Strategies To Design Selective Histone Deacetylase Inhibitors

This review classifies drug-design strategies successfully implemented in the development of histone deacetylase (HDAC) inhibitors, which have many applications including cancer treatment. Our focus is on especially demanded selective HDAC inhibitors and their structure-activity relationships in relation to corresponding protein structures. The main part of the paper is divided into six subsections each narrating how optimization of one of six structural features can influence inhibitor selectivity. It starts with the impact of the zinc binding group on selectivity, continues with the optimization of the linker placed in the substrate binding tunnel as well as the adjustment of the cap group interacting with the surface of the protein, and ends with the addition of groups targeting class-specific sub-pockets: the side-pocket-, lower-pocket- and foot-pocket-targeting groups. The review is rounded off with a conclusion and an outlook on the future of HDAC inhibitor design.     

Investigation on the effectiveness of the repair method 8.3 “Corrosion protection by increasing the electrical resistivity” in chloride-containing concrete Part 2: Chloride redistribution in concrete after application of a system sealing surface protective coating

This DFG-funded research project aimed to gain a better understanding of the mechanisms of the W-Cl repair principle within the framework of fundamental investigations, to contribute to the creation of the necessary basis for a broader application of the repair principle in practice. The focus was on the development of a model to describe the chloride redistribution after the application of a system sealing surface protective coating. On the basis of Fick's second law of diffusion, a mathematical model with a self-contained analytical solution was developed, with the help of which the chloride redistribution after application of a system sealing surface protective coating can be calculated under the idealized assumption of complete water saturation of the concrete. Furthermore, the influence of the dehydration of the concrete, expected as a result of the application of the repair principle W-Cl, on the chloride redistribution was investigated. On the basis of laboratory tests and numerical simulations, material-specific reduction functions were developed to quantify the relationship between the chloride diffusion coefficient and the ambient humidity.     

Enhancing the sweetening power of lactose by enzymatic modification in the reformulation of dairy products

Lactose solutions of up to 50% (w/v) were incubated with lactases and glucose isomerases for subsequent implementation in dairy product samples to enhance sweetness. A degree of hydrolysis of >90% and of isomerisation of 50% were attainable. The sensory sweetening power of lactose in solutions of up to 50% (w/v) can be enhanced 2–3 times. Based on sensory experiments, application of this bi‐enzymatic system in yoghurt and pudding samples allowed for a 10–20% (w/w) reduction in the total sugar content, whilst retaining equal sweetness. The growth of yoghurt starter cultures was not affected, yet furosine formation more than doubled in high heated, enzyme‐modified milk.     

Open innovation in Russian state-owned enterprises

ABSTRACT

This paper studies open innovation practices in Russian state-owned enterprises (SOEs). In 2011, the Russian Government set ambitious goals in science, technology and innovation, and uses its large SOEs as channels to achieve these targets. These initiatives focus on the collaboration among innovation actors and introduce open innovation (OI) principles. Based on a large-scale innovation survey, we compare private enterprises to state-owned peers and present selected case studies. Our data support the claim that Russian SOEs are driving the demand for technology and mainly absorb incoming OI activities. Different to their peers, SOEs extend their OI activities to the country’s knowledge producers, such as research and technology organisations (RTOs), and leading universities. They work on incorporating scientific knowledge that could, indeed, hold the key to globally competitive technological innovations, but also have better capabilities to include business partners.

Abbreviation : OI: Open innovation; SOE: State-owned enterprise; RTO: Research and technology organisation; STI: Science, technology and innovation.     

Diamine oxidase supplementation improves symptoms in patients with histamine intolerance

Food Science and Biotechnology - Histamine intolerance (HIT) is thought to be caused by a disproportionate amount of histamine in the body. The enzyme diamine oxidase (DAO) is considered for the...     

