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Article ; Online: Conformity of pre-design studies on Lakhta-Center influence on the Saint Petersburg historical panorama and scenery spots

Fedorov Oleg / Lobanov Yury

E3S Web of Conferences, Vol 164, p

2020 Volume 05013

Abstract: The present study is aimed to identify influence of Lakhta-Center visibility by means of photofixation results' analysis and their comparison with the results of the landscape and visual analysis performed by the Saint Petersburg Regional Committee of ... ...

Abstract	The present study is aimed to identify influence of Lakhta-Center visibility by means of photofixation results' analysis and their comparison with the results of the landscape and visual analysis performed by the Saint Petersburg Regional Committee of the International Council on Monuments and Sights (ICOMOS), report on research of Lakhta-Center high-rise dominant visibility influence on Saint Petersburg protected panoramas (2012), and assessment analysis of requested deviations' influence on formation of compositional and environmental characteristics of the urban environment based on a 3D reference model of the Saint Petersburg territory (2011). The study is supported by actual photos of cityscapes, thus, allowing assessing the situation reasonably and rationally. The performed work resulted in graphic materials, including photos and maps with reviews and classification of Lakhta-Center visibility upon perception of the main city panoramas from the tourist route combining the most popular sights of the city.
Keywords	Environmental sciences ; GE1-350
Language	English
Publishing date	2020-01-01T00:00:00Z
Publisher	EDP Sciences
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: What is the future of bromodomains in targeted drug development?

Fedorov, Oleg

Future medicinal chemistry

2014 Volume 6, Issue 10, Page(s) 1101–1103

MeSH term(s)	Animals ; Chromatin/metabolism ; Drug Discovery/methods ; Histone Acetyltransferases/antagonists & inhibitors ; Histone Acetyltransferases/metabolism ; Humans ; Molecular Targeted Therapy/methods ; Protein Methyltransferases/antagonists & inhibitors ; Protein Methyltransferases/metabolism ; Transcription Factors/antagonists & inhibitors ; Transcription Factors/metabolism
Chemical Substances	Chromatin ; Transcription Factors ; Protein Methyltransferases (EC 2.1.1.-) ; Histone Acetyltransferases (EC 2.3.1.48)
Language	English
Publishing date	2014-06
Publishing country	England
Document type	Editorial
ISSN	1756-8927
ISSN (online)	1756-8927
DOI	10.4155/fmc.14.64
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Choosing variable-frequency drive systems for the mining process units

Kugusheva Natalia / Semenov Alexander / Yakushev Ilya / Pavlova Svetlana / Egorov Ayaal / Fedorov Oleg

E3S Web of Conferences, Vol 244, p

2021 Volume 09011

Abstract: Mining enterprises are energy intensive facilities. The capacity of single technological units can reach 5 MW. Variable-frequency drive systems are often used to set them in motion. The paper analyzes the features of choosing and using variable-frequency ...

Abstract	Mining enterprises are energy intensive facilities. The capacity of single technological units can reach 5 MW. Variable-frequency drive systems are often used to set them in motion. The paper analyzes the features of choosing and using variable-frequency drives under diamond mining conditions. The study objective is to formulate and formalize the problems of introducing and operating variable-frequency drives at diamond-mining enterprises to further develop and implement guidelines for improving the performance of this drive type. To achieve this objective, the use of variable frequency drives in various process units of diamond mining should be studied and analyzed. The units are considered, for which in recent years, electric drive systems have been groundlessly (according to the authors) chosen by the engineering staff of enterprises. A technical and economic comparison of low-voltage frequency converters with the same power but different control modes is performed. The economic indicators of introducing high-voltage and low-voltage frequency converters into an existing electric drive system are calculated and represented as a comparative table. Conclusions are made on the need to proceed with the research and develop guidelines for implementing frequency converters at diamond-mining enterprises.
Keywords	Environmental sciences ; GE1-350
Subject code	600
Language	English
Publishing date	2021-01-01T00:00:00Z
Publisher	EDP Sciences
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Imidazo[1,2-b]pyridazines as inhibitors of DYRK kinases.

