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Masao Ohashi Takuji Oyama Endy Widya Putranto Tsuyoshi Waku Hiromi Nobusada Ken Kataoka Kenji Matsuno Masakazu Yashiro Kosuke Morikawa Nam-ho Huh Hiroyuki Miyachi 《Bioorganic & medicinal chemistry》2013,21(8):2319-2332
In the continuing study directed toward the development of peroxisome proliferator-activated receptor gamma (hPPARγ) agonist, we attempted to improve the water solubility of our previously developed hPPARγ-selective agonist 3, which is insufficiently soluble for practical use, by employing two strategies: introducing substituents to reduce its molecular planarity and decreasing its hydrophobicity via replacement of the adamantyl group with a heteroaromatic ring. The first approach proved ineffective, but the second was productive. Here, we report the design and synthesis of a series of α-benzyl phenylpropanoic acid-type hPPARγ partial agonists with improved aqueous solubility. Among them, we selected (R)-7j, which activates hPPARγ to the extent of about 65% of the maximum observed with a full agonist, for further evaluation. The ligand-binding mode and the reason for the partial-agonistic activity are discussed based on X-ray-determined structure of the complex of hPPARγ ligand-binding domain (LBD) and (R)-7j with previously reported ligand-LDB structures. Preliminal apoptotic effect of (R)-7j against human scirrhous gastric cancer cell line OCUM-2MD3 is also described. 相似文献
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Junichiro Futami Yuki Atago Akari Azuma Endy Widya Putranto Rie Kinoshita Hitoshi Murata Masakiyo Sakaguchi 《Biochemistry and Biophysics Reports》2016
It is now known that multicomponent protein assemblies strictly regulate many protein functions. The S100 protein family is known to play various physiological roles, which are associated with alternative complex formations. To prepare sufficient amounts of heterodimeric S100A8 and S100A9 proteins, we developed a method for bicistronic coexpression from a single-vector system using Escherichia coli cells as a host. The complex formation between S100A8 and S100A9 appears to be dependent on the thermodynamic stability of the protein during expression. The stable S100A8/A9 heterodimer complex spontaneously formed during coexpression, and biologically active samples were purified by cation-exchange chromatography. Semi-stable homodimers of S100A8 and S100A9 were also formed when expressed individually. These results suggest that the assembly of S100 protein complexes might be regulated by expression levels of partner proteins in vivo. Because protein assembly occurs rapidly after protein synthesis, coexpression of relevant proteins is crucial for the design of multicomponent recombinant protein expression systems. 相似文献
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A simple and accurate model of high-temperature treatment of wood can assist in the process design and the evaluation of performance of equipment. The high-temperature treatment of wood is essentially a drying process under linearly-increased gas temperature up to final temperature of 220-230 °C which is a challenging process to model. This study is aimed to assess the applicability and accuracy of the reaction engineering approach (REA) to model the heat treatment of wood. In order to describe the process using the REA, the maximum activation energy (ΔEv,b) is evaluated according to the corresponding external conditions during the heat treatment. Results indicate that the REA coupled with the heat balance describes both moisture content and temperature profiles during the heat treatment very well. A good agreement towards the experimental data is indicated. It has also been shown that the current model is highly comparable in accuracy with the complex models. 相似文献
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Masakiyo Sakaguchi Hitoshi Murata Yumi Aoyama Toshihiko Hibino Endy Widya Putranto I. Made Winarsa Ruma Yusuke Inoue Yoshihiko Sakaguchi Ken-ichi Yamamoto Rie Kinoshita Junichiro Futami Ken Kataoka Keiji Iwatsuki Nam-ho Huh 《The Journal of biological chemistry》2014,289(34):23389-23402
