merten C, Gontla R, Daniliuc CG, Antonchick AP, Waldmann H (2017). General Enantioselective C-H Activation with Efficiently Tunable Cyclopentadienyl Ligands. Angew Chem Int Ed Engl 56(9):2429-2434
doi: 10.1002/anie.201611981.

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 56(9):2423-2428
doi: 10.1002/anie.201610957.

Laraia L, Ohsawa K, Konstantinidis G, Robke L, Wu YW, Kumar K, Waldmann H (2017). Discovery of Novel Cinchona-Alkaloid-Inspired Oxazatwistane Autophagy Inhibitors. Angew Chem Int Ed Engl 56(8):2145-2150.
doi: 10.1002/anie.201611670.


2016

Martín-Gago P, Fansa EK, Wittinghofer A, Waldmann H (2016). Structure-based development of PDEδ inhibitors. Biol Chem
doi: 10.1515/hsz-2016-0272.

Schröder P, Bauer JO, Strohmann C, Kumar K, Waldmann H (2016). Synthesis of an Iridoid-Inspired Compound Collection and Discovery of Autophagy Inhibitors. J Org Chem 81(21):10242-10255.
doi: 10.1021/acs.joc.6b01185

Murarka S, Martín-Gago P, Schultz-Fademrecht C, Al Saabi A, Baumann M, Fansa EK, Ismail S, Nussbaumer P, Wittinghofer A, Waldmann H (2016). Development of Pyridazinone Chemotypes Targeting the PDEδ Prenyl Binding Site. Chemistry
doi: 10.1002/chem.201603222.

Jaiswal M, Fansa EK, Kösling SK, Mejuch T, Waldmann H, Wittinghofer A (2016). Novel Biochemical and Structural Insights into the Interaction of Myristoylated Cargo with Unc119 Protein and Their Release by Arl2/3. J Biol Chem 291(39):20766-78.
doi: 10.1074/jbc.M116.741827.

Cromm PM, Spiegel J, Küchler P, Dietrich L, Kriegesmann J, Wendt M, Goody RS, Waldmann H, Grossmann TN (2016). Protease-Resistant and Cell-Permeable Double-Stapled Peptides Targeting the Rab8a GTPase. ACS Chem Biol 11(8):2375-82.
doi: 10.1021/acschembio.6b00386.

Mejuch T, Waldmann H (2016). Synthesis of Lipidated Proteins. Bioconjug Chem 27(8):1771-83.
doi: 10.1021/acs.bioconjchem.6b00261.

Kapoor S, Waldmann H, Ziegler S (2016). Novel approaches to map small molecule-target interactions. Bioorg Med Chem 24(15):3232-45.
doi: 10.1016/j.bmc.2016.05.020.

Murarka S, Golz C, Strohmann C, Antonchick AP & Waldmann H (2016). Biology-Oriented Synthesis of 3,3- Spiro (2-tetrahydrofuranyl)- oxindoles. Synthesis 49:87-95.
doi: 10.1055/s-0035-1561665.

Sperlich B, Kapoor S, Waldmann H, Winter R, Weise K (2016). Regulation of K-Ras4B Membrane Binding by Calmodulin. Biophys J 111(1):113-22.
doi: 10.1016/j.bpj.2016.05.042.

Erwin N, Sperlich B, Gavriet G, Waldmann H. Weise K, Winter R. (2016). Lipoprotein Insertion into Membranes of Various Complexity: Lipid Sorting, Interfacial Adsorption and Protein Clustering. Phys. Chem. Chem. Phys. 18:8954-62.
doi: 10.1039/C6CP00563B.

Perez-Galan P, Waldmann H. Weise K, Winter R. (2016). Building polycyclic indole scaffolds via gold(I)-catalyzed intra- and intermolecular cyclization reactions of 1,6-enynes. Tetrahedron special issue 72:3647-52.
doi: 10.1016/j.tet.2016.03.020.

Kötzner L, Leutzsch M, Sievers S, Patil S, Waldmann H, Zheng Y, Thiel W, List (2016). The Organocatalytic Approach to Enantiopure 2H- and 3H-Pyrroles: Inhibitors of the Hedgehog Signaling Pathway. Angew Chem Int Ed Engl 55(27):7693-7.
doi: 10.1002/anie.201602932.

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

Tschapalda K, Zhang YQ, Liu L, Golovnina K, Schlemper T, Eichmann TO, Lal-Nag M, Sreenivasan U, McLenithan J, Ziegler S, Sztalryd C, Lass A, Auld D, Oliver B, Waldmann H, Li Z, Shen M, Boxer MB, Beller M (2016). A Class of Diacylglycerol Acyltransferase 1 Inhibitors Identified by a Combination of Phenotypic High-throughput Screening, Genomics, and Genetics. EBioMedicine 8:49-59.
doi: 10.1016/j.ebiom.2016.04.014.

