@article{MeynersMertensWessigetal.2017,
  author    = {Meyners, Christian and Mertens, Monique and Wessig, Pablo and Meyer-Almes, Franz-Josef},
  title     = {A Fluorescence-Lifetime-Based Binding Assay for Class IIa Histone Deacetylases},
  series = {Chemistry - a European journal},
  volume    = {23},
  journal   = {Chemistry - a European journal},
  number    = {13},
  publisher = {Wiley-VCH},
  address   = {Weinheim},
  issn      = {0947-6539},
  doi       = {10.1002/chem.201605140},
  pages     = {3107 -- 3116},
  year      = {2017},
  abstract  = {Class IIa histone deacetylases (HDACs) show extremely low enzymatic activity and no commonly accepted endogenous substrate is known today. Increasing evidence suggests that these enzymes exert their effect rather through molecular recognition of acetylated proteins and recruiting other proteins like HDAC3 to the desired target location. Accordingly, class IIa HDACs like bromodomains have been suggested to act as "Readers" of acetyl marks, whereas enzymatically active HDACs of class I or IIb are called "Erasers" to highlight their capability to remove acetyl groups from acetylated histones or other proteins. Small-molecule ligands of class IIa histone deacetylases (HDACs) have gained tremendous attention during the last decade and have been suggested as pharmaceutical targets in several indication areas such as cancer, Huntington's disease and muscular atrophy. Up to now, only enzyme activity assays with artificial chemically activated trifluoroacetylated substrates are in use for the identification and characterization of new active compounds against class IIa HDACs. Here, we describe the first binding assay for this class of HDAC enzymes that involves a simple mix-and-measure procedure and an extraordinarily robust fluorescence lifetime readout based on [1,3]dioxolo[4,5-f]benzodioxole-based ligand probes. The principle of the assay is generic and can also be transferred to class I HDAC8.},
  language  = {en}
}
@article{daSilvaVarellaJonesetal.2019,
  author    = {da Silva, Filipe Ferreira and Varella, Marcio T. do N. and Jones, Nykola C. and Hoffmann, Soren Vronning and Denifl, Stephan and Bald, Ilko and Kopyra, Janina},
  title     = {Electron-Induced Reactions in 3-Bromopyruvic Acid},
  series = {Chemistry - a European journal},
  volume    = {25},
  journal   = {Chemistry - a European journal},
  number    = {21},
  publisher = {Wiley-VCH},
  address   = {Weinheim},
  issn      = {0947-6539},
  doi       = {10.1002/chem.201806132},
  pages     = {5498 -- 5506},
  year      = {2019},
  abstract  = {3-Bromopyruvic acid (3BP) is a potential anticancer drug, the action of which on cellular metabolism is not yet entirely clear. The presence of a bromine atom suggests that it is also reactive towards low-energy electrons, which are produced in large quantities during tumour radiation therapy. Detailed knowledge of the interaction of 3BP with secondary electrons is a prerequisite to gain a complete picture of the effects of 3BP in different forms of cancer therapy. Herein, dissociative electron attachment (DEA) to 3BP in the gas phase has been studied both experimentally by using a crossed-beam setup and theoretically through scattering and quantum chemical calculations. These results are complemented by a vacuum ultraviolet absorption spectrum. The main fragmentation channel is the formation of Br- close to 0 eV and within several resonant features at 1.9 and 3-8 eV. At low electron energies, Br- formation proceeds through sigma* and pi* shape resonances, and at higher energies through core-excited resonances. It is found that the electron-capture cross-section is clearly increased compared with that of non-brominated pyruvic acid, but, at the same time, fragmentation reactions through DEA are significantly altered as well. The 3BP transient negative ion is subject to a lower number of fragmentation reactions than those of pyruvic acid, which indicates that 3BP could indeed act by modifying the electron-transport chains within oxidative phosphorylation. It could also act as a radio-sensitiser.},
  language  = {en}
}
@article{LaskovGehlKruegeretal.2006,
  author    = {Laskov, Pavel and Gehl, Christian and Kr{\"u}ger, Stefan and M{\"u}ller, Klaus-Robert},
  title     = {Incremental support vector learning: analysis, implementation and applications},
  series = {Journal of machine learning research},
  volume    = {7},
  journal   = {Journal of machine learning research},
  publisher = {MIT Press},
  address   = {Cambridge, Mass.},
  issn      = {1532-4435},
  pages     = {1909 -- 1936},
  year      = {2006},
  abstract  = {Incremental Support Vector Machines (SVM) are instrumental in practical applications of online learning. This work focuses on the design and analysis of efficient incremental SVM learning, with the aim of providing a fast, numerically stable and robust implementation. A detailed analysis of convergence and of algorithmic complexity of incremental SVM learning is carried out. Based on this analysis, a new design of storage and numerical operations is proposed, which speeds up the training of an incremental SVM by a factor of 5 to 20. The performance of the new algorithm is demonstrated in two scenarios: learning with limited resources and active learning. Various applications of the algorithm, such as in drug discovery, online monitoring of industrial devices and and surveillance of network traffic, can be foreseen.},
  language  = {en}
}