Publications

This article presents the rapid identification of novel indolylarylsulfone (IAS) derivatives as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) for HIV-1 through a miniaturized click-chemistry-based combinatorial library approach. Utilizing copper(i)-catalyzed azide-alkyne cycloaddition (CuAAC), a reliable and biocompatible click chemistry technique, the researchers synthesized and characterized a series of IAS derivatives. Several compounds selected through the <i>in situ</i> enzyme inhibition assay demonstrated promising activity in subsequent cellular level tests. Notably, compound C1N4 displayed the most potent anti-HIV-1 IIIB activity with an EC₅₀ of 0.024 μM and low cytotoxicity (CC₅₀ > 215.88 μM). Molecular docking studies provided insights into the binding mode of these novel compounds within the NNIBP, aiding in the structure-based design of future NNRTIs. The findings underscore the potential of click chemistry in the discovery of new anti-HIV agents with improved efficacy and safety profiles.

We report on the detection of high-contrast and narrow Coherent Population Trapping (CPT) Ramsey fringes in a Cs vapor cell using a simple-architecture laser system. The latter allows the combination of push-pull optical pumping (PPOP) and a temporal Ramsey-like pulsed interrogation. An originality of the optics package is the use of a single Mach-Zehnder electro-optic modulator (MZ EOM) both for optical sidebands generation and light switch for pulsed interaction. Typical Ramsey fringes with a linewidth of 166 Hz and a contrast of 33 % are detected in a cm-scale buffer-gas filled Cs vapor cell. This technique could be interesting for the development of high-performance and low power consumption compact vapor cell clocks based on CPT.

Selective laser melting (SLM) is an additive manufacturing technique in which functional, complex parts can be created directly by selectively melting layers of powder. This process is characterized by highly localized high heat inputs during very short interaction times and will therefore significantly affect the microstructure. In this research, the development of the microstructure of the Ti–6Al–4V alloy processed by SLM and the influence of the scanning parameters and scanning strategy on this microstructure are studied by light optical microscopy. The martensitic phase is present, and due to the occurrence of epitaxial growth, elongated grains emerge. The direction of these grains is directly related to the process parameters. At high heat inputs it was also found that the intermetallic phase Ti3Al is precipitated during the process.

Additive manufacturing techniques are getting more and more established as reliable methods for producing porous metal implants thanks to the almost full geometrical and mechanical control of the designed porous biomaterial. Today, Ti6Al4V ELI is still the most widely used material for porous implants, and none or little interest goes to pure titanium for use in orthopedic or load-bearing implants. Given the special mechanical behavior of cellular structures and the material properties inherent to the additive manufacturing of metals, the aim of this study is to investigate the properties of selective laser melted pure unalloyed titanium porous structures. Therefore, the static and dynamic compressive properties of pure titanium structures are determined and compared to previously reported results for identical structures made from Ti6Al4V ELI and tantalum. The results show that porous Ti6Al4V ELI still remains the strongest material for statically loaded applications, whereas pure titanium has a mechanical behavior similar to tantalum and is the material of choice for cyclically loaded porous implants. These findings are considered to be important for future implant developments since it announces a potential revival of the use of pure titanium for additively manufactured porous implants.

Thermally induced phase separation (TIPS) was used to produce spherical polypropylene–zirconia composite powder for selective laser sintering (SLS). The influence of the composition of the composite starting powder and the SLS parameters on the density and strength of the composite SLS parts was investigated, allowing realizing SLS parts with a relative density of 36%. Pressure infiltration (PI) and warm isostatic pressing (WIPing) were applied to increase the green density of the ZrO2–PP SLSed parts. Infiltrating the SLS parts with an aqueous 30vol.% ZrO2 suspension allowed to increase the sintered density from 32 to 54%. WIPing (135°C and 64MPa) of the SLS and SLS/infiltrated complex shape green polymer–ceramic composite parts prior to debinding and sintering allowed raising the sintered density of the 3mol Y2O3 stabilized ZrO2 parts to 92 and 85%, respectively.

Porous titanium alloys are considered promising bone-mimicking biomaterials. Additive manufacturing techniques such as selective laser melting allow for manufacturing of porous titanium structures with a precise design of micro-architecture. The mechanical properties of selective laser melted porous titanium alloys with different designs of micro-architecture have been already studied and are shown to be in the range of mechanical properties of bone. However, the fatigue behavior of this biomaterial is not yet well understood. We studied the fatigue behavior of porous structures made of Ti6Al4V ELI powder using selective laser melting. Four different porous structures were manufactured with porosities between 68 and 84% and the fatigue S–N curves of these four porous structures were determined. The three-stage mechanism of fatigue failure of these porous structures is described and studied in detail. It was found that the absolute S–N curves of these four porous structures are very different. In general, given the same absolute stress level, the fatigue life is much shorter for more porous structures. However, the normalized fatigue S–N curves of these four structures were found to be very similar. A power law was fitted to all data points of the normalized S–N curves. It is shown that the measured data points conform to the fitted power law very well, R 2 =0.94. This power law may therefore help in estimating the fatigue life of porous structures for which no fatigue test data is available. It is also observed that the normalized endurance limit of all tested porous structures (<0.2) is lower than that of corresponding solid material (c.a. 0.4).

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The DNA sequence of the gene for the yeast glycolytic enzyme, 3-phosphoglycerate kinase (PGK), has been obtained by sequencing part of a 3.1 kbp HindIII fragment obtained from the yeast genome. The structural gene sequence corresponds to a reading frame of 1251 bp coding for 416 amino acids with no intervening DNA sequences. The amino acid sequence is approximately 65 percent homologous with human and horse PGK protein sequences and is in general agreement with the published protein sequence for yeast PGK. As for other highly expressed structural genes in yeast, the coding sequence is highly codon biased with 95 percent of the amino acids coded for by a select 25 codons (out of 61 possible). Besides structural DNA sequence, 291 bp of 5'-flanking sequence and 286 bp of 3'-flanking sequence were determined. Transcription starts 36 nucleotides upstream from the translational start and stops 86-93 nucleotides downstream from the translational stop. These results suggest a non-polyadenylated mRNA length of 1373 to 1380 nucleotides, which is consistent with the observed length of 1500 nucleotides for polyadenylated PGK mRNA. A sequence TATATATAAA is found at 145 nucleotides upstream from the translational start. This sequence resembles the TATAAA box that is possibly associated with RNA polymerase II binding.