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Publications

Original Publications:


Burkhart JL, Müller R, Kazmaier U. Syntheses and Evaluation of Simplified Pretubulysin Analogues. Eur. J. Org. Chem. 2011, 3050–3059.

Geppert T, Reisen F, Pillong M, Hähnke V, Tanrikulu Y, Koch CP, Perna AM, Perez TB, Schneider P, Schneider G. Virtual screening for compounds that mimic protein-protein interface epitopes. J. Comput. Chem. 2012, 33, 573−579.

Chai Y, Shan S, Weissman KJ, Hu S, Zhang Y, Müller R. Heterologous expression and genetic engineering of the tubulysin biosynthetic gene cluster using Red/ET recombineering and inactivation mutagenesis. Chemistry & Biology, 2012, 19 (3), 361−371.

Burkhart JL, Kazmaier U. A Click Approach towards Tubulysin-Analogues and Tubulysin-Dolastatin Chimera. RSC Advances 2012, 3785–3790.

Herrmann J, Wiedmann RM, Elnakady YA, Ullrich A, Rohde M, Kazmaier U, Vollmar AM, Müller R. Pretubulysins: from a hypothetical biosynthetic intermediate to potential lead in tumor therapy. PLoS One, 2012, 7, e37416, 1–12.

Eirich J, Burkhart JL, Ullrich A, Vollmar AM, Zahler S, Kazmaier U, Sieber SA. Pretubulysin derived probes as novel tools for monitoring the microtubule network via activity-based protein profiling and fluorescence microscopy. Mol. BioSyst. 2012, 8, 2067–2075.

Rath S, Liebl J, Fürst R, Ullrich A, Burkhart JL, Kazmaier U, Herrmann J, Müller R, Günther, M, Schreiner L, Wagner E, Vollmar AM, Zahler S. Anti-angiogenic effects of the tubulysin precursor pretubulysin and of simplified pretubulysin derivatives. Brit. J. Pharmacol. 2012, 167, 1048–1061.

Okanya PW, Mohr KI, Gerth K, Steinmetz H, Huch V, Jansen R , Müller R. Hyaladione, an S-methyl cyclohexadiene-dione from Hyalangium minutum. J. Nat. Prod.2012, 75, 768−770.

Hüttel S, Müller R. Methods to optimize myxobacterial fermentations using off-gas analysis. Microbial Cell Factories 2012, 11 (1), 59.

Wiedmann RM, von Schwarzenberg K, Palamidessi A, Schreiner L, Kubisch R, Liebl J, Schempp C, Trauner D, Vereb G, Zahler S, Wagner E, Müller R, Scita G, Vollmar AM. The V-ATPase-inhibitor archazolid abrogates tumor metastasis via inhibition of endocytic activation of the Rho-GTPase Rac1. Cancer Res. 2012, 72 (22), 5976−87.

Becker D, Kazmaier U. The Ireland-Claisen rearrangement as a key step in the synthesis of tubuphenylalanines. J. Org. Chem. 2013, 78, 59−65.

Herrmann J, Hüttel S, Müller R. Discovery and Biological Activity of New Chondramides from Chondromyces sp. ChemBioChem 2013, 14(13), 1573−80

Zeino M, Zhao Q, Eichhorn T, Herrmann J, Müller R, Efferth T. Molecular docking studies of myxobacterialdisorazoles and tubulysins to tubulin, J. Biosci. Med. 2013, 3 (1), 37−44

Von Schwarzenberg K, Wiedmann RM, Oak P, Schulz S, Zischka H, Wanner G, Efferth T, Trauner D, Vollmar AM. Mode of cell death induction by pharmacological vacuolar H+-ATPase (V-ATPase) inhibition. J. Biol. Chem. 2013, 288(2), 1385−96.

Von Schwarzenberg K, Lajtos T, Vereb G, Simon L, Müller R, Vollmar AM. V-ATPase inhibition overcomes trastuzumab resistance in breast cancer. Mol Oncol. 2014, 8(1), 9-19.

Kubisch R, Fröhlich T, Arnold GJ, Schreiner L, von Schwarzenberg K, Roidl A, Vollmar AM, Wagner E. ATPase inhibition by archazolid leads to lysosomal dysfunction resulting in impaired cathepsin B activation in vivo. Int J Cancer. 2014, 134(10), 2478-88.

Rath S, Liebl J, Fürst R, Vollmar AM, Zahler S. Regulation of endothelial cell migration by v-ATPase. Angiogenesis. 2014, 17(3), 587-601.

Kretzschmann VK, Gellrich D, Ullrich A, Zahler S, Vollmar AM, Kazmaier U, Fürst R. Novel tubulin antagonist pretubulysin displays antivascular properties in vitro and in vivo. Arterioscler Thromb Vasc Biol. 2014, 34(2), 294-303.

