cometadata/datacite-rtg-text-other-reclassification-records huggingface dataset:
Prodrugs of thiolamines as radioprotective agents
Creators: name: Koch, Kimberly Elaine
Publisher: name: University of Utah
Year: 2012
Subjects: Thiazolidine Compounds
Toxicity

description: he radiotherapy of tumor tissue is highly effective but can be limited by the damage caused to normal tissue during exposure to the solid tumor to radiation.  Sulfydryl-containing compounds have long been known to possess radio-protective properties.  Of all the compounds that have been studies as potential radio-protective agents over the past 50 years, cysteamine and L-cysteine are still considered among the most efficacious.  Unfortunately, their therapeutic usefulness has been limited by their toxicity at radio-protective doses.   The classical prodrug approach to drug design may provide a way to solve these toxicity-related problems.  Four prodrugs were synthesized, tow of cysteamine and two of L-cysteine, by a chemical condensation between the thiolamine and the carbonyl group of either D-ribose or D-glucose (RibCyst, BlcCyst, and GlcCys, respectively).. These thiazolidine compounds undergo nonenzymatic ring opening and subsequent hydrolysis to release the free drug.  The dissociation process produces a relatively constant supply of the thiolamine, which may eliminate toxicity due to the presence of a high concentration of the compound at any time.  Extensive toxicity studies utilizing both 3-day growth curve and clonogenic toxicity assays were performed on exponentially growing V79 cells.  The results indicate that the inherent toxicity of cysteamine is greatly reduced when given as a prodrug, thus confirming from a toxicity standpoint the usefulness of constructing proddrugs of cysteamine.  L-Cysteine exhibited limited toxicity in the assays used, but when toxicity was seen, it was eliminated when the amino acid was provided as RibCys or a slightly reduced when given as GlyCys.  The ability of the parent compounds and their respective prodrugs to alter the normal response of V79 cells to ionizing radiation was also studied using a clonogenic assay.  The results indicate that the radioprotective ability of both cysteamine and L-cysteine is reduced when given as prodrugs under the conditions studied.  This may be due to differing hydrolysis rate of the prodrugs or the kinetics of cell uptake.  The capacity of these compounds to protect against radiation-inducted DNA single strand breaks was determined using the alkaline elution technique.  Protection against DNA damage was seen with the cysteamine series. In fact, the cysteamine prodrugs were more protective than cysteamine itself.  The behavior of L-cysteine and its prodrugs was the opposite of the cysteamine series.  L-Cysteine was able to protect against DNA damage as efficiently as cysteamine, whereas the L-cysteine prodrugs showed limited ability to protect under the conditions testsed.
New verification method for embedded systems
Creators: name: Thacker, Robert A
Publisher: name: University of Utah
Year: 2012
Subjects: Embedded systems
Petri nets
Verification

description: Cyber-physical systems, in which computers control real-world mechanisms, are ever more pervasive in our society. These complex systems, containing a mixture of software, digital hardware, and analog circuitry, are often employed in circumstances where their correct behavior is crucial to the safety of their operators. Therefore, verifi cation of such systems would be of great value. This dissertation introduces a modeling and   veri fication methodology sufficiently powerful to manage the complications inherent in this mixeddiscipline design space.
Brief an [Johann Bernoulli]
Creators: name: Lambertenghi, Luigi
Publisher: name: [s.n.]
Year: 1780

description: von Luigi Lambertenghi
description: Öffentliche Bibliothek der Universität Basel
description: Französisch
description: Verzeichnung=Description=Inventaire Januar 2015 HAN-Katalogisierungsregeln Vollständige Rekatalogisierung nach Standortverzeichnis und Briefkatalog
A study of inhibitors of d-glycero-β-d-manno-heptose-1-phosphate adenylyltransferase from Burkholderia pseudomallei as a potential antibiotic target
Creators: name: Kim, Suwon
name: Jo, Seri
name: Kim, Mi-Sun
name: Shin, Dong Hae
Publisher: name: Taylor & Francis
Year: 2021
Subjects: subject: Biochemistry
subject: Pharmacology
subject: Biotechnology
subject: 39999 Chemical Sciences not elsewhere classified
subject: FOS: Chemical sciences
subject: Ecology
subject: FOS: Biological sciences
subject: 69999 Biological Sciences not elsewhere classified
subject: 110309 Infectious Diseases
subject: FOS: Health sciences

description: d-Glycero-β-d-manno-heptose-1-phosphate adenylyltransferase from Burkholderia pseudomallei (BpHldC) is the fourth enzyme in the ADP‐l‐glycero‐β‐d‐manno‐heptose biosynthesis pathway producing a lipopolysaccharide core. Therefore, BpHldC is an anti-melioidosis target. Three ChemBridge compounds purchased from ChemBridge Corporation (San Diego, CA) were found to have an effective inhibitory activity on BpHldC. Interestingly, ChemBridge 7929959 was the most effective compound due to the presence of the terminal benzyl group. The enzyme kinetic study revealed that most of them show mixed type inhibitory modes against ATP and βG1P. The induced-fit docking indicated that the medium affinity of ChemBridge 7929959 is originated from its benzyl group occupying the substrate-binding pocket of BpHldC. The inhibitory role of terminal aromatic groups was proven with ChemBridge 7570508. Combined with the previous study, ChemBridge 7929959 is found to work as a dual inhibitor against both HldC and HddC. Therefore, three ChemBridge compounds can be developed as a potent anti-melioidosis agent with a novel inhibitory concept.
Working fluid selection for an increased efficiency hybridized geothermal-solar thermal power plant in Newcastle, Utah
Creators: name: Carnell, John Walter
Publisher: name: University of Utah
Year: 2012
Subjects: Hybridized geothermal-solar
Geothermal
Power plant
Solar thermal
Working fluid
Newcastle
Utah

