generation-subcutaneous-intrahepatic-human-hepatocellular-carcinoma

Generation of Subcutaneous and Intrahepatic Human Hepatocellular Carcinoma Xenografts in Immunodeficient Mice

In  vivo experimental models of hepatocellular carcinoma (HCC) that recapitulate  the human disease provide a valuable platform for research into disease  ...

University Health Network

We describe a systematic study of how macrocyclization in the Pâ‚-Pâ‚ƒ region of hydroxyethylamine-based inhibitors of Î²-site amyloid precursor protein (APP)-cleaving enzyme (BACE1) modulates in vitro activity. This study reveals that in a number of instances macrocyclization of bis-terminal dienes leads to improved potency toward BACE1 and selectivity against cathepsin D (CatD), as well as greater amyloid Î²-peptide (AÎ²)-lowering activity in HEK293T cells stably expressing APPSW. However, for several closely related analogs the benefits of macrocyclization are attenuated by the effects of other structural features in different regions of the molecules. X-ray crystal structures of three of these novel macrocyclic inhibitors bound to BACE1 revealed their binding conformations and interactions with the enzyme.

Hydroxyethylamine-based inhibitors of BACE1: Pâ‚-Pâ‚ƒ macrocyclization can improve potency, selectivity, and cell activity.

This study aims to investigate the expression of human kallikrein 6 (hK6) in gastric cancer, gastric ulcer and normal gastric mucosa tissues and its biological significance.

Expression and biological significance of human kallikrein 6 in gastric cancer tissues.

Aerosol was collected with Anderson cascade sampler at three altitudes of the Mount Huang in the summer 2011. Samples were analyzed by the ion chromatography (IC, Metrohm). The results showed that the mean mass concentrations of all the ions were 13.21 microg x m(-1), 10.94 microg x m(-3), 9.97 microg x m(-3), at the foot, mid height and the summit of the mountain, respectively. The mass concentration of water-soluble components of aerosol decreased with altitude. The major anion and cation of aerosols were SO4(2-) and NH4+, respectively. The descending order of mass concentration of major ionic species was: SO4(2-) > NH4+ > Ca2+ > NO3- and NH4+ account for about 75% of total ionic concentrations of PM2.1 in three sampling sites. The concentration of SO4(2-) and NH4+ decreased conspicuously with altitude. The major cation and anion of coarse mode particles were Ca2+ and NO3-, respectively. The slope of the linear regression line between anion and cation of PM10 and PM2.1 approximates 1, indicating acid-base balance in aerosol particles. Aerosols over the region Mount Huang were influenced by anthropogenic source of surrounding areas to a certain extent. The result also suggested that the correlation between NH4+ and SO4(2-) was 0. 98 and these ions predominantly existed in the form of (NH4)2SO4 and NH4HSO4. Backward trajectory analysis revealed that the air mass was originated from southern coastal regions, the East China Sea, the Yellow Sea and the northern China. Due to the northern air masses go through heavily polluted areas, concentrations of water-soluble ions in these air masses were higher than that of other air masses. The concentration of K+ in northern air mass was several times higher than that in southwestern air mass.

Article	Year
Hydroxyethylamine-based inhibitors of BACE1: Pâ‚-Pâ‚ƒ macrocyclization can improve potency, selectivity, and cell activity. Bioorganic & medicinal chemistry letters\| PubMed ID: 23769639	2013
Expression and biological significance of human kallikrein 6 in gastric cancer tissues. Contemporary oncology (PoznaÅ„, Poland)\| PubMed ID: 23788964	2013
[Chemical characteristics of water-soluble components of aerosol particles at different altitudes of the Mount Huang in the summer]. Huan jing ke xue= Huanjing kexue / [bian ji, Zhongguo ke xue yuan huan jing ke xue wei yuan hui "Huan jing ke xue" bian ji wei yuan hui.]\| PubMed ID: 23914556	2013

Kui Chen

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