Auswahl der wissenschaftlichen Literatur zum Thema „PKSim“

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Zeitschriftenartikel zum Thema "PKSim"

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Li, Ronald C., Shekman L. Wong und Keith K. H. Chan. „EXPANDED VERSION OF PKSIM FOR PHARMACOKINETIC SIMULATIONS OF BOTH METABOLITE AND PARENT DRUGS“. American Journal of Therapeutics 4, Nr. 1 (Januar 1997): 16–22. http://dx.doi.org/10.1097/00045391-199701000-00004.

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Mangzira Kemung, Hefa, Loh Teng-Hern Tan, Kok-Gan Chan, Hooi-Leng Ser, Jodi Woan-Fei Law, Learn-Han Lee und Bey-Hing Goh. „Streptomyces sp. Strain MUSC 125 from Mangrove Soil in Malaysia with Anti-MRSA, Anti-Biofilm and Antioxidant Activities“. Molecules 25, Nr. 15 (03.08.2020): 3545. http://dx.doi.org/10.3390/molecules25153545.

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There is an urgent need to search for new antibiotics to counter the growing number of antibiotic-resistant bacterial strains, one of which is methicillin-resistant Staphylococcus aureus (MRSA). Herein, we report a Streptomyces sp. strain MUSC 125 from mangrove soil in Malaysia which was identified using 16S rRNA phylogenetic and phenotypic analysis. The methanolic extract of strain MUSC 125 showed anti-MRSA, anti-biofilm and antioxidant activities. Strain MUSC 125 was further screened for the presence of secondary metabolite biosynthetic genes. Our results indicated that both polyketide synthase (pks) gene clusters, pksI and pksII, were detected in strain MUSC 125 by PCR amplification. In addition, gas chromatography-mass spectroscopy (GC-MS) detected the presence of different chemicals in the methanolic extract. Based on the GC-MS analysis, eight known compounds were detected suggesting their contribution towards the anti-MRSA and anti-biofilm activities observed. Overall, the study bolsters the potential of strain MUSC 125 as a promising source of anti-MRSA and antibiofilm compounds and warrants further investigation.
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Uchiba, Mitsuhiro, Kenji Okajima, Kazunori Murakami, Hiroaki Okabe, Shosuke Okamoto und Yoshio Okada. „Effects of Plasma Kallikrein Specific Inhibitor and Active-site Blocked Factor VIIa on the Pulmonary Vascular Injury Induced by Endotoxin in Rats“. Thrombosis and Haemostasis 78, Nr. 04 (1997): 1209–14. http://dx.doi.org/10.1055/s-0038-1657716.

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SummaryThe acute respiratory distress syndrome (ARDS) is a serious complication of sepsis. To evaluate the role of the coagulation system in the pathogenesis of ARDS in sepsis, we examined the effects of the administration of a synthetic plasma kallikrein specific inhibitor (PKSI) and of active-site blocked factor VIIa (DEGR-VIIa) on the pulmonary vascular injury induced by E. coli endotoxin (ET) in rats. Administration of PKSI prevented the pulmonary vascular injury induced by ET as well as pulmonary histological changes in animals administered ET, but it did not affect the intravascular coagulation. The opposite effect was seen with DEGR-VIIa, which prevented the intravascular coagulation but not the pulmonary vascular injury. PKSI did not inhibit the activation of the complement system induced by ET leading to the activation of neutrophils.Findings suggest that PKSI may prevent the pulmonary vascular injury induced by ET by inhibiting kallikrein, which activates the neutrophils. The intrinsic pathway of coagulation may be more important than the extrinsic pathway in the pulmonary vascular injury produced byET.
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Ginolhac, Aurélien, Cyrille Jarrin, Benjamin Gillet, Patrick Robe, Petar Pujic, Karine Tuphile, Hélène Bertrand et al. „Phylogenetic Analysis of Polyketide Synthase I Domains from Soil Metagenomic Libraries Allows Selection of Promising Clones“. Applied and Environmental Microbiology 70, Nr. 9 (September 2004): 5522–27. http://dx.doi.org/10.1128/aem.70.9.5522-5527.2004.

