| 1. |
- Eriksson, Leif A., 1964-, et al.
(författare)
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Tetrazole derivatives as cytochrome p450 inhibitors
- 2019
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Patent (populärvet., debatt m.m.)abstract
- According to the invention there is provided a compound of formula I, wherein R1 and R2 have meanings given in the description, which compounds are useful in the treatment of skin disorders and other diseases.
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| 2. |
- Fagan, V., et al.
(författare)
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COMPARE analysis of the toxicity of an iminoquinone derivative of the imidazo[5,4-f]benzimidazoles with NAD(P)H:quinone Oxidoreductase 1 (NQO1) activity and computational docking of quinones as NQO1 substrates
- 2012
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Ingår i: Bioorganic & Medicinal Chemistry. - : Elsevier BV. - 0968-0896 .- 1464-3391. ; 20:10, s. 3223-3232
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Tidskriftsartikel (refereegranskat)abstract
- Synthesis and cytotoxicity of imidazo[5,4-f]benzimidazolequinones and iminoquinone derivatives is described, enabling structure-activity relationships to be obtained. The most promising compound (an iminoquinone derivative) has undergone National Cancer Institute (NCI) 60 cell line (single and five dose) screening, and using the NCI COMPARE program, has shown correlation to NQO1 activity and to other NQO1 substrates. Common structural features suggest that the iminoquinone moiety is significant with regard to NQO1 specificity. Computational docking into the active site of NQO1 was performed, and the first comprehensive mitomycin C (MMC)-NQO1 docking study is presented. Small distances for hydride reduction and high binding affinities are characteristic of MMC and of iminoquinones showing correlations with NQO1 via COMPARE analysis. Docking also indicated that the presence of a substituent capable of hydrogen bonding to the His194 residue is important in influencing the orientation of the substrate in the NQO1 active site, leading to more efficient reduction. (C) 2012 Elsevier Ltd. All rights reserved.
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| 3. |
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| 4. |
- Karlsson, Mikael, 1978, et al.
(författare)
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Characterisation of silicon, zirconium and aluminium coated titanium dioxide pigments recovered from paint waste
- 2019
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Ingår i: Dyes and Pigments. - : Elsevier BV. - 0143-7208 .- 1873-3743. ; 162, s. 145-152
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Tidskriftsartikel (refereegranskat)abstract
- © 2018 Elsevier Ltd Titanium dioxide (TiO2) is the major white pigment used by the paint industry. However, the production of TiO2is associated with a high carbon footprint. An alternative source of pigment could be created by developing a method to recover it from waste paint. In this paper two rutile pigments with different surface treatments were recovered from paint by a thermal recycling process. The pigments were analysed using powder x-ray diffraction (XRD), X-ray photoelectron spectroscopy (XPS), surface area measurements (BET), laser diffraction for particle size analysis and zeta potential measurements before and after the recycling process. It was concluded that the rutile cores of both pigments were intact and there were no major changes in particle size distribution or surface charge for either pigment induced by the recycling process. However, XPS and zeta potential measurements showed that the surface coating of the pigments can be more or less degraded depending on the chemical nature, which might imply the need for further re-coating after-treatment. Another option would be to find another application for the pigment where the quality and function of the coating is of less importance.