description: Renewable sources of energy are of extreme importance to reduce greenhouse gas emissions from traditional power plants. Such renewable sources include geothermal and solar thermal energy. These involve harnessing the heat from underground water sources or from solar irradiance. The heat energy is used to vaporize a working fluid which turns a turbine and generator system to produce electricity. The working fluid is then condensed and reused in the cycle. The working fluid needs to be carefully selected based on the geothermal brine temperature or the amount of solar irradiation available and the fluid's thermodynamic properties. There are many low temperature geothermal resources that have the potential to generate commercial electricity, but due to their low temperatures cannot do so efficiently. The efficiency of geothermal power plants can be increased by adding solar energy. A commercially successful method of concentrating solar power is the solar trough. A solar trough is a parabolic mirror that focuses solar energy onto a collector tube. A heat transfer fluid is circulated within the tube to collect the energy. This heat transfer fluid would be heated and passed through a heat exchanger with the working fluid in a binary power plant to increase the working fluid's enthalpy. There are vast quantities of solar irradiance data available for many locations throughout the United States. The data of interest are the direct normal irradiance which is measured by a pyrheliometer and a solar tracking device. Published data have shown that the direct normal radiation can be as high as 1,000 W/m2 during peak hours of the day with a daily average, during sunlight hours, of 850 W/m2. With these energy rates it could be advantageous to use this solar energy to increase the enthalpy of a power system. Specific measurements should be made at a geothermal site in order to know if such a project is feasible. If the project is feasible, a working fluid for the power cycle should be selected and an economic analysis should be performed in order to make project recommendations.
Mechanism of cannabinoid incorporation in hair
Creators: name: Smeal, Stacy Janine
Publisher: name: University of Utah
Year: 2012
Subjects: Analysis
Drugs

description: Analysis of hair for the detection of illegal and therapeutic drugs has become a widely accepted alternative or complementary method to traditional urinalysis. Hair pigmentation has been shown to play a role in the incorporation of drug into hair. Drug basicity has increased the incorporation of certain basic compounds, such as cocaine, codeine, amphetamine, and phencyclidine, into pigmented hair compared to non-pigmented hair through their interactions with melanin in hair. However, the nonbasic cannabinoids should not show the same differential incorporation as do some basic drugs.  We hypothesized that delta-9-tetrahydrocannabinol (THC) and 11 -nor-delta-9-tetrahydrocannabinol (THCA) incorporated into hair by a mechanism independent of melanin binding. THC and THCA in pigmented and nonpigmented hair collected from Long-Evans rats administered THC did not statistically differ.  Cultured pigmented melanocytes (PM) and nonpigmented melanocytes (NPM) were employed to examine the effect of pigmentation on the influx and efflux of THC and THCA into and out of hair cell types. There was no difference in the influx of THC and THCA into PM and NPM, with the exception of THC in NPM at 15s and 150 min The efflux of THC and THCA further support the hypothesis that factor/s other than pigmentation effect cannabinoid retention in PM and NPM. There was no significant difference between the amount of THC effluxed from PM and NPM. THCA efflux from PM was significantly greater than NPM at 1,5, 30, and 60 min.  Indirect immunofluorescence was used to observe sites of THC and COC (positive control) localization within the hair follicle. No fluorescence was evident in either pigmented or nonpigmented hair follicle sections at any time after a single dose of THC. After multiple administrations, THC was localized with epidermal keratins and sebaceous glands, not the melanosomes of the hair follicle. In contrast to THC, COC associated with the dense population of melanosomes in the cortex of the pigmented hair follicle. In conclusion, the data presented in this dissertation demonstrate that THC and THCA incorporate into hair by a mechanism independent of hair pigmentation, and suggest its incorporation is influenced by the indirect deposition via sebum and skin.
Mechanistic modelling of microbial communities with insights from an in vitro pig gut model
Creators: name: Gardner, Brian
name: Gonzalez Villeta, Laura C.
name: Leng, Joy
name: Hassan, Marwa M.
name: Chambers, Mark
name: La Ragione, Roberto M.
name: Lo Iacono, Giovanni
Publisher: name: Zenodo
Year: 2022
Subjects: FED-AMR
mechanistic modelling
microbiome

description: The gut microbiota play a key role in the health of animals and humans. However, the dynamic properties and stability of the microbiota are poorly understood. We propose a regression technique for parameter inference of a mechanistic model to describe the temporal dynamics of these microbial communities. The model could be used for measuring community resilience against external perturbing factors, such as antibiotic therapy.
Cyclocephala pseudoconfusa Ratcliffe 1992
Creators: name: Hielkema, Auke J.
name: Hielkema, Meindert A.
Publisher: name: Zenodo
Year: 2019
Subjects: Biodiversity
Taxonomy
Animalia
Arthropoda
Insecta
Coleoptera
Dynastidae
Cyclocephala
Cyclocephala pseudoconfusa

description: § Cyclocephala pseudoconfusa Ratcliffe, 1992
Cyclocephala pseudoconfusa Ratcliffe 1992: 185 (Brazil (NA))
Distribution. Brazil (NA): Ratcliffe 1992: 185 (NA); Moore et al. 2018b: 234.
description: Published as part of Hielkema, Auke J. & Hielkema, Meindert A., 2019, An annotated checklist of the Scarabaeoidea (Insecta: Coleoptera) of the Guianas, pp. 1-306 in Insecta Mundi 732 (732) on page 178, DOI: 10.5281/zenodo.3678492
8-Mercaptoguanine-based inhibitors of Mycobacterium tuberculosis dihydroneopterin aldolase: synthesis, in vitro inhibition and docking studies
Creators: name: de Matos Czeczot, Alexia
name: Roth, Candida Deves
name: Ducati, Rodrigo Gay
name: Pissinate, Kenia
name: Rambo, Raoní Scheibler
name: Timmers, Luís Fernando Saraiva Macedo
name: Abbadi, Bruno Lopes
name: Macchi, Fernanda Souza
name: Pestana, Víctor Zajaczkowski
name: Basso, Luiz Augusto
name: Machado, Pablo
name: Bizarro, Cristiano Valim
Publisher: name: Taylor & Francis
Year: 2021
Subjects: subject: Biochemistry
subject: Pharmacology
subject: Biotechnology
subject: 39999 Chemical Sciences not elsewhere classified
subject: FOS: Chemical sciences
subject: 69999 Biological Sciences not elsewhere classified
subject: FOS: Biological sciences
subject: 110309 Infectious Diseases
subject: FOS: Health sciences
subject: 60506 Virology