Braig S, Wiedmann R, Liebl H, Kubisch R, Schreiner L, Abhari BA, Wagner E, Kazmaier U, Fulda S, Vollmar AM. Pretubulysin: a new option for the treatment of metastatic cancer. Cell Death Dis. 2014, 16, 5:e1001.

Kubisch R, von Gamm M, Braig S, Ullrich A, Burkhart JL, Colling L, Scherer O, Hermann J, Müller R, Werz O, Kazmaier U, Vollmar AM. Simplified pretubulysin-derivatives and their biological effects on cancer cells. J Nat Prod. 2014, 77(3), 536-42.

Schempp CM, von Schwarzenberg K, Schreiner L , Kubisch R, Müller R, Wagner E, Vollmar AM. V-ATPase inhibition regulates anoikis resistance and metastasis of cancer cells. Mol Cancer Ther. 2014, 13(4), 926-37.

Förster F, Braig S, Moser C, Kubisch R, Busse J, Wagner E, Schmöckel E, Mayr D, Schmitt S, Zischka H, Huettel S, Müller R, Vollmar AM. Targeting the actin cytoskeleton: selective anti-tumor action via trapping PKCε. Cell Death Dis. 2014, 28, 5:e1398.

Menhofer M, Bartel D, Kubisch R, Busse J, Wagner E, Müller R, Vollmar AM, Zahler S. In vitro and in vivo characterization of the actin polymerizing compound Chondramide as angiogenic inhibitor. Cardiovasc Res. 2014, 104(2), 303-14.

Menhofer M, Kubisch R, Schreiner L, Zorn M, Förster F, Müller R, Rädler JO, Wagner E, Vollmar AM, Zahler S. The actin targeting compound Chondramide inhibits breast cancer metastasis via reduction of cellular contractility. PLoS One. 2014, 9(11), e112542.  

Reker D, Perna AM, Rodrigues T, Schneider P, Reutlinger M, Mönch B, Koeberle A, Lamers C, Gabler M, Steinmetz H, Müller R, Schubert-Zsilavecz M, Werz O, Schneider G. Revealing the macromolecular targets of complex natural products. Nat Chem. 2014, 6(12), 1072-8. 

Scherer O, Steinmetz H, Kaether C, Weinigel C, Barz D, Kleinert H, Menche D, Müller R, Pergola C, Werz O. Targeting V-ATPase in primary human monocytes by archazolid potently represses the classical secretion of cytokines due to accumulation at the endoplasmic reticulum. Biochem Pharmacol. 2014, 91(4), 490-500. 

Hamm R, Chen YR, Seo EJ, Zeino M, Wu CF, Müller R, Yang NS, Efferth T. Induction of cholesterol biosynthesis by archazolid B in T24 bladder cancer cells. Biochem Pharmacol. 2014, 91(1), 18-30.

Hoffmann J, Kazmaier U. A straightforward approach towards cyclic photoactivatable tubulysin derivatives. Angew Chem Int Ed Engl. 2014, 13;53(42):11356-60. 

Bohnert M., Scherer O., Wiechmann K., König S., Dahse H.-M., Hoffmeister D., Werz O. Melleolides induce rapid cell death in human primary monocytes and cancer cells. Bioorg Med Chem 2014, 22, 3856-61. 

Hoffmann J, Gorges J, Junk L, Kazmaier U. Synthesis of pretubulysin-derivatives via the TubUgi-approach. Org Biomol Chem. 2015, 7;13(21):6010-20. 

Karmann L, Schultz K, Herrmann J, Müller R, Kazmaier U. Total syntheses and biological evaluation of miuraenamides. Angew Chem Int Ed Engl. 2015, 7;54(15):4502-7. 

Schneider LS, von Schwarzenberg K, Lehr T, Ulrich M, Kubisch-Dohmen R, Liebl J, Trauner D, Menche D, Vollmar AM. Vacuolar-ATPase Inhibition Blocks Iron Metabolism to Mediate Therapeutic Effects in Breast Cancer. Cancer Res. 2015, 15;75(14):2863-74. 

Zhang, S., Schneider, L.S., Vick, B., Grunert, M., Jeremias, I., Menche, D., Müller, R., Vollmar, A. M. and Liebl, J. Anti-leukemic effects of the V-ATPase inhibitor Archalozid A, Oncotarget 2015, 6 (41): 43508-28.

Braig, S., Schmidt, S., Stoiber, K., Händel, C., Möhn, T., Werz, O., Müller, R., Zahler, S., Koeberle, A., Käs, J.A., Vollmar, A.M. Pharmacological targeting of membrane rigidity: Implications on cancer cell migration and invasion, New. J. Phys. 2015, 17: 1-11.