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| 5. |
- Boge, Lukas, 1987
(författare)
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Lipid-based liquid crystals as drug delivery vehicles for antimicrobial peptides
- 2017
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Licentiatavhandling (övrigt vetenskapligt/konstnärligt)abstract
- The development of antimicrobial resistance is a great challenge within the health sector around the world. The demand for new efficient treatments is alarming in order to treat various bacterial infections in the near future. Antimicrobial peptides (AMPs) are a group of novel antibiotics that have gain more and more attraction the past decade. However, AMPs suffers from relatively low stability due to proteolytic and chemical degradation. As a consequence, carrier systems protecting the AMPs are highly needed for achieving efficient treatments. In this thesis, lyotropic liquid crystalline (LC) structures consisting of cubic glycerol monooleate/water and hexagonal glycerol monooleate/oleic acid/water have been examined as carriers for three AMPs (AP114, DPK-060 and LL-37). Both bulk gels and discrete dispersed structures, i.e. cubosomes and hexosomes have been studied. Moreover, two different peptide loading approaches for the cubosomes were tested and compared; pre- and post-loading. Characterization of the LC structures was performed using small-angle x-ray scattering (SAXS), dynamic light scattering, ζ-potential, and cryogenic transmission electron microscopy (Cryo-TEM) and peptide loading efficacy by liquid chromatography. The antimicrobial effect of the AMP loaded LC nanoparticles (LCNPs) was studied in vitro using minimum inhibitory concentration (MIC) and time-kill assays. Proteolytic protection was investigated by incubating the formulations with two elastases and the antimicrobial effect after proteolysis was studied using radial diffusion assay (RDA). Results showed that the most hydrophobic peptide (AP114) was prone to induce an increase in negative curvature of the bulk cubic LC gel, hence pushing the system towards a hexagonal structure. The most polar peptide (DPK-060) induced a decrease in negative curvature while LL-37 did not change the LC phase at all. The hexagonal LC phase was not affected by any of the AMPs. The cubic pre- and post-loaded LCNPs displayed promising antimicrobial activity, and sometimes could a synergetic effect be observed, resulting in a slightly better activity than the unformulated AMP. The hexagonal LCNPs were found to be very efficient in encapsulating the AMPs, but did not display any antimicrobial effect, indicating insufficient delivery of peptide to the bacteria. Moreover, cubosomes post-loaded with LL-37 was found to protect the peptide from proteolytic degradation, resulting in a significant better bactericidal effect after proteolysis.
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| 6. |
- Danelius, Emma, et al.
(författare)
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Flexibility is important for inhibition of the MDM2/p53 protein-protein interaction by cyclic β-hairpins
- 2016
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Ingår i: Organic and Biomolecular Chemistry. - : Royal Society of Chemistry (RSC). - 1477-0520 .- 1477-0539. ; 14, s. 10386-10393
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Tidskriftsartikel (refereegranskat)abstract
- © 2016 The Royal Society of Chemistry.Protein-protein interactions that have large, flat and featureless binding sites are difficult drug targets. In the development of their modulators conventional drug discovery strategies are often unsuccessful. Gaining a detailed understanding of the binding mode of protein-protein interaction inhibitors is therefore of vast importance for their future pharmaceutical use. The MDM2/p53 protein pair is a highly promising target for cancer treatment. Disruption of the protein complex using p53 α-helix mimetics has been shown to be a successful strategy to control p53 activity. To gain further insight into the binding of inhibitors to MDM2, the flexibility of four cyclic β-hairpins that act as α-helical mimetics and potential MDM2/p53 interaction inhibitors was investigated in relation to their inhibitory activity. MDM2-binding of the mimetics was determined using fluorescence polarization and surface plasmon resonance assays, whereas their conformation and dynamics in solution was described by the combined experimental and computational NAMFIS analysis. Molecular flexibility was shown to be important for the activity of the cyclic β-hairpin based MDM2 inhibitors.
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| 7. |
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| 8. |
- Schmidt, Florian, et al.
(författare)
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Ammonia in breath and emitted from skin
- 2013
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Ingår i: Journal of Breath Research. - : IOP Publishing. - 1752-7155 .- 1752-7163. ; 7:1
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Tidskriftsartikel (refereegranskat)abstract
- Ammonia concentrations in exhaled breath (eNH(3)) and skin gas of 20 healthy subjects were measured on-line with a commercial cavity ring-down spectrometer and compared to saliva pH and plasma ammonium ion (NH4+), urea and creatinine concentrations. Special attention was given to mouth, nose and skin sampling procedures and the accurate quantification of ammonia in humid gas samples. The obtained median concentrations were 688 parts per billion by volume (ppbv) for mouth-eNH(3), 34 ppbv for nose-eNH3, and 21 ppbv for both mouth-and nose-eNH(3) after an acidic mouth wash (MW). The median ammonia emission rate from the lower forearm was 0.3 ng cm(-2) min(-1). Statistically significant (p < 0.05) correlations between the breath, skin and plasma ammonia/ammonium concentrations were not found. However, mouth-eNH(3) strongly (p < 0.001) correlated with saliva pH. This dependence was also observed in detailed measurements of the diurnal variation and the response of eNH(3) to the acidic MW. It is concluded that eNH(3) as such does not reflect plasma but saliva and airway mucus NH4+ concentrations and is affected by saliva and airway mucus pH. After normalization with saliva pH using the Henderson-Hasselbalch equation, mouth-eNH(3) correlated with plasma NH4+, which points to saliva and plasma NH4+ being linked via hydrolysis of salivary urea.
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| 10. |
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