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ABSTRACT The metagenomic approach provides direct access to diverse unexplored genomes, especially from uncultivated bacteria in a given environment. This diversity can conceal many new biosynthetic pathways. Type I polyketide synthases (PKSI) are modular enzymes involved in the biosynthesis of many natural products of industrial interest. Among the PKSI domains, the ketosynthase domain (KS) was used to screen a large soil metagenomic library containing more than 100,000 clones to detect those containing PKS genes. Over 60,000 clones were screened, and 139 clones containing KS domains were detected. A 700-bp fragment of the KS domain was sequenced for 40 of 139 randomly chosen clones. None of the 40 protein sequences were identical to those found in public databases, and nucleic sequences were not redundant. Phylogenetic analyses were performed on the protein sequences of three metagenomic clones to select the clones which one can predict to produce new compounds. Two PKS-positive clones do not belong to any of the 23 published PKSI included in the analysis, encouraging further analyses on these two clones identified by the selection process.
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Świgoń, Marzena, und Karsten Weber. „Managing Knowledge and Information by Students“. Journal of Information & Knowledge Management 13, Nr. 04 (Dezember 2014): 1450030. http://dx.doi.org/10.1142/s0219649214500300.

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The concept of Personal Knowledge and Information Management (PKIM) is based, among others, on two theories: Personal Information Management (PTM) and Personal Knowledge Management (PKM), which hitherto were both subjects of separate studies. Moreover, the concept of PKIM is related to IL, which is a concept of information skills and competences of individuals — a person who manages knowledge has to be information literate. Some of the empirical studies results in the field of PKIM, started in Poland and recently continued in Germany, are presented. As the research method an unstructured questionnaire with open questions was used. Given the results of the survey as well as taking into account the subject literature, the concepts of PIM, PKM, and Information Literacy (IL) seem to be compatible and connected with each other. Our respondents perceive Knowledge and Information as well as knowledge management (KM) and information management (IM) in the context of learning and studying as integrated areas of interests. Although they do see differences between them, interconnections and relations seem more important. Furthermore, KM and IM are recognized as tools of coping with information overload. All aspects that have repercussions on KM and IM are related to three categories: personal characteristics, environment (macro and micro environment), and knowledge and information sources.
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Mien, Pham Thi, Dao Viet Ha, Hoang Xuan Ben, Bin Chen, Lan Liu und Phan Minh-Thu. „Antimicrobial Activities of Sponge-Derived Microorganisms from Coastal Waters of Central Vietnam“. Journal of Marine Science and Engineering 8, Nr. 8 (08.08.2020): 594. http://dx.doi.org/10.3390/jmse8080594.

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Bacteria associated with invertebrates are considered as good sources for biologically active compounds. Sponge-derived bacteria were screened for antimicrobial activities, the presence of the cluster genes of polyketide synthases (PKSs) and non-ribosomal peptide synthetases (NRPSs), and through a colony picking method. Crude extracts of broth cultures were tested for microbial inhibition. Eleven out of 25 isolated strains showed inhibition of at least one of eight tested indicator microorganisms. Antimicrobial activities were observed in the strains coded HM5, HM6, and HM9 with the presence of NRPS and PKSII genes, whereas the isolate HM21 held both NRPS and PKSII and inhibited only the growth of Bacillus subtilis by the well diffusion method and only inhibited Serratia marcescens by the colony picking method. Two isolates, HM5 and HM6, belonged to the species of Bacillus. Interestingly, the isolate HM9 was nearest to Streptomyces mexicanusT NBRC100915 (GenBank accession number AB249966) with 94% sequence similarity. This potent strain HM9 could possibly be considered as a new species and a good source for bioactive compound discovery. Some isolates showed NRPS/PKS genes but did not exhibit antimicrobial activity. Thus, we suggested that both molecular and traditional methods should be conducted for the screening of antimicrobial producers.
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Oiwa, Kazuhiro, Osamu Matsuo, Shigeru Ueshima, Kiyotaka Okada, Yoshio Okada, Shosuke Okamoto, John Giddings, Junichiro Yamamoto und Masaru Hashimoto. „Suppression of argatroban-induced endogenous thrombolysis by PKSI-527, and antibodies to TPA and UPA, evaluated in a rat arterial thrombolysis model“. Thrombosis and Haemostasis 89, Nr. 05 (2003): 820–25. http://dx.doi.org/10.1055/s-0037-1613467.