Scherer O., Maeß M., Lindner S., Garscha U., Weinigel C., Rummler S., Werz O., Lorkowski S. A procedure for efficient non-viral siRNA transfection of primary human monocytes using nucleofection. J Immunol Methods 2015, 4722, 118-24

J. P. Gölz, S. Bockelmann, K. Mayer, H.-J. Steinhoff, H. Wieczorek, M. Huss, J. P. Klare, D. Menche. EPR Studies of V-ATPase with Spin-Labeled Inhibitors DCC and Archazolid: Interaction Dynamics with Proton Translocating Subunit c
ChemMedChem 2016, 11, 420-428. (Honorary illustration of back cover)

Becker D, Kazmaier U. Synthesis of Simplified Halogenated Chondramide Derivatives as new Actin-binding Agents. Eur. J. Org. Chem. 2015(12), 2591–2602.

Hoffmann J, Gorges J, Junk L, Kazmaier U. Synthesis of Pretubulysin-Derivatives via the TubUgi-Approach. Org. Biomol. Chem. 2015(21), 13, 6010–6020.

Becker D, Kazmaier U. Synthesis and Biological Evaluation of Dichlorinated Chondramide Derivatives. Eur. J. Org. Chem. 2015(19), 4198–4213. 

Wolfram S., Wielsch N., Hupfer Y., Mönch B., Lu-Walther H.-W., Heintzmann R., Werz O., Svatoš A., Pohnert G. A metabolic probe-enabled strategy reveals uptake and protein targets of polyunsaturated aldehydes in the diatom Phaeodactylum tricornutum. PLoS ONE 2015, 10, e0140927. 

Schneider, L.S., Ulrich, M. Lehr, T., Menche, D., Müller, R. and von Schwarzenberg, K. MDM2 antagonist nutlin-3a sensitizes tumors to V-ATPase inhibition, Mol. Oncol. 2016, 10 (7): 1054-62. 

Foerster F, Chen T, Altmann KH, Vollmar AM. Actin-binding doliculide causes premature senescence in p53 wild type cells. Bioorg Med Chem. 2016, 15;24(2):123-9. 

Essig S., Schmalzbauer B., Bretzke S., Scherer O., Koeberle A., Werz O., Müller R., Menche D. Predictive Bioinformatic Assignment of Methyl-Bearing Stereocenters: Total Synthesis and an Additional Molecular Target of Ajudazol B. J. Org. Chem. 2016, 81,1333-57

Lehmann J, Richers J, Pöthig A, Sieber SA. Synthesis of ramariolide natural products and discovery of their targets in mycobacteria.
Chem Commun (Camb). 2016,53(1):107-110. 

Mandl FA, Kirsch VC, Ugur I, Kunold E, Vomacka J, Fetzer C, Schneider S, Richter K, Fuchs TM, Antes I, Sieber SA. Natural-Product-Inspired Aminoepoxybenzoquinones Kill Members of the Gram-Negative Pathogen Salmonella by Attenuating Cellular Stress Response.
Angew Chem Int Ed Engl. 2016;55(47):14852-14857. 

Zhao W, Lorenz N, Jung K, Sieber SA. Fimbrolide Natural Products Disrupt Bioluminescence of Vibrio By Targeting Autoinducer Biosynthesis and Luciferase Activity. Angew Chem Int Ed Engl. 2016;55(3):1187-91. 

Bartel K., Winzi M., Ulrich M., Koeberle A., Menche D., Werz O., Müller R., Guck J., Vollmar A., von Schwarzenberg K. V-ATPase inhibition increases cancer cell stiffness and blocks membrane related Ras signaling - a new option for HCC therapy. Oncotarget 2017, 8(6):9476-9487.

Truebenbach I., Gorges J., Kuhn J., Kern S., Baratti E., Kazmaier U., Wagner E., Lächelt U. Sequence-Defined Oligoamide Drug Conjugates of Pretubulysin and Methotrexate for Folate Receptor Targeted Cancer Therapy. Macromol Biosci. 2017,  doi: 10.1002/mabi.201600520. 

Thomas L., Rao Z., Gerstmeier J., Raasch M., Weinigel C., Rummler S., Menche D., Müller R., Pergola C., Mosig A., Werz O. Selective upregulation of TNFα expression in classically-activated human monocyte-derived macrophages (M1) through pharmacological interference with V-ATPase. Biochem Pharmacol 2017, 130, 71-82. 

Pergola C., Schubert K., Pace S., Ziereisen J., Nikels F., Scherer O., Hüttel S., Zahler S., Vollmar A., Weinigel C., Rummler S., Müller R., Raasch M., Mosig A., Koeberle A., Werz O. Modulation of actin dynamics as potential macrophage subtype-targeting anti-tumour strategy. Sci Rep 2017, 7, 41434. 