description: The dihydroneopterin aldolase (DHNA, EC 4.1.2.25) activity of FolB protein is required for the conversion of 7,8-dihydroneopterin (DHNP) to 6-hydroxymethyl-7,8-dihydropterin (HP) and glycolaldehyde (GA) in the folate pathway. FolB protein from Mycobacterium tuberculosis (MtFolB) is essential for bacilli survival and represents an important molecular target for drug development. S8-functionalized 8-mercaptoguanine derivatives were synthesised and evaluated for inhibitory activity against MtFolB. The compounds showed IC50 values in the submicromolar range. The inhibition mode and inhibition constants were determined for compounds that exhibited the strongest inhibition. Additionally, molecular docking analyses were performed to suggest enzyme-inhibitor interactions and ligand conformations. To the best of our knowledge, this study describes the first class of MtFolB inhibitors.
Brief an Johann Bernoulli
Creators: name: Lengnich, Karl Benjamin
Publisher: name: [s.n.]
Year: 1791

description: von [Carl Benjamin] Lengnich
description: Mit Oblate
description: Öffentliche Bibliothek der Universität Basel
description: Deutsch
description: Verzeichnung=Description=Inventaire Januar 2015 HAN-Katalogisierungsregeln Vollständige Rekatalogisierung nach Standortverzeichnis und Briefkatalog
Leptynoptera sulfurea Crawford
Creators: name: Cadwell, J. S.
Publisher: name: Zenodo
Year: 1942
Subjects: Biodiversity
Taxonomy
Animalia
Arthropoda
Insecta
Hemiptera
Triozidae
Leptynoptera
Leptynoptera sulfurea

description: 1. Leptynoptera sulfurea Crawford, Philip. Jour. Sci. 15 (2): 147, pl. 1, figs. 5, 6, 1919. Leptynoptera sulfurea variety rubrocincta Uichanco, Philip. Jour. Sci. 18 (3): 271, pls. 1, 3, 4, 5, figs. 4, 20, 38, 48, 1921. Leptynoptera didactyla Laing, Ann. Mag. Nat. Hist. IX, 9: 554, fig. 1, 1922. Yigo, Nov. 13, reared from Calophyllum inophyllum leaves, Swezey; Umatac, on beach, on Calophyllum inophyllum, May 28, Swezey. L. sulfurea was described from Amboina, Moluccas, on a single specimen, without mention of food plant. The variety rubrocincta was described from the Philippines as occurring on Calophyllum inophyllum, the young feeding beneath the rolled over edge of the leaves. The Guam specimens were reared from the same tree, and similarly situated on the leaves. They agree pretty well with the characters which Uichanco gives as distinctions between the variety and sulfurea, except that the Guam specimens lack the reel markings on the abdomen. Uichanco had one female in which these were not evident. He concludes: "When more is known about the Moluccan insect, the variety rubrocincta may finally have to be merged with the species." The species didactyla described from Fiji in 1922, on Calophylluni inophyllum seems more likely to be the same as Guam material, especially on account of white lines on the thorax which are not mentioned in the description of sulfurea. As Calophyllum inophyllum is widely spread in Pacific tropics, no doubt this psyllid will be found more widely spread when more collecting is done. The tree occurs in Hawaii, but does not have the psyllid.
description: Published as part of Cadwell, J. S., 1942, Psyllidae from Guam, pp. 20-22 in Insects of Guam I, Honolulu, Hawaii :Bernice P. Bishop Museum Bulletin 172 on page 20, DOI: 10.5281/zenodo.5159783
Brief an [Johann] Bernoulli
Creators: name: Lengnich, Karl Benjamin
Publisher: name: [s.n.]
Year: 1786

description: von [Carl Benjamin] Lengnich
description: Mit Spuren von einer roten Oblate
description: Öffentliche Bibliothek der Universität Basel
description: Deutsch
description: Verzeichnung=Description=Inventaire Januar 2015 HAN-Katalogisierungsregeln Vollständige Rekatalogisierung nach Standortverzeichnis und Briefkatalog
description: Bl. 251: Preisliste
Novel mutual prodrug of 5-fluorouracil and heme oxygenase-1 inhibitor (5-FU/HO-1 hybrid): design and preliminary in vitro evaluation
Creators: name: Salerno, Loredana
name: Vanella, Luca
name: Sorrenti, Valeria
name: Consoli, Valeria
name: Ciaffaglione, Valeria
name: Fallica, Antonino N.
name: Canale, Vittorio
name: Zajdel, Paweł
name: Pignatello, Rosario
name: Intagliata, Sebastiano
Publisher: name: Taylor & Francis
Year: 2021
Subjects: subject: Biochemistry
subject: Medicine
subject: Cell Biology
subject: Genetics
subject: FOS: Biological sciences
subject: Molecular Biology
subject: Pharmacology
subject: Biotechnology
subject: 39999 Chemical Sciences not elsewhere classified
subject: FOS: Chemical sciences
subject: Developmental Biology
subject: Cancer
subject: Hematology

description: In this work, the first mutual prodrug of 5-fluorouracil and heme oxygenase1 inhibitor (5-FU/HO-1 hybrid) has been designed, synthesised, and evaluated for its in vitro chemical and enzymatic hydrolysis stability. Predicted in silico physicochemical properties of the newly synthesised hybrid (3) demonstrated a drug-like profile with suitable Absorption, Distribution, Metabolism, and Excretion (ADME) properties and low toxic liabilities. Preliminary cytotoxicity evaluation towards human prostate (DU145) and lung (A549) cancer cell lines demonstrated that 3 exerted a similar effect on cell viability to that produced by the reference drug 5-FU. Among the two tested cancer cell lines, the A549 cells were more susceptible for 3. Of note, hybrid 3 also had a significantly lower cytotoxic effect on healthy human lung epithelial cells (BEAS-2B) than 5-FU. Altogether our results served as an initial proof-of-concept to develop 5-FU/HO-1 mutual prodrugs as potential novel anticancer agents.
Brief an [Johann Bernoulli]
Creators: name: Langguth, Christian August
Publisher: name: [s.n.]
Year: 1789

description: von [Christian August] Langguth
description: Öffentliche Bibliothek der Universität Basel
description: Deutsch
description: Verzeichnung=Description=Inventaire Januar 2015 HAN-Katalogisierungsregeln Vollständige Rekatalogisierung nach Standortverzeichnis und Briefkatalog
Brief an Joh[ann] Bernoulli
Creators: name: Lengnich, Karl Benjamin
Publisher: name: [s.n.]
Year: 1789