Henderson, Scott H / Sorrell, Fiona J / Bennett, James M / Fedorov, Oleg / Hanley, Marcus T / Godoi, Paulo H / Ruela de Sousa, Roberta / Robinson, Sean / Navratilova, Iva Hopkins / Elkins, Jonathan M / Ward, Simon E

European journal of medicinal chemistry

2024 Volume 269, Page(s) 116292

Abstract: Selective inhibitors of DYRK1A are of interest for the treatment of cancer, Type 2 diabetes and neurological disorders. Optimization of imidazo [1,2-b]pyridazine fragment 1 through structure-activity relationship exploration and in silico drug design ... ...

Abstract	Selective inhibitors of DYRK1A are of interest for the treatment of cancer, Type 2 diabetes and neurological disorders. Optimization of imidazo [1,2-b]pyridazine fragment 1 through structure-activity relationship exploration and in silico drug design efforts led to the discovery of compound 17 as a potent cellular inhibitor of DYRK1A with selectivity over much of the kinome. The binding mode of compound 17 was elucidated with X-ray crystallography, facilitating the rational design of compound 29, an imidazo [1,2-b]pyridazine with improved kinase selectivity with respect to closely related CLK kinases.
MeSH term(s)	Humans ; Dyrk Kinases ; Diabetes Mellitus, Type 2/drug therapy ; Protein Kinase Inhibitors/chemistry ; Structure-Activity Relationship ; Pyridazines/chemistry ; Iohexol/analogs & derivatives
Chemical Substances	Dyrk Kinases (EC 2.7.1.-) ; compound 17 (31122-84-6) ; Protein Kinase Inhibitors ; Pyridazines ; Iohexol (4419T9MX03)
Language	English
Publishing date	2024-03-07
Publishing country	France
Document type	Journal Article
ZDB-ID	188597-2
ISSN	1768-3254 ; 0009-4374 ; 0223-5234
ISSN (online)	1768-3254
ISSN	0009-4374 ; 0223-5234
DOI	10.1016/j.ejmech.2024.116292
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Article ; Online: Analysis of the global energy resource market

Volotkovskaya Yulia / Volotkovskaya Natalya / Semenov Alexander / Semkova Anastasia / Fedorov Oleg / Vladimirov Oleg

E3S Web of Conferences, Vol 178, p

2020 Volume 01058

Abstract: The paper analyses the global demand for various energy resources in recent years. Nowadays, qualitative and quantitative changes in structure of distribution and consumption of energy resources take place. The paper has reviewed a number of papers ... ...

Abstract	The paper analyses the global demand for various energy resources in recent years. Nowadays, qualitative and quantitative changes in structure of distribution and consumption of energy resources take place. The paper has reviewed a number of papers predicting two-fold increase in the global energy production market by 2040. A number of other papers also predict the shift of energy demand from the USA and EU countries to the Asian market. The paper presents percentage distribution of world’s energy requirements satisfied by the six types of resources among which oil, gas, and coil are still predominant. Some papers have stated that the demand for natural gas will continue to grow faster than the demand for oil or coil in the future. To confirm or deny this theory the authors have designed the mathematical model showing trends in demand for gas compared to the total demand for oil and coal; as a result, two different polynomial functions have been obtained with almost the same probability confirming this prediction. Trends in energy production and change of global energy demand across regions over the past twenty years have been studied. The studies show that, in general, energy production has been increased for the last decade. However, due to economic crises fluctuations, energy production in EU countries has abruptly decreased; it results in displacement of the EU countries from the market by the countries of the Middle East and the Near East. The paper also notes such important factors as decrease in solid fuel production in Great Britain; steady increasing importance of renewable energy sources for the last few years; reducing of the rate of nuclear energy development by some key countries; general lack of energy recourses in EU countries, etc.
Keywords	Environmental sciences ; GE1-350
Subject code	690 ; 339
Language	English
Publishing date	2020-01-01T00:00:00Z
Publisher	EDP Sciences
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Influence of smart metering systems on increasing the accuracy of calculation electrical power losses in electrical networks

Musaev Timur / Khabibullin Marat / Kamaliev Ramil / Fedorov Oleg / Valeev Ilgiz / Vladimirov Oleg

E3S Web of Conferences, Vol 220, p

2020 Volume 01026

Abstract: The article discusses the possibility of using data from smart electricity meters (SEM) to increase the accuracy of calculation losses in 0.4 kV low-voltage networks. An increase in accuracy can be achieved using actual data about the load graph of ... ...