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SummaryWe have previously confirmed, using a rat mesenteric arteriole thrombolysis model, that thrombin inhibition induces endogenous thrombolysis in vivo. In addition, we have shown that thrombin-activatable fibrinolysis inhibitor (TAFI) plays a role in the down regulation of endogenous thrombolysis. However, the mechanism of endogenous thrombolysis or spontaneous plasmin generation in vivo remains unclear.It has been shown in an in vitro system that plasma kallikrein activates pro-urokinase (pro uPA) and/or plasminogen, resulting in plasmin generation. These findings suggest that spontaneous fibrinolysis might be mediated by tPA and plasma kallikrein-dependent uPA. The aim of the present study was to examine whether these mechanisms play a dominant role in endogenous thrombolysis in vivo, using our rat mesenteric arterial thrombolysis model.Argatroban infusion enhanced endogenous thrombolysis. PKSI-527, anti uPA and anti tPA IgGs suppressed argatroban-induced thrombolysis. Also, the antibody IgG preparations suppressed endogenous thrombolysis in the absence of argatroban. In the presence of PKSI-527, anti tPA IgG was more effective than anti uPA IgG in suppressing argatroban-induced thrombolysis. The results suggested that both tPA and plasma kallikrein-mediated uPA activation and tPA release contribute to endogenous fibrinolytic or thrombolytic mechanisms.
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Ramadoan, Sri, Pudji Muljono und Ismail Pulungan. „PERAN PKSM DALAM MENINGKATKAN FUNGSI KELOMPOK TANI DAN PARTISIPASI MASYARAKAT DI KABUPATEN BIMA, NTB“. Jurnal Penelitian Sosial dan Ekonomi Kehutanan 10, Nr. 3 (30.09.2013): 199–210. http://dx.doi.org/10.20886/jpsek.2013.10.3.199-210.

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Ramadoan, Sri, Pudji Muljono und Ismail Pulungan. „PERAN PKSM DALAM MENINGKATKAN FUNGSI KELOMPOK TANI DAN PARTISIPASI MASYARAKAT DI KABUPATEN BIMA, NTB“. Jurnal Penelitian Sosial dan Ekonomi Kehutanan 10, Nr. 3 (September 2013): 199–210. http://dx.doi.org/10.20886/jsek.2013.10.3.199-210.

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Chikita, Wulan. „ANALISIS KUALITAS BUTIR SOAL UJIAN AKHIR SEMESTER GASAL MATA PELAJARAN PKSM KELAS XI TEKNIK SEPEDA MOTOR“. Jurnal Pendidikan Vokasi Otomotif 2, Nr. 1 (20.07.2020): 23–32. http://dx.doi.org/10.21831/jpvo.v2i1.28361.

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This research was conducted with the aim to determine the quality of items about odd Semester Final Exam Subjects of Electrical Maintenance of Class XI Motorcycle Engineering at SMK Negeri 1 Bumiratu Nuban Academic Year 2018/2019. The research method used is descriptive method with a quantitative approach. The data collection technique uses the documentation method, to obtain test questions and answer keys as well as answers to all students who take the exam. The population of the study was grade XI Motorcycle Engineering SMK Negeri 1 Bumiratu Nuban 2018/2019. The results in terms of the question validity aspects as much as 57% including valid categories and 43% invalid. In terms of reliability, the reliability coefficient is 0.79 which means it has a high coefficient. Then in terms of the level of difficulty as much as 5% including the easy category, 53% including the medium category, 37% including the difficult category and 5% including the very difficult category. In terms of distinguishing factors, there were 5% of questions including excellent categories, 43% including good categories, 20% including sufficient categories, 22% including bad categories and 10% including categories that had to be discarded. From the aspect of deceptive effectiveness, there are only 7.5% of questions for which all the deceivers function effectively.
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Dissertationen zum Thema "PKSim"

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Leding, Albin. „Recommendation for first pharmacokinetic in vivo experiment design with a pharmacometric informed approach“. Thesis, Uppsala universitet, Institutionen för farmaci, 2021. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-447311.