description: von [Carl Benjamin] Lengnich
description: Mit Oblate
description: Öffentliche Bibliothek der Universität Basel
description: Deutsch
description: Verzeichnung=Description=Inventaire Januar 2015 HAN-Katalogisierungsregeln Vollständige Rekatalogisierung nach Standortverzeichnis und Briefkatalog
Design, synthesis and in vitro and in vivo biological evaluation of flurbiprofen amides as new fatty acid amide hydrolase/cyclooxygenase-2 dual inhibitory potential analgesic agents
Creators: name: Deplano, Alessandro
name: Karlsson, Jessica
name: Moraca, Federica
name: Svensson, Mona
name: Cristiano, Claudia
name: Morgillo, Carmine Marco
name: Fowler, Christopher J.
name: Russo, Roberto
name: Catalanotti, Bruno
name: Onnis, Valentina
Publisher: name: Taylor & Francis
Year: 2021
Subjects: subject: Biochemistry
subject: Medicine
subject: Pharmacology
subject: Biotechnology
subject: 39999 Chemical Sciences not elsewhere classified
subject: FOS: Chemical sciences
subject: Immunology
subject: FOS: Clinical medicine
subject: 69999 Biological Sciences not elsewhere classified
subject: FOS: Biological sciences
subject: Hematology
subject: 110309 Infectious Diseases
subject: FOS: Health sciences

description: Compounds combining dual inhibitory action against FAAH and cyclooxygenase (COX) may be potentially useful analgesics. Here, we describe a novel flurbiprofen analogue, N-(3-bromopyridin-2-yl)-2-(2-fluoro-(1,1'-biphenyl)-4-yl)propanamide (Flu-AM4). The compound is a competitive, reversible inhibitor of FAAH with a Ki value of 13 nM and which inhibits COX activity in a substrate-selective manner. Molecular modelling suggested that Flu-AM4 optimally fits a hydrophobic pocket in the ACB region of FAAH, and binds to COX-2 similarly to flurbiprofen. In vivo studies indicated that at a dose of 10 mg/kg, Flu-AM4 was active in models of prolonged (formalin) and neuropathic (chronic constriction injury) pain and reduced the spinal expression of iNOS, COX-2, and NFκB in the neuropathic model. Thus, the present study identifies Flu-AM4 as a dual-action FAAH/substrate-selective COX inhibitor with anti-inflammatory and analgesic activity in animal pain models. These findings underscore the potential usefulness of such dual-action compounds.
[Betsy Ulrich]
Creators: name: Ellenrieder, Maria
Publisher: name: [s.n.]
Year: 1818
Subjects: Meyer-Ulrich, Betsy1802-1856

description: Porträt von Elisabeth Meyer-Ulrich (1802-1856), der Mutter von Conrad Ferdinand Meyer (1825-1898)
description: Marie Ellenrieder pinx
description: Auf der Rückseite mit Pinsel in Schwarz von der Künstlerin signiert und datiert
description: Vermerke mit Bleistift auf dem Keilrahmen oben: "4638/2" und "Betsy Meyer"
description: Aus dem Nachlass von Camilla Meyer, 1936 Exemplar der Zentralbibliothek Zürich, Graphische Sammlung und Fotoarchiv
Unterlagen zu den Protokollen der Sitzungen des Verwaltungsrats I
Creators: name: Hero
Publisher: name: [s.n.]
Year: 1949

description: Enthält: Protokollmitschriften (stenographiert), Orientierender Bericht, Kapitalerhöhung und Umstellung des Nennwerts der bisherigen Aktien, Korrespondenz etc.
description: Deutsch
Unterlagen zu den Protokollen der Sitzungen des Verwaltungsrats II
Creators: name: Hero
Publisher: name: [s.n.]
Year: 1964

description: Enthält: Ideenskizze über die Entwicklung des Hero-Konzerns, Übernahme Conservenfabrik St. Gallen, Finanzbedarf, Tiefkühlprodukte, Orientierung über Geschäftsgang etc.
description: Darin: Verzeichnis
description: Deutsch
Synthesis, potential antitumor activity, cell cycle analysis, and multitarget mechanisms of novel hydrazones incorporating a 4-methylsulfonylbenzene scaffold: a molecular docking study
Creators: name: Abdel-Aziz, Alaa A.-M.
name: El-Azab, Adel S.
name: AlSaif, Nawaf A.
name: Obaidullah, Ahmad J.
name: Al-Obaid, Abdulrahman M.
name: Al-Suwaidan, Ibrahim A.
Publisher: name: Taylor & Francis
Year: 2021
Subjects: subject: Biophysics
subject: Biochemistry
subject: Cell Biology
subject: Genetics
subject: FOS: Biological sciences
subject: Pharmacology
subject: Biotechnology
subject: 39999 Chemical Sciences not elsewhere classified
subject: FOS: Chemical sciences
subject: 69999 Biological Sciences not elsewhere classified
subject: Cancer
subject: Hematology

description: Hydrazone is a bioactive pharmacophore that can be used to design antitumor agents. We synthesised a series of hydrazones (compounds 4–24) incorporating a 4-methylsulfonylbenzene scaffold and analysed their potential antitumor activity. Compounds 6, 9, 16, and 20 had the most antitumor activity with a positive cytotoxic effect (PCE) of 52/59, 27/59, 59/59, and 59/59, respectively, while compounds 5, 10, 14, 15, 18, and 19 had a moderate antitumor activity with a PCE of 11/59–14/59. Compound 20 was the most active and had a mean 50% cell growth inhibition (GI50) of 0.26 µM. Compounds 9 and 20 showed the highest inhibitory activity against COX-2, with a half-maximal inhibitory concentration (IC50) of 2.97 and 6.94 μM, respectively. Compounds 16 and 20 significantly inhibited EGFR (IC50 = 0.2 and 0.19 μM, respectively) and HER2 (IC50 = 0.13 and 0.07 μM, respectively). Molecular docking studies of derivatives 9, 16, and 20 into the binding sites of COX-2, EGFR, and HER2 were carried out to explore the interaction mode and the structural requirements for antitumor activity. Compound 20 (MG_MID = 0.26 µM) is nearly 65-fold more potent than celecoxib (MG_MID = 17.5 µM), 3-fold more potent than 5-Fu (MG_MID = 0.90 µM), 30-fold more potent than erlotinib (MG_MID = 7.68 µM), and 9-fold more potent than gefitinib (MG_MID = 2.1 µM) and sorafenib (MG_MID = 2.33 µM).
Brief an Gottfried Kirch
Creators: name: Langenmantel, Hieronymus Ambrosius
Publisher: name: [s.n.]
Year: 1686

