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wszystkich: 2029
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- Publikacje 1537 wyników po odfiltrowaniu
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Synthesis of the inosine 5'-monophosphate dehydrogenase (IMPDH) inhibitors
PublikacjaIn this review are summrized newly described IMPDH inhibitors. The article concerns both synthetic pathways and biological activities of the most promising compounds.
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Novel synthesis scheme and in vitro antimicrobial evaluation of a panel of (E)-2-aryl-1-cyano-1-nitroethenes
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Synthesis of the inosine 5′-monophosphate dehydrogenase (IMPDH) inhibitors
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Antiglycoxidative properties of amantadine – a systematic review and comprehensive in vitro study
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The synthesis and biological activity of lipophilic derivatives of bicine conjugated with n3-(4-methoxyfumaroyl)-l-2,3-diaminopropanoic acid(fmdp) - an inhibitor of glucosamine-6-phosphate synthase
PublikacjaOtrzymano serię pochodnych bicyny połączonych z inhibitorem syntazy glukozamino-6-fosforanu (fmdp)oraz zbadano ich właściwości lipofilowe i aktywność przeciwgrzybową. otrzymane związki charakteryzowały się wyższą llipofilowością niż fmdp. wszystkie otrzymane związki wykazywały także wyższą aktywność przeciwgrzybową niż fmdp.
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Chemical reactivity and antimicrobial activity of N-substituted maleimides
PublikacjaZsyntezowano kilkanaście N-podstawionych maleimidów, zawierających w swojej strukturze podstawniki o różnej wielkości i polarności.Maleimidy o charakterze obojętnym wykazywały silny efekt przeciwgrzybowy; ich aktywność przeciwbakteryjna była zróżnicowana. Niską aktywność przeciwbakteryjną, ale wysoką aktywność cytostatyczną stwierdzono dla maleimidów o charakterze zasadowym. Reaktywność chemiczna i lipofilowość miały wpływ na aktywność...
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Flavonoids as inhibitors of human neutrophil elastase
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Flavonoids as tyrosinase inhibitors in in silico and in vitro models: basic framework of SAR using a statistical modelling approach
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Development of potent and effective SARS-CoV-2 main protease inhibitors based on maleimide analogs for the potential treatment of COVID-19
PublikacjaIn the present work, we report a new series of potent SARS-CoV-2 Main Protease (Mpro) inhibitors based on maleimide derivatives. The inhibitory activities were tested in an enzymatic assay using recombinant Mpro (3CL Protease from coronavirus SARS-CoV-2). Within the set of new Mpro inhibitors, 6e demonstrated the highest activity in the enzymatic assay with an IC50 value of 8.52 ± 0.44 mM. The IC50 value for Nirmatrelvir (PF-07321332,...
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Palindromic carbazole derivatives: unveiling their antiproliferative effect via topoisomerase II catalytic inhibition and apoptosis induction
PublikacjaHuman DNA topoisomerases are essential for crucial cellular processes, including DNA replication, transcription, chromatin condensation, and maintenance of its structure. One of the significant strategies employed in cancer treatment involves the inhibition of a specific type of topoisomerase, known as topoisomerase II (Topo II). Carbazole derivatives, recognised for their varied biological activities, have recently become a significant...
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Novel amides of mycophenolic acid and some heterocyclic derivatives as immunosuppressive agents
PublikacjaThe group of new amide derivatives of mycophenolic acid (MPA) and selected heterocyclic amines was synthesised as potential immunosuppressive agents functioning as inosine-5'-monophosphate dehydrogenase (IMPDH) uncompetitive inhibitors. The synthesis employed uronium-type activating system (TBTU/HOBt/DIPEA) while or phosphonic acid anhydride method (T3P/Py) facilitating amides to be obtained in moderate to excellent yields without...
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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
PublikacjaIn 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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Design, synthesis and biological evaluation of novel N-phosphorylated and O-phosphorylated tacrine derivatives as potential drugs against Alzheimer’s disease
PublikacjaIn this work, we designed, synthesised and biologically investigated a novel series of 14N- and O-phosphorylated tacrine derivatives as potential anti-Alzheimer’s disease agents. In the reaction of 9-chlorotacrine and corresponding diamines/aminoalkylalcohol we obtained diamino and aminoalkylhydroxy tacrine derivatives. Next, the compounds were acid to give final products 6–13 and 16–21 that were characterised by 1H, 13 C, 31P...