Abstract	The article discusses the possibility of using data from smart electricity meters (SEM) to increase the accuracy of calculation losses in 0.4 kV low-voltage networks. An increase in accuracy can be achieved using actual data about the load graph of electricity consumers (in this case, 6(10)-0.4 kV transformer substations are meant). To date, the operating load factor is taken equal to 0.5, which does not always correspond to the actual data. Using SEM, actual load graphs can be obtained, which enable more accurate determination of the operating load factor. Consequently, the accuracy of calculation of electrical energy losses will be increased.
Keywords	Environmental sciences ; GE1-350
Language	English
Publishing date	2020-01-01T00:00:00Z
Publisher	EDP Sciences
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Automatic voltage regulation system construction for synchronous generator of a small hydro power plant using thyristor pathogens

Kadyrov Ishembek / Karaeva Nurzat / Andarbekov Zheenbek / Azamat Bakytuulu / Fedorov Oleg / Vladimirov Oleg

E3S Web of Conferences, Vol 178, p

2020 Volume 01036

Abstract: The article presents indicators of the hydropower potential of Kyrgyzstan, shows the share of small hydropower plants in the production of electric energy in the energy sector of the republic, reveals the problematic issues that need to be revealed in ... ...

Abstract	The article presents indicators of the hydropower potential of Kyrgyzstan, shows the share of small hydropower plants in the production of electric energy in the energy sector of the republic, reveals the problematic issues that need to be revealed in this work. A brief description of the existing automatic voltage regulation system and automatic field blanking system is given. Based on the analysis of existing systems, their shortcomings were identified and the main functions formulated for automatic voltage regulation systems in both static and dynamic modes associated with starting and stopping the generator, loading and dumping, as well as protective measures taken to ensure reliability operation of the hydraulic unit. The result of the research is the development of the main functional blocks in the system of automatic voltage regulation with a thyristor pathogen and a brief explanation of their work. The synthesis technique of the excitation current regulator of a synchronous generator and the main indicators obtained in the modernization process are shown. In conclusion, all the functions inherent in the modernized system for automatically controlling the excitation of a synchronous generator, aimed at the safe operation of the hydraulic unit, are noted.
Keywords	Environmental sciences ; GE1-350
Subject code	600
Language	English
Publishing date	2020-01-01T00:00:00Z
Publisher	EDP Sciences
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Light-Mediated Dual Phosphine-/Copper-Catalyzed Atom Transfer Radical Addition Reaction.

Fedorov, Oleg V / Scherbinina, Sofya I / Levin, Vitalij V / Dilman, Alexander D

The Journal of organic chemistry

2019 Volume 84, Issue 17, Page(s) 11068–11079

Abstract: The atom transfer radical addition reaction catalyzed by triphenylphosphine and copper(I) halide is described. The reaction proceeds under irradiation with 365 nm light using a light-emitting diode and was performed in regular glassware. The proposed ... ...

Abstract	The atom transfer radical addition reaction catalyzed by triphenylphosphine and copper(I) halide is described. The reaction proceeds under irradiation with 365 nm light using a light-emitting diode and was performed in regular glassware. The proposed mechanism involves the formation of quaternary phosphonium salt, which undergoes single electron reduction by copper(I) salt via photo-induced electron transfer. The method works well for terminal alkenes and activated organic halides such as esters of bromo- and iodoacetic acid and bromoacetonitrile.
Language	English
Publishing date	2019-08-26
Publishing country	United States
Document type	Journal Article
ZDB-ID	123490-0
ISSN	1520-6904 ; 0022-3263
ISSN (online)	1520-6904
ISSN	0022-3263
DOI	10.1021/acs.joc.9b01649
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Article ; Online: Discovery of a Potent, Selective, and Cell-Active SPIN1 Inhibitor.