description: von Hieron. Ambros. Langenmantel
description: Mit rotem Siegel
description: Öffentliche Bibliothek der Universität Basel
description: Lateinisch
description: Verzeichnung=Description=Inventaire Januar 2015 HAN-Katalogisierungsregeln Vollständige Rekatalogisierung nach Standortverzeichnis und Briefkatalog
Quinazolin-4(3H)-one based potential multiple tyrosine kinase inhibitors with excellent cytotoxicity
Creators: name: Mirgany, Tebyan O.
name: Abdalla, Ashraf N.
name: Arifuzzaman, Md
name: Rahman, A. F. M. Motiur
name: Al-Salem, Huda S.
Publisher: name: Taylor & Francis
Year: 2021
Subjects: subject: Biochemistry
subject: Pharmacology
subject: 39999 Chemical Sciences not elsewhere classified
subject: FOS: Chemical sciences
subject: 69999 Biological Sciences not elsewhere classified
subject: FOS: Biological sciences
subject: Cancer

description: A series of quinazolin-4(3H)-one derivatives were synthesised and evaluated for their cytotoxicity against human Caucasian breast adenocarcinoma (MCF-7) and human ovarian carcinoma (A2780) cell lines. Cytotoxicity of the most tested compounds was 2- to 30-fold more than the positive control lapatinib (IC50 of 2j = 3.79 ± 0.96; 3j = 0.20 ± 0.02; and lapatinib = 5.9 ± 0.74) against MCF7 cell lines except two compounds (IC50 of 2 b = 15.72 ± 0.07 and 2e = 14.88 ± 0.99). On the other hand, cytotoxicity was 4 − 87 folds (IC50 of 3a = 3.00 ± 1.20; 3 g = 0.14 ± 0.03) more the positive control lapatinib (IC50 = 12.11 ± 1.03) against A2780 cell lines except compound 2e (IC50 = 16.43 ± 1.80). Among the synthesised quinazolin-4(3H)-one derivatives, potent cytotoxic 2f-j and 3f-j were investigated for molecular mechanism of action. Inhibitory activities of the compounds were tested against multiple tyrosine protein kinases (CDK2, HER2, EGFR and VEGFR2) enzymes. As expected, all the quinazolin-4(3H)-one derivatives were showed comparable inhibitory activity against those kinases tested, especially, compound 2i and 3i showed potent inhibitory activity against CDK2, HER2, EGFR tyrosine kinases. Therefore, molecular docking analysis for quinazolin-4(3H)-one derivatives 2i and 3i were performed, and it was revealed that compounds 2i and 3i act as ATP non-competitive type-II inhibitor against CDK2 kinase enzymes and ATP competitive type-I inhibitor against EGFR kinase enzymes. However, in case of HER2, compounds 2i act as ATP non-competitive type-II inhibitor and 3i act as ATP competitive type-I inhibitor. Docking results of known inhibitors were compared with synthesised compounds and found synthesised 2i and 3i are superior than the known inhibitors in case of interactions. In addition, in silico drug likeness properties of quinazolin-4(3H)-one derivatives showed better predicted ADME values than lapatinib.
Brief an [Johann] Bernoulli
Creators: name: Lengnich, Karl Benjamin
Publisher: name: [s.n.]
Year: 1788

description: von [Carl Benjamin] Lengnich
description: Mit Oblate
description: Öffentliche Bibliothek der Universität Basel
description: Deutsch
description: Verzeichnung=Description=Inventaire Januar 2015 HAN-Katalogisierungsregeln Vollständige Rekatalogisierung nach Standortverzeichnis und Briefkatalog
Brief an [Johann] Bernoulli
Creators: name: Lambertenghi, Luigi
Publisher: name: [s.n.]
Year: 1779

description: von Luigi Lambertenghi
description: Mit rotem Siegel
description: Öffentliche Bibliothek der Universität Basel
description: Französisch
description: Druck: Astronomisches Jahrbuch für das Jahr ... : nebst einer Sammlung der neuesten in die astronomischen Wissenschaften einschlagenden Abhandlungen, Beobachtungen und Nachrichten / mit Genehmhaltung der Königl. Akademie der Wissenschaften. - Berlin : Lange, 1782, II, 133-134
description: Verzeichnung=Description=Inventaire Januar 2015 HAN-Katalogisierungsregeln Vollständige Rekatalogisierung nach Standortverzeichnis und Briefkatalog
Use of spatial transformations and reference frames: individual differences in spatial ability
Creators: name: Tarampi, Margaret Romaine
Publisher: name: University of Utah
Year: 2015
Subjects: Dance
Expertise
Individual differences
Spatial ability
Spatial thinking
Spatial transformations

description: The use of spatial transformations is ubiquitous in everyday cognitive processing from reading maps to planning actions to reasoning. Use and proficiency in spatial transformations may vary based on both spatial ability and spatial expertise. Spatial ability is the ability to create, maintain, and transform visual imagery. Spatial expertise is knowledge, skills, or characteristics related to spatial thinking that can be used to differentiate outstanding individuals from less outstanding individuals. Three classes of spatial transformations-object-based (i.e., object rotation), perspective-based (i.e., body rotation), and effector-based (i.e., body-part rotation)-and their relationship to three spatial abilities-spatial orientation, spatial visualization, and kinesthetic imagery-were examined. Participants (controls and dancers) completed psychometric tests predicted to recruit the three spatial ability factors. They also performed timed computer-based spatial transformations of bodies and body-parts in two types of tasks (same/different and left/right). Overall, performance on the transformations as a function of task type and stimulus was predicted differentially by the three spatial ability factors. This suggests that three distinct processes are involved. Furthermore, dancer performance on the transformation tasks suggested more dynamic versus static processing of stimuli than controls.
Cyclocephala pugnax Arrow 1914
Creators: name: Hielkema, Auke J.
name: Hielkema, Meindert A.
Publisher: name: Zenodo
Year: 2019
Subjects: Biodiversity
Taxonomy
Animalia
Arthropoda
Insecta
Coleoptera
Dynastidae
Cyclocephala
Cyclocephala pugnax

