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.     

Droplet Entrainment Analysis in a Flash Evaporator with an Image-Based Measurement Technique

Local droplet sizes and volumes of entrained liquid are captured with an image-based measurement technique for comparison with a conventional, integral method for entrainment analysis. Experiments in a forced circulation flash evaporation were performed for different operating conditions and with two different chemical systems. Droplet size and frequency rise with an increase in thermal energy input. The local readings confirm the trends found by the integral measurement method. The modification of the image-based probe enables the detection of small (≈ 10 µm) and at the same time fast droplets under challenging operating conditions, such as vacuum and superheated feed similar to industrial process conditions.     

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.     

Tropfenbewegung und Stofftransport in technischen Flüssig/flüssig-Systemen. Teil 2: Auswirkung von Grenzflächeneffekten und Verunreinigungen

The design of a liquid/liquid contact apparatus necessitates the knowledge of fluid dynamics and mass transfer in the dispersion. Prediction of process parameters is challenging due to swarm and interfacial effects. Single drop investigations are suitable to enable a sophisticated dimensioning based on few simple experiments combined with published theories and correlations. In the first part of this article, the fundamentals of fluid dynamics and mass transfer in absence of interfacial effects were explained. Here, an overview of relevant interfacial phenomena and the influence of different substances typically occurring in technical applications as impurities or accompanying components is given.     

Identification and Composition of Clasper Scent Gland Components of the Butterfly Heliconius erato and Its Relation to Mimicry

The butterfly Heliconius erato occurs in various mimetic morphs. The male clasper scent gland releases an anti-aphrodisiac pheromone and additionally contains a complex mixture of up to 350 components, varying between individuals. In 114 samples of five different mimicry groups and their hybrids 750 different compounds were detected by gas chromatography/mass spectrometry (GC/MS). Many unknown components occurred, which were identified using their mass spectra, gas chromatography/infrared spectroscopy (GC/IR)-analyses, derivatization, and synthesis. Key compounds proved to be various esters of 3-oxohexan-1-ol and (Z)-3-hexen-1-ol with (S)-2,3-dihydrofarnesoic acid, accompanied by a large variety of other esters with longer terpene acids, fatty acids, and various alcohols. In addition, linear terpenes with up to seven uniformly connected isoprene units occur, e. g. farnesylfarnesol. A large number of the compounds have not been reported before from nature. Discriminant analyses of principal components of the gland contents showed that the iridescent mimicry group differs strongly from the other, mostly also separated, mimicry groups. Comparison with data from other species indicated that Heliconius recruits different biosynthetic pathways in a species-specific manner for semiochemical formation.     

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...