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Search results for: RATIONAL DRUG DESIGN
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Biopolymer based nanomaterials in drug delivery systems: A review
PublicationDrug delivery systems (DDS) are used to achieve a higher therapeutic effects of a pharmaceutical drug or natural compound in a specific diseased site with minimal toxicological effect and these systems consists of liposomes, microspheres, gels, prodrugs and many. Nanotechnology is a rapidly developing multi-disciplinary science that ensures the fabrication of the polymers to nanometer scale for various medical applications. Uses...
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Antipsychotic drug prescription sequence analysis in relation to death occurrence and cardiometabolic drug usage: A retrospective longitudinal study
PublicationThe potential role of antipsychotics in increasing cardiovascular risk of mortality is still debated. The aim of this study was to assess the death risk associated with sequences of first-generation antipsychotic (FGA) and second-generation antipsychotic (SGA) prescriptions, including clozapine and lithium, and drugs for cardiometabolic diseases. We conducted a retrospective longitudinal analysis involving 84,881 patients who received...
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Ocena narzędzi wspomagających zarządzanie przedsięwzięciami informatycznymi na przykładzie IBM Rational Method Composer
PublicationRozdział przedstawia zalety i wady oprogramowania wspomagającego zarządzanie przedsięwzięciami informatycznymi. Skupia się na ocenie technologii informatycznej spopularyzowanej na rynku przez firmę IBM jako Rational Method Composer. W rozdziale zostały zaproponowane kryteria oceny z punktu widzenia menedżera zarządzającego przedsięwzięciem oraz oceny w zależności od stopnia spełnienia tego kryterium. Ponadto przeprowadzona została...
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Innovative design of hybrid powered inland vessel
PublicationOne of the most demanding task for European countries is rational transportation system taking into account fuel efficient and ecological propulsion. The paper presents innovative design of hybrid powered inland vessel. The most important aspects regarding new design and technical solutions are being presented, including numerical and experimental research on hull form. Combined diesel-electric propulsion supported by solar panel...
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Rational method of grit chamber efficiency determination
PublicationAlthough grot chambers are designed with utmost care, they still remain difficuly to control. As concentration of grit is non-uniform, representative measurements of the sand concentration is a very complex issue. In the paper the results of measure,ents performed at WTP in Gdańsk and Gdynia were analyzed. The proposed method to determine grit chambers efficiency is based on comparison of suspension flow in the inlet and flux of...
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Pharmacokinetics and pharmacodynamics of propofol and fentanyl in patients undergoing abdominal aortic surgery - a study of pharmacodynamic drug-drug interactions
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Drug-drug interaction potential of antitumor acridine agent C-1748: The substrate of UDP-glucuronosyltransferases 2B7, 2B17 and the inhibitor of 1A9 and 2B7
PublicationBackground The compound 9-(2′-hydroxyethylamino)-4-methyl-1-nitroacridine (C-1748), the promising antitumor agent developed in our laboratory was determined to undergo phase I metabolic pathways. The present studies aimed to know its biotransformation with phase II enzymes – UDP-glucuronosyltransferases (UGTs) and its potential to be engaged in drug-drug interactions arising from the modulation of UGT activity. Methods UGT-mediated...
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Effective Drug Concentration and Selectivity Depends on Fraction of Primitive Cells
PublicationPoor efficiency of chemotherapeutics in the eradication of Cancer Stem Cells (CSCs) has been driving the search for more active and specific compounds. In this work, we show how cell density-dependent stage culture profiles can be used in drug development workflows to achieve more robust drug activity (IC50 and EC50) results. Using flow cytometry and light microscopy, we characterized the cytological stage profiles of the HL-60-,...
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Rational determination of dynamic characteristics of fluid-flow Reactors
PublicationPodstawowa charakterystykę reaktorów stanowi krzywa rozkładu czasu zatrzymania. Jej dokładne wyznaczenie jest trudne i kosztowne. W pracy zaproponowano wykorzystanie metody aproksymacyjnej, polegającej na zastąpieniu rzeczywistej funkcji przez jej przebieg uproszczony. Zaproponowano aproksymację rozkładem trójkątnym. Na konkretnym przykładzie pokazano, że metoda ta daje lepsze wyniki niż powszechnie stosowany model przepływu tłokowego.
