168 SCIENTIFIC REPORTS | Publications • Dehn,R., Katsuyama,Y., Weber,A., Gerth,K., Jansen,R., Steinmetz,H., Höfle,G., Müller,R., & Kirschning,A. (<strong>2011</strong>) Molecular basis of elansolid biosynthesis: evidence for an unprecedented quinone methide inititiated intramolecular Diels-Alder cycloaddition / macrolactonization. Angewandte Chemie 50, 532-536. • Huntley,S., Hamann,N., Wegener-Feldbrugge,S., Treuner-Lange,A., Kube,M., Reinhardt,R., Klages,S., Müller,R., Ronning,C.M., Nierman,W.C., & Sogaard-Andersen,L. (<strong>2011</strong>) Comparative genomic analysis of fruiting body formation in Myxococcales. Molecular Biology and Evolution 28, 1083-1097. • Steinmetz,H., Gerth,K., Jansen,R., Schlager,N., Dehn,R., Reinecke,S., Kirschning,A., & Müller,R. (<strong>2011</strong>) Elansolid A, a unique macrolide antibiotic from Chitinophaga sancti isolated as two stable atropisomers. Angewandte Chemie International Edtion 50, 532-536. • Wenzel,S.C. & Müller,R. (<strong>2011</strong>) Myxobacteria - Unique microbial secondary metabolic factories. In: Comprehensive Natural Products II: Chemistry and Biology, Elsevier Science & Technology, Oxford, pp. 189-222. • Anderl,T., Nicolas,L., Munkemer,J., Baro,A., Sasse,F., Steinmetz,H., Jansen,R., Hofle,G., Taylor,R.E., & Laschat,S. (<strong>2011</strong>) Gephyronic Acid, a Missing Link between Polyketide Inhibitors of Eukaryotic Protein Synthesis (Part II): Total Synthesis of Gephyronic Acid. Angewandte Chemie International Edition, in press. • Garcia,R., Pistorius,D., Stadler,M., & Müller,R. (<strong>2011</strong>) Fatty acid Related Phylogeny of Myxobacteria as an Approach to Discover Polyunsaturated Omega-3/6 Fatty Acids. Journal of Bacteriology, in press. • Okanya,P.W., Mohr,K.I., Gerth,K., Jansen,R., & Müller,R. (<strong>2011</strong>) Marinoquinolines A-F, Pyrroloquinolines from Ohtaekwangia kribbensis (Bacteroidetes). Journal of Natural Products, in press. • Pistorius,D., Ullrich,A., Lucas,S., Hartmann,R.W., Kazmaier,U., & Müller,R. (<strong>2011</strong>) Biosynthesis of 2-Alkyl-4(1H)-Quinolones in Pseudomonas aeruginosa: Potential for Therapeutic Interference with Pathogenicity. ChemBioChem, in press. • Rachid,S., Huo,L., Herrmann,J., Stadler,M., Kopcke,B., Bitzer,J., & Müller,R. (<strong>2011</strong>) Mining the cinnabaramide biosynthetic pathway to generate novel proteasome inhibitors. ChemBioChem, in press. • Zander,W., Gerth,K., Mohr,K.I., Kessler,W., Jansen,R., & Müller,R. (<strong>2011</strong>) Roimatacene, an antibiotic against gram-negative bacteria isolated from cystobacter Cb G35 (myxobacteria). Chemistry - A European Journal, in press. Dept. of Drug Delivery – HIPS | Prof. Dr. Claus-Michael Lehr • Beisner,J., Dong,M., Taetz,S., Nafee,N., Griese,E.U., Schaefer,U., Lehr,C.-M., Klotz,U., & Murdter,T.E. (<strong>2010</strong>) Nanoparticle mediated delivery of 2’-O-methyl-RNA leads to efficient telomerase inhibition and telomere shortening in human lung cancer cells. Lung Cancer 68, 346-354. • Bur,M., Huwer,H., Muys,L., & Lehr,C.-M. (<strong>2010</strong>) Drug transport across pulmonary epithelial cell monolayers: effects of particle size, apical liquid volume, and deposition technique. Journal of Aerosol Medicine and Pulmonary Drug Delivery 23, 119-127. • Ciana,A., Meier,K., Daum,N., Gerbes,S., Veith,M., Lehr,C.