A new series of 4
-1,3-benzothiazine dyes were prepared and fully characterized in an aqueous medium. Benzothiazine salts were synthesized either through the classical synthetic pathway using ...Buchwald-Hartwig amination or through economical and environmentally friendly electrochemical synthesis. The latest synthetic approach employs successful electrochemical intramolecular dehydrogenative cyclization of
-benzylbenzenecarbothioamides to form 4
-1,3-benzothiazines. 4
-1,3-Benzothiazines were evaluated as novel DNA/RNA probes. Through the use of several methods such as UV/vis spectrophotometric titrations, circular dichroism and thermal melting experiments, the binding of four benzothiazine-based molecules to polynucleotides was examined. Compounds
and
acted as DNA/RNA groove binders, thus suggesting the potential of these compounds as novel DNA/RNA probes. This is a proof-of-concept study and will be expanded to include SAR/QSAR studies.
Introduction. The reconstruction of large postoperative defects after oncologic surgery of the head and neck remains challenging. Regional flaps are considered a less expensive reconstructive option ...compared to free flaps. The pectoralis major flap is one of the most versatile choices for the reconstruction of large head and neck defects. Case report. We present technical key points for safe harvesting of pectoralis major flap for two cases in a university-affiliated tertiary care medical center. Both patients were male, with an average age of 64 years. The defects that required reconstruction in Case 1 were on the lateral neck region and, in Case 2, on the anterior side of the neck. Flaps were used for covering the pharyngocutaneous fistula after total laryngectomy and irradiation. The donor site was closed primarily. Flaps in both patients healed primarily without complications. Conclusion. The pectoralis major flap has a constant vascular pedicle and can successfully be used for the reconstruction of large head and neck defects. In order to obtain absolute flap survival, the operative technique must be impeccable.
The process of identifying the protein targets and off-targets of a biologically active compound is of great importance in modern drug discovery. Various chemical proteomics approaches have been ...established for this purpose. To compare the different approaches, and to understand which method would provide the best results, we have chosen the EGFR inhibitor lapatinib as an example molecule. Lapatinib derivatives were designed using linkers with motifs, including amino (amidation), alkyne (click chemistry) and the diazirine group (photo-affinity). These modified lapatinib analogues were validated for their ability to inhibit EGFR activity in vitro and were shown to pull down purified recombinant EGFR protein. In all of the approaches evaluated here, we identified EGFR as the main protein target from the lysate of immortalised cell line expressing EGFR, thus validating its potential use to identify unknown protein targets. Taken together, the results reported here give insight into the cellular activities of lapatinib.
In this paper, the influence of traffic flow volume and meteorological conditions on carbon monoxide (CO), particulate matter (PM), ozone (O3) and sulphur dioxide (SO2) concertation is determined ...based on the measurements conducted at a selected location over a 784-hour period. Multivariate Analysis of Variance (MANOVA) and Analysis of Variance (ANOVA) were applied to the data set. Regression analysis was also used to determine trends in pollutant concentrations as a function of traffic flow and meteorological parameters. Analysis of the obtained data indicates a statistically significant relationship between traffic volume and meteorological parameters on the one hand and pollutants on the other. However, increase in the value of certain input variables does not necessarily result in the increase in pollutant concentration. CO and O3 showed a significant dependence on the number of vehicles, while for SO2 the influence of commercial vehicles was greater than that of passenger cars. The relationship between the number of vehicles and PM was not evident at the study site.
The transport sector is the second largest source of greenhouse gas pollution in terms of total carbon dioxide emissions in the European Union. Reducing emissions in transport is more expensive than ...in other sectors because transport is still heavily reliant on fossil fuels. For years, electric vehicles have played a prominent role in the transport sector in terms of solving the f harmful gas emissions problem. They have the potential to reduce CO2 emissions by offering an alternative to conventional vehicles based on internal combustion engines. Although they have zero CO2 emissions in the tailpipe, electric vehicles require the consumption of electricity to produce them as well as to power the battery, which contributes to the creation of CO2 emissions. The paper compares the use of a delivery vehicle with an internal combustion engine and an electric vehicle in the field of road transportation of the postal sector from the aspect of environmental sustainability. The electric vehicle use showed a lower generation of CO2 by 114.2 g/km, taking into account the average emission of carbon dioxide for electric vehicles according to the data of the European Union.