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Rational multistep methods via modified φj-functions
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Convergence of rational multistep methods of Adams-Padé type
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Antimicrobial molecular nanocarrier–drug conjugates
PublicationMany antimicrobial drugs are poorly active against pathogenic microbes causing intracellular infections, such as Mycobacterium tuberculosis or Plasmodium falciparum. On the other hand, several known antimicrobial agents are not effective enough because of their limited cellular penetration. A common feature of both challenges is the inability of an active agent to cross the biological membrane(s). One of the possible approaches...
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Progress in targeting tumor cells by using drug-magnetic nanoparticles conjugate.
PublicationTo limit the cytotoxicity of anticancer drugs against healthy cells, an appropriate carrier should be synthesized to deliver the drug to the tumor tissue only. A good solution is to anchor a magnetic nanoparticle to the molecule of the drug and to use a properly directed external magnetic field. We have shown that the improved by us synthesis of the conjugate of doxorubicin with iron-oxide magnetic nanoparticles allows a substantial...
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Natural carbon-based quantum dots and their applications in drug delivery: A review
PublicationNatural carbon based quantum dots (NCDs) are an emerging class of nanomaterials in the carbon family. NCDs have gained immense acclamation among researchers because of their abundance, eco-friendly nature, aqueous solubility, the diverse functionality and biocompatibility when compared to other conventional carbon quantum dots (CDs).The presence of different functional groups on the surface of NCDs such as thiol, carboxyl, hydroxyl,...
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Novel 1,2,4-Oxadiazole Derivatives in Drug Discovery
PublicationAbstract: Five-membered 1,2,4-oxadiazole heterocyclic ring has received considerable attention because of its unique bioisosteric properties and an unusually wide spectrum of biological activities. Thus, it is a perfect framework for the novel drug development. After a century since the 1,2,4-oxadiazole have been discovered, the uncommon potential attracted medicinal chemists’ attention, leading to the discovery of a few presently...
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Pharmaceutical and forensic drug applications of chiral supercritical fluid chromatography
PublicationTHE SUPERCRITICAL FLUID IS AN EXCELLENT CHOICE AS THE CHROMATOGRAPHIC MOBILE PHASE BECAUSE IT ALLOWS RAPID SEPARATION WITH HIGH EFFICIENCY AND APPLICATIONS INVOLVING ENANTIORESOLUTION ARE COMMON. SUPERCRITICAL FLUID CHROMATOGRAPHY (SFC) IS INCREASINGLY USED FOR ANALYTICAL, SEMI-PREPARATIVE AND PREPARATIVE PURIFICATION OF CHIRAL COMPOUNDS, INCLUDING PRODUCTION OF ENANTIOMERS THAT ARE MAINLY ENCOUNTERED DURING DRUG DEVELOPMENT. SFC...
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Rational Use of Primary Energy in Single-Family Residential Houses
PublicationThis work presents results of the primary energy use for heating residential single-family house. Analysis includes domestic hot water system (DHW) and heating, ventilation and air condition system (HVAC). During researches the conventional and alternative energy sources (natural gas, biomass, fuel oil, bituminous coal, lignite or electric energy obtained from electric power system – EPS) were used in DHW and HVAC systems. Furthermore...
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Design of a microrobotic wrist for needle laparoscopic surgery
PublicationThe paper addresses the design of a micro wrist for needle laparoscopic surgery (needlescopy) using MEMS technology and an original 3 degree of freedom, 3D architecture. Advancement in needlescopy drives the development of multi-dof micro-tools 1-2mmin diameter with 3D mobility but standard available fabricationtechniques are for 2.5D structures. The paper discusses thedevelopment steps and design solutions for the realization...
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Diatomaceous earth as a drug-loaded carrier in a glass-ionomer cement
PublicationThe effect of a natural filler (diatomaceous earth [DE], a promising drug-delivery agent) and its content was investigated on the performance of a model glass-ionomer cement (GIC). Three sample series, differing in DE content (0, 2.5 and 5 wt%), were prepared using a commercial GIC as a matrix (3M Ketac Molar Easymix). The resultant surface microhardness and roughness, wear performance, and compressive strength of the samples were...