-M., & Minetti,G. (<strong>2010</strong>) A dynamic ratio of the alpha+ and alpha- isoforms of the tight junction protein ZO-1 is characteristic of Caco-2 cells and correlates with their degree of differentiation. Cell Biology International 34, 669-678. • Collnot,E.M., Baldes,C., Schaefer,U.F., Edgar,K.J., Wempe,M.F., & Lehr,C.-M. (<strong>2010</strong>) Vitamin E TPGS P-glycoprotein inhibition mechanism: influence on conformational flexibility, intracellular ATP levels, and role of time and site of access. Molecular Pharmaceutics 7, 642-651. • Gaschen,A., Lang,D., Kalberer,M., Savi,M., Geiser,T., Gazdhar,A., Lehr,C.-M., Bur,M., Dommen,J., Baltensperger,U., & Geiser,M. (<strong>2010</strong>) Cellular responses after exposure of lung cell cultures to secondary organic aerosol particles. Environmental Science and Technology 44, 1424-1430. • Henning,A., Schneider,M., Nafee,N., Muijs,L., Rytting,E., Wang,X., Kissel,T., Grafahrend,D., Klee,D., & Lehr,C.-M. (<strong>2010</strong>) Influence of particle size and material properties on mucociliary clearance from the airways. Journal of Aerosol Medicine and Pulmonary Drug Delivery 23, 233-241. • Henning,A., Hein,S., Schneider,M., Bur,M., & Lehr,C.-M. (<strong>2010</strong>) Pulmonary drug delivery: medicines for inhalation. Handbook of Experimental Pharmacology 171-192. • Lehmann,A.D., Daum,N., Bur,M., Lehr,C.-M., Gehr,P., & Rothen- Rutishauser,B.M. (<strong>2010</strong>) An in vitro triple cell co-culture model with primary cells mimicking the human alveolar epithelial barrier. European Journal of Pharmaceutics and Biopharmaceutics 77, 398-406. • Leonard,F., Collnot,E.M., & Lehr,C.-M. (<strong>2010</strong>) A three-dimensional coculture of enterocytes, monocytes and dendritic cells to model inflamed intestinal mucosa in vitro. Molecular Pharmaceutics 7, 2103-2119. • Melero,A., Lehr,C.-M., Schafer,U.F., & Garrigues,T.M. (<strong>2010</strong>) Wistar rat skin as surrogate for human skin in nortriptyline hydrochloride patch studies. International Journal of Pharmaceutics 384, 137-139. • Muendoerfer,M., Schaefer,U.F., Koenig,P., Walk,J.S., Loos,P., Balbach,S., Eichinger,T., & Lehr,C.-M. (<strong>2010</strong>) Online monitoring of transepithelial electrical resistance (TEER) in an apparatus for combined dissolution and permeation testing. International Journal of Pharmaceutics 392, 134-140. • Neumeyer,A., Bukowski,M., Veith,M., Lehr,C.-M., & Daum,N. (<strong>2010</strong>) Interaction of nanoparticles and cells - cellular uptake and cytotoxic effects in vitro. In Modern Polymeric Materials for Environmental Applications (Pielichowski,K., ed), pp. 239-246. Cracow. • Philippi,C., Loretz,B., Schaefer,U.F., & Lehr,C.-M. (<strong>2010</strong>) Telomerase as an emerging target to fight cancer - Opportunities and challenges for nanomedicine. Journal of Controlled Release 146, 228-240. • Reum,N., Fink-Straube,C., Klein,T., Hartmann,R.W.*., Lehr,C.-M., & Schneider,M. (<strong>2010</strong>) Multilayer coating of gold nanoparticles with drug-polymer coadsorbates. Langmuir 26, 16901-16908. • Rytting,E., Bur,M., Cartier,R., Bouyssou,T., Wang,X., Kruger,M., Lehr,C.