Xiong, Yan / Greschik, Holger / Johansson, Catrine / Seifert, Ludwig / Gamble, Vicki / Park, Kwang-Su / Fagan, Vincent / Li, Fengling / Chau, Irene / Vedadi, Masoud / Arrowsmith, Cheryl H / Brennan, Paul / Fedorov, Oleg / Jung, Manfred / Farnie, Gillian / Liu, Jing / Oppermann, Udo / Schüle, Roland / Jin, Jian

Journal of medicinal chemistry

2024 Volume 67, Issue 7, Page(s) 5837–5853

Abstract: The methyl-lysine reader protein SPIN1 plays important roles in various human diseases. However, targeting methyl-lysine reader proteins has been challenging. Very few cellularly active SPIN1 inhibitors have been developed. We previously reported that ... ...

Abstract	The methyl-lysine reader protein SPIN1 plays important roles in various human diseases. However, targeting methyl-lysine reader proteins has been challenging. Very few cellularly active SPIN1 inhibitors have been developed. We previously reported that our G9a/GLP inhibitor UNC0638 weakly inhibited SPIN1. Here, we present our comprehensive structure-activity relationship study that led to the discovery of compound
MeSH term(s)	Humans ; Animals ; Mice ; Structure-Activity Relationship ; Tudor Domain ; Lysine
Chemical Substances	methyl-lysine ; Lysine (K3Z4F929H6)
Language	English
Publishing date	2024-03-27
Publishing country	United States
Document type	Journal Article
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.4c00121
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Article ; Online: DFG-1 Residue Controls Inhibitor Binding Mode and Affinity, Providing a Basis for Rational Design of Kinase Inhibitor Selectivity.

Schröder, Martin / Bullock, Alex N / Fedorov, Oleg / Bracher, Franz / Chaikuad, Apirat / Knapp, Stefan

Journal of medicinal chemistry

2020 Volume 63, Issue 18, Page(s) 10224–10234

Abstract: Selectivity remains a challenge for ATP-mimetic kinase inhibitors, an issue that may be overcome by targeting unique residues or binding pockets. However, to date only few strategies have been developed. Here we identify that bulky residues located N- ... ...

Abstract	Selectivity remains a challenge for ATP-mimetic kinase inhibitors, an issue that may be overcome by targeting unique residues or binding pockets. However, to date only few strategies have been developed. Here we identify that bulky residues located N-terminal to the DFG motif (DFG-1) represent an opportunity for designing highly selective inhibitors with unexpected binding modes. We demonstrate that several diverse inhibitors exerted selective, noncanonical binding modes that exclusively target large hydrophobic DFG-1 residues present in many kinases including PIM, CK1, DAPK, and CLK. By use of the CLK family as a model, structural and biochemical data revealed that the DFG-1 valine controlled a noncanonical binding mode in CLK1, providing a rationale for selectivity over the closely related CLK3 which harbors a smaller DFG-1 alanine. Our data suggest that targeting the restricted back pocket in the small fraction of kinases that harbor bulky DFG-1 residues offers a versatile selectivity filter for inhibitor design.
MeSH term(s)	Binding Sites ; Crystallography, X-Ray ; Humans ; Hydrophobic and Hydrophilic Interactions ; Mutagenesis, Site-Directed ; Mutation ; Protein Binding ; Protein Domains ; Protein Kinase Inhibitors/chemistry ; Protein Kinase Inhibitors/metabolism ; Protein-Serine-Threonine Kinases/chemistry ; Protein-Serine-Threonine Kinases/genetics ; Protein-Serine-Threonine Kinases/metabolism ; Protein-Tyrosine Kinases/chemistry ; Protein-Tyrosine Kinases/genetics ; Protein-Tyrosine Kinases/metabolism
Chemical Substances	Protein Kinase Inhibitors ; Clk dual-specificity kinases (EC 2.7.1.-) ; Protein-Tyrosine Kinases (EC 2.7.10.1) ; Protein-Serine-Threonine Kinases (EC 2.7.11.1)
Language	English
Publishing date	2020-08-27
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.0c00898
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