description: Cyclocephala pugnax Arrow, 1914
Cyclocephala pugnax Arrow 1914: 274 (“Guianas”)
Distribution. Guyana: Endrödi 1966a: 289, 1985a: 72, 135; Lachaume 1992: 13; Moore et al. 2018b: 234. Suriname: Endrödi 1985a: 72, 135; Lachaume 1992: 13; Moore et al. 2018b: 234. French Guiana: Endrödi 1966a: 289 (Suriname Cayenne [> Fr. Guiana!]), 1985a: 72, 135; Lachaume 1992: 13; Duranton 2011: 14; Ponchel 2011: 60; Dupuis 2016b: 109; Moore et al. 2018b: 234. “Guianas”: Arrow 1914: 274, 1937b: 15; Blackwelder 1944: 252. Brazil (NA): Arrow 1914: 274; Endrödi 1966a: 289 (NA), 1985a: 72, 135; Lachaume 1992: 13; Moore et al. 2018b: 234. Other: Endrödi 1966a: 289 (Bolivia, Peru), 1985a: 72, 135 (Bolivia, Peru); Lachaume 1992: 13 (Bolivia, Peru); Moore et al. 2018b: 234 (Bolivia, Colombia, Peru).
Note. Endrödi (1966a: 289) records Cyclocephala pugnax for Suriname with the location “Cayenne.” This record for Suriname is copied into Endrödi (1985a: 72, 135), Lachaume (1992: 13) and Moore et al. (2018b: 234). As Cayenne is situated in French Guiana rather than Suriname, this is not a valid record for the latter country. We are unaware of any other records from Suriname. Although this species has been found in Guyana and French Guiana and is thus likely also present in Suriname, this has yet to be confirmed.
description: Published as part of Hielkema, Auke J. & Hielkema, Meindert A., 2019, An annotated checklist of the Scarabaeoidea (Insecta: Coleoptera) of the Guianas, pp. 1-306 in Insecta Mundi 732 (732) on page 178, DOI: 10.5281/zenodo.3678492
Iontophoretic transport mechanisms across skin
Creators: name: Sims, Sandra Marie
Publisher: name: University of Utah
Year: 2012
Subjects: Drug Delivery Systems
Ion Transport
Iontophoresis
Models, Biological
Salicylates
Skin Absorption
Tetraethylammonium Compounds

description: Iontophoresis is the process of increasing the penetration rate of ions into or through a membrane by the application of an external electric field across the membrane. The Nernst-Planck theory has been used to describe the flux enhancement of ions across membranes during iontophoresis. This theory neglects secondary effects such as convective solvent flow and permeability increases due to membrane alterations which result from the applied field. Therefore, the mechanisms whereby charged and uncharged solutes transport across skin under the influence of an applied electric field were investigated.  The modified Nernst-Planck theory, which includes convective solvent flow contributions to the total flux of ions, has been used to describe the flux enhancement of neutral (glucose) and charged (tetraethylammonium ion and salicylate ion) solutes during iontophoresis. Using glucose and a model, net negatively charged membrane (Nuclepore\circler), solvent flow was shown to be in the direction of counterion (cation) movement. An estimate of the solvent flow velocity was obtained from the glucose flux using the modified Nernst-Planck theory. This velocity value was then used to predict the flux enhancements of a monovalent cation and anion. Comparisons between the theoretical prediction and experimental data using tetraethylammonium ion (cation) and salicylate ion (anion) showed good agreement.  A physical model was developed to gain a more mechanistic understanding of the solvent flow process. The Poisson-Boltzmann equation, which relates the surface potential to the surface charge density, was solved numerically for the radial electric potential profile within a cylindrical pore. The potential profile was then used with the equations of fluid motion to predict the electro-osmotic velocity. The membrane pore partitioning behavior for the tetraethylammonium and salicylate ions was then predicted at selected ionic strengths using the best estimates of the electrical potential profile. The agreement between experimental and theoretical partition coefficient values was very good.  Iontophoretic studies employing human skin demonstrated that there were both electro-osmosis effects and field induced membrane alterations in addition to direct electric field effects on ion transport. Membrane alterations occurred at 1000mV but not at lower voltages. These alterations reversed after removal of the applied voltage. Mannitol flux enhancement in human skin showed only a 20-25% solvent flow contribution to the modified Nernst-Planck flux for monovalent cations and anions. Experiments with tetraethylammonium and salicylate ions were in good agreement with the predictions of the modified Nernst-Planck equation when membrane alteration effects were taken into consideration.
Design, synthesis, in silico studies and in vitro evaluation of isatin-pyridine oximes hybrids as novel acetylcholinesterase reactivators
Creators: name: Kitagawa, Daniel A. S.
name: Rodrigues, Rafael B.
name: Silva, Thiago N.
name: dos Santos, Wellington V.
name: da Rocha, Vinicius C. V.
name: de Almeida, Joyce S. F. D.
name: Bernardo, Leandro B.
name: Carvalho-Silva, Taynara
name: Ferreira, Cintia N.
name: da Silva, Angelo A. T.
name: Simas, Alessandro B. C.
name: Nepovimova, Eugenie
name: Kuča, Kamil
name: França, Tanos C. C.
name: de A. Cavalcante, Samir F.
Publisher: name: Taylor & Francis
Year: 2022
Subjects: subject: Biochemistry
subject: Medicine
subject: Pharmacology
subject: Biotechnology
subject: 39999 Chemical Sciences not elsewhere classified
subject: FOS: Chemical sciences
subject: 69999 Biological Sciences not elsewhere classified
subject: FOS: Biological sciences
subject: 80699 Information Systems not elsewhere classified
subject: FOS: Computer and information sciences
subject: 111714 Mental Health
subject: FOS: Health sciences
subject: 110309 Infectious Diseases