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.

Schürmann M, Janning P, Ziegler S, Waldmann H (2016). Small-Molecule Target Engagement in Cells. Cell Chem Biol 23(4):435-41.
doi: 10.1016/j.chembiol.2016.03.008.

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.

Illich DJ, Zhang M, Ursu A, Osorno R, Kim KP, Yoon J, Araúzo-Bravo MJ, Wu G, Esch D, Sabour D, Colby D, Grassme KS, Chen J, Greber B, Höing S, Herzog W, Ziegler S, Chambers I, Gao S, Waldmann H, Schöler HR (2016). Distinct Signaling Requirements for the Establishment of ESC Pluripotency in Late-Stage EpiSCs. Cell Rep 15(4):787–800.
doi: 10.1016/j.celrep.2016.03.073.

Cromm PM, Schaubach S, Spiegel J, Fürstner A, Grossmann TN, Waldmann H (2016). Orthogonal ring-closing alkyne and olefin metathesis for the synthesis of small GTPase-targeting bicyclic peptides. Nat Commun 7:11300.
doi: 10.1038/ncomms11300.

Erwin N, Sperlich B, Garivet G, Waldmann H, Weise K, Winter R (2016). Lipoprotein insertion into membranes of various complexity: lipid sorting, interfacial adsorption and protein clustering. Phys Chem Chem Phys 18(13):8954-62.
doi: 10.1039/c6cp00563b.

Sellstedt M, Schwalfenberg M, Ziegler S, Antonchick AP, Waldmann H (2016). Trienamine catalyzed asymmetric synthesis and biological investigation of a cytochalasin B-inspired compound collection. Org Biomol Chem 14(1):50-4.
doi: 10.1039/c5ob02272j.


2015

Pahl A, Lakemeyer M, Vielberg MT, Hackl MW, Vomacka J, Korotkov VS, Stein ML, Fetzer C, Lorenz-Baath K, Richter K, Waldmann H, Groll M, Sieber SA (2015). Reversible Inhibitors Arrest ClpP in a Defined Conformational State that Can Be Revoked by ClpX Association. Angew Chem Int Ed Engl 54(52):15892-6.
doi: 10.1002/anie.201507266.

Cromm PM, Spiegel J, Grossmann TN, Waldmann H (2015). Direct Modulation of Small GTPase Activity and Function. Angew Chem Int Ed Engl 54(46):13516-37.
doi: 10.1002/anie.201504357.

Mejuch T, van Hattum H, Triola G, Jaiswal M, Waldmann H (2015). Specificity of Lipoprotein Chaperones for the Characteristic Lipidated Structural Motifs of their Cognate Lipoproteins. Chembiochem (17):2460-5.
doi: 10.1002/cbic.201500355.

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.

Mei R, Kumar K, Waldmann H (2015). Divergent Gold(I)-Catalyzed Skeletal Rearrangements of 1,7-Enynes. Chemistry 21(39):13526-30.
doi: 10.1002/chem.201502843.

Gilleron J, Paramasivam P, Zeigerer A, Querbes W, Marsico G, Andree C, Seifert S, Amaya P, St ter M, Koteliansky V, Waldmann H, Fitzgerald K, Kalaidzidis Y, Akinc A, Maier MA, Manoharan M, Bickle M, Zerial M (2015). Identification of siRNA delivery enhancers by a chemical library screen. Nucleic Acids Res 43(16):7984-8001.
doi: 10.1093/nar/gkv762.

Ursu A, Waldmann H (2015). Hide and seek: Identification and confirmation of small molecule protein targets. Bioorg Med Chem Lett 25(16):3079-86.
doi: 10.1016/j.bmcl.2015.06.023.

Vendrell-Navarro G, R a F, Bujons J, Brockmeyer A, Janning P, Ziegler S, Messeguer A, Waldmann H (2015). Positional Scanning Synthesis of a Peptoid Library Yields New Inducers of Apoptosis that Target Karyopherins and Tubulin. Chembiochem 16(11):1580-7.
doi: 10.1002/cbic.201500169.

Hackl MW, Lakemeyer M, Dahmen M, Glaser M, Pahl A, Lorenz-Baath K, Menzel T, Sievers S, B ttcher T, Antes I, Waldmann H, Sieber SA (2015). Phenyl Esters Are Potent Inhibitors of Caseinolytic Protease P and Reveal a Stereogenic Switch for Deoligomerization. J Am Chem Soc 137(26):8475-83.
doi: 10.1021/jacs.5b03084.