-M., & Kissel,T. (<strong>2010</strong>) In vitro and in vivo performance of biocompatible negatively-charged salbutamol-loaded nanoparticles. Journal of Controlled Release 141, 101-107. • Santander-Ortega,M.J., Stauner,T., Loretz,B., Ortega-Vinuesa,J.L., Bastos-Gonzalez,D., Wenz,G., Schaefer,U.F., & Lehr,C.-M. (<strong>2010</strong>) Nanoparticles made from novel starch derivatives for transdermal drug delivery. Journal of Controlled Release 141, 85-92. • Hahn,T., Hansen,S., Neumann,D., Kostka,K.-H., Lehr,C.-M., Muys,L., & Schaefer,U.F. (<strong>2011</strong>) Infrared densitometry: A fast and non-destructive method for exact stratum corneum depth calculation for in vitro tape-stripping. Skin Pharmacology and Physiology 23, 183-192. • Hahn,T., Winkler,K., Lehr,C.-M., & Schäfer,U.F. (<strong>2011</strong>) Ointment bases and the rate of water loss of the skin [Salbengrundlagen und die Wasserabgaberate der Haut]. Deutsche Apotheker Zeitung 150, 59-62. • Hansen,S., Selzer,D., Schaefer,U.F., & Kasting,G.B. (<strong>2011</strong>) An extended database of keratin binding. Journal of Pharmaceutical Sciences 100, 1712-1726. • Hein,S., Bur,M., Schaefer,U.F., & Lehr,C.-M. (<strong>2011</strong>) A new Pharmaceutical Aerosol Deposition Device on Cell Cultures (PADDOCC) to evaluate pulmonary drug absorption for metered dose dry powder formulations. European Journal of Pharmacology and Biopharmacology 77, 132-138.
SCIENTIFIC REPORTS | Publications 169 • Khvedelidze,M., Mdzinarashvili,T., Partskhaladze,T., Nafee,N., Schaefer,U.F., Lehr,C.-M., & Schneider,M. (<strong>2011</strong>) Calorimetric and spectrophotometric investigation of PLGA nanoparticles and their complex with DNA. Journal of Thermal Analysis and Calorimetry 99, 337-348. • Maurer,F., Daum,N., Schaefer,U.F., Lehr,C.-M., & Bauer,P. (<strong>2011</strong>) Plant genetic factors for iron homeostasis affect iron bioavailability in Caco-2 cells. Food <strong>Research</strong> International 43, 1661-1665. • Patzelt,A., Richter,H., Knorr,F., Schafer,U., Lehr,C.-M., Dahne,L., Sterry,W., & Lademann,J. (<strong>2011</strong>) Selective follicular targeting by modification of the particle sizes. Journal of Control Release 150, 45-48. • Schulze,C., Schaefer,U.F., Ruge,C.A., Wohlleben,W., & Lehr,C.-M. (<strong>2011</strong>) Interaction of metal oxide nanoparticles with lung surfactant protein A. European Journal of Pharmaceutics and Biopharmaceutics 77, 376-383. Dept. of Drug Design and Optimisation – HIPS | Prof. Dr. Rolf Hartmann • Gobbi,S., Zimmer,C.*., Belluti,F., Rampa,A., Hartmann,R.W.*., Recanatini,M., & Bisi,A. (<strong>2010</strong>) Novel highly potent and selective nonsteroidal aromatase inhibitors: synthesis, biological evaluation and structure-activity relationships investigation. Journal of Medicinal Chemistry 53, 5347-5351. • Haller,F., Moman,E., Hartmann,R.W.*., Adamski,J., & Mindnich,R. (<strong>2010</strong>) Molecular framework of steroid/retinoid discrimination in 17beta-hydroxysteroid dehydrogenase type 1 and photoreceptorassociated retinol dehydrogenase. Journal of Molecular Biology 399, 255-267. • Heinzerling,L., Hartmann,R.W.*., Frotscher,M., & Neumann,D. (<strong>2011</strong>) Predicting putative inhibitors of 17beta-HSD1. Molecular Informatics 29, 695-705. • Hille,U.E., Zimmer,C., Vock,C.A., & Hartmann,R.W.