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Algebraic periods of self-maps of a rational exterior space of rank 2
PublicationArtykuł stanowi kompletny opis okresów algebraicznych dla odwzorowań wymiernej przestrzeni zewnętrznej rangi 2 w siebie.
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Disposition of Drugs of Abuse and Their Metabolites in Wastewater as a Method of the Estimation of Drug Consumption
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Determination of the chemical structure of potencial organic impurities occuring in the drug substance opopramol
PublicationThe tricyclic antipsychotic and antidepressant drug opipramol was examined with regard to the chemical structure of its organic impurities. Impurities were isolated from the technical product by chromatographic methods and their chemical structures were estabilished by HMNR, MS and FTIR.
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Double layer adhesive silicone dressing as a potential dermal drug delivery film in scar treatment
PublicationThe present studies focused on the evaluation of design of an adhesive silicone film intended for scar treatment. Developed silicone double layer film was examined in terms of its future relevance to therapy and applicability on the human skin considering properties which included in vitro permeability of water vapor and oxygen. In order to adapt the patches for medical use in the future there were tested such properties as...
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Zero-Pole Approach in Microwave Passive Circuit Design
PublicationIn this thesis, optimization strategies for design of microwave passive structures including filters, couplers, antenna and impedance transformer and construction of various surroogate models utilized to fasten the design proces have been discussed. Direct and hybrid optimization methodologies including space mapping and multilevel algorithms combined with various surrogate models at different levels of fidelity have been utilized...
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Longitudinal drug synergy assessment using convolutional neural network image-decoding of glioblastoma single-spheroid cultures
PublicationAbstract Background In recent years, drug combinations have become increasingly popular to improve therapeutic outcomes in various diseases, including difficult to cure cancers such as the brain cancer glioblastoma. Assessing the interaction between drugs over time is critical for predicting drug combination effectiveness and minimizing the risk of therapy resistance. However, as viability readouts of drug combination experiments...
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Smart Cities System Design Method Based on Case Based Reasoning
PublicationThe objective of this paper is to present the results of research carried out to develop a design method for Smart Cities systems. The method is based on the analysis of design cases of Smart Cities systems in cities, the selection of the city appropriate to the requirements for implementation and application. The Case Based Reasoning method was used to develop the proposed design methodology, along with mechanisms of the conversion...
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The Imidazoacridinone Antitumor Drug, C-1311, Is Metabolized by Flavin Monooxygenases but Not by Cytochrome P450s.
PublicationPrezentowane w publikacji wyniki badań mają na celu wyjaśnienie roli enzymów wątrobowych w metabolizmie przeciwnowotworowych pochodnych C-1311 oraz C-1330. Oba związki inkubowane były z frakcją mikrosomalną oraz enzymami rekombinantowymi należącymi do grypy cytochromu P450, FMO oraz UGT. Badania wykazały, że oba związki są metabolizowane przez enzymy frakcji mikrosomalnej, ale nie przez enzymy cytochromu P450. Aktywność enzymatyczna...
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Determination of the chemical structure of potential organic impurities occurring in drug substance opipramol
PublicationThe tricyclic antipsychotic and antidepressant drug opipramol (opipramole) was examined with regard to the chemical structure of its organic impurities. Impurities were isolated from the technical product by chromatographic methods and their chemical structures were established by 1H NMR, MS and FTIR and further confirmed by comparison with commercially available products or with products obtained by independent synthesis, and...
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PROSPECTS FOR RATIONAL USE OF MINERAL RESOURCES OF THE DZHAKSY-KLYCH DEPOSIT, THE ARAL REGION
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Time-limited trial – searching for rational solutions in the functioning of intensive care units
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Key success factors for small design offices in the bidding process
PublicationCompetition in the design office market is high, therefore it is important to be aware of the conditions determining the competitive advantage, thus increasing the bidding effectiveness. For this reason, the aim of the article is to identify key success factors (KSF) increasing successful bidding of a small design office. The factors were identified and then analysed based on a literature review, expert interviews and using Group...
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The influence of small amount of substances present in tissue on the optical spectrum of immunosuppressive drug
PublicationIn this paper, we describe how commonly present in tissue substances - sodium chloride and glucose - affect the optical spectrum of an immunosuppressive drug (Cyclaid® by Apotex). Prepared samples were investigated using the spectrophotometer in the spectrum range from 250 nm to 1100 nm. The maximum wavelength shift calculated on the basis of measurement results is not bigger than the measurement wavelength step. So, it can be...