Murarka S, Jia ZJ, Merten C, Daniliuc CG, Antonchick AP, Waldmann H (2015). Rhodium(II)-catalyzed enantioselective synthesis of troponoids. Angew Chem Int Ed Engl 54(26):7653-6.
doi: 10.1002/anie.201502233.

Potowski M, Golz C, Strohmann C, Antonchick AP, Waldmann H (2015). Biology-oriented synthesis of benzopyrano[3,4-c]pyrrolidines. Bioorg Med Chem 23(12):2895-903.
doi: 10.1016/j.bmc.2015.02.044.

Sankar MG, Mantilli L, Bull J, Giordanetto F, Bauer JO, Strohmann C, Waldmann H, Kumar K (2015). Stereoselective synthesis of a natural product inspired tetrahydroindolo[2,3-a]-quinolizine compound library. Bioorg Med Chem 23(11):2614-20.
doi: 10.1016/j.bmc.2015.01.019.

Berg V, Rusch M, Vartak N, J ngst C, Schauss A, Waldmann H, Hedberg C, Pallasch CP, Bastiaens PI, Hallek M, Wendtner CM, Frenzel LP (2015). miRs-138 and -424 control palmitoylation-dependent CD95-mediated cell death by targeting acyl protein thioesterases 1 and 2 in CLL. Blood 125(19):2948-57.
doi: 10.1182/blood-2014-07-586511.

Venda 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.

Danda A, Kumar K, Waldmann H (2015). A general catalytic reaction sequence to access alkaloid-inspired indole polycycles. Chem Commun (Camb) 51(35):7536-9.
doi: 10.1039/c5cc01555c.

Arndt HD, Rizzo S, N cker C, Wakchaure VN, Milroy LG, Bieker V, Calderon A, Tran TT, Brand S, Dehmelt L, Waldmann H (2015). Divergent solid-phase synthesis of natural product-inspired bipartite cyclodepsipeptides: total synthesis of seragamide A. Chemistry 21(14):5311-6.
doi: 10.1002/chem.201500368.

Potowski M, Merten C, Antonchick AP, Waldmann H (2015). Catalytic aerobic oxidation and tandem enantioselective cycloaddition in cascade multicomponent synthesis. Chemistry 21(13):4913-7.
doi: 10.1002/chem.201500125.

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.

Jia ZJ, Daniliuc CG, Antonchick AP, Waldmann H (2015). Phosphine-catalyzed dearomatizing [3+2] annulations of isoquinolinium methylides with allenes. Chem Commun (Camb) 51(6):1054-7.
doi: 10.1039/c4cc08555h.

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.

Vendrell-Navarro G, Brockmeyer A, Waldmann H, Janning P, Ziegler S (2015). Identification of the targets of biologically active small molecules using quantitative proteomics. Methods Mol Biol 1263:263-86.
doi: 10.1007/978-1-4939-2269-7_21.


2014

Klaus C, Schneider U, Hedberg C, Schütz AK, Bernhagen J, Waldmann H, Gassler N, Kaemmerer E (2014). Modulating effects of acyl-CoA synthetase 5-derived mitochondrial Wnt2B palmitoylation on intestinal Wnt activity. World J Gastroenterol 20(40):14855-64.
doi: 10.3748/wjg.v20.i40.14855.

Eschenbrenner-Lux V, Kumar K, Waldmann H (2014). The asymmetric hetero-Diels-Alder reaction in the syntheses of biologically relevant compounds. Angew Chem Int Ed Engl 53(42):11146-57.
doi: 10.1002/anie.201404094

van Hattum H, Waldmann H (2014). Chemical biology tools for regulating RAS signaling complexity in space and time. Chem Biol 21(9):1185-95.
doi: 10.1016/j.chembiol.2014.08.001.

Tran TT, Gerding-Reimers C, Schölermann B, Stanitzki B, Henkel T, Waldmann H, Ziegler S (2014). Podoverine A--a novel microtubule destabilizing natural product from the Podophyllum species. Bioorg Med Chem 22(18):5110-6.
doi: 10.1016/j.bmc.2014.01.039.

van Hattum H, Waldmann H (2014). Biology-oriented synthesis: harnessing the power of evolution. J Am Chem Soc 136(34):11853-9.
doi: 10.1021/ja505861d.

Basu S, Waldmann H (2014). Polymer supported synthesis of a natural product-inspired oxepane library. Bioorg Med Chem 22(16):4430-44.
10.1016/j.bmc.2014.05.039.

Spiegel J, Cromm PM, Zimmermann G, Grossmann TN, Waldmann H (2014). Small-molecule modulation of Ras signaling. Nat Chem Biol 10(8):613-22.
doi: 10.1038/nchembio.1560.

