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Search results for: STS
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Analiza awarii masztów na STS Pogoria
Publication''Pogoria'' - żaglowiec szkolny uczestniczyła w trakcie ''TALL SHIP RACE 2009'' w rejsie na trasie Gdynia-St.Petesburg. W dniu 7 lipca 2009 roku w trakcie bezpośredniej rywalizacji z płynącą obok siostrzaną - nieco młodszą - ''Kaliakrą'' (jacht płynął lewym halsem, kursem 055, przy wietrze ESE o sile 6B), podczas nadmiernego wyostrzenia do wietru, nastąpiło złamanie fokmasztu, a w konsekwencji - pozostałych dwóch masztów. W artykule...
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Nanostructure characterization of (SmS)1.19TaS2 by means of STM/STS
PublicationW publikacji przedstawiono badania za pomocą techniki STM i STS powierzchni kryształów warstwowego związki typu misfit(SmS)1.19TaS2. Badania pozwalają sądzić, że powierzchniową warstwą jest warstwa Sm-S.
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Trajectory planning for Service Ship during emergency STS transfer operation
PublicationIn this paper trajectory for approaching during emergency STS transfer operation with oil spill is considered as a sequence of navigation manoeuvres in specific navigational environment. The designed way points - ship positions and speed are determined as reference values to support navigator in decision making during steering and to mitigate the risk of collision which mostly results from exceeding the speed limit of approaching....
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Geometry optimization of steroid sulfatase inhibitors - the influence on the free binding energy with STS
PublicationIn the paper we review the application of two techniques (molecular mechanics and quantum mechanics) to study the influence of geometry optimization of the steroid sulfatase inhibitors on the values of descriptors coded their chemical structure and their free binding energy with the STS protein. We selected 22 STS-inhibitors and compared their structures optimized with MM+, PM7 and DFT B3LYP/6–31++G* approaches considering separately...
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Navigational decision support system during approach manoeuvre in emergency STS transfer operation
PublicationThe paper is concerned with the problem of safe trajectory planning for approaching during emergency STS (Ship to Ship) transfer operation with oil spill. The safe trajectory means that the way points does not cross in the area of the environment with the static and dynamic obstacles and at the same time satisfies ship's stopping and speed deceleration performance. The evolutionary path planning algorithm is used to determine trajectory...
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New potent STS inhibitors based on fluorinated 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamates
PublicationA series of fluorinated analogs based on the frameworks of 4-(1- phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamates have been synthesized as steroid sulfatase (STS) inhibitors. The design of chemical structures of new potential STS inhibitors was supported by molecular docking techniques to identify potential interactions between inhibitors and amino acid residues located in the STS active site. The STS inhibitory potency was evaluated...
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Projektowanie, synteza oraz badanie aktywności biologicznej nowych inhibitorów sulfatazy steroidowej (STS) na bazie amidosiarczanowych pochodnych triazoli i oksadiazoli
PublicationNiniejsza dysertacja dotyczy szeregu badań z wykorzystaniem technik modelowania molekularnego oraz metod syntezy nowych inhibitorów STS opartych o rdzenie pierścieni heterocyklicznych 1,2,3-triazolu oraz 1,2,4-oksadiazolu. Aktywność inhibicyjna otrzymanych pochodnych została oznaczona w testach in vitro z wykorzystaniem enzymu wyizolowanym z łożyska ludzkiego oraz znakowanym radioizotopowo siarczanem estronu, a także w teście komórkowych...
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Projektowanie, synteza fosforowych i tiofosforowych pochodnych kumaryny, bifenylu, tyraminy oraz flawonoidów i badanie ich aktywności biologicznej jako potencjalnych inhibitorów sulfatazy steroidowej (STS)
PublicationChoroby nowotworowe są jednym z najpoważniejszych problemów z jakimi zmaga się współczesne społeczeństwo. Rak piersi jest jedną z głównych przyczyn zgonów wśród kobiet w krajach rozwiniętych, dlatego też niezbędne jest opracowanie nowych, skutecznych metod leczenia. Podstawowym problemem w selektywnym zwalczaniu komórek nowotworowych jest ich wysokie podobieństwo do komórek prawidłowych. W związku z dowodami na znaczący udział...