*. (<strong>2011</strong>) First selective CYP11B1 inhibitors for the treatment of cortisol-dependent diseases. ACS Medicinal Chemistry Letters 2, 2-6. • Marchais-Oberwinkler,S., Wetzel,M., Ziegler,E., Kruchten,P., Werth,R., Henn,C., Hartmann,R.W.*., & Frotscher,M. (<strong>2011</strong>) New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases. Journal of Medicinal Chemistry 54, 534-547. • Oster,A., Klein,T., Henn,C., Werth,R., Marchais-Oberwinkler,S., Frotscher,M., & Hartmann,R.W.*. (<strong>2011</strong>) Bicyclic substituted hydroxyphenylmethanone type inhibitors of 17 beta-hydroxysteroid dehydrogenase Type 1 (17 beta-HSD1): the role of the bicyclic moiety. ChemMedChem 6, 476-487. • Stefanachi,A., Favia,A.D., Nicolotti,O., Leonetti,F., Pisani,L., Catto,M., Zimmer,C., Hartmann,R.W.*., & Carotti,A. (<strong>2011</strong>) Design, Synthesis, and Biological Evaluation of Imidazolyl Derivatives of 4,7-Disubstituted Coumarins as Aromatase Inhibitors Selective over 17-alpha- Hydroxylase/C17-20 Lyase. Journal of Medicinal Chemistry 54, 1613- 1625. • Wetzel,M., Marchais-Oberwinkler,S., & Hartmann,R.W.*. (<strong>2011</strong>) 17beta-HSD2 inhibitors for the treatment of osteoporosis: Identification of a promising scaffold. Bioorganic and Medicinal Chemistry 19, 807-815. • Yadav,M.R., Sabale,P.M., Giridhar,R., Zimmer,C., Haupenthal,J., & Hartmann,R.W.*. (<strong>2011</strong>) Synthesis of some novel androstanes as potential aromatase inhibitors. Steroids 76, 464-470. • Hu,Q., Yin,L., Jagusch,C., Hille,U.E., & Hartmann,R.W.*. (<strong>2010</strong>) Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors. Journal of Medicinal Chemistry 53, 5049-5053. • Hu,Q., Jagusch,C., Hille,U.E., Haupenthal,J., & Hartmann,R.W.*. (<strong>2010</strong>) Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prostate cancer. Journal of Medicinal Chemistry 53, 5749-5758. • Hu,Q., Negri,M., Olgen,S., & Hartmann,R.W. (<strong>2010</strong>) The role of fluorine substitution in biphenyl methylene imidazole-type CYP17 inhibitors for the treatment of prostate carcinoma. ChemMedChem 5, 899-910. • Negri,M., Recanatini,M., & Hartmann,R.W.*. (<strong>2010</strong>) Insights in 17beta-HSD1 enzyme kinetics and ligand binding by dynamic motion investigation. PLoS ONE 5, e12026. • Oster,A., Hinsberger,S., Werth,R., Marchais-Oberwinkler,S., Frotscher,M., & Hartmann,R.W.*. (<strong>2010</strong>) Bicyclic substituted hydroxyphenylmethanones as novel inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogendependent diseases. Journal of Medicinal Chemistry 53, 8176-8186. • Oster,A., Klein,T., Werth,R., Kruchten,P., Bey,E., Negri,M., Marchais- Oberwinkler,S., Frotscher,M., & Hartmann,R.W.*. (<strong>2010</strong>) Novel estrone mimetics with high 17beta-HSD1 inhibitory activity. Bioorganic and Medicinal Chemistry 18, 3494-3505. • Reum,N., Fink-Straube,C., Klein,T., Hartmann,R.W.*., Lehr,C.-M., & Schneider,M. (<strong>2010</strong>) Multilayer coating of gold nanoparticles with drug-polymer coadsorbates. Langmuir 26, 16901-16908. • Zimmer,C., Hafner,M., Zender,M., Ammann,D., Hartmann,R.W.*., & Vock,C.A. (<strong>2010</strong>) N-(Pyridin-3-yl)benzamides as selective inhibitors of human aldosterone synthase (CYP11B2). Bioorganic and Medicinal Chemistry Letters 21, 186-190.