Kolundžić F, Murali A, Pérez-Galán P, Bauer JO, Strohmann C, Kumar K, Waldmann H (2014). A cyclization-rearrangement cascade for the synthesis of structurally complex chiral gold(I)-aminocarbene complexes. Angew Chem Int Ed Engl 53(31):8122-6.
doi: 10.1002/anie.201403651.

Vogel A, Nikolaus J, Weise K, Triola G, Waldmann H, Winter R, Herrmann A, Huster D (2014). Interaction of the human N-Ras protein with lipid raft model membranes of varying degrees of complexity. Biol Chem 395(7-8):779-89.
doi: 10.1515/hsz-2013-0294.

Lukinavičius G, Reymond L, D'Este E, Masharina A, Göttfert F, Ta H, Güther A, Fournier M, Rizzo S, Waldmann H, Blaukopf C, Sommer C, Gerlich DW, Arndt HD, Hell SW, Johnsson K (2014). Fluorogenic probes for live-cell imaging of the cytoskeleton. Nat Methods 11(7):731-3.
doi: 10.1038/nmeth.2972.

Zimmermann G, Schultz-Fademrecht C, Küchler P, Murarka S, Ismail S, Triola G, Nussbaumer P, Wittinghofer A, Waldmann H (2014). Structure guided design and kinetic analysis of highly potent benzimidazole inhibitors targeting the PDEδ prenyl binding site. J Med Chem 57(12):5435-48.
doi: 10.1021/jm500632s.

Rizzo S, Waldmann H (2014). Development of a natural-product-derived chemical toolbox for modulation of protein function. Chem Rev 114(9):4621-39.
doi: 10.1021/cr400442v.

Narayan R, Potowski M, Jia ZJ, Antonchick AP, Waldmann H (2014). Catalytic enantioselective 1,3-dipolar cycloadditions of azomethine ylides for biology-oriented synthesis. Acc Chem Res.47(4):1296-310.
doi: 10.1021/ar400286b.

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.

Eschenbrenner-Lux V, K chler 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.

Vartak N, Papke B, Grecco HE, Rossmannek L, Waldmann H, Hedberg C, Bastiaens PI (2014). The autodepalmitoylating activity of APT maintains the spatial organization of palmitoylated membrane proteins. Biophys J 106(1):93-105.
doi: 10.1016/j.bpj.2013.11.024.

Bruss H, Schuster H, Martinez R, Kaiser M, Antonchick AP, Waldmann H (2014). Synthesis of the B-seco limonoid core scaffold. Beilstein J Org Chem 10:194-208.
doi: 10.3762/bjoc.10.15.


2013

Narayan R, Bauer JO, Strohmann C, Antonchick AP, Waldmann H (2013). Catalytic enantioselective synthesis of functionalized tropanes reveals novel inhibitors of hedgehog signaling. Angew Chem Int Ed Engl 52(49):12892-6.
doi: 10.1002/anie.201307392.

Takayama H, Jia ZJ, Kremer L, Bauer JO, Strohmann C, Ziegler S, Antonchick AP, Waldmann H (2013). 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(47):12404-8.
doi: 10.1002/anie.201306948.

Werkmüller A, Triola G, Waldmann H, Winter R (2013). Rotational and translational dynamics of ras proteins upon binding to model membrane systems. Chemphyschem 14(16):3698-705.
doi: 10.1002/cphc.201300617.

Potowski M, Antonchick AP, Waldmann H (2013). Catalytic asymmetric exo-selective [6+3] cycloaddition of iminoesters with fulvenes. Chem Commun (Camb) 49(71):7800-2.
doi: 10.1039/c3cc43824d.

Dakas P-Y, Parga JA, Höing S, Schöler HR, Sterneckert J, Kumar K & Waldmann H (2013). Discovery of Neuritogenic Compound Classes Inspired by Natural Products. Angew Chem Int Ed 52:9576 –95813.
doi: 10.1002/anie.201302045

Zimmermann G, Papke B, Ismail S, Vartak N, Chandra A, Hoffmann M, Hahn SA, Triola G, Wittinghofer A, Bastiaens PI, Waldmann H (2013). Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling. Nature 497(7451):638-42.
doi: 10.1038/nature12205.

Kapoor S, Werkmüller A, Goody RS, Waldmann H, Winter R (2013). Pressure modulation of Ras-membrane interactions and intervesicle transfer. J Am Chem Soc 135(16):6149-56.
doi: 10.1021/ja312671j.

Antonchick AP, López-Tosco S, Parga J, Sievers S, Schürmann M, Preut H, Höing S, Schöler HR, Sterneckert J, Rauh D, Waldmann H (2013). Highly enantioselective catalytic synthesis of neurite growth-promoting secoyohimbanes. Chem Biol 20(4):500-9.
doi: 10.1016/j.chembiol.2013.03.011.