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Analiza ststystyczna w zarządzaniu produkcją, Zarządzanie i inżynieria produkcji, II stopnia, sem. 1, 2022/2023
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Projektowanie synteza oraz badanie aktywności biologicznej nowych inhibitorów Sulfatazy Steroidowej (STS) na bazie związków fosforoorganicznych
ProjectsProject realized in Faculty of Chemistry according to UMO-2011/03/D/NZ7/03985 agreement from 2012-08-06
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Design, synthesis and biological evaluation of the new steroid sulfatase (STS) inhibitors based on sulfamate analogs containing C-F bonds
ProjectsProject realized in Department of Organic Chemistry according to UMO-2015/19/N/NZ7/00938 agreement from 2016-07-22
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Analysis of antibiotic resistance in Escherichia coli isolated from the Reda River and the Oliwski Stream using basic statistical methods = Zastosowanie metod ststystycznych do analizy antybiotykoodporności bakterii wskaźnikowych pochodzących z rzeki Redy i Potoku Oliwskiego
PublicationIn this study distribution of antimicrobial resistance patterns among fecal indicator bacteria (Escherichia coli and Enterococcus spp.) was examined in two watercourses. The susceptibility analyses were carried out against the antimicrobial agents, important in treating human E. coli and enterococcal infection. Water samples were obtained from the Oliwski Stream and from the Reda River. On each watercourse the five representative...
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Recent progress in the development of steroid sulfatase inhibitors – examples of the novel and most promising compounds from the last decade
PublicationThe purpose of this review article is to provide an overview of recent achievements in the synthesis of novel steroid sulfatase (STS) inhibitors. STS is a crucial enzyme in the biosynthesis of active hormones (including estrogens and androgens) and, therefore, represents an extremely attractive molecular target for the development of hormone-dependent cancer therapies. The inhibition of STS may effectively reduce the availability...
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New potent steroid sulphatase inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives
PublicationIn the present work, we report a new class of potent steroid sulphatase (STS) inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives. Within the set of new STS inhibitors, 6-(1-(1,2,3-trifluorophenyl)-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate 3L demonstrated the highest activity in the enzymatic assay inhibiting the STS activity to 7.98% at 0.5 µM concentration. Furthermore, to verify...
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Synthesis and biological evaluation of thiophosphate tricyclic coumarin derivatives as steroid sulfatase inhibitors
PublicationSteroid sulfatase (STS) enzyme inhibition is an important approach to the management of hormone-dependent breast cancer. In this paper, we report convenient methods for the synthesis and biological evaluation of thiophosphate tricyclic coumarin analogs exhibiting STS activity. The described methods are based on the straightforward preparation of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-2-one, 3-hydroxy- 7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one,...
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Novel steroid sulfatase inhibitors based on N ‐thiophosphorylated 3‐(4‐aminophenyl)‐coumarin‐7‐O‐sulfamates
PublicationIn the present work, we described convenient methods for the synthesis ofN-thiophosphorylated 3-(4-aminophenyl)-coumarin-7-O-sulfamates as steroid sulfatase(STS) inhibitors. To design the structures of the potential STS inhibitors, molecularmodeling techniques were used. A computational docking method was used to deter-mine the binding modes of the synthesized inhibitors as well as to identify potentialinteractions between specified...
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Approach Manoeuvre During Emergency Ship-to-Ship Transfer Operation with Oil Spill
PublicationOne of the major activities during Ship to Ship (STS) transfer operation at sea is to safe approach the Ship to be Lightered (SBL) which moves on a constant heading with slow speed or drifting. In the paper described the manoeuvring problem for approaching during emergency STS transfer operation with oil spill. The approach manoeuvre is considered as a sequence of navigation manoeuvres in specific navigational environment with...
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Synthesis and biological evaluation of N-acylated tyramine sulfamates containing C-F bonds as steroid sulfatase inhibitors
PublicationSteroid sulfatase (STS) is responsible for the hydrolysis of biologically inactive sulfated steroids into their active un-sulfated forms and promotes the growth of various hormone-dependent cancers (e.g., breast cancer). Therefore, the STS enzyme is a promising therapeutic target for the treatment of steroid-sensitive cancers. Herein, we report the synthesis and biological evaluation of sulfamate analogs as potential STS inhibitors...