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Tuberculosis, the leading cause of death by a single infection disease caused by bacteria, requires long treatments and the bacteria are prone to develop drug resistance. Therefore, new efficient treatment regiments needs developing, which requires new tools for drug development. A major reason for discontinuance of a drug under development is undesired pharmacokinetic properties. Therefore, it is important to have early information of this, preferably the first time the drug is tested in animals. The first in vivo pharmacokinetic experiment is often done in mice and the only information present at this stage are often in vitro values and physicochemical properties. Physiological-based pharmacokinetic modelling can be used to extrapolate from in vitro to in vivo values. From this, the first in vivo pharmacokinetic experiment can be designed, often with the goal of reducing the amount of mice. This goal is one of the three R.s and it is called Reduction. To explore the Reduction of an experiment population pharmacokinetic modelling can be utilized via exploration of the imprecision, bias and probability of an informative experiment to evaluate if a design meets the goal of Reduction. In this report a recommendation of the first in vivo pharmacokinetic experiment is presented. This is based on in vitro values and physicochemical properties that are common in anti-tuberculosis drugs. If the probability of an informative experiment is critical, a terminal sampling of 40 mice is recommended. If imprecision and bias are necessary, zipper sampling of 10 mice is recommended.
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Leding, Albin. „Optimized design recommendation for first pharmacokinetic in vivo experiments for new tuberculosis drugs using pharmacometrics modelling and simulation“. Thesis, Uppsala universitet, Institutionen för farmaci, 2021. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-447311.

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Tuberculosis, the leading cause of death by a single infection disease caused by bacteria, requires long treatments and the bacteria are prone to develop drug resistance. Therefore, new efficient treatment regiments needs developing, which requires new tools for drug development. A major reason for discontinuance of a drug under development is undesired pharmacokinetic properties. Therefore, it is important to have early information of this, preferably the first time the drug is tested in animals. The first in vivo pharmacokinetic experiment is often done in mice and the only information present at this stage are often in vitro values and physicochemical properties. Physiological-based pharmacokinetic modelling can be used to extrapolate from in vitro to in vivo values. From this, the first in vivo pharmacokinetic experiment can be designed, often with the goal of reducing the amount of mice. This goal is one of the three R.s and it is called Reduction. To explore the Reduction of an experiment population pharmacokinetic modelling can be utilized via exploration of the imprecision, bias and probability of an informative experiment to evaluate if a design meets the goal of Reduction. In this report a recommendation of the first in vivo pharmacokinetic experiment is presented. This is based on in vitro values and physicochemical properties that are common in anti-tuberculosis drugs. If the probability of an informative experiment is critical, a terminal sampling of 40 mice is recommended. If imprecision and bias are necessary, zipper sampling of 10 mice is recommended.
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Bücher zum Thema "PKSim"

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Indonesia. Direktorat Kesejahteraan Anak, Keluarga dan Lanjut Usia., Hrsg. Laporan hasil evaluasi pelaksanaan program peningkatan kesejahteraan sosial keluarga muda melalui kelompok usaha bersama keluarga muda mandiri (PKSKM melalui KUBE-KMM). [Jakarta]: Badan Kesejahteraan Sosial Nasional, Deputi Bidang Peningkatan Kesejahteraan Sosial, Direktorat Kesejahteraan Anak, Keluarga dan Lanjut Usia, 2000.

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Buchteile zum Thema "PKSim"

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Enna, S. J., und David B. Bylund. „PKSI-527“. In xPharm: The Comprehensive Pharmacology Reference, 1. Elsevier, 2007. http://dx.doi.org/10.1016/b978-008055232-3.63458-0.

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Konferenzberichte zum Thema "PKSim"

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Ahmad, Azlin, Rubiyah Yusof und Yasue Mitsukura. „Pheromone-based Kohonen Self-Organizing Map (PKSOM) in clustering of tropical wood species: Performance and scalability“. In 2015 10th Asian Control Conference (ASCC). IEEE, 2015. http://dx.doi.org/10.1109/ascc.2015.7244589.

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