Publications

This paper presents a performance evaluation test for laser line scanners on 3D coordinate measuring machines (CMMs). Laser line scanners are becoming more popular in recent years, mainly for free form inspection tasks and reverse engineering. Error specification of these scanners is difficult because of many influencing factors like surface quality, surface orientation and scan depth. Therefore, procedures for evaluation and verification of conventional contact probes (e.g. touch-trigger probes) are not appropriate for non-contact laser line scanners. A straightforward test method that uses a planar test artefact is proposed. It enables to identify the influence of in-plane and out-of-plane angle, as well as scan depth on systematic and random errors of the laser scanner. Experimental results show that the tested commercial laser scanner, after calibration, exhibits systematic errors of about 10μm.

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Our previous efforts have led to the development of two potent NNRTIs, K-5a2 and 25a, exhibiting effective anti-HIV-1 potency and resistance profiles compared with etravirine. However, both inhibitors suffered from potent hERG inhibition and short half-life. In this article, with K-5a2 and etravirine as leads, series of novel fluorine-substituted diarylpyrimidine derivatives were designed via molecular hybridization and bioisosterism strategies. The results indicated <b>24b</b> was the most active inhibitor, exhibiting broad-spectrum activity (EC₅₀ = 3.60-21.5 nM) against resistant strains, significantly lower cytotoxicity (CC₅₀= 155 μM), and reduced hERG inhibition (IC₅₀ > 30 μM). Crystallographic studies confirmed the binding of <b>24b</b> and the role of the fluorine atom, as well as optimal contacts of a nitrile group with the main-chain carbonyl group of H235. Furthermore, <b>24b</b> showed longer half-life and favorable safety properties. All the results demonstrated that <b>24b</b> has significant promise in circumventing drug resistance as an anti-HIV-1 candidate.

No abstract is provided for this article.

Selective laser melting (SLM) is a promising technique for the production of biometallic scaffolds for orthopedic applications due to its ability for fast turnover times and production of customised complex geometrical parts. The present work demonstrates the production of various unit cell design scaffolds of low E-modulus Ti-xNb-yZr . 3 Unit cells were produced at 3 different pore sizes (1000, 750 and 500 μm). Micro-CT and compression testing was carried out for each design showing a stiffness range within the range of bone.

The immunomodulating and murine cytomegalovirus (MCMV)-inhibiting effects of the synthetic lipid A subunit analogue GLA-60 were investigated in different strains of immunodeficient mice. Peritoneal natural killer (NK) cells obtained from nude (nu/nu) C57BL/6 mice or normal NMRI mice, which had been treated intraperitoneally with 10 micrograms of GLA-60 1 day earlier, exhibited a greater cytolytic activity than those from untreated mice. GLA-60 also stimulated NK cell activity in SCID (severe combined immune deficiency) mice (which are T and B cell-defective), but not in NK cell-defective beige (C57BL/6 bg/bg) mice. GLA-60 also enhanced the phagocytic activity of peritoneal macrophages in beige, nude and NMRI mice, but not in SCID mice. GLA-60, when administered as a single 150 micrograms dose 1 day before infection, completely protected beige mice against MCMV-associated mortality. It also caused a significant increase in the life-span of MCMV-infected nude and SCID mice.

Targeting ribonuclease H (RNase H) has emerged as a highly promising strategy for treating HIV-1. In this study, a series of novel 3-hydrazonoindolin-2-one derivatives were designed and synthesized as potential inhibitors of HIV-1 RNase H. Notably, several of these derivatives displayed micromolar inhibitory activity. Among the compounds examined, the hit compound demonstrated potent inhibition of HIV-1 RNase H, boasting a Ki value of 2.31 μM. Additionally, the most potent compound of this general structure exhibited remarkable inhibitory activity, with Ki values of 0.55 μM. Through docking studies, the key interactions of this ligand within the active site of RNase H were uncovered. This novel chemical structure can be regarded as a prospective scaffold for the future development of RNase H inhibitors.