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Synthesis and biological evaluation of fluorinated 3-phenylcoumarin-7-O-sulfamate derivatives as steroid sulfatase inhibitors
PublicationIn the present work, we report the initial results of our study on a series of 3-phenylcoumarin sulfamate-based compounds containing C-F bonds as a novel inhibitors of steroid sulfatase (STS). The new compounds are potent STS inhibitors, possessing more than 10 times higher inhibitory potency than coumarin-7-O-sulfamate. In the course of our investigation, compounds 2b and 2c demonstrated the highest inhibitory effect in the enzymatic...
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Phosphate and Thiophosphate Biphenyl Analogs as Steroid Sulfatase Inhibitors
PublicationIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate and thiophosphate biphenyl derivatives exhibiting steroid sulfatase (STS) activity. The described synthesis is based on straightforward preparation of biphenyl-4-ol and 40-hydroxybiphenyl- 4-carboxylic acid ethyl ester modified with various phosphate or thiophosphate moieties. The inhibitory effects of these compounds were...
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Synthesis and steroid sulfatase inhibitory activities of N-alkanoyl tyramine phosphates and thiophosphates
PublicationA series of phosphate and thiophosphate analogs based on the frameworks of N-alkanoyl tyramines have been synthesized and biologically evaluated. Their binding modes have been modeled using docking techniques. The inhibitory effects of the synthesized compounds were tested on STS isolated from the human placenta as well as the MCF-7, MDA-MB-231 and SkBr3 cancer cell lines. Most of the new STS inhibitors possessed potent activity...
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Synthesis of bicoumarin thiophosphate derivatives as steroid sulfatase inhibitors
PublicationBased on the frameworks of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy- 7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c] chromen-6-one, a series of bicoumarin thiophosphate analogs have been synthesized and biologically evaluated. Additionally, their binding modes have been modeled using docking techniques. The inhibitory properties of the synthesized compounds...
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Synthesis and steroid sulfatase inhibitory activities of N-phosphorylated 3-(4-aminophenyl)-coumarin-7-O-sulfamates
PublicationIn the present work, we report convenient methods for the synthesis and biological evaluation of N-phosphorylated derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as potential steroid sulfatase (STS) inhibitors. Their binding modes were modeled using docking techniques. The inhibitory effects of the synthesized compounds were tested on STS isolated from human placenta. All of the newly synthesised coumarin derivatives were...
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Steroid Sulfatase Inhibitors Based on Phosphate and Thiophosphate Flavone Analogs
PublicationA series of phosphate and thiophosphate flavone derivatives were synthesized and biologically evaluated in vitro for inhibition of steroid sulfatase (STS) activity. The described synthesis includes the straightforward preparation of 7-hydroxy-2-phenyl-4H-chromen-4-one 3a, 2-(4-fluorophenyl)-7-hydroxy-4H-chromen-4-one 3b, 7-hydroxy-2-(4-(trifluoromethyl)phenyl)-4H-chromen-4-one 3c, 7-hydroxy-2-(p-tolyl)-4H-chromen-4-one 3d modified...
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Synthesis and biological evaluation of fluorinated N-benzoyl and N-phenylacetoyl derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as steroid sulfatase inhibitors
PublicationIn the present work, we report convenient methods for the synthesis of 3-(4-aminophenyl)-coumarin-7-O-sulfamate derivatives N-acylated with fluorinated analogues of benzoic or phenylacetic acid as steroid sulfatase (STS) inhibitors. The design of these potential STS inhibitors was supported by molecular modeling techniques. Additionally, computational docking methods were used to determine the binding modes of the synthesized inhibitors...
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Krzysztof Druet dr inż.
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Phosphate tricyclic coumarin analogs as steroid sulfatase inhibitors: synthesis and biological activity.
PublicationIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate tricyclic coumarin derivatives as potential steroid sulfatase inhibitors. The described synthesis includes the straightforward preparation of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c]chromen-6-one modified...
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Structure and Randomness in Planning and Reinforcement Learning
PublicationPlanning in large state spaces inevitably needs to balance the depth and breadth of the search. It has a crucial impact on the performance of a planner and most manage this interplay implicitly. We present a novel method \textit{Shoot Tree Search (STS)}, which makes it possible to control this trade-off more explicitly. Our algorithm can be understood as an interpolation between two celebrated search mechanisms: MCTS and random...