description: Organophosphorus poisoning caused by some pesticides and nerve agents is a life-threating condition that must be swiftly addressed to avoid casualties. Despite the availability of medical countermeasures, the clinically available compounds lack a broad spectrum, are not effective towards all organophosphorus toxins, and have poor pharmacokinetics properties to allow them crossing the blood-brain barrier, hampering cholinesterase reactivation at the central nervous system. In this work, we designed and synthesised novel isatin derivatives, linked to a pyridinium 4-oxime moiety by an alkyl chain with improved calculated properties, and tested their reactivation potency against paraoxon- and NEMP-inhibited acetylcholinesterase in comparison to the standard antidote pralidoxime. Our results showed that these compounds displayed comparable in vitro reactivation also pointed by the in silico studies, suggesting that they are promising compounds to tackle organophosphorus poisoning.
Morpholine-based chalcones as dual-acting monoamine oxidase-B and acetylcholinesterase inhibitors: synthesis and biochemical investigations
Creators: name: Sasidharan, Rani
name: Eom, Bo Hyun
name: Heo, Jeong Hyun
name: Park, Jong Eun
name: Abdelgawad, Mohamed A.
name: Musa, Arafa
name: Gambacorta, Nicola
name: Nicolotti, Orazio
name: Manju, Sreedharannair Leelabaiamma
name: Mathew, Bijo
name: Kim, Hoon
Publisher: name: Taylor & Francis
Year: 2021
Subjects: subject: Biochemistry
subject: Cell Biology
subject: Molecular Biology
subject: Neuroscience
subject: Pharmacology
subject: Biotechnology
subject: 39999 Chemical Sciences not elsewhere classified
subject: FOS: Chemical sciences
subject: 111714 Mental Health
subject: FOS: Health sciences
subject: Hematology

description: Nine compounds (MO1–MO9) containing the morpholine moiety were assessed for their inhibitory activities against monoamine oxidases (MAOs) and acetylcholinesterase (AChE). Most of the compounds potently inhibited MAO-B; MO1 most potently inhibited with an IC50 value of 0.030 µM, followed by MO7 (0.25 µM). MO5 most potently inhibited AChE (IC50 = 6.1 µM), followed by MO9 (IC50 = 12.01 µM) and MO7 most potently inhibited MAO-A (IC50 = 7.1 µM). MO1 was a reversible mixed-type inhibitor of MAO-B (Ki = 0.018 µM); MO5 reversibly competitively inhibited AChE (Ki = 2.52 µM); and MO9 reversibly noncompetitively inhibited AChE (Ki = 7.04 µM). MO1, MO5 and MO9 crossed the blood–brain barrier, and were non-toxic to normal VERO cells. These results show that MO1 is a selective inhibitor of MAO-B and that MO5 is a dual-acting inhibitor of AChE and MAO-B, and that both should be considered candidates for the treatment of Alzheimer’s disease.
Cyclocephala putrida Burmeister 1847
Creators: name: Hielkema, Auke J.
name: Hielkema, Meindert A.
Publisher: name: Zenodo
Year: 2019
Subjects: Biodiversity
Taxonomy
Animalia
Arthropoda
Insecta
Coleoptera
Dynastidae
Cyclocephala
Cyclocephala putrida

description: Cyclocephala putrida Burmeister, 1847
Cyclocephala putrida Burmeister 1847: 51 (Chile - LECTOTYPE)
Distribution. Guyana: Endrödi 1966a: 291, 1985a: 108, 143; Lachaume 1992: 16; Moore et al. 2018b: 235. Suriname: Lachaume 1992: 16. French Guiana: Endrödi 1966a: 291, 1985a: 108, 143; Lachaume 1992: 16; Duranton 2011: 14 (?); Moore et al. 2018b: 235. Brazil: Endrödi 1966a: 291, 1985a: 108, 143; Lachaume 1992: 16; Moore et al. 2018b: 235. Venezuela: Endrödi 1966a: 291, 1985a: 108, 143; Lachaume 1992: 16; Moore et al. 2018b: 235. Other: Burmeister 1847: 51 (Chile); Arrow 1937b: 15 (Chile); Blackwelder 1944: 252 (Argentina, Chile); Endrödi 1966a: 291 (Argentina - designation NEO- TYPE Cyclocephala putrida, Bolivia, Chile, Paraguay, Uruguay), 1985a: 108, 143 (Argentina, Bolivia, Paraguay, Uruguay); Dechambre 1991: 124 (Chile - designation LECTOTYPE Cyclocephala putrida); Lachaume 1992: 16 (Argentina, Bolivia, Paraguay, Uruguay); Ponchel 2011 (not mentioned); Dupuis 2016b (not mentioned); Moore et al. 2018b: 235 (Argentina, Bolivia, Chile, Paraguay, Uruguay).
Note 1. The neotype of Cyclocephala putrida designated in Endrödi (1966a: 291) was rendered invalid when type material from Burmeister was recovered and a lectotype was designated in Dechambre (1991: 124).
Note 2. Endrödi (1966a: 291, 1985a: 108), Dechambre (1991: 124), Lachaume (1992: 16) and Moore et al. (2018b: 235) mention Cyclocephala putrida for the Guianas. However, Duranton (2011: 13) apparently saw no definite specimens from French Guiana, and the species is not mentioned in the checklists for French Guiana by Ponchel (2011) and Dupuis (2016b). We are unaware of recent records from northern South America and consider the occurrence of this species in the research area and Venezuela in need of confirmation.
description: Published as part of Hielkema, Auke J. & Hielkema, Meindert A., 2019, An annotated checklist of the Scarabaeoidea (Insecta: Coleoptera) of the Guianas, pp. 1-306 in Insecta Mundi 732 (732) on pages 178-179, DOI: 10.5281/zenodo.3678492
Discovery of new quinolines as potent colchicine binding site inhibitors: design, synthesis, docking studies, and anti-proliferative evaluation
Creators: name: Hagras, Mohamed
name: Deeb, Moshira A. El
name: Elzahabi, Heba S. A.
name: Elkaeed, Eslam B.
name: Mehany, Ahmed B. M.
name: Eissa, Ibrahim H.
Publisher: name: Taylor & Francis
Year: 2021
Subjects: subject: Biochemistry
subject: Cell Biology
subject: Pharmacology
subject: 39999 Chemical Sciences not elsewhere classified
subject: FOS: Chemical sciences
subject: 69999 Biological Sciences not elsewhere classified
subject: FOS: Biological sciences
subject: Cancer
subject: Hematology

