@unpublished{EnglertStoyArrowsmithetal.2019,
  author    = {Englert, Lukas and Stoy, Andreas and Arrowsmith, Merle and M{\"u}ssig, Jonas H. and Thaler, Melanie and Deißenberger, Andrea and H{\"a}fner, Alena and B{\"o}hnke, Julian and Hupp, Florian and Seufert, Jens and Mies, Jan and Damme, Alexander and Dellermann, Theresa and Hammond, Kai and Kupfer, Thomas and Radacki, Krzysztof and Thiess, Torsten and Braunschweig, Holger},
  title     = {Stable Lewis Base Adducts of Tetrahalodiboranes: Synthetic Methods and Structural Diversity},
  series = {Chemistry - A European Journal},
  journal   = {Chemistry - A European Journal},
  doi       = {10.1002/chem.201901437},
  url       = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-184888},
  year      = {2019},
  abstract  = {A series of 22 new bis(phosphine), bis(carbene) and bis(isonitrile) tetrahalodiborane adducts has been synthesized, either by direct adduct formation with highly sensitive B2X4 precursors (X = Cl, Br, I) or by ligand exchange at stable B2X4(SMe2)2 precursors (X = Cl, Br) with labile dimethylsulfide ligands. The isolated compounds have been fully characterized using NMR spectroscopic, (C,H,N)- elemental and, for 20 of these compounds, X-ray crystallographic analysis, revealing an unexpected variation in the bonding motifs. Besides the classical B2X4L2 diborane(6) adducts, some of the more sterically demanding carbene ligands induce a halide displacement leading to the first halide-bridged monocationic diboron species, [B2X3L2]A (A = BCl4, Br, I). Furthermore, low-temperature 1:1 reactions of B2Cl4 with sterically demanding N-heterocyclic carbenes led to the formation of kinetically unstable mono-adducts, one of which was structurally characterized. A comparison of the NMR and structural data of new and literature-known bis-adducts shows several trends pertaining to the nature of the halides and the stereoelectronic properties of the Lewis bases employed.},
  language  = {en}
}
@phdthesis{Seufert2016,
  author    = {Seufert, Florian},
  title     = {Entwicklung von Inhibitoren des „macrophage infectivity potentiator"-Proteins},
  url       = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-134820},
  school      = {Universit{\"a}t W{\"u}rzburg},
  year      = {2016},
  abstract  = {Die Melioidose und die Legion{\"a}rskrankheit werden von den beiden Erregern Burkholderia pseudomallei bzw. Legionella pneumophila verursacht. Eine hohe Mortalit{\"a}tsrate trotz langwieriger Behandlungen sowie die zunehmende Resistenz vieler Bakterien gegen{\"u}ber den eingesetzten Antibiotika verdeutlichen die Notwendigkeit alternativer Behandlungsmethoden. Als neues Angriffsziel gilt das bereits in vielen Pathogenen gefundene „macrophage infectivity potentiator"-Protein, kurz Mip, das als Virulenzfaktor die Infektion forciert. Bei Legionella pneumophilia ist LpMip daf{\"u}r verantwortlich, dass das Bakterium in die Lunge eindringen kann. Dabei {\"u}berwindet der Erreger mit Hilfe des Mips die Epithelzellschicht und die extrazellul{\"a}re Matrix. F{\"u}r BpMip ist der Sachverhalt der Invasion noch Gegenstand aktueller Forschung. Beide Mips zeigen eine hohe Sequenzhomologie zu humanem FKBP12 (FK506-bindende Proteine) und geh{\"o}ren deshalb zur Superfamilie der Peptidyl-Prolyl-cis/trans-Isomerasen (PPIasen), die die F{\"a}higkeit besitzen, die cis/trans-Isomerisierung von Peptidbindungen der Aminos{\"a}ure Prolin zu katalysieren. Die bereits bekannten FKBP12- und Mip-Inhibitoren Rapamycin und FK506 sind aufgrund ihrer immunsuppressiven Wirkung nicht zur Behandlung der beiden Krankheiten einsetzbar. Im Vorfeld dieser Arbeit konnte durch Synthese des literaturbekannten nicht-immunsuppressiven FKBP12-Inhibitors eine Leitstruktur gewonnen werden, die sowohl die PPIase-Aktivit{\"a}t von LpMip als auch von BpMip inhibiert. Zun{\"a}chst konnten in dieser Arbeit durch Optimierung des Synthesewegs die Inhibitoren enantiomerenrein hergestellt werden. Ebenso wurde verifiziert, dass das S-Enantiomer das aktivere Konfigurationsisomer ist. Daneben wurde durch Synthese der Verbindung 8a/S-8a die anti-PPIase-Aktivit{\"a}t und die L{\"o}slichkeit im PBS-Puffer verbessert sowie die Zytotoxizit{\"a}t im Vergleich zu S-1a gesenkt Diese Verbindung zeigte jedoch eine schlechte Aktivit{\"a}t im Infektionsassay. In weiteren Kooperationen mit dem Biozentrum W{\"u}rzburg und dem Dstl wurden die Inhibitoren ebenfalls erfolgreich an den Mips von Chlamydia trachomatis, Neisseria gonorrhoeae, Francisella tularensis undYersinia pestis getestet. In dieser Arbeit wurden erstmals Mip-Inhibitoren an Burkholderien in einer In-vivo-Studie untersucht. Die Wirksamkeit der Inhibitoren im Tiermodell soll in Folgestudien bewiesen werden. Damit ist eine aussichtsreiche Basis f{\"u}r zuk{\"u}nftige alternative Behandlungsmethoden der gram-negativer Bakterien gelegt.},
  subject      = {Burkholderia},
  language  = {de}
}
@article{HartungSeufertBergesetal.2012,
  author    = {Hartung, Andreas and Seufert, Florian and Berges, Carsten and Gessner, Viktoria H. and Holzgrabe, Ulrike},
  title     = {One-Pot Ugi/Aza-Michael Synthesis of Highly Substituted 2,5-Diketopiperazines with Anti-Proliferative Properties},
