The first chemoselective asymmetric hydrogenation of (1-bromo-1-alkenyl)boronic esters to (alfa-bromoalkyl)boronic esters was reported in this paper. Excellent chemoselectivities and full conversions with good enantioselectivities were achieved for alkyl derivatives by homogenous asymmetric hydrogenation with Ir-P,N catalysts. (alfa-Haloalkyl)boronic esters are the only precursors for the preparation of a-amino boronic acids, which are the key constituent of some proteasome inhibitors, such as bortezomib.
COBISS.SI-ID: 1555036
In this paper new assay for quantification of PEGylated proteins, which have partially or completely masked epitopes, was described. In this case, standard ELISA is not usefull, because antibodies can not bind to masked epitopes. New assay utilizes binding of histidine rich proteins to immobilized nickel ions and biotin-streptavidin, one of the stongest non-covalent interacitons in the nature. Using this new method, crossing of PEGylated TNF conjugates across Caco2 epithelial barier was evaluated.
COBISS.SI-ID: 31571161
In this article we describe the development of an in-line monitoring approach for the fluid bed drying and coating steps of production of enteric coated pellets by NIR. NIR spectroscopy is a well-established technique for observing the fluid bed process, for example to monitor the particle moisture and size. In addition, our results show that also other important pellet characteristics can be accurately predicted inline using developed classical and hierarchical calibration models. Moreover, the finished product enteric coating performance determined by classical analytical technique is in excellent agreement to the inline NIR predictions.
COBISS.SI-ID: 1571932
N-(5-(5-nitro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)4-oxo-2-thioxo-1,3-thiazolidin-3-yl)nicotinamide, a 2-oxoindolinylidene derivative with novel structure scaffold, was evaluated for inhibition potency against the MurD enzyme from Escherichia coli using an enzyme steady-state kinetics study. The compound exerted competitive inhibition with respect to UMA, a MurD substrate, and affected bacterial growth. The binding mode of novel inhibitor was determined and compared to naphthalene-N-sulfonamide-D-Glu derivatives, transition state mimicking inhibitors, UMA and AMP-PCP, an ATP analog. It binds to the UDP/MurNAc binding region. In contrast to transition state mimicking inhibitors, it does not interact with the enzyme's C-terminal domain, which can be beneficial for ligand binding. A pharmacophore pattern was established for the design of novel drugs having a propensity to inhibit a broad spectrum of Mur enzymes.
COBISS.SI-ID: 1563996
The aim of the research was to investigate how Lactobacillus gasseri K7 and enterohemorrhagic Escherichia coli O157:H7 modulate the blood transcriptome of mice possessing an intact microbiota. Different groups of mice were inoculated with different bacterial strains (single or co-inoculated) and the transcriptome was analyzed. The transcriptome could distinguish between the five treatment groups - genes characteristic of bacterial infection, in particular inflammation, were up‐regulated in the mice inoculated with E. coli., while L. gasseri had only mild effects on the transcriptome but modified the gene expression induced by E. coli. The results suggest that the blood cell transcriptome can be used as a source of biomarkers to monitor the impact of probiotics in subclinical models of infectious disease.
COBISS.SI-ID: 3338376