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Projektowanie, synteza oraz badanie aktywności biologicznej amidosiarczanowych inhibitorów sulfatazy steroidowej zawierających w swojej konstytucji ugrupowania fosforowe lub wiązania C-F
PublicationWedług Światowej Organizacji Zdrowia (WHO) estrogeny są jednymi z głównych czynników stymulujących wzrost nowotworów hormonozależnych. Dlatego też, projektowanie oraz synteza nowych, skuteczniejszych środków wpływających na biosyntezę estrogenów stanowi ogromne wyzwanie dla współczesnej medycyny. W ostatnich latach liczne ośrodki naukowe na całym świecie prowadzą intensywne badania związane z poszukiwaniem nowych, skutecznych inhibitorów...
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Development of Sulfamoylated 4‑(1-Phenyl‑1H‑1,2,3-triazol-4-yl)phenol Derivatives as Potent Steroid Sulfatase Inhibitors for Efficient Treatment of Breast Cancer
PublicationWe present here the advances achieved in the development of new sulfamoylated 4-(1-phenyl-1H-1,2,3-triazol-4-yl)phenol derivatives as potent steroid sulfatase (STS) inhibitors for the treatment of breast cancer. Prompted by promising biological results and in silico analysis, the initial series of similar compounds were extended, appending a variety of m-substituents at the outer phenyl ring. The inhibition profiles of the newly...
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Case study of masts damage of the sail training vessel POGORIA
PublicationArtykuł przedstawia opis i analizę przyczyn zdarzenia polegającego na utracie masztów w lipcu 2009 przez barkentynę sts ''POGORIA'' w trakcie regat Tall Ships Race 2009. Przedstawiono podstawowe okoliczności stanowiące tło zdarzenia, dokonano anlizy przyczyn w skali globalnej, zaprezentowano analizę szczegółową utraty nośności konstrukcji stalowej, a na tym tle wypunktowano szczegółowe przyczyny leżące u źródeł wypadku. We wnioskach...
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Atimicrobial Resistance of Enterococcus spp. in Muncipal wasterwater Treatment Plant - Model Study
PublicationIn this study the removal of resistant Enterococcus spp. was evaluated using the laboratory-scale wastewater treatment model plant (M-WWTP), designed as a multiphase (anaerobic, anoxic and aerobic) system (Q = 27 dm3 per day) and continuously supplied with the wastewater obtained from the full-scale WWTP, after grid. The activated sludge from the secondary clarifier was recirculated to the anaerobic chamber (with the ratio equal...
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Obrony prac doktorskich na Wydziale Chemicznym
EventsDn. 04.11.2022 r. o godz. 11.00 w Audytorium 1.4 Wydziału Chemicznego PG (budynek nr 5) odbędzie się w trybie hybrydowym obrona pracy doktorskiej mgr. inż. Karola Biernackiego.
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May Staphylococcus lugdunensis Be an Etiological Factor of Chronic Maxillary Sinuses Infection?
PublicationStaphylococcus lugdunensis is an opportunistic pathogen found in the healthy human skin microbiome bacterial community that is able to cause infections of diverse localization, manifestation, and course, including laryngological infections, such as necrotizing sinusitis. Chronic maxillary sinusitis is a disease present in up to one third of European and American populations, and its etiology is not fully described. Within this...
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Grzegorz Ronowski dr hab. inż.
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Emerging oxidized and defective phases in low-dimensional CrCl3
PublicationTwo-dimensional (2D) magnets such as chromium trihalides CrX3 (X ¼ I, Br, Cl) represent a frontier for spintronics applications and, in particular, CrCl3 has attracted research interest due its relative stability under ambient conditions without rapid degradation, as opposed to CrI3. Herein, mechanically exfoliated CrCl3 flakes are characterized at the atomic scale and the electronic structures of pristine, oxidized, and defective...
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History of World Architecture I 2021/22
e-Learning CoursesThe course History of World Architecture (HWA I) is obligatory on the first semester of study at the Faculty of Architecture at Gdańsk University ofTechnology. It lasts 15 weeks, finishes with the exam, and consists of 15 two-hour lectures and 15 two-hour exercises. The merit of the course includes Western World architecture, beginning from Prehistory and Antiquity (Sumer, Egypt, Greece, Rome), up to the end of the Middle Ages....