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Generalized temperature dependence model for anammox process kinetics
PublikacjaTemperature is a key operational factor influencing the anammox process kinetics. In particular, at temperatures below 15 °C, the specific anammox activity (SAA) considerably decreases. This study aimed to describe the temperature dependence of the anammox process kinetics in the temperature range from 10 to 55 °C, including the specific characteristics of“cold anammox”. The commonly used Arrhenius and extended and modifiedRatkowsky...
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The New LM-PCR/Shifter Method for the Genotyping of Microorganism
PublikacjaTechniques relies on the ligation of appropriates adapters (LM-PCR) as AFLP, PCR MP and ADSRRS are successfully used for epidemiological studies for prokaryotic and eukaryotic microorganisms. In this study we propose a new method, called the LM-PCR/Shifter, based on the use of a Class IIS restriction enzyme giving restriction fragments with different 4 base 5' overhangs (Shifter) and the ligation of appropriate oligonucleotide...
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Targeting Spike‐ACE2 Interface of SARS‐CoV‐2 and its Omicron Variant: A Comparative Screening of Potential Inhibitors for Existing and Anticipating Variants Using Molecular Modelling Approach
PublikacjaThe recent COVID pandemic has shown major impact on public health and economic crisis. Despite the development of many vaccines and drugs against the severe acute respiratory syndrome (SARS) coronavirus 2, the pandemic still persists. The continued spread of the virus is largely driven by the emergence of viral variants such as α, β, γ, delta, epsilon spike, omicron and its subvariants (BA.1,2,3) which can evade the current vaccines...
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A Novel Cryptic Clostridial Peptide That Kills Bacteria by a Cell Membrane Permeabilization Mechanism
PublikacjaThis work reports detailed characteristics of the antimicrobial peptide Intestinalin (P30), which is derived from the LysC enzyme of Clostridium intestinale strain URNW. The peptide shows a broader antibacterial spectrum than the parental enzyme, showing potent antimicrobial activity against clinical strains of Gram-positive staphylococci and Gram-negative pathogens and causing between 3.04 ± 0.12 log kill for Pseudomonas aeruginosa...
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Antifungal Effect of Penicillamine Due to the Selective Targeting of L-Homoserine O-Acetyltransferase
PublikacjaDue to the apparent similarity of fungal and mammalian metabolic pathways, the number of established antifungal targets is low, and the identification of novel ones is highly desirable. The results of our studies, presented in this work, indicate that the fungal biosynthetic pathway of L-methionine, an amino acid essential for humans, seems to be an attractive perspective. The MET2 gene from Candida albicans encoding L-homoserine...
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Overproduction of CaMet15p native and His-tag versions.
Dane BadawczeEnzyme of fungal L-methionine biosynthetic pathway: O-acetylhomoserine sulfhydrylase (Met15p) could be exploited as molecular target for antifungal chemotherapy. The goal of the study was to obtain conditions optimal for protein production with the use of prokaryotic cells. The constructed expression plasmids, designed in three different versions: encoding...
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The electrochemical studies of CB-PLA electrode after surface activation by proteinase K digestion
Dane BadawczeThe dataset contains the electrochemical studies performed to evaluate surface activation of the CB-PLA 3D printed electrodes by enzymatic hydrolysis in a solution containing proteinase K (72h digestion period). Different enzyme concentrations were evaluated: 0.2, 0.4, 0.6 and 0.8 mg/ml. The studies were performed before surface activation, during and...
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Overproduction of CaStr2p native and His-tag versions.
Dane BadawczeEnzyme of fungal L-methionine biosynthetic pathway: cystathionine-γ-synthase (CaStr2p) could be exploited as molecular target for antifungal chemotherapy. The goal of the study was to obtain conditions optimal for protein production with the use of prokaryotic cells. The constructed expression plasmids, designed in three different versions: encoding...
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Overproduction of homoserine O-acetyltransferase (CaMet2p) native and His-tag versions.
