Traditionally Heuristic-Analytical Type of Teaching: Theory and Practice

The article substantiates the scientific and theoretical provisions of the traditionally heuristic-analytical type of education, which is understood as a type of education that combines cognitive, creative, and analytical activities enter higher education, that is, reproductive and productive education. The main purpose of the study is to experimentally test the effectiveness of using heuristic-analytical training in the learning process. In the course of the research, the method of experimental research was used. It was stated that most of the respondents in the experimental group should have a high degree of development of professionally important skills, while the majority of respondents in the control group have an average level of development

Identification of novel 2-benzoxazolinone derivatives with specific inhibitory activity against the HIV-1 nucleocapsid protein

In this report, we present a new benzoxazole derivative endowed with inhibitory activity against the HIV-1 nucleocapsid protein (NC). NC is a 55-residue basic protein with nucleic acid chaperone properties, which has emerged as a novel and potential pharmacological target against HIV-1. In the pursuit of novel NC-inhibitor chemotypes, we performed virtual screening and in vitro biological evaluation of a large library of chemical entities. We found that compounds sharing a benzoxazolinone moiety displayed putative inhibitory properties, which we further investigated by considering a series of chemical analogues. This approach provided valuable information on the structure-activity relationships of these compounds and, in the process, demonstrated that their anti-NC activity could be finely tuned by the addition of specific substituents to the initial benzoxazolinone scaffold. This study represents the starting point for the possible development of a new class of antiretroviral agents targeting the HIV-1 NC protein

Implementing Blended Learning at Technical University: Advantages and Challenges

The article is devoted to the problem of the blended learning implementation in the process of foreign language teaching at a technical university. It is focused on the purposes of blended learning and its benefits as well as the challenges, you can face while implementing a blended learning approach. Implementing of blended learning as innovation leads to a number of changes in self-determination and the ways in which the student and teacher work. Students acquire the space of freedom and responsibility in which they learn to make an informed choice and to be responsible for its consequences. Teachers begin to function in new roles for themselves, in particular, they move away from the role of the translator to the role of the tutor. The research examines the opportunities of this educational technology to narrow the gap in students’ level of proficiency in a foreign language through an individual approach to learning, which corresponds to the main trend of the development of the modern educational system

Cтратегии и технологии инновационного развития корпораций

У монографії представлено результати дослідження й систематизації теоретичних, науково-методологічних і практичних положень та розробок щодо стратегій та технологій інноваційного розвитку корпорацій. Запропоновано і обґрунтовано технології управління інноваційним розвитком підприємств, стратегії розвитку бізнесу, визначено сучасні реалії та тенденції корпоративного маркетингу, культури та соціальної відповідальності бізнесу, запропоновано нові підходи у корпоративному управлінні, обґрунтовано доцільність використання краудтехнологій фінансування інноваційних проектів, визначено підхо-ди щодо управління персоналом корпорацій в поведінковій економіці. Для науковців та фахівців сфери економіки та управління підприємствам

Selection and characterization of molecules that target the HIV-1 nucleocapsid protein

La tri-thérapie utilisée pour le traitement du VIH-1 est efficace mais limitée par l'apparition de résistances. Par conséquent, des cibles virales alternatives sont nécessaires. Une des cibles les plus prometteuses est la protéine nucléocapside (NC), qui est hautement conservée et qui joue un rôle essentiel dans le cycle viral. Dans ce contexte, le projet européen THINPAD a eu pour but de développer des inhibiteurs de la NC en combinant plusieurs approches : criblage virtuel, criblage secondaire in vitro, tests antiviraux et de toxicité. Pour le criblage in vitro, nous avons utilisé le test de déstabilisation de cTAR, hautement spécifique de l’activité chaperonne de NC. Cinq séries de molécules ont été sélectionnées par les premiers criblages et tests antiviraux. Après des études de relation structure-activité, une seule des cinq séries a été poursuivie jusqu’aux tests d'efficacité chez les souris. Les composés de cette série présentent une activité antivirale à des concentrations nanomolaires, mais ne sont pas actifs dans le modèle murin. Les études de mécanisme d'action ont révélés que leur activité antivirale était bien consécutive au ciblage de la NC.Highly Active Anti-Retroviral Therapy (HAART) is successfully used for HIV-1 treatment, but is hampered by the appearance of drug resistance. Thereby, alternative drug targets are required. One of the most promising target is the nucleocapsid protein (NC), which is highly conserved and plays essential role in HIV life cycle. In this context, the European project THINPAD was organized with the aim to develop NC inhibitors. To fulfil this objective, several approaches were used, including virtual screening, in vitro secondary screening, in cellulo antivirals tests, and toxicity evaluation. For in vitro screening, the specific NC-promoted cTAR destabilization assay was used. Five series of molecules were selected by the first screenings and antiviral tests. After structure-activity relationship studies, only one series was continued until efficacy testing in mice. The compounds of this series exhibit antiviral activity at nanomolar concentrations but are not active in the murine model. The mechanisms of action studies revealed that their antiviral activity was indeed consecutive to the targeting of the NC

Selection and characterization of molecules that target the HIV-1 nucleocapsid protein