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Design thinking (DT) for the design and planning education of engineer-architects
PublicationEngineers are facing new challenges connected with globalisation, digitisation and the increased complexity of the design process. This calls for new, more interdisciplinary and user-oriented approaches to problem- solving. In this article, the authors analyse design thinking (DT) as a method to support the education of engineers specialising in architecture and urban planning. Identified in this study are the opportunities this...
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The Influence of the Co-Dopant Dexamethasone Phosphate on the Electrodeposition Process and Drug-Release Properties of Polypyrrole-Salicylate on Iron
PublicationIn this work, the influence of incorporation of two anti-inflammatory drugs dexamethasone phosphate and sodium salicylate on the electrodeposition process of polypyrrole (PPy) film on iron has been studied. The incorporation of the agents into PPy has been carried out in a one-step electropolymerization process on oxidizable iron. The role of each drug agent during the deposition process has been discussed. The morphological and...
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Encapsulation of an anticancer drug Isatin inside a host nano-vehicle SWCNT: a molecular dynamics simulation
PublicationThe use of carbon nanotubes as anticancer drug delivery cargo systems is a promising modality as they are able to perforate cellular membranes and transport the carried therapeutic molecules into the cellular components. Our work describes the encapsulation process of a common anticancer drug, Isatin (1H-indole-2,3-dione) as a guest molecule, in a capped single-walled carbon nanotube (SWCNT) host with chirality of (10,10). The...
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Theoretical Encapsulation of Fluorouracil (5-FU) Anti-Cancer Chemotherapy Drug into Carbon Nanotubes (CNT) and Boron Nitride Nanotubes (BNNT)
PublicationIntroduction: Chemotherapy with anti-cancer drugs is considered the most common approach for killing cancer cells in the human body. However, some barriers such as toxicity and side effects would limit its usage. In this regard, nano-based drug delivery systems have emerged as cost-effective and efficient for sustained and targeted drug delivery. Nanotubes such as carbon nanotubes (CNT) and boron nitride nanotubes (BNNT) are promising...
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Cancer stem cells and escape from drug-induced premature senescence in human lung tumor cells: implications for drug resistance and in vitro drug screening models
PublicationBadania z użyciem modelu komórek nowotworu płuc A549 wykazały, że komórki te po traktowaniu lekami uszkadzającymi DNA zatrzymują proliferację i wchodzą w stan starzenia komórkowego. Jednak post-inkubacja tych komórek prowadzi do powrotu do stanu proliferacji małej frakcji komórek. Wykazaliśy, że frakcja ta związana jest z obecnością komórek pierwotnych nowotworu w populacji komórek A549. Powrót do stanu proliferacji komóek A549...
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Nanosize effect of clay mineral nanoparticles on the drug diffusion processes in polyurethane nanocomposite hydrogels
PublicationStudies of swelling and release of naproxen sodium (NAP) solution by polyurethane nanocomposite hydrogels containing Cloisite® 30B (organically modified montmorillonite (OMMT)) have been performed. Polyurethane nanocomposite hydrogels are hybrid, nontoxic biomaterials with unique swelling and release properties in comparison with unmodified hydrogels. These features enable to use nanocomposite hydrogels as a modern wound dressing....
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Bovine Serum Albumin – Hydroxyapatite Nanoflowers as Potential Local Drug Delivery System of Ciprofloxacin
PublicationIntroduction: Hybrid nanoflowers are structures consisting of organic (enzymes, proteins, nucleic acids) and inorganic components (mostly metal phosphates) with a flower-like hierarchical structure. Novel hybrid nanoflowers based on bovine serum albumin (BSA) and hydroxyapatite (HA) were obtained and characterized. Study on BSA-HA nanoflowers as potential drug delivery system is reported for the first time. Methods: Embedding ciprofloxacin...
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Exposure to non-opioid analgesics during pregnancy and the risk of adverse drug reactions
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Optical properties of the chemotherapy drugs used in the central nervous system lymphoma therapy: monitoring drug delivery
PublicationOur aim is to optically monitor the delivery of the chemotherapy drugs for brain tumours, particularly used in the central nervous system (CNS) lymphoma therapy. In vivo monitoring would help to optimize the treatment and avoiding unnecessary medications. Moreover, it would be beneficial to be able to measure which of the multi-regimen drugs actually do penetrate and how well into the brain tissue. There exist several potential...