Dane BadawczeEnzyme of fungal L-methionine biosynthetic pathway: homoserine O-acetyltransferase (Met2p) could be exploited as molecular target for antifungal chemotherapy. The goal of the study was to obtain conditions optimal for protein production with the use of prokaryotic cells. The constructed expression plasmids, designed in three different versions: encoding...
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Chronic without haemorrhage or perforation - Male, 62 - Tissue image [4140730008823991]
Dane BadawczeThis is the histopathological image of STOMACH tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.
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Marek Przyborski dr hab. inż.
OsobyMarek Przyborski (ur. 20.03.1964 r. w Chełmży) – specjalista z zakresu teledetekcji i fotogrametrii bliskiego zasięgu. Prowadzi badania w zakresie wykorzystania tzw. „szybkich kamer” do analizy zjawisk szybkozmiennych. Współautor i autor publikacji traktujących o szeroko rozumianej teledetekcji w zastosowaniach związanych z budownictwem, transportem, inżynierią środowiska oraz bezpieczeństwem narodowym. Jest autorem licznych publikacji...
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Fatty acids as molecular carriers in cleavable antifungal conjugates
PublikacjaConjugates composed of C2-18 fatty acid (FA) residues as a molecular carrier and 5-fluorocytosine (5-FC) as an active agent, released upon the action of intracellular esterases on the ester bond between FA and “trimethyl lock” intramolecular linker, demonstrate good in vitro activity against human pathogenic yeasts of Candida spp. The minimal inhibitory concentrations (MIC) values for the most active conjugates containing caprylic...
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Związki biologicznie aktywne w żywności i napojach
PublikacjaJuż od dłuższego czasu daje się zauważyć wzrost zainteresownia związkami biologicznie aktywnymi w żywności (szczególnie pochodzenia roślinnego) oraz napojach i sokach. W wielu ośrodkach naukowych trwają badania ukierunkowane na określenie aktywności przeciwutleniającej badanych próbek oraz oznaczenie zawartości polifenoli i innych związków o właściwościach przeciwutleniających (m.in. witaminy C oraz tokoferoli). W pracy przedstawiono...
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DDLMS PCR double digestion Ligation Mediated Suppression PCR - a new technique for bacterial specific differentiation
PublikacjaA new diagnostic kit for K. oxytoca specific differentiation based on ddLMS PCR (ang. double digest ligation Mediated PCR) technique is shown. As a species-specific DNA fragment pehX gene, encoding the enzyme polygalactouronase, was chosen. The genome sequence of K. oxytoca is digested with two endonucleases: AclI and BclI which cut DNA before and after pehX gene. The polymorphic DNA fragments are ligated with AclI-end-specific...
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Which transport policies increase physical activity of the whole of society? A systematic review
PublikacjaPurpose: There is strong evidence of the links between car-dependence and the physical inactivity pandemic. Physical inactivity accounts for 6–10% of major non-communicable diseases. Research consistently shows that unlike passive transport, active transport is associated with higher total daily physical activity (PA). While there are public policies that support PA in transport and, as a result, overall PA levels, the specific...
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The Use of an Autoencoder in the Problem of Shepherding
PublikacjaThis paper refers to the problem of shepherding clusters of passive agents consisting of a large number of objects by a team of active agents. The problem of shepherding and the difficulties that arise with the increasing number of data describing the location of agents have been described. Several methods for reducing the dimensionality of data are presented. Selected autoencoding method using a Restricted Boltzmann Machine is...
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Jednofazowy falownik napięcia z aktywnym obwodem odsprzęgającym
PublikacjaZnanym zagadnieniem w jednofazowych falownikach napięcia jest pobieranie ze źródła napięcia stałego składowej przemiennej o częstotliwości dwukrotnie większej od częstotliwości generowanej przez falownik. Jednym z rozwiązań problemu jest stosowanie dużej baterii kondensatorów elektrolitycznych, lecz lepszym sposobem z punktu widzenia niezawodności i gęstości mocy przekształtnika jest stosowanie aktywnych układów odsprzęgania mocy....