description: Discovering of new anticancer agents with potential activity against tubulin polymerisation is still a promising approach. Colchicine binding site inhibitors are the most relevant anti-tubulin polymerisation agents. Thus, new quinoline derivatives have been designed and synthesised to possess the same essential pharmacophoric features of colchicine binding site inhibitors. The synthesised compounds were tested in vitro against a panel of three human cancer cell lines (HepG-2, HCT-116, and MCF-7) using colchicine as a positive control. Comparing to colchicine (IC50 = 7.40, 9.32, and 10.41 µM against HepG-2, HCT-116, and MCF-7, respectively), compounds 20, 21, 22, 23, 24, 25, 26, and 28 exhibited superior cytotoxic activities with IC50 values ranging from 1.78 to 9.19 µM. In order to sightsee the proposed mechanism of anti-proliferative activity, the most active members were further evaluated in vitro for their inhibitory activities against tubulin polymerisation. Compounds 21 and 32 exhibited the highest tubulin polymerisation inhibitory effect with IC50 values of 9.11 and 10.5 nM, respectively. Such members showed activities higher than that of colchicine (IC50 = 10.6 nM) and CA-4 (IC50 = 13.2 nM). The impact of the most promising compound 25 on cell cycle distribution was assessed. The results revealed that compound 25 can arrest the cell cycle at G2/M phase. Annexin V and PI double staining assay was carried out to explore the apoptotic effect of the synthesised compounds. Compound 25 induced apoptotic effect on HepG-2 thirteen times more than the control cells. To examine the binding pattern of the target compounds against the tubulin heterodimers active site, molecular docking studies were carried out.
Cyclocephala quercina Burmeister 1847
Creators: name: Hielkema, Auke J.
name: Hielkema, Meindert A.
Publisher: name: Zenodo
Year: 2019
Subjects: Biodiversity
Taxonomy
Animalia
Arthropoda
Insecta
Coleoptera
Dynastidae
Cyclocephala
Cyclocephala quercina

description: Cyclocephala quercina Burmeister, 1847
Cyclocephala quercina Burmeister 1847: 54 (French Guiana - LECTOTYPE)
= Cyclocephala obesa Burmeister 1847: 59 (Guyana - LECTOTYPE) - Dechambre and Duranton 2005: 67 (syn. nov.)
Distribution. Guyana: Burmeister 1847: 59 (as C. obesa); Endrödi 1966a: 268 (designation LECTOTYPE Cyclocephala obesa), 1985a: 98, 139 (as C. obesa); Moore et al. 2018b: 237. Suriname: MHCN - NEW COUNTRY RECORD (Suriname, Para, 1 km W of Zanderij, (5°27′37″N, 55°13′21″W). 5-I-2011. A. J. Hielkema. On UV/HPL in savanna forest.); NZCS. French Guiana: Burmeister 1847: 54; Endrödi 1966a: 268, 294 (as C. obesa; as C. quercina); Endrödi 1985a: 98, 139 (as C. obesa); Dechambre 1991: 124 (designation LECTOTYPE Cyclocephala quercina); Duranton 2011: 14 (as C. obesa; as C. quercina); Ponchel 2011: 60; Dupuis 2016b: 109; Moore et al. 2018b: 237. “Guianas”: Arrow 1937b: 13, 15 (as C. obesa; as C. quercina); Blackwelder 1944: 252 (as C. obesa; as C. quercina). Venezuela: Endrödi 1966a: 268 (as C. obesa); Endrödi 1985a: 98, 139 (as C. obesa); Moore et al. 2018b: 237. Other: Endrödi 1966a: 268 (as C. obesa); Endrödi 1985a: 98, 139, 147 (Costa Rica, Ecuador, Honduras, Trinidad and Tobago, U.S.A. as C. obesa; none - as C. quercina); Moore et al. 2018b: 237 (Ecuador, Trinidad and Tobago).
Note 1. Endrödi (1966a: 294, 1985a: 147) mentions not seeing any specimens of Cyclocephala quercina, but according to Endrödi (1966a: 268, 1985a: 98, 139) he did examine specimens of C. obesa.
Note 2. According to Ratcliffe (2003: 225), the records in Endrödi (1966a: 268, 1985a: 98, 139) of Cyclocephala obesa (now a synonym of C. quercina) from Costa Rica, Honduras and the U.S.A. are incorrect, as this is a South American species.
Note 3. Despite the synonymization of Cyclocephala obesa with C. quercina in Dechambre and Duranton (2005: 67), Duranton (2011: 14) lists both names again as separate species. The reason for this is unknown to us.
description: Published as part of Hielkema, Auke J. & Hielkema, Meindert A., 2019, An annotated checklist of the Scarabaeoidea (Insecta: Coleoptera) of the Guianas, pp. 1-306 in Insecta Mundi 732 (732) on page 179, DOI: 10.5281/zenodo.3678492
Collaborative and adaptive wildlife management in a changing climate
Creators: name: Williamson, Jeremiah I.
Publisher: name: University of Utah
Year: 2014
Subjects: Adaptive management
Climate change
Collaboration
Public lands
Wildlife

description: Wildlife, one of the United States' most treasured natural resources, faces a dire future. Changing climate conditions will upend the natural world wild creatures inhabit. Dramatic shifts in precipitation, spreading disease, cascading ecological events, and catastrophic events such as wildfires and floods will present wildlife with challenges of a degree and frequency not seen in U.S. history. These shifts in climate will in turn bring to bear great pressure on the heralded U.S. approach to wildlife management. Ill equipped to respond to the jurisdictional fragmentation and scientific uncertainty that will predominate wildlife management in a changing climate, U.S. wildlife managers must seek out new tools to cope with the difficulties that lie ahead. Collaborative governance and adaptive management-management techniques designed to cope with fragmentation and uncertainty-have obvious appeal. While both have failed to date to deliver their theoretical appeal in practice, these failures can be readily attributed to inadequate implementation efforts. Remedying those deficiencies can greatly increase the likelihood of successful implementation. The federal land management agencies, which oversee the vast majority of wildlife habitat in the United States, are well suited to advance collaborative and adaptive experiments in wildlife habitat management. Acting as hubs to deploy collaboration and adaptation more broadly in the context of wildlife management, the Forest Service, Bureau of Land Management, Fish and Wildlife Service, and National Park Service should incorporate implementation baselines to ensure the appropriate and sufficient deployment of collaborative and adaptive processes. Such efforts will not eliminate the grave risks wild animals face, but will help wildlife managers to have at least a chance of ushering the United States' other inhabitants through the storm.