The receptor for advanced glycation end products (RAGE) is involved in the pathogenesis of many inflammatory, degenerative, and hyperproliferative diseases, including cancer. Previously, we revealed mechanisms of downstream signaling from ligand-activated RAGE, which recruits TIRAP/MyD88. Here, we showed that DNAX-activating protein 10 (DAP10), a transmembrane adaptor protein, also binds to RAGE. By artificial oligomerization of RAGE alone or RAGE-DAP10, we found that RAGE-DAP10 heterodimer formation resulted in a marked enhancement of Akt activation, whereas homomultimeric interaction of RAGE led to activation of caspase 8. Normal human epidermal keratinocytes exposed to S100A8/A9, a ligand for RAGE, at a nanomolar concentration mimicked the pro-survival response of RAGE-DAP10 interaction, although at a micromolar concentration, the cells mimicked the pro-apoptotic response of RAGE-RAGE. In transformed epithelial cell lines, A431 and HaCaT, in which endogenous DAP10 was overexpressed, and S100A8/A9, even at a micromolar concentration, led to cell growth and survival due to RAGE-DAP10 interaction. Functional blocking of DAP10 in the cell lines abrogated the Akt phosphorylation from S100A8/A9-activated RAGE, eventually leading to an increase in apoptosis. Finally, S100A8/A9, RAGE, and DAP10 were overexpressed in the psoriatic epidermis. Our findings indicate that the functional interaction between RAGE and DAP10 coordinately regulates S100A8/A9-mediated survival and/or apoptotic response of keratinocytes. 相似文献
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Sands Roger Nugroho Putranto B. Leung David W.M. Sun Osbert J. Clinton Peter W. 《Plant and Soil》2000,225(1-2):213-225
This study examined the reciprocal effects of growing ryegrass, lotus and other weed species in competition with radiata pine
on soil CO2 and O2 concentrations and on the growth and root respiration of the radiata pine. Soil O2 concentrations decreased and soil CO2 concentrations increased with increasing soil depth. Radiata pine plus competing species slightly reduced soil O2 concentrations and markedly increased soil CO2 concentrations (up to 40 mmol mol−1) compared with radiata pine alone. The dry weights of shoots and roots, and the root respiration rates of radiata pine grown
with competing vegetation were much less than those for radiata pine alone. This probably was not solely caused by competition
for nutrients water or light since adequate water and nutrients were supplied to all treatments and the radiata pine overtopped
the competing vegetation. When radiata pine roots were raised in NaHCO3 solutions equivalent to a range of CO2 concentrations, succinate dehydrogenase activity (a metabolic indicator of mitochondrial respiration) and elongation rates
of roots decreased as CO2 concentrations increased from 0 to 40 mmol mol−1. This suggests that the elevated CO2 concentrations found in the experiments in soil was the cause, at least in part, of the reduced growth of radiata pine in
competition with other species.
This revised version was published online in June 2006 with corrections to the Cover Date. 相似文献
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Length–weight relationships of three demersal fish species caught from the eastern region of Java Sea,Indonesia 下载免费PDF全文
M. Saleh T. W. C. Putranto A. Arisandi A. Soegianto 《Zeitschrift fur angewandte Ichthyologie》2018,34(1):213-215
Length–weight relationship (LWR) parameters were determined for three demersal fish species Nuchequula gerreoides, Scarus scaber and Therapon theraps. The fishes were collected by seine net (the mesh size of wing: 12.70 cm, body: 3.81 cm, cod end: 2.54 cm, and total length of net: 20 m) in eastern region of Java Sea Indonesia during October 2016 – March 2017. The total length of these species (14.3 cm for N. gerreoides, 24.5 cm for S. scaber and 21.5 cm for T. theraps) were longer than previous studies. The b values of the LWR were 2.967 for N. gerreoides, 3.046 for S. scaber and 3.0475 for T. theraps. 相似文献
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Trisnadi Widyaleksono Catur Putranto Riska Andriani Anita Munawwaroh Bambang Irawan 《Marine and Freshwater Behaviour and Physiology》2014,47(5):349-360
The prawn Macrobrachium sintangense is likely to be subjected to occasional exposure to combined metal and saline stressors in its natural environment. This research evaluated the acute toxicity (96?h LC50) of cadmium (Cd) on the prawn M. sintangense, with respect to the osmoregulatory capacity (OC) of prawns and to document histological changes in the gills after exposure to sublethal Cd concentrations at different salinities. The 96?h LC50 of Cd to M. sintangense decreased with increasing salinity. The 96?h LC50 values were 89.12 (72.53–109.50), 681.26 (554.20–837.46) and 825.37 (676.99–1006.27) μg CdL?1 at 0, 10 and 20 ppt, respectively. The OC of prawns exposed to 30?μg?CdL?1 at 0 ppt and to 300?μg?CdL?1 at10 ppt decreased significantly compared with that of control prawns exposed to 0 and 10 ppt respectively. Swelling, hyperplasia and necrosis of gill lamellae resulting in the loss of marginal canals were observed in the gills of prawns exposed to 30?μg?CdL?1 at 0 ppt and to 300?μg?CdL?1 at 10 ppt for 7?days. 相似文献
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Rudi Putranto Endjad Mudjaddid Hamzah Shatri Mizanul Adli Diah Martina 《BioPsychoSocial medicine》2017,11(1):29