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Antibacterial evaluation of bioactive modifiers of bone cements: antibiotics, nanometals and chitosan
PublikacjaModern biomaterials in addition to their basic tasks, can serve as carriers of active substance. The release of a bioactive particles allows to locally fight infection or its prevent it. Bone cements additionally to their basic applications in orthopedic surgery can also serve to deliver locally active substances. Currently, only antibiotics are routinely used as modifiers for bone cements. Bioactive bone cements constitute...
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Beta-galactosidases from a psychrotolerant Arthrobacter isolates and their potential use
PublikacjaEnzymes from extremophiles, especially psychrophiles and psychrotolerant microorganisms are currently intensively studied because of their unusual structural and functional properties. One of these enzymes is a cold-adapted - galactosidase (EC 3.2.1.23) which catalyzes the hydrolysis of - 1,4-glycosidic bonds in -galactosides. The most common - galactoside is lactose, a disaccharide which makes up 2-7% of milk. The majority of...
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WSPÓŁPRACA BLOKU GAZOWO-PAROWEGO Z OBIEGIEM ORC = Combinded power plant in cooperation with ORC
PublikacjaIn the paper presented is the idea of a combined gas and steam power plant cooperation with a low temperature organic Rankine cycle ORC unit. Considerations presented in the paper are accomplished for the Gorzów CHP. The intention of present analysis is heat recovery of low temperature energy and its further use in ORC cycle in order to produce electricity, without increase in fuel consumption. Waste energy is recovered from the...
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TRUSS JOINT WITH POSITIVE ECCENTRICITY EXPERIMENTAL RESEARCH
PublikacjaDue to the technological reasons in modern lightweight steel trusses, fabricated from cold- formed sections, positive eccentricities appear in the truss nodes what induce additional forces in the truss chords. To account for the real load-carrying capacity of truss node area the steel structure research in scale 1:1 were conducted. The experiments consisted of two parts: preliminary and proper one, when conclusions from...
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Amino Acid Based Antimicrobial Agents – Synthesis and Properties
PublikacjaStructures of several dozen of known antibacterial, antifungal or antiprotozoal agents are based on the amino acid scaffold. In most of them, the amino acid skeleton is of a crucial importance for their antimicrobial activity, since very often they are structural analogs of amino acid intermediates of different microbial biosynthetic pathways. Particularly, some aminophosphonate or aminoboronate analogs of protein amino acids are...
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Chronic viral hepatitis B without delta-agent - Male, 41 - Tissue image [4090730007938341]
Dane BadawczeThis is the histopathological image of LIVER AND INTRAHEPATIC BILE DUCTS tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.
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Chronic viral hepatitis B without delta-agent - Male, 41 - Tissue image [4090730007934111]
Dane BadawczeThis is the histopathological image of LIVER AND INTRAHEPATIC BILE DUCTS tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: Pannoramic 250 3DHistech slide scanner (20x magnification) and saved to DICOM format.
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Thermal self-action effects of acoustic beam in a vibrationally relaxing gas
PublikacjaThermal self-action of acoustic beam in a molecular gas with excited internal degrees of molecules’ freedom, is studied. This kind of thermal self-action differs from that in a Newtonian fluid. Heating or cooling of a medium takes place due to transfer of internal vibrational energy. Equilibrium and non-equilibrium gases, which may be acoustically active, are considered. A beam in an acoustically active gas is self-focusing unlike...
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Augmenting digital documents with negotiation capability
PublikacjaActive digital documents are not only capable of performing various operations using their internal functionality and external services, accessible in the environment in which they operate, but can also migrate on their own over a network of mobile devices that provide dynamically changing execution contexts. They may imply conflicts between preferences of the active document and the device the former wishes to execute on. In the...
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A robust 18-pulse diode rectifier with coupled reactors
PublikacjaThe article presents the principle of operation and selected results of simulation and laboratory tests of the 18-pulse rectifier system with coupled reactors and small series active power filter. The presented system makes it possible to reduce, especially in distribution supply networks, undesired higher current harmonics. The 18-pulse nature of operation of the rectifier is reached using a set of coupled three-phase network...
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Power electronic transformer based on cascaded H-bridge converter
PublikacjaIn this paper the control strategy of power electronic transformer (PET) is proposed. The analyzed structure of PET uses two seven-level cascaded H-bridge (CHB) rectifiers. The electrical power of PET is transferred between DC-links of CHB converters using dual-active-bridges (DABs) and low voltage high frequency transformers. The roposed solution allows for controlling the active and reactive power with a low level of harmonic...