La tri-thérapie utilisée pour le traitement du VIH-1 est efficace mais limitée par l'apparition de résistances. Par conséquent, des cibles virales alternatives sont nécessaires. Une des cibles les plus prometteuses est la protéine nucléocapside (NC), qui est hautement conservée et qui joue un rôle essentiel dans le cycle viral. Dans ce contexte, le projet européen THINPAD a eu pour but de développer des inhibiteurs de la NC en combinant plusieurs approches : criblage virtuel, criblage secondaire in vitro, tests antiviraux et de toxicité. Pour le criblage in vitro, nous avons utilisé le test de déstabilisation de cTAR, hautement spécifique de l’activité chaperonne de NC. Cinq séries de molécules ont été sélectionnées par les premiers criblages et tests antiviraux. Après des études de relation structure-activité, une seule des cinq séries a été poursuivie jusqu’aux tests d'efficacité chez les souris. Les composés de cette série présentent une activité antivirale à des concentrations nanomolaires, mais ne sont pas actifs dans le modèle murin. Les études de mécanisme d'action ont révélés que leur activité antivirale était bien consécutive au ciblage de la NC.Highly Active Anti-Retroviral Therapy (HAART) is successfully used for HIV-1 treatment, but is hampered by the appearance of drug resistance. Thereby, alternative drug targets are required. One of the most promising target is the nucleocapsid protein (NC), which is highly conserved and plays essential role in HIV life cycle. In this context, the European project THINPAD was organized with the aim to develop NC inhibitors. To fulfil this objective, several approaches were used, including virtual screening, in vitro secondary screening, in cellulo antivirals tests, and toxicity evaluation. For in vitro screening, the specific NC-promoted cTAR destabilization assay was used. Five series of molecules were selected by the first screenings and antiviral tests. After structure-activity relationship studies, only one series was continued until efficacy testing in mice. The compounds of this series exhibit antiviral activity at nanomolar concentrations but are not active in the murine model. The mechanisms of action studies revealed that their antiviral activity was indeed consecutive to the targeting of the NC

Perfection of remuneration system in a construction company

Subject of research: some aspects of perfection of remuneration system in a construction company. Purpose of work: to define modern problems of remuneration organization in construction industry to ground the directions of remuneration system perfection in construction companies and in the industry as a whole. Methodology of work. The work is done by means of analytical researches of the transition process to a market economy which may provide an improved remuneration system in the construction company. Results. We distinguished the features of remuneration system in construction industry and suggested the introduction of grading system to substantially increase the labor productivity providing an opportunity to define all-level compensation on the basis of comparison of relative cost of different work areas (positions) suitable for all workers of a company. Scope of the results: State and private management of a construction company. Results of the study can be introduced by the heads of construction companies to use these new methods of encouraging workers financially that will substantially reduce company’s expenses and promote its efficiency. Conclusions. Construction industry is characterized by different building assembling works that demand a new effective remuneration system stimulating labor efficiency. A new approach to the remuneration system provides for the rejection of the traditional time-based or complexity-term systems; this approach is a system of grading. The introduction of a modern remuneration system in construction companies will provide an objective estimation of positions and stuff efficiency and, consequently, valid reward of employees, which is one of the main requirements for remuneration systems in market conditions and optimizes the wage fund

Implementing Blended Learning at Technical University: Advantages and Challenges

The article is devoted to the problem of the blended learning implementation in the process of foreign language teaching at a technical university. It is focused on the purposes of blended learning and its benefits as well as the challenges, you can face while implementing a blended learning approach. Implementing of blended learning as innovation leads to a number of changes in self-determination and the ways in which the student and teacher work. Students acquire the space of freedom and responsibility in which they learn to make an informed choice and to be responsible for its consequences. Teachers begin to function in new roles for themselves, in particular, they move away from the role of the translator to the role of the tutor. The research examines the opportunities of this educational technology to narrow the gap in students’ level of proficiency in a foreign language through an individual approach to learning, which corresponds to the main trend of the development of the modern educational system

Biochemistry

UHRF1 plays a central role in the maintenance and transmission of epigenetic modifications by recruiting DNMT1 to hemimethylated CpG sites via its SET and RING-associated (SRA) domain, ensuring error-free duplication of methylation profiles. To characterize SRA-induced changes in the conformation and dynamics of a target 12 bp DNA duplex as a function of the methylation status, we labeled duplexes by the environment-sensitive probe 2-aminopurine (2-Ap) at various positions near or far from the central CpG recognition site containing either a nonmodified cytosine (NM duplex), a methylated cytosine (HM duplex), or methylated cytosines on both strands (BM duplex). Steady-state and time-resolved fluorescence indicated that binding of SRA induced modest conformational and dynamical changes in NM, HM, and BM duplexes, with only slight destabilization of base pairs, restriction of global duplex flexibility, and diminution of local nucleobase mobility. Moreover, significant restriction of the local motion of residues flanking the methylcytosine in the HM duplex suggested that these residues are more rigidly bound to SRA, in line with a slightly higher affinity of the HM duplex as compared to that of the NM or BM duplex. Our results are consistent with a "reader" role, in which the SRA domain scans DNA sequences for hemimethylated CpG sites without perturbation of the structure of contacted nucleotides