Helium droplet assisted synthesis of plasmonic Ag@ZnO core@shell nanoparticles

Plasmonic Ag@ZnO core@shell nanoparticles are formed by synthesis inside helium droplets with subsequent deposition and controlled oxidation. The particle size and shape can be controlled from spherical sub-10 nm particles to larger elongated structures. An advantage of the method is the complete absence of solvents, precursors, and other chemical agents. The obtained particle morphology and elemental composition have been analyzed by scanning transmission electron microscopy (STEM) and energy dispersive X-ray spectroscopy (EDS). The results reveal that the produced particles form a closed and homogeneous ZnO layer around a 2–3 nm Ag core with a uniform thickness of (1.33 ± 0.15) nm and (1.63 ± 0.31) nm for spherical and wire-like particles, respectively. The results are supported by ultraviolet photoelectron spectroscopy (UPS), which indicates a fully oxidized shell layer for the particles studied by STEM. The plasmonic properties of the produced spherical Ag@ZnO core@shell particles are investigated by two-photon photoelectron (2PPE) spectroscopy. Upon excitation of the localized surface plasmon resonance in Ag at around 3 eV, plasmonic enhancement leads to the liberation of electrons with high kinetic energy. This is observed for both Ag and Ag@ZnO particles, showing that even if a Ag cluster is covered by the ZnO layer, a plasmonic enhancement can be observed by photoelectron spectroscopy.

     

Technical note: Evaluation of a triaxial accelerometer for monitoring selected behaviors in dairy calves

The objectives of this study were (1) to develop an algorithm for the acceleration sensor of the Smartbow Eartag (Smartbow GmbH, Weibern, Austria) to distinguish between postures (lying and standing or locomotion) and to detect 6 kinds of activities (milk intake, water intake, solid feed intake, ruminating, licking or sucking without milk intake, and other activities) in dairy calves and (2) to evaluate this sensor for identifying these behaviors in dairy calves compared with observations from video. Accelerometers were applied to the left ears of 15 preweaned Holstein dairy calves. Calves were kept in a group pen and received milk replacer from an automatic calf feeder. Based on 38 h of acceleration data and video observation, an algorithm was established to detect the predefined behaviors. Using cross-validation, video recordings were used to analyze whether a behavior was detected correctly by the developed algorithm. For posture, sensitivity (94.4%), specificity (94.3%), precision (95.8%), and accuracy (94.3%) were high. Cohen's kappa was calculated as 0.88. For the 6 defined activities, overall (i.e., aggregated for all activities) accuracy was 70.8% and kappa was calculated as 0.58. Some activities (e.g., ruminating, feed intake, other activities) were identified better than others. In conclusion, the developed algorithm based on the acceleration data of the Smartbow Eartag was successful in detecting lying behavior, rumination, feed intake, and other activities in calves, but further development of the underlying algorithm will be necessary to produce reliable results for milk and water intake.     

How scientific research reacts to international public health emergencies: a global analysis of response patterns

As of the middle of April 2020, the unprecedented COVID-19 pandemic has claimed more than 137,000 lives (https://coronavirus.jhu.edu/map.html). Because of its extremely fast spreading, the attention of the global scientific community is now focusing on slowing down, containing and finally stopping the spread of this disease. This requires the concerted action of researchers and practitioners of many related fields, raising, as always in such situations the question, of what kind of research has to be conducted, what are the priorities, how has research to be coordinated and who needs to be involved. In other words, what are the characteristics of the response of the global research community on the challenge? In the present paper, we attempt to characterise, quantify and measure the response of academia to international public health emergencies in a comparative bibliometric study of multiple outbreaks. In addition, we provide a preliminary review of the global research effort regarding the defeat of the COVID-19 pandemic. From our analysis of six infectious disease outbreaks since 2000, including COVID-19, we find that academia always responded quickly to public health emergencies with a sharp increase in the number of publications immediately following the declaration of an outbreak by the WHO. In general, countries/regions place emphasis on epidemics in their own region, but Europe and North America are also concerned with outbreaks in other, developed and less developed areas through conducting intensive collaborative research with the core countries/regions of the outbreak, such as in the case of Ebola in Africa. Researches in the fields of virology, infectious diseases and immunology are the most active, and we identified two characteristic patterns in global science distinguishing research in Europe and America that is more focused on public health from that conducted in China and Japan with more emphasis on biomedical research and clinical pharmacy, respectively. Universities contribute slightly less than half to the global research output, and the vast majority of research funding originates from the public sector. Our findings on how academia responds to emergencies could be beneficial to decision-makers in research and health policy in creating and adjusting anti-epidemic/-pandemic strategies.