TY - JOUR A1 - Stephan, H. A1 - Kubeil, M. A1 - Emmerling, Franziska A1 - Müller, C.E. T1 - Polyoxometalates as versatile enzyme inhibitors N2 - Polyoxometalates (POMs) are inorganic cluster compounds that have been shown to possess a number of pharmacological properties, including antidiabetic, antibacterial, antiprotozoal, antiviral and anticancer activities. Their molecular mechanism of action is largely unknown. However, several studies indicate that many of their activities may be due to the inhibition of enzymes, in particular, of those enzymes that are accessible from the extracellular space and do not require the penetration of cell membranes. In this review, we describe the recent progress in the preparation and optimization of POMs, and an evaluation of their use as inhibitors of different families of enzymes. The next important steps in this area of research will be to gain a better understanding of the interactions of POMs with enzymes on a structural level through an X-ray crystallographic study of enzyme–POM complexes and the analysis of structure–activity relationships. Furthermore, POMs with increased stability and in vivo half-lives have to be prepared. Surface modification may allow the targeting of POM drugs at their sites of action. KW - Cluster compounds KW - Poly­oxometalates KW - Metalloprotein mimics KW - Enzymes KW - Inhibitors KW - Bioinorganic chemistry PY - 2013 DO - https://doi.org/10.1002/ejic.201201224 SN - 1434-1948 SN - 1099-0682 VL - 2013 IS - 10-11 SP - 1585 EP - 1594 PB - Wiley-VCH Verl. CY - Weinheim AN - OPUS4-28076 LA - eng AD - Bundesanstalt fuer Materialforschung und -pruefung (BAM), Berlin, Germany ER - TY - JOUR A1 - Stephan, H. A1 - Walther, M. A1 - Fähnemann, S. A1 - Ceroni, P. A1 - Molloy, J.K. A1 - Bergamini, G. A1 - Heisig, F. A1 - Müller, C.E. A1 - Kraus, Werner A1 - Comba, P. T1 - Bispidines for dual imaging N2 - The efficient transformation of the hexadentate bispidinol 1 into carbamate derivatives yields functional bispidines enabling convenient functionalization for targeted imaging. The BODIPY-substituted bispidine 3 combines a coordination site for metal ions, such as radioactive 64CuII, with a fluorescent unit. Product 3 was thoroughly characterized by standard analytical methods, single crystal X-ray diffraction, radiolabeling, and photophysical analysis. The luminescence of ligand 3 was found to be strongly dependent on metal ion coordination: CuII quenches the BODIPY fluorescence, whereas NiII and ZnII ions do not affect it. It follows that, in imaging applications with the positron emitter 64CuII, residues of its origin from enriched 64Ni and the decay products 64NiII and 64ZnII, efficiently restore the fluorescence of the ligand. This allows for monitoring of the emitted radiation as well as the fluorescence signal. The stability of the 64CuII–3 complex is investigated by transmetalation experiments with ZnII and NiII, using fluorescence and radioactivity detection, and the results confirm the high stability of 64CuII–3. In addition, metal complexes of ligand 3 with the lanthanide ions TbIII, EuIII, and NdIII are shown to exhibit emission of the BODIPY ligand and the lanthanide ion, thus enabling dual emission detection. KW - Bispidines KW - Chelates KW - Imaging agents KW - Lanthanides KW - Radiolabeling KW - Nuclear medical application KW - Radioactive labelling KW - SPECT PY - 2014 DO - https://doi.org/10.1002/chem.201404086 SN - 0947-6539 SN - 1521-3765 VL - 20 IS - 51 SP - 17011 EP - 17018 PB - Wiley-VCH Verl. CY - Weinheim AN - OPUS4-32320 LA - eng AD - Bundesanstalt fuer Materialforschung und -pruefung (BAM), Berlin, Germany ER - TY - CONF A1 - Miccoli, Lorenzo A1 - Müller, U. A1 - Silva, B. A1 - Da Porto, F. A1 - Hracov, S. A1 - Pospisil, S. A1 - Adami, C.-E. A1 - Vintzileou, E. A1 - Vasconcelos, G. A1 - Poletti, E. ED - Jasienko, J. T1 - Overview of different strengthening techniques applied on walls used in historical structures T2 - SAHC 2012 - 8th International conference on structural analysis of historical constructions CY - Wroclaw, Poland DA - 2012-10-15 KW - Stone masonry KW - Brick masonry KW - Earthen materials KW - Half timbered walls KW - Grouting PY - 2012 SN - 978-83-7125-216-7 SN - 0860-2395 VL - 3 SP - 2870 EP - 2878 PB - DWE CY - Wroclaw, Poland AN - OPUS4-27275 LA - eng AD - Bundesanstalt fuer Materialforschung und -pruefung (BAM), Berlin, Germany ER -