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pH-Responsive Drug Delivery Nanoplatforms as Smart Carriers of Unsymmetrical Bisacridines for Targeted Cancer Therapy
PublicationSelective therapy and controlled drug release at an intracellular level remain key challenges for effective cancer treatment. Here, we employed folic acid (FA) as a self-navigating molecule in nanoconjugates containing quantum dots (QDs) and β-cyclodextrin (β-CD) for the delivery of antitumor unsymmetrical bisacridine compound (C-2028) to lung and prostate cancers as well as normal cells. The bisacridine derivative can form the...
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Drug-resistant and hospital-associated Enterococcus faecium from wastewater, riverine estuary and anthropogenically impacted marine catchment basin.
PublicationEnterococci, ubiquitous colonizers of humans and other animals, play an increasingly important role in health-care associated infections (HAIs). Acquisition of resistance determinants not only seriously limits available therapeutic options but also increases available gene pool for other species. It is believed that the recent evolution of two clinically relevant species, Enterococcus faecalis and Enterococcus faecium occurred...
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HDAC Inhibitors: Innovative Strategies for Their Design and Applications
PublicationHistone deacetylases (HDACs) are a large family of epigenetic metalloenzymes that are involved in gene transcription and regulation, cell proliferation, differentiation, migration, and death, as well as angiogenesis. Particularly, disorders of the HDACs expression are linked to the development of many types of cancer and neurodegenerative diseases, making them interesting molecular targets for the design of new efficient drugs...
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Drug-Eluting Biopsy Needle as a Novel Strategy for Antimicrobial Prophylaxis in Transrectal Prostate Biopsy
PublicationOBJECTIVES: To preclinically evaluate drug-eluting biopsy needles (patent pending WO2016118026) as a new potential way of antimicrobial prophylaxis for transrectal prostate biopsy. METHODS: Twenty steel biopsy needles have been coated with polyvinyl alcohol, ciprofloxacin, and amikacin. Modified biopsy needles have been randomly divided into 3 groups (1:2:1 ratio). Needles from group I were immersed for 30 minutes in dedicated...
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Development of Technical Creativity Featuring Modified TRIZ-AM Inventive Principle to Support Design for Additive Manufacturing
Publicationhe design for additive manufacturing (DFAM) processing was introduced to fully utilise the design freedom provided by additive manufacturing (AM). Consequently, appropriate design methodologies have become essential for this technology. Recently, many studies have identified the importance of DFAM method utilisation to produce AM parts, and TRIZ is a strategy used to formalise design methodologies....
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Towards defragmented Lighting Design: concatenating research theories for effective use in design practices.
PublicationThis paper aims to provide guidelines for transferring design research to practice in the realm of lighting. It is based on the premise that design research in lighting should function as a development of practice, instead of being a distraction to it. Design research refers to the scholarly inquiry that seeks to advance design by studying and improving it in systematic and scientific ways by expanding, testing and operationalizing...
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ENCAPSULATION OF ROXITHROMYCIN INTO GELLAN GUM MATRICES AND THE IMPACT OF OTHER NATURAL POLYMERS ON DRUG RELEASE
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A five-year retrospective study shows increasing rates of antimicrobial drug resistance in Cabo Verde for both Staphylococcus aureus and Escherichia coli
PublicationObjectives Data on baseline drug resistance is important in informing future antimicrobial stewardship programs. So far, no data on the antimicrobial drug resistance of clinical isolates was available for the African archipelago of Cabo Verde. Methods We have performed a retrospective analysis over five-years (2013-17) of the antimicrombial drug susceptibility profiles of clinical isolates in the two main hospitals of Cabo Verde....
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Risk Management in "Agile" methodologies using the example of Scrum and the IBM Rational Team Concert tool
PublicationProject risk is one of the key areas which should be subjected to a thorough analysis in any IT project. Project managers undertake steps to minimize risks, both in terms of organization (matching people to tasks or roles) as well as in terms of technology (using appropriate tools for the management and execution of tasks). Every method of project management defines and describes the processes and techniques related to knowledge...