  series = {Molecules},
  volume    = {17},
  journal   = {Molecules},
  number    = {12},
  doi       = {10.3390/molecules171214685},
  url       = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-130423},
  pages     = {14685-14699},
  year      = {2012},
  abstract  = {The well-known Ugi reaction of aldehydes with amines, carboxylic acids and isocyanides leads to the formation of acyclic alpha-acylaminocarboxamides. Replacement of the carboxylic acid derivatives with beta-acyl substituted acrylic acids gives access to highly substituted 2,5-diketopiperazines in one single reaction-step without additives or complex reaction procedures. The obtained diketopiperazines show anti-proliferative effects on activated T cells and represent therefore potential candidates for targeting unwanted T cell-mediated immune responses.},
  language  = {en}
}
@article{WamserSeufertHalletal.2021,
  author    = {Wamser, Florian and Seufert, Anika and Hall, Andrew and Wunderer, Stefan and Hoßfeld, Tobias},
  title     = {Valid statements by the crowd: statistical measures for precision in crowdsourced mobile measurements},
  series = {Network},
  volume    = {1},
  journal   = {Network},
  number    = {2},
  issn      = {2673-8732},
  doi       = {10.3390/network1020013},
  url       = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-284154},
  pages     = {215 -- 232},
  year      = {2021},
  abstract  = {Crowdsourced network measurements (CNMs) are becoming increasingly popular as they assess the performance of a mobile network from the end user's perspective on a large scale. Here, network measurements are performed directly on the end-users' devices, thus taking advantage of the real-world conditions end-users encounter. However, this type of uncontrolled measurement raises questions about its validity and reliability. The problem lies in the nature of this type of data collection. In CNMs, mobile network subscribers are involved to a large extent in the measurement process, and collect data themselves for the operator. The collection of data on user devices in arbitrary locations and at uncontrolled times requires means to ensure validity and reliability. To address this issue, our paper defines concepts and guidelines for analyzing the precision of CNMs; specifically, the number of measurements required to make valid statements. In addition to the formal definition of the aspect, we illustrate the problem and use an extensive sample data set to show possible assessment approaches. This data set consists of more than 20.4 million crowdsourced mobile measurements from across France, measured by a commercial data provider.},
  language  = {en}
}
@article{ScheupleinLohrVivoliVegaetal.2023,
  author    = {Scheuplein, Nicolas Julian and Lohr, Theresa and Vivoli Vega, Mirella and Ankrett, Dyan and Seufert, Florian and Kirchner, Lukas and Harmer, Nicholas J. and Holzgrabe, Ulrike},
  title     = {Fluorescent probe for the identification of potent inhibitors of the macrophage infectivity potentiator (Mip) protein of Burkholderia pseudomallei},
  series = {SLAS Discovery},
  volume    = {28},
  journal   = {SLAS Discovery},
  number    = {5},
  doi       = {10.1016/j.slasd.2023.03.004},
  url       = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-349784},
  pages     = {211-222},
  year      = {2023},
  abstract  = {Highlights • Synthesis of a new tracer molecule. • Robust and easy screening method for a broad range of compound activities. • FP assay validation considering limited use of starting material, DMSO tolerance, variation in incubation time and temperature. • Possibility of extension to HTP assay. Abstract The macrophage infectivity potentiator (Mip) protein belongs to the immunophilin superfamily. This class of enzymes catalyzes the interconversion between the cis and trans configuration of proline-containing peptide bonds. Mip has been shown to be important for the virulence of a wide range of pathogenic microorganisms, including the Gram-negative bacterium Burkholderia pseudomallei. Small molecules derived from the natural product rapamycin, lacking its immunosuppression-inducing moiety, inhibit Mip's peptidyl-prolyl cis-trans isomerase (PPIase) activity and lead to a reduction in pathogen load in vitro. Here, a fluorescence polarization assay (FPA) to enable the screening and effective development of BpMip inhibitors was established. A fluorescent probe was prepared, derived from previous pipecolic scaffold Mip inhibitors labeled with fluorescein. This probe showed moderate affinity for BpMip and enabled a highly robust FPA suitable for screening large compound libraries with medium- to high-throughput (Z factor ∼ 0.89) to identify potent new inhibitors. The FPA results are consistent with data from the protease-coupled PPIase assay. Analysis of the temperature dependence of the probe's binding highlighted that BpMip's ligand binding is driven by enthalpic rather than entropic effects. This has considerable consequences for the use of low-temperature kinetic assays.},
  language  = {en}
}