Rox K., Rohde M., Chhatwal G.S., Müller R. Disorazoles Block Group A Streptococcal Invasion into Epithelial Cells Via Interference with the Host Factor Ezrin. Cell Chem Biol. 2017; 2482:159-170.

Merk H., Messer P., Ardelt M.A., Lamb D.C., Zahler S., Müller R., Vollmar A.M., Pachmayr J. Inhibition of the V-ATPase by Archazolid A - a new strategy to inhibit EMT. Mol Cancer Ther. 2017 Nov;16(11):2329-2339. doi: 10.1158/1535-7163.MCT-17-0129. Epub 2017 Aug 3

Trauner D., Cheng B., Müller R. Total Syntheses of Cystobactamids and Structural Confirmation of Cystobactamid 919-2. Angew Chem Int Ed Engl. 2017, doi: 10.1002/anie.201705387. [Epub ahead of print]

Viehrig K., Surup F., Volz C., Herrmann J., Abou Fayad A., Adam S., Köhnke J., Trauner D., Müller R. Structure and Biosynthesis of Crocagins: Polycyclic Posttranslationally Modified Ribosomal Peptides from Chondromyces crocatus. Angew Chem Int Ed Engl. 2017;56(26):7407-7410. 

Schwenk R., Stehning T., Bischoff I., Ullrich A., Kazmaier U., Fürst R., The anti-metastatic action of the microtubule-targeting agent pretubulysin is associated with the trapping of tumor cells to the endothelium. Oncotarget 2017, 77622–77633. 

Moser C., Rüdiger D., Förster F., von Blume J., Yu P., Küster B., Kazmaier U., Vollmar A.M., Zahler S. “Persistent inhibition of cell migration by sub-toxic doses of miuraenamide, an actin nucleator”, Sci. Rep. 2017, 7, 16407. 

Gorges J., Kjaerulff L., Panter F., Hoffmann T., Kazmaier U., Müller R. Structure, total synthesis and biosynthesis of Chloromyxamides - myxobacterial tetrapeptides featuring an uncommon 6-chloromethyl-5-methoxypipecolic acid building block. Angew. Chem. 2018, in press. 

Klein P.M., Kern S., Lee D.J., Schmaus J., Höhn M., Gorges J., Kazmaier U., Wagner E. Folate receptor-directed orthogonal click-functionalization of siRNA lipopolyplexes for tumor cell killing in vivo. Biomaterials. 2018 Sep;178:630-642. doi: 10.1016/j.biomaterials.2018.03.031. Epub 2018 Mar 19.

Stoiber K., Nagło O., Pernpeintner C., Zhang S., Koeberle A., Ulrich M., Werz O., Müller R., Zahler S., Lohmüller T., Feldmann J., Braig S.Targeting de novo lipogenesis as a novel approach in anti-cancer therapy. Br J Cancer. 2018;118(1):43-51. doi: 10.1038/bjc.2017.374. 

Glatzel D.K., Koeberle A., Pein H., Löser K., Stark A., Keksel N., Werz O., Müller R., Bischoff I., Fürst R. Acetyl-CoA carboxylase 1 regulates endothelial cell migration by shifting the phospholipid composition. J Lipid Res. 2018;59(2):298-311. doi: 10.1194/jlr.M080101

 

Reviews:


Fürst R, Vollmar AM. A new perspective on old drugs: non-mitotic actions of tubulin-binding drugs play a major role in cancer treatment. Pharmazie. 2013, 68(7), 478-83. 

Kazmaier U, Ullrich A, Hoffmann J. Synthetic Approaches towards Tubulysins and their Derivatives. Open Nat. Prod. J. 2013, 6, 12−30. 

Kretzschmann VK, Fürst R. Plant-derived vascular disrupting agents – compounds, actions, and clinical trials. Phytochem Rev. 2014, 13, 191-206. 

Sieber SA. Naturstoffe als Leitstrukturen für antibakterielle Wirkstoffe. Drug Res (Stuttg). 2014, Suppl 1:S8.  

Scheeff S., Menche D. Total syntheses of the archazolids: an emerging class of novel anticancer drugs. Beilstein J Org Chem. 2017;13:1085-1098. doi: 10.3762/bjoc.13.108.


Book Chapters: 

Plaza, A. and Müller, R. (2014) Myxobacteria: Chemical diversity and screening strategies In: A. Osbourn, R. J. Goss and G. T. Carter (Eds) Natural Products: Discourse, Diversity, and Design, John Wiley & Sons, Inc., Hoboken, NJ, USA, epub ahead of print.


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