Nowadays, we face many problems in the field of transport. The application of intelligent transport systems should improve problems related to congestion management, road safety, access to data in ...the transport environment, and environmental protection. The paper presents two concepts that are key to the improvement and development of the transport sector. The development and application of automatic vehicle location since the 1960s has led to an improvement in the efficiency of transport companies’ operations and the quality of their services. This technology has led to improved efficiency of the transport service, better utilisation of resources and improved quality of service. However, the most modern concept that initiates the improvement of existing solutions and encourages the development of new solutions in the field of transport is the IoT (Internet of Things) concept. In freight transport, the application of IoT technology enables cost management, reduction of CO2 emissions and avoidance of congestion through the use of alternative routes.
Long non-coding RNAs (lncRNAs) show patterns of tissue- and cell type-specific expression that are very similar to those of protein coding genes and consequently have the potential to control stem ...and progenitor cell fate decisions along a differentiation trajectory. To understand the roles that lncRNAs may play in hematopoiesis, we selected a subset of mouse lncRNAs with potentially relevant expression patterns and refined our candidate list using evidence of conserved expression in human blood lineages. For each candidate, we assessed its possible role in hematopoietic differentiation in vivo using competitive transplantation. Our studies identified two lncRNAs that were required for hematopoiesis. One of these, Spehd, showed defective multilineage differentiation, and its silencing yielded common myeloid progenitors that are deficient in their oxidative phosphorylation pathway. This effort not only suggests that lncRNAs can contribute to differentiation decisions during hematopoiesis but also provides a path toward the identification of functional lncRNAs in other differentiation hierarchies.
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•Conserved differential expression of syntelogs to enrich functional lncRNAs•Bone marrow transplant of lncRNA-depleted HSCs uncovers in vivo functional lncRNAs•Spehd is required for differentiation during reconstitution and homeostasis•Myeloid progenitors depleted of Spehd show oxidative phosphorylation defects
Delás et al. identify Spehd as an lncRNA expressed in hematopoietic stem and progenitor cells and required for in vivo differentiation during transplantation and homeostasis.
Uveal melanoma is a rare malignancy. Its clinical course is highly agressive. At thetime of diagnosis, extraocular extension is present in most of the cases.We present a case of 69-year-old white man ...admitted for sharp orbital pain. Advanced uveal melanoma was diagnosed. We found black-colored tumor rotruding from the left eye and multiple cutaneous metastases on the scalp. CT scan revealed intracranial tumor mimicking meningeoma in the left parietal region. Lymhogenous metastases were not found and other hematogenous metastases were excluded. After biopsy of the eye tumor and excisional biopsy of one skin tumor, the uveal melanoma was diagnosed and the left orbital exenteration and extirpation of intracranial tumor were performed. The reconstruction was performed using galeacutaneous flap harvested from craniotomy flap. Postoperative course was uneventful and the patient was released from pain. He refused the additional oncological treatment. After four months, he died of liver metastatic disease.The uveal melanoma is highly aggressive malignancy and isolated subdural metastasis is quite rare. The reconstruction with transposed galeacutaneous flap is versatile and secure technique after orbital exenteration.
Headway variability has a negative impact on the public transport passengers’ perception of service quality. However, most of the existing methods aimed at improving the headway regularity operate in ...real time and require precise vehicle location data, making it difficult to implement them in practice. On the other hand, planning-level methods can be used to increase the resilience of public passenger transport (PPT) to the accumulation of headway disturbances. As this is typically done from the operator’s perspective, the passengers’ perspective tends to be overlooked, motivating the current work. In this article, an optimisation procedure for evaluating the viability of diametrical line splitting in terms of passenger travel time and headway regularity is proposed. The aim is to increase the robustness/resistance of the PPT system to the propagation of headway disturbances without reducing the service quality. The developed optimisation procedure was validated by applying it to real data pertaining to an urban PPT line. The results show that there is a positive correlation between the transport demand and the effects of the optimisation procedure, whereby an increase in the primary headway disturbance increases the sensitivity of the optimisation procedure to the transport demand.
The rapid expansion of urban areas requires the application of more capacious technologies of public passenger transport. New public transport technologies should provide satisfactory transport ...characteristics with acceptable capital investment and a short implementation period. Two basic public passenger transport technologies that can provide good transport quality with reasonable investment are Bus rapid transit (BRT) and Light rail transit (LRT). The characteristics of these public transport subsystems largely depend on the implemented technological elements. Within this paper, a comparison of BRT and LRT will be performed based on SWOT analysis, so that city administrations can make appropriate strategic decisions when choosing technology.
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