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Ancillary services to grids provided with distributed generation
PublikacjaThe paper introduces system for utilization of the customer-side generated energy. Additionally system can secure some ancillary services to grids. Those services include: current active filtering, load voltage stabilization and in case of grid voltage faults - uninterruptible load supplying (possible with energy storage device). Presented experimental results confirm flexibility of this arrangement in processes of power delivery...
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Characterization of recombinant homocitrate synthase from Candida albicans
PublikacjaLYS21 and LYS22 genes from Candida albicans encoding isoforms of homocitrate synthase (HCS), an enzyme catalyzing the first committed step in the L-lysine biosynthetic pathway, were cloned and expressed as NoligoHistagged fusion proteins in Escherichia coli. The purified gene products revealed HCS activity, i.e. catalyzed the condensation of α-ketoglutarate with acetyl-coenzyme A to yield homocitrate. The recombinant enzymes were purified...
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Progress, Challenge, and Perspective of Bimetallic TiO2-Based Photocatalysts
PublikacjaBimetallic TiO2-based photocatalysts have attracted considerable attention in recent years as a class of highly active catalysts and photocatalysts under both UV and Vis light irradiation. Bimetallic noble metal structures deposited on TiO2 possess the ability to absorb visible light, in a wide wavelength range (broad LSPR peak), and therefore reveal the highest level of activity as a result of utilization of a large amount of...
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Effect of copper and silver modification of NH2-MIL-125(Ti) on the photoreduction of carbon dioxide to formic acid over this framework under visible-light irradiation
PublikacjaCu and Ag enhance the photocatalytic activities of metal–organic frameworks (MOFs) toward CO2 conversion because of their CO2 adsorption capacities and effects on the lowest unoccupied molecular orbital (LUMO) overpotentials of MOFs. However, to date, targeted introduction of metals into MOFs to achieve visible (Vis)- light-active photocatalysts for CO2 photoconversion has not been realized. Herein, a series of aminefunctionalized...
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Smart acoustic band structures
PublikacjaSmart acoustic band structures exhibit very interesting and non-standard physical properties due to the periodic nature of their certain characteristic on different scale levels. They manifest mostly in their frequency spectra as socalled frequency band-gaps or stop-bands, what has a great impact on the behaviour of these structures in relation to the propagation of vibro-acoustic signals that can be transmitted through the structures...
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Heat transfer in plate heat exchanger channels: experimental validation of selected correlation equations
PublikacjaThis study is focused on experimental investigation of selected type of brazed plate heat exchanger. The Wilson approach was applied in order to estimate heat transfer coefficients for the PHEx passages. The main aim of the paper was to experimentally check ability of several correlations published in the literature to predict heat transfer coefficients by comparison experimentally obtained data with appropriate predictions. The...
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Heat transfer in plate heat exchanger channels: experimental validation of selected correlation equations
PublikacjaThis study is focused on experimental investigation of selected type of brazed plate heat exchanger. The Wilson approach was applied in order to estimate heat transfer coefficients for the PHEx passages. The main aim of the paper was to experimentally check ability of several correlations published in the literature to predict heat transfer coefficients by comparison experimentally obtained data with appropriate predictions. The...
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A new division of bacterial UvrA homologues
PublikacjaThe UvrA protein is a DNA-binding and damage-recognition enzyme which participates in the prokaryotic type nucleotide excision repair (NER) pathway. It has recently been noted that some bacterial genomes comprise additional uvrA genes which encode five distinct types of UvrA homologue. We investigated the sequences of over 2400 bacterial genomes and found 130 examples of bacteria containing uvrA 2 genes. The sequence analyses conducted...
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Polysaccharides-Based Hybrid Materials for Bio- and Non-Bio Sectors. Edytorial
PublikacjaThis special edition spotlights the recent research in the design, development, and emerging applications of polysaccharides-based hybrid materials for biotechnological and biomedical purposes. All the articles published in this issue underscore the significance of materials derived from cellulose, alginate, chitosan, starch, and carrageenan for various applications, including enzyme production, encapsulation, targeted drug delivery,...