Ziegler S, Pries V, Hedberg C, Waldmann H (2013). Target identification for small bioactive molecules: finding the needle in the haystack. Angew Chem Int Ed Engl 52(10):2744-92.
doi: 10.1002/anie.201208749.

Gersch M, Gut F, Korotkov VS, Lehmann J, Böttcher T, Rusch M, Hedberg C, Waldmann H, Klebe G, Sieber SA (2013). The mechanism of caseinolytic protease (ClpP) inhibition. Angew Chem Int Ed Engl 52(10):3009-14.
doi: 10.1002/anie.201204690.

Zimmermann TJ, Roy S, Martinez NE, Ziegler S, Hedberg C, Waldmann H (2013). Biology-oriented synthesis of a tetrahydroisoquinoline-based compound collection targeting microtubule polymerization. Chembiochem 14(3):295-300.
doi: 10.1002/cbic.201200711.

Eschenbrenner-Lux V, Dückert H, Khedkar V, Bruss H, Waldmann H, Kumar K (2013). Cascade syntheses routes to the centrocountins. Chemistry 19(7):2294-304.
doi: 10.1002/chem.201203714.

Voigt T, Gerding-Reimers C, Ngoc Tran TT, Bergmann S, Lachance H, Schölermann B, Brockmeyer A, Janning P, Ziegler S, Waldmann H (2013). A natural product inspired tetrahydropyran collection yields mitosis modulators that synergistically target CSE1L and tubulin. Angew Chem Int Ed Engl 52(1):410-4.
doi: 10.1002/anie.20120572.

Zimmermann TJ, Bürger M, Tashiro E, Kondoh Y, Martinez NE, Görmer K, Rosin-Steiner S, Shimizu T, Ozaki S, Mikoshiba K, Watanabe N, Hall D, Vetter IR, Osada H, Hedberg C, Waldmann H (2013). Boron-based inhibitors of acyl protein thioesterases 1 and 2. Chembiochem 14(1):115-22.
doi: 10.1002/cbic.201200571.

Weise K, Huster D, Kapoor S, Triola G, Waldmann H, Winter R (2013). Gibbs energy determinants of lipoprotein insertion into lipid membranes: the case study of Ras proteins. Faraday Discuss 161:549-61.
doi: 10.1039/C2FD20100C.

Over B, Wetzel S, Grütter C, Nakai Y, Renner S, Rauh D, Waldmann H (2013). Natural-product-derived fragments for fragment-based ligand discovery. Nat Chem 5(1):21-8.
doi: 10.1038/nchem.1506.

Köhnke M, Delon C, Hastie ML, Nguyen UT, Wu YW, Waldmann H, Goody RS, Gorman JJ, Alexandrov K (2013). Rab GTPase prenylation hierarchy and its potential role in choroideremia disease. PLoS One 8(12):e81758.
doi: 10.1371/journal.pone.0081758.


2012

Willmann D, Lim S, Wetzel S, Metzger E, Jandausch A, Wilk W, Jung M, Forne I, Imhof A, Janzer A, Kirfel J, Waldmann H, Schüle R, Buettner R (2012). Impairment of prostate cancer cell growth by a selective and reversible lysine-specific demethylase 1 inhibitor. Int J Cancer 131(11):2704-9.
doi: 10.1002/ijc.27555.

Matcha K, Madduri AV, Roy S, Ziegler S, Waldmann H, Hirsch AK, Minnaard AJ (2012). Total synthesis of (-)-doliculide, structure-activity relationship studies and its binding to F-actin. Chembiochem 13(17):2537-48.
doi: 10.1002/cbic.201200512.

Yi L, Chen YX, Lin PC, Schröder H, Niemeyer CM, Wu YW, Goody RS, Triola G, Waldmann H (2012). Direct immobilization of oxyamine-modified proteins from cell lysates. Chem Commun (Camb) 48(88):10829-31.
doi: 10.1039/c2cc35237k.

Sos ML, Dietlein F, Peifer M, Schöttle J, Balke-Want H, Müller C, Koker M, Richters A, Heynck S, Malchers F, Heuckmann JM, Seidel D, Eyers PA, Ullrich RT, Antonchick AP, Vintonyak VV, Schneider PM, Ninomiya T, Waldmann H, Büttner R, Rauh D, Heukamp LC, Thomas RK (2012). A framework for identification of actionable cancer genome dependencies in small cell lung cancer. Proc Natl Acad Sci U S A 109(42):17034-9.
doi: 10.1073/pnas.1207310109.

Stigter EA, Guo Z, Bon RS, Wu YW, Choidas A, Wolf A, Menninger S, Waldmann H, Blankenfeldt W, Goody RS (2012). Development of selective, potent RabGGTase inhibitors. J Med Chem 55(19):8330-40.
doi: 10.1021/jm300624s.

