| 1. |
- Andersson, Charlotta S., 1979-, et al.
(författare)
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A dynamic c terminal segment in the mycobacterium tuberculosis mn/fe r2lox protein can adopt a helical structure with possible functional consequences
- 2012
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Ingår i: Chemistry and Biodiversity. - 1612-1872. ; 9:9, s. 1981-1988
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Tidskriftsartikel (refereegranskat)abstract
- Mycobacterium tuberculosis R2-like ligand-binding oxidase (MtR2lox) belongs to a recently discovered group of proteins that are homologous to the ribonucleotide reductase R2 proteins. MtR2lox carries a heterodinuclear Mn/Fe cofactor and, unlike R2 proteins, a large ligand-binding cavity. A unique tyrosine-valine cross link is also found in the vicinity of the active site. To date, all known structures of R2 and R2lox proteins show a disordered C-terminal segment. Here, we present two new crystal forms of MtR2lox, revealing an ordered helical C-terminal. The ability of alternating between an ordered and disordered state agrees well with bioinformatic analysis of the protein sequence. Interestingly, ordering of the C-terminal helix shields a large positively charged patch on the protein surface, potentially used for interaction with other cellular components. We hypothesize that the dynamic C-terminal segment may be involved in control of protein function in vivo.
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| 2. |
- Danieli, B, et al.
(författare)
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Synthesis and biological evaluation of paclitaxel-thiocoichicine hybrids
- 2004
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Ingår i: Chemistry & Biodiversity. - Wiley. - 1612-1872. ; 1:2, s. 327-345
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Tidskriftsartikel (refereegranskat)abstract
- The bifunctional taxoid-colchicinoid hybrids 6-8 were synthesized and evaluated in assays of cytotoxicity and tubulin assembly/disassembly. All compounds showed a high degree of cytotoxicity, but, while 6 and 7 behaved as bifunctional tubulin binders not unlike an equimolecular mixture of taxol and thiocolchicine, 8 was surprisingly devoid of tubulin activity, acting on a distinct and yet to identify molecular target.
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| 3. |
- Hersleth, Hans-Petter, et al.
(författare)
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The Influence of X-Rays on the Structural Studies of Peroxide-Derived Myoglobin Intermediates
- 2008
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Ingår i: CHEMISTRY & BIODIVERSITY. - WILEY-V C H VERLAG GMBH. - 1612-1872. ; 5:10, s. 2067-2089
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Forskningsöversikt (refereegranskat)abstract
- In recent years, the awareness of potential radiation damage of metal centers in protein crystals during crystallographic data collection has received increasing attention. The radiation damage can lead to radiation-induced changes and reduction of the metal sites. One of the research fields where these concerns have been comprehensively addressed is the study of the reaction intermediates of the heme peroxidase and oxygenase reaction cycles. For both the resting states and the high-valent intermediates, the X-rays used in the structure determination have given undesired side effects through radiation-induced changes to the trapped intermediates. However, X-rays have been used to generate and trap the peroxy/hydroperoxy state in crystals. In this review, the structural work and the influence of X-rays on these intermediates in myoglobin are summarized and viewed in light of analogous studies on similar intermediates in peroxidases and oxygenases.
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| 4. |
- Norden, B, et al.
(författare)
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Analysis and understanding of high-dimensionality data by means of multivariate data analysis
- 2005
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Ingår i: Chemistry & Biodiversity. - Verlag Helvetica Chimica Acta. - 1612-1872. ; 2:11, s. 1487-1494
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Tidskriftsartikel (refereegranskat)abstract
- Multivariate analysis such as principal-components analysis (PCA) and partial-least-squares-discriminant analysis (PLS-DA) have been applied to peptidomics data from clinical urine samples subjected to LC/MS analysis. We show that it is possible to use these methods to get information from a complex set of clinical data. The aim of the work is to use this information as a first step in the further search for clinical biomarker data. It is possible to identify peptide-biomarker fingerprints related to disease diagnosis and progression. Further, we review clinical proteomics and pharmacogenomics data analyzed with the same multivariate approach.
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| 5. |
- Pathmasiri, Wimal, et al.
(författare)
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Aryl ketones from Acronychia pedunculata with cyclooxygenase-2 inhibitory effects
- 2005
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Ingår i: Chemistry & biodiversity. - 1612-1872. ; 2:4, s. 463-469
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Tidskriftsartikel (refereegranskat)abstract
- 1-[2,4-Dihydroxy-6-methoxy-3,5-bis(3-methylbut-2-en-1-yl)phenyl]ethanone (1), and a new aryl ketone, named acrovestenol (2), were isolated as cyclooxygenase-2 (COX-2) inhibitory principles from a CH2Cl2 extract of the bark of Acronychia pedunculata by a bioassay-guided fractionation procedure. Compound 2 inhibited COX-2 with an IC50 value of 142.0+/-2.15 microM, compared to the COX-2 inhibitory reference compound NS-398 with an IC50 value of 11.3+/-1.12 microM. Compound 1 inhibited COX-2-catalyzed PG biosynthesis with 68% at a concentration of 500 microM. The structures were determined by UV, IR, and 1D- and 2D-NMR, including TOCSY, HSQC-DEPT, and HMBC, and MS investigations.
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| 6. |
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