Güldenhaupt J, Rudack T, Bachler P, Mann D, Triola G, Waldmann H, Kötting C, Gerwert K (2012). N-Ras forms dimers at POPC membranes. Biophys J 103(7):1585-93.
doi: 10.1002/anie.201204394.

Kapoor S, Weise K, Erlkamp M, Triola G, Waldmann H, Winter R (2012). The role of G-domain orientation and nucleotide state on the Ras isoform-specific membrane interaction. Eur Biophys J 41(10):801-13.
doi: 10.1007/s00249-012-0841-5.

Potowski M, Bauer JO, Strohmann C, Antonchick AP, Waldmann H (2012). Highly enantioselective catalytic [6+3] cycloadditions of azomethine ylides. Angew Chem Int Ed Engl 51(38):9512-6.
doi: 10.1002/anie.201204394.

Tnimov Z, Guo Z, Gambin Y, Nguyen UT, Wu YW, Abankwa D, Stigter A, Collins BM, Waldmann H, Goody RS, Alexandrov K (2012). Quantitative analysis of prenylated RhoA interaction with its chaperone, RhoGDI. J Biol Chem 287(32):26549-62.
doi: 10.1074/jbc.M112.371294.

Weise K, Kapoor S, Werkmüller A, Möbitz S, Zimmermann G, Triola G, Waldmann H, Winter R (2012). Dissociation of the K-Ras4B/PDEδ complex upon contact with lipid membranes: membrane delivery instead of extraction. J Am Chem Soc 134(28):11503-10.
doi: 10.1021/ja305518h.

Lachance H, Wetzel S, Kumar K, Waldmann H (2012). Charting, navigating, and populating natural product chemical space for drug discovery. J Med Chem 55(13):5989-6001.
doi: 10.1021/jm300288g.

Tóth R, Gerding-Reimers C, Deeks MJ, Menninger S, Gallegos RM, Tonaco IA, Hübel K, Hussey PJ, Waldmann H, Coupland G (2012). Prieurianin/endosidin 1 is an actin-stabilizing small molecule identified from a chemical genetic screen for circadian clock effectors in Arabidopsis thaliana. Plant J 71(2):338-52.
doi: 10.1111/j.1365-313X.2012.04991.x.

Waldmann H (2012). Drug discovery … the third in the band! Angew Chem Int Ed Engl 51(26):6284-5.
doi: 10.1002/anie.201201102.

Milroy LG, Rizzo S, Calderon A, Ellinger B, Erdmann S, Mondry J, Verveer P, Bastiaens P, Waldmann H, Dehmelt L, Arndt HD (2012). Selective chemical imaging of static actin in live cells. J Am Chem Soc 134(20):8480-6.
doi: 10.1021/ja211708z.

Stewart JD, Marchan R, Lesjak MS, Lambert J, Hergenroeder R, Ellis JK, Lau CH, Keun HC, Schmitz G, Schiller J, Eibisch M, Hedberg C, Waldmann H, Lausch E, Tanner B, Sehouli J, Sagemueller J, Staude H, Steiner E, Hengstler JG (2012). Choline-releasing glycerophosphodiesterase EDI3 drives tumor cell migration and metastasis. Proc Natl Acad Sci U S A 109(21):8155-60.
doi: 10.1073/pnas.1117654109.

Richter A, Rose R, Hedberg C, Waldmann H, Ottmann C (2012). An optimised small-molecule stabiliser of the 14-3-3-PMA2 protein-protein interaction. Chemistry 18(21):6520-7.
doi: 10.1002/chem.201103761.

Görmer K, Bürger M, Kruijtzer JA, Vetter I, Vartak N, Brunsveld L, Bastiaens PI, Liskamp RM, Triola G, Waldmann H (2012). Chemical-biological exploration of the limits of the Ras de- and repalmitoylating machinery. Chembiochem 13(7):1017-23.
doi: 10.1002/cbic.201200078.

Deraeve C, Guo Z, Bon RS, Blankenfeldt W, DiLucrezia R, Wolf A, Menninger S, Stigter EA, Wetzel S, Choidas A, Alexandrov K, Waldmann H, Goody RS, Wu YW (2012). Psoromic acid is a selective and covalent Rab-prenylation inhibitor targeting autoinhibited RabGGTase. J Am Chem Soc 134(17):7384-91.
doi: 10.1021/ja211305j.

Das D, Tnimov Z, Nguyen UT, Thimmaiah G, Lo H, Abankwa D, Wu Y, Goody RS, Waldmann H, Alexandrov K (2012). Flexible and general synthesis of functionalized phosphoisoprenoids for the study of prenylation in vivo and in vitro. Chembiochem 13(5):674-83.
doi: 10.1002/cbic.201100733.

Samatov TR, Wolf A, Odenwälder P, Bessonov S, Deraeve C, Bon RS, Waldmann H, Lührmann R (2012). 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(5):640-4.
doi: 10.1002/cbic.201100790.

Potowski M, Schürmann M, Preut H, Antonchick AP, Waldmann H (2012). Programmable enantioselective one-pot synthesis of molecules with eight stereocenters. Nat Chem Biol 8(5):428-30.
doi: 10.1038/nchembio.901.

Xu J, Hedberg C, Dekker FJ, Li Q, Haigis KM, Hwang E, Waldmann H, Shannon K (2012). Inhibiting the palmitoylation/depalmitoylation cycle selectively reduces the growth of hematopoietic cells expressing oncogenic Nras. Blood 119(4):1032-5.
doi: 10.1182/blood-2011-06-358960.

Triola G, Waldmann H, Hedberg C (2012). Chemical biology of lipidated proteins. ACS Chem Biol 7(1):87-99.
doi: 10.1021/cb200460u.

Kapoor S, Triola G, Vetter IR, Erlkamp M, Waldmann H, Winter R (2012). Revealing conformational substates of lipidated N-Ras protein by pressure modulation. Proc Natl Acad Sci U S A 109(2):460-5.
doi: 10.1073/pnas.1110553109.

Bürger M, Zimmermann TJ, Kondoh Y, Stege P, Watanabe N, Osada H, Waldmann H, Vetter IR (2012). Crystal structure of the predicted phospholipase LYPLAL1 reveals unexpected functional plasticity despite close relationship to acyl protein thioesterases. J Lipid Res 53(1):43-50.
doi: 10.1194/jlr.M019851.


2011

Dückert H, Pries V, Khedkar V, Menninger S, Bruss H, Bird AW, Maliga Z, Brockmeyer A, Janning P, Hyman A, Grimme S, Schürmann M, Preut H, Hübel K, Ziegler S, Kumar K, Waldmann H (2011). Natural product-inspired cascade synthesis yields modulators of centrosome integrity. Nat Chem Biol 8(2):179-84.
doi: 10.1038/nchembio.758.

Wetzel S, Bon RS, Kumar K, Waldmann H (2011). Biology-oriented synthesis. Angew Chem Int Ed Engl 50(46):10800-26.
doi: 10.1002/anie.201007004.

Ismail SA, Chen YX, Rusinova A, Chandra A, Bierbaum M, Gremer L, Triola G, Waldmann H, Bastiaens PI, Wittinghofer A (2011). Arl2-GTP and Arl3-GTP regulate a GDI-like transport system for farnesylated cargo. Nat Chem Biol 7(12):942-9.
doi: 10.1038/nchembio.686.

Rusch M, Zimmermann TJ, Bürger M, Dekker FJ, Görmer K, Triola G, Brockmeyer A, Janning P, Böttcher T, Sieber SA, Vetter IR, Hedberg C, Waldmann H (2011). Identification of acyl protein thioesterases 1 and 2 as the cellular targets of the Ras-signaling modulators palmostatin B and M. Angew Chem Int Ed Engl 50(42):9838-42.
doi: 10.1002/anie.201102967.

Hedberg C, Dekker FJ, Rusch M, Renner S, Wetzel S, Vartak N, Gerding-Reimers C, Bon RS, Bastiaens PI, Waldmann H (2011). Development of highly potent inhibitors of the Ras-targeting human acyl protein thioesterases based on substrate similarity design. Angew Chem Int Ed Engl 50(42):9832-7.
doi: 10.1002/anie.201102965.

Eberhardt L, Kumar K, Waldmann H (2011). Exploring and exploiting biologically relevant chemical space. Curr Drug Targets 12(11):1531-46.
doi: 10.2174/138945011798109482.

Eisenberg S, Beckett AJ, Prior IA, Dekker FJ, Hedberg C, Waldmann H, Ehrlich M, Henis YI (2011). Raft protein clustering alters N-Ras membrane interactions and activation pattern. Mol Cell Biol 31(19):3938-52.
doi: 10.1128/MCB.05570-11.

Chen YX, Triola G, Waldmann H (2011). Bioorthogonal chemistry for site-specific labeling and surface immobilization of proteins. Acc Chem Res 44(9):762-73.
doi: 10.1021/ar200046h.

Wittstein K, Kumar K, Waldmann H (2011). Gold(I)-catalyzed synthesis of benzoxocines by an 8-endo-dig cyclization. Angew Chem Int Ed Engl 50(39):9076-80.
doi: 10.1002/anie.201103832.

Wagner BK, Gilbert TJ, Hanai J, Imamura S, Bodycombe NE, Bon RS, Waldmann H, Clemons PA, Sukhatme VP, Mootha VK (2011). A small-molecule screening strategy to identify suppressors of statin myopathy. ACS Chem Biol;6(9):900-4.
doi: 10.1021/cb200206w.

S ckigt J, Antonchick AP, Wu F, Waldmann H (2011). The Pictet-Spengler reaction in nature and in organic chemistry. Angew Chem Int Ed Engl 50(37):8538-64.
doi: 10.1002/anie.201008071.

Yi L, Sun H, Itzen A, Triola G, Waldmann H, Goody RS, Wu YW (2011). One-pot dual-labeling of a protein by two chemoselective reactions. Angew Chem Int Ed Engl 50(36):8287-90.
doi: 10.1002/anie.201100840.

Richter A, Hedberg C, Waldmann H (2011). Enantioselective synthesis of the C10-C20 fragment of fusicoccin A. J Org Chem 76(16):6694-702.
doi: 10.1021/jo201020v.

Schuster H, Martinez R, Bruss H, Antonchick AP, Kaiser M, Sch rmann M, Waldmann H (2011). Synthesis of the B-seco limonoid scaffold. Chem Commun (Camb) 47(23):6545-7.
doi: 10.1039/c1cc11388g.

He YP, Tan H, Arve L, Baumann S, Waldmann H, Arndt HD (2011). Biphenomycin B and derivatives: total synthesis and translation inhibition. Chem Asian J 6(6):1546-56.
doi: 10.1002/asia.201000908.

Bon RS, Guo Z, Stigter EA, Wetzel S, Menninger S, Wolf A, Choidas A, Alexandrov K, Blankenfeldt W, Goody RS, Waldmann H (2011). Structure-guided development of selective RabGGTase inhibitors. Angew Chem Int Ed Engl 50(21):4957-61.
doi: 10.1002/anie.201101210.

Hakki T, H bel K, Waldmann H, Bernhardt R (2011). The development of a whole-cell based medium throughput screening system for the discovery of human aldosterone synthase (CYP11B2) inhibitors: old drugs disclose new applications for the therapy of congestive heart failure, myocardial fibrosis and hypertension. J Steroid Biochem Mol Biol 125(1-2):120-8.
doi: 10.1016/j.jsbmb.2010.12.011.

Dueckert H, Khedkar V, Waldmann H, Kumar K (2011). Lewis base catalyzed [4+2] annulation of electron-deficient chromone-derived heterodienes and acetylenes. Chemistry 17(18):5130-7.
doi: 10.1002/chem.201003572.

Basu S, Ellinger B, Rizzo S, Deraeve C, Schuermann M, Preut H, Arndt HD, Waldmann H (2011). Biology-oriented synthesis of a natural-product inspired oxepane collection yields a small-molecule activator of the Wnt-pathway. Proc Natl Acad Sci U S A 108(17):6805-10.
doi: 10.1073/pnas.1015269108.

Radtke L, Willot M, Sun H, Ziegler S, Sauerland S, Strohmann C, Fr hlich R, Habenberger P, Waldmann H, Christmann M (2011). Total synthesis and biological evaluation of (-)-englerin A and B: synthesis of analogues with improved activity profile. Angew Chem Int Ed Engl 50(17):3998-4002.
doi: 10.1002/anie.201007790.

M cklinghoff S, van Otterlo WA, Rose R, Fuchs S, Zimmermann TJ, Dominguez Seoane M, Waldmann H, Ottmann C, Brunsveld L (2011). Design and evaluation of fragment-like estrogen receptor tetrahydroisoquinoline ligands from a scaffold-detection approach. J Med Chem 54(7):2005-11.
doi: 10.1021/jm1011116.

Vintonyak VV, Waldmann H, Rauh D (2011). Using small molecules to target protein phosphatases. Bioorg Med Chem 19(7):2145-55.
doi: 10.1016/j.bmc.2011.02.047.

Weise K, Kapoor S, Denter C, Nikolaus J, Opitz N, Koch S, Triola G, Herrmann A, Waldmann H, Winter R (2011). Membrane-mediated induction and sorting of K-Ras microdomain signaling platforms. J Am Chem Soc 133(4):880-7.
doi: 10.1021/ja107532q.

Hakkim A, Fuchs TA, Martinez NE, Hess S, Prinz H, Zychlinsky A, Waldmann H (2011). Activation of the Raf-MEK-ERK pathway is required for neutrophil extracellular trap formation. Nat Chem Biol 7(2):75-7.
doi: 10.1038/nchembio.496.

Waldmann H (2011). Herbert Waldmann. Angew Chem Int Ed Engl 50(2):346-8.
doi